2-(Diethylamino)-N-(2,6-dimethylphenyl)acetamide HCl (Lidocaine; Lignocaine; Xylocaine) by Asch

Query Query Cl

1. Query

Results

Date

1 substances in Reaxys

2018-05-14 08h:42m:45s (UTC)

H N N O

Search as: As drawn ) AND (IDE.XRN=3917968))

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Reaxys ID 3917968 View in Reaxys

1/1 CAS Registry Number: 73-78-9 Chemical Name: lidocaine hydrochloride; lignocaine hydrochloride; Lidocaine hydrochloride; 2-((2,6-dimethylphenyl)amino)-N,N-diethyl-2-oxoethan-1-aminium chloride; 2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide hydrochloride; 2-diethylamino-N-(2,6-dimethylphenyl)acetamide hydrochloride; ω-diethylamino-2,6-dimethylacetanilide hydrochloride Linear Structure Formula: C6H3(CH3)2NHCOCH2N(CH2CH3)2*HCl Molecular Formula: C14H22N2O*ClH Molecular Weight: 270.802 Type of Substance: isocyclic InChI Key: IYBQHJMYDGVZRY-UHFFFAOYSA-N Note:

N O Cl

H HN

Substance Label (25) Label References 10

Ganapati, Shweta; Zavalij, Peter Y.; Eikermann, Matthias; Isaacs, Lyle; Organic and Biomolecular Chemistry; vol. 14; nb. 4; (2016); p. 1277 - 1287, View in Reaxys

Adamo, Andrea; Beingessner, Rachel L.; Behnam, Mohsen; Chen, Jie; Jamison, Timothy F.; Jensen, Klavs F.; Monbaliu, Jean-Christophe M.; Myerson, Allan S.; Revalor, Eve M.; Snead, David R.; Stelzer, Torsten; Weeranoppanant, Nopphon; Wong, Shin Yee; Zhang, Ping; Science; vol. 352; nb. 6281; (2016); p. 61 - 67, View in Reaxys

325

Oda, Shingo; Fujiwara, Ryoichi; Kutsuno, Yuki; Fukami, Tatsuki; Itoh, Tomoo; Yokoi, Tsuyoshi; Nakajima, Miki; Drug Metabolism and Disposition; vol. 43; nb. 6; (2015); p. 812 - 818, View in Reaxys

Lebedyeva, Iryna O.; Oliferenko, Alexander A.; Oliferenko, Polina V.; Hromas, Robert A.; Neubert, John K.; Caudle, Robert M.; Wickersham, Jay; Castleman, William L.; Altschuler, Gary I.; Ostrov, David A.; Hall, C. Dennis; Katritzky, Alan R.; Journal of Materials Chemistry B; vol. 3; nb. 43; (2015); p. 8492 - 8498, View in Reaxys

Buyuktimkin, Tuba; Wurster, Dale Eric; Journal of Pharmaceutical Sciences; vol. 104; nb. 8; (2015); p. 2566 - 2573, View in Reaxys

LID

Huang, Jason Haitao; Thalhammer, Johann G.; Raymond, Stephen A.; Strichartz, Gary R.; Journal of Pharmacology and Experimental Therapeutics; vol. 282; nb. 2; (1997); p. 802 - 811, View in Reaxys; Wang, Sheng; Zeng, Dong; Niu, Jiao; Wang, Hanjie; Wang, Liangliang; Li, Qin; Li, Changyi; Song, Hao; Chang, Jin; Zhang, Lianyun; Journal of Materials Chemistry B; vol. 2; nb. 7; (2014); p. 877 - 884, View in Reaxys

Yokoyama, Shoko; Toxicology Letters; vol. 100-101; (1998); p. 365 - 368, View in Reaxys; Varshosaz, Jaleh; Jaffari, Fariba; Karimzadeh, Sara; Scientia Pharmaceutica; vol. 74; nb. 4; (2006); p. 209 - 223, View in Reaxys; Horita, Daisuke; Todo, Hiroaki; Sugibayashi, Kenji; Chemical and Pharmaceutical Bulletin; vol. 62; nb. 6; (2014); p. 578 - 585, View in Reaxys

LidHCl

Deryabina, Maria A.; Hansen, Steen H.; Jensen, Henrik; Analytical Chemistry; vol. 80; nb. 1; (2008); p. 203 - 208, View in Reaxys; Snchez-Leija; Pojman; Luna-Brcenas; Mota-Morales; Journal of Materials Chemistry B; vol. 2; nb. 43; (2014); p. 7495 - 7501, View in Reaxys

[Lid][Cl]

Wang, Hui; Gurau, Gabriela; Shamshina, Julia; Cojocaru, O. Andreea; Janikowski, Judith; Macfarlane, Douglas R.; Davis Jr., James H.; Rogers, Robin D.; Chemical Science; vol. 5; nb. 9; (2014); p. 3449 - 3456, View in Reaxys

LID HCl

Hirata, Kazumasa; Mohammed, Diar; Hadgraft, Jonathan; Lane, Majella E.; International Journal of Pharmaceutics; vol. 477; nb. 1-2; (2014); p. 416 - 420, View in Reaxys

1 HCl

Braga, Dario; Chelazzi, Laura; Grepioni, Fabrizia; Dichiarante, Elena; Chierotti, Michele R.; Gobetto, Roberto; Crystal Growth and Design; vol. 13; nb. 6; (2013); p. 2564 - 2572, View in Reaxys

LD-HCl

Torres, Daniel R.; Blanco, Luis H.; Martinez, Fleming; Vargas, Edgar F.; Journal of Chemical and Engineering Data; vol. 52; nb. 5; (2007); p. 1700 - 1703, View in Reaxys

Hou, Chia-Hui; Tzeng, Jann-Inn; Chen, Yu-Wen; Lin, Ching-Nan; Lin, Mao-Tsun; Tu, Chieh-Hsien; Wang, JhiJoung; European Journal of Pharmacology; vol. 544; nb. 1-3; (2006); p. 10 - 16, View in Reaxys

LDCHC

Schmidt, Andrea C.; Pharmaceutical Research; vol. 22; nb. 12; (2005); p. 2121 - 2133, View in Reaxys

b; Lido

Berggren, Sofia; Hoogstraate, Janet; Fagerholm, Urban; Lennernaes, Hans; European Journal of Pharmaceutical Sciences; vol. 21; nb. 4; (2004); p. 553 - 560, View in Reaxys

M 5505

Ryan, Stephen E.; Baenziger, John E.; Molecular Pharmacology; vol. 55; nb. 2; (1999); p. 348 - 355, View in Reaxys; Tanaka, Yoshio; Kamibayashi, Makoto; Yamashita, Yoko; Imai, Toshiyasu; Tanaka, Hikaru; Nakahara, Tsutomu; Ishii, Kunio; Shigenobu, Koki; Naunyn-Schmiedeberg's Archives of Pharmacology; vol. 365; nb. 1; (2002); p. 56 - 66, View in Reaxys

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Lig

Darcy; Kelly; Leonard; Henry; Toxicology Letters; vol. 128; nb. 1-3; (2002); p. 207 - 214, View in Reaxys

Merck 5505

Nishiguchi, Eiko; Hamada, Nobushiro; Shindo, Junichi; European Journal of Pharmacology; vol. 286; nb. 1; (1995); p. 1 - 8, View in Reaxys; Kreilgaard; Pharmaceutical Research; vol. 18; nb. 3; (2001); p. 367 - 373, View in Reaxys

L-HCl

Valenta; Cladera; O'Shea; Hadgraft; Journal of Pharmaceutical Sciences; vol. 90; nb. 4; (2001); p. 485 - 492, View in Reaxys; Dollo, Gilles; Estebe, Jean-Pierre; Le Corre, Pascal; Chevanne, Francois; Ecoffey, Claude; Le Verge, Roger; European Journal of Pharmaceutical Sciences; vol. 13; nb. 3; (2001); p. 319 - 323, View in Reaxys

LIDO

Barat, Stephen A.; Turkall, Rita M.; Toxicology Letters; vol. 89; nb. 3; (1996); p. 201 - 206, View in Reaxys; Nakahara, Tsutomu; Yunoki, Motonari; Moriuchi, Hiroshi; Sakamato, Kenji; Ishii, Kunio; Naunyn-Schmiedeberg's Archives of Pharmacology; vol. 361; nb. 6; (2000); p. 605 - 609, View in Reaxys

lidoHCl

Alfons, Katarina; Journal of Pharmaceutical Sciences; vol. 87; nb. 12; (1998); p. 1527 - 1530, View in Reaxys

Merck 5503

Schwarz, Stephan K. W.; Puil, Ernest; British Journal of Pharmacology; vol. 124; nb. 8; (1998); p. 1633 - 1642, View in Reaxys

Negwer8 4242

Wyeth, Richard P.; Soulsby, Michael E.; Vesely, David L.; Kennedy, Richard H.; Life Sciences; vol. 60; nb. 7; (1997); p. 473 - 477, View in Reaxys

MERCK 5505

Butcher; Cechetto; American Journal of Physiology - Regulatory Integrative and Comparative Physiology; vol. 268; nb. 1 37-1; (1995); p. R214-R222, View in Reaxys

Merck 12,5505

Jackson; Graff; Richardson; Hargreaves; European Journal of Pharmacology; vol. 284; nb. 3; (1995); p. 321 - 325, View in Reaxys

Patent-Specific Data (1) Prophetic ComReferences pound prophetic product

Patent; The Procter and Gamble Company; US6338855; (2002); (B1) English, View in Reaxys

Druglikeness (1) 1 of 1

LogP

2.611

H Bond Donors

H Bond Acceptors

Rotatable Bonds

TPSA

32.34

Lipinski Number

Veber Number

Highest Clinical Phase (1) Highest Clinical Phase Marketed Melting Point (9) 1 of 9

Melting Point [°C]

131 - 133

Location

supporting information

Badawi, Hassan M.; Förner, Wolfgang; Ali, Shaikh A.; Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy; vol. 152; (2016); p. 92 - 100, View in Reaxys 2 of 9

Melting Point [°C]

73 - 74

Location

supporting information

Crystallizes With

water

Amount (Melting Point) [mol]

Badawi, Hassan M.; Förner, Wolfgang; Ali, Shaikh A.; Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy; vol. 152; (2016); p. 92 - 100, View in Reaxys 3 of 9

Melting Point [°C]

69.84

Wojnarowska, Zaneta; Paluch, Krzysztof J.; Shoifet, Evgeni; Schick, Christoph; Tajber, Lidia; Knapik, Justyna; Wlodarczyk, Patryk; Grzybowska, Katarzyna; Hensel-Bielowka, Stella; Verevkin, Sergey P.; Paluch, Marian; Journal of the American Chemical Society; vol. 137; nb. 3; (2015); p. 1157 - 1164, View in Reaxys 4 of 9

Melting Point [°C]

80 - 82

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Snchez-Leija; Pojman; Luna-Brcenas; Mota-Morales; Journal of Materials Chemistry B; vol. 2; nb. 43; (2014); p. 7495 7501, View in Reaxys 5 of 9

Melting Point [°C]

75.8

Braga, Dario; Chelazzi, Laura; Grepioni, Fabrizia; Dichiarante, Elena; Chierotti, Michele R.; Gobetto, Roberto; Crystal Growth and Design; vol. 13; nb. 6; (2013); p. 2564 - 2572, View in Reaxys 6 of 9

Melting Point [°C]

Comment (Melting Point)

Mol(s) H2O

Schmidt, Andrea C.; Pharmaceutical Research; vol. 22; nb. 12; (2005); p. 2121 - 2133, View in Reaxys 7 of 9

Melting Point [°C]

129

Schmidt, Andrea C.; Pharmaceutical Research; vol. 22; nb. 12; (2005); p. 2121 - 2133, View in Reaxys 8 of 9

Melting Point [°C]

Solvent (Melting Point)

ethanol; petroleum ether

Comment (Melting Point)

with:1 Mol.H2O (solvent).

Hach; Protiva; Chemicke Listy; vol. 47; (1953); p. 729,730; Collection of Czechoslovak Chemical Communications; vol. 18; (1953); p. 684,686; Chem.Abstr.; (1955); p. 204, View in Reaxys 9 of 9

Melting Point [°C]

128 - 129

Solvent (Melting Point)

butan-2-one

Loefgren; Arkiv foer Kemi; vol. 22A; nb. 18; (1946); p. 11, View in Reaxys Association (MCS) (4) 1 of 4

Description (Association (MCS))

Association with compound

Solvent (Association (MCS))

water

Temperature (Association (MCS)) [°C]

24.99

Partner (Association (MCS))

ω-cyclodextrin

Soni, Surbhi; Pal, Amalendu; Journal of Solution Chemistry; vol. 45; nb. 5; (2016); p. 665 - 674, View in Reaxys 2 of 4

Description (Association (MCS))

Association with compound

Solvent (Association (MCS))

water

Temperature (Association (MCS)) [°C]

24.99

Partner (Association (MCS))

alpha cyclodextrin

Soni, Surbhi; Pal, Amalendu; Journal of Solution Chemistry; vol. 45; nb. 5; (2016); p. 665 - 674, View in Reaxys 3 of 4

Description (Association (MCS))

Association with compound

Solvent (Association (MCS))

1,2-dichloro-ethane

Temperature (Association (MCS)) [°C]

Partner (Association (MCS))

cholesterol

Deryabina, Maria A.; Hansen, Steen H.; Jensen, Henrik; Analytical Chemistry; vol. 80; nb. 1; (2008); p. 203 - 208, View in Reaxys 4 of 4

Description (Association (MCS))

IR spectrum of the complex

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Partner (Association (MCS))

nicotinic acetylcholine receptor

Ryan, Stephen E.; Baenziger, John E.; Molecular Pharmacology; vol. 55; nb. 2; (1999); p. 348 - 355, View in Reaxys Boundary Surface Phenomena (MCS) (1) 1 of 1

Description (Boundary Surface Phenomena (MCS))

Surface potential

Temperature (Boundary Surface Phenomena (MCS)) [°C]

Partner (Boundary Surface heptaethylene glycol dodecyl ether Phenomena (MCS)) Yokoyama, Shoko; Toxicology Letters; vol. 100-101; (1998); p. 365 - 368, View in Reaxys Chromatographic Data (2) Chromatographic References data HPLC (High performance liquid chromatography)

Zergiebel, Stephanie; Fleck, Christian; Arndt, Hans-Dieter; Enzensperger, Christoph; Seeling, Andreas; Drug Research; vol. 67; nb. 8; (2017); p. 466 - 475, View in Reaxys

GC (Gas chromatography)

Atila, Alptug; Kadioglu, Yucel; Asian Journal of Chemistry; vol. 26; nb. 19; (2014); p. 6650 - 6654, View in Reaxys

Complex Phase Equilibria (MCS) (5) 1 of 5

Description (Complex Phase Equilibria (MCS))

Phase equilibrium

Partner (Complex Phase Equilibria (MCS))

propylene glycol; glyceryl monooleate

Alfons, Katarina; Journal of Pharmaceutical Sciences; vol. 87; nb. 12; (1998); p. 1527 - 1530, View in Reaxys 2 of 5

Description (Complex Phase Equilibria (MCS))

Phase equilibrium

Partner (Complex Phase Equilibria (MCS))

poly(ethylene glycol); glyceryl monooleate

Alfons, Katarina; Journal of Pharmaceutical Sciences; vol. 87; nb. 12; (1998); p. 1527 - 1530, View in Reaxys 3 of 5

Description (Complex Phase Equilibria (MCS))

Phase equilibrium

Partner (Complex Phase Equilibria (MCS))

propylene glycol; Miglyol 812

Alfons, Katarina; Journal of Pharmaceutical Sciences; vol. 87; nb. 12; (1998); p. 1527 - 1530, View in Reaxys 4 of 5

Description (Complex Phase Equilibria (MCS))

Phase equilibrium

Partner (Complex Phase Equilibria (MCS))

poly(ethylene glycol); glyceryl monooleate; 2-diethylamino-N-(2,6-dimethylphenyl)-acetamide

Alfons, Katarina; Journal of Pharmaceutical Sciences; vol. 87; nb. 12; (1998); p. 1527 - 1530, View in Reaxys 5 of 5

Description (Complex Phase Equilibria (MCS))

Phase equilibrium

Partner (Complex Phase Equilibria (MCS))

propylene glycol; glyceryl monooleate; 2-diethylamino-N-(2,6-dimethylphenyl)-acetamide

Alfons, Katarina; Journal of Pharmaceutical Sciences; vol. 87; nb. 12; (1998); p. 1527 - 1530, View in Reaxys Crystal Phase (1) Description (Crystal Phase) Glass transition temperature

References Wojnarowska, Zaneta; Paluch, Krzysztof J.; Shoifet, Evgeni; Schick, Christoph; Tajber, Lidia; Knapik, Justyna; Wlodarczyk, Patryk; Grzybowska, Katarzyna; Hensel-Bielowka, Stella; Verevkin, Sergey P.; Paluch, Marian; Journal of the American Chemical Society; vol. 137; nb. 3; (2015); p. 1157 - 1164, View in Reaxys

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Dissociation Exponent (5) 1 of 5

Dissociation Exponent (pK)

7.53

Dissociation Group

Temperature (Dissociation Exponent) [°C]

Solvent (Dissociation Exponent)

water

Type (Dissociation Exponent)

a1/apparent

Buyuktimkin, Tuba; Wurster, Dale Eric; Journal of Pharmaceutical Sciences; vol. 104; nb. 8; (2015); p. 2566 - 2573, View in Reaxys 2 of 5

Dissociation Exponent (pK)

7.92

Dissociation Group

N(+)-H

Temperature (Dissociation Exponent) [°C]

Solvent (Dissociation Exponent)

water

Method (Dissociation Exponent)

potentiometric

Type (Dissociation Exponent)

a1/apparent

Comment (Dissociation Exponent)

Brandariz, Isabel; Iglesias, Emilia; Supramolecular Chemistry; vol. 23; nb. 9; (2011); p. 607 - 614, View in Reaxys 3 of 5

Dissociation Exponent (pK)

7.86

Type (Dissociation Exponent)

a1/apparent

Kobayashi, Yoichi; Komatsu, Tsunehisa; Sumi, Machiko; Numajiri, Sachihiko; Miyamoto, Misao; Kobayashi, Daisuke; Sugibayashi, Kenji; Morimoto, Yasunori; European Journal of Pharmaceutical Sciences; vol. 21; nb. 4; (2004); p. 471 - 477, View in Reaxys 4 of 5

Dissociation Exponent (pK)

-0.930949

Type (Dissociation Exponent)

a1/apparent

Valenta; Cladera; O'Shea; Hadgraft; Journal of Pharmaceutical Sciences; vol. 90; nb. 4; (2001); p. 485 - 492, View in Reaxys 5 of 5

Dissociation Exponent (pK)

7.97

Temperature (Dissociation Exponent) [°C]

Solvent (Dissociation Exponent)

H2O

Method (Dissociation Exponent)

potentiometric

Type (Dissociation Exponent)

a1/apparent

Shklyaev, V. S.; Pantsurkin, V. I.; Vakhrina, N. I.; Vakhrin, M. I.; Pharmaceutical Chemistry Journal; vol. 14; nb. 4; (1980); p. 239 - 244; Khimiko-Farmatsevticheskii Zhurnal; vol. 14; nb. 4; (1980); p. 49 - 55, View in Reaxys Electrochemical Behaviour (1)

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Description (Electrochemical Behaviour)

References

Electrolytic dissoci- Al-Saadi; Sneader; Arzneimittel-Forschung/Drug Research; vol. 41; nb. 2; (1991); p. 115 - 118, View in Reaxys; ation / protonation Shklyaev, V. S.; Pantsurkin, V. I.; Vakhrina, N. I.; Vakhrin, M. I.; Pharmaceutical Chemistry Journal; vol. 14; nb. 4; equilibrium (1980); p. 239 - 244; Khimiko-Farmatsevticheskii Zhurnal; vol. 14; nb. 4; (1980); p. 49 - 55, View in Reaxys Electrochemical Characteristics (2) 1 of 2

Description (Electrochemical Characteristics)

polarographic current/voltage curve

Solvent (Electrochemical Characteristics)

acetate buffer; acetonitrile

pH-Value (Electrochemical Characteristics)

4.8

Baczynski, Emil; Piwonska, Agata; Fijalek, Zbigniew; Acta Poloniae Pharmaceutica - Drug Research; vol. 59; nb. 5; (2002); p. 333 - 339, View in Reaxys 2 of 2

Description (Electrochemical Characteristics)

voltammetry

Solvent (Electrochemical Characteristics)

acetate buffer

pH-Value (Electrochemical Characteristics)

4.8

Baczynski, Emil; Piwonska, Agata; Fijalek, Zbigniew; Acta Poloniae Pharmaceutica - Drug Research; vol. 59; nb. 5; (2002); p. 333 - 339, View in Reaxys Energy Data (MCS) (1) 1 of 1

Description (Energy Data (MCS))

Enthalpy of solution

Partner (Energy Data (MCS))

water

Brodin; Nyqvist-Mayer; Wadsten; Forslund; Broberg; Journal of Pharmaceutical Sciences; vol. 73; nb. 4; (1984); p. 481 484, View in Reaxys Liquid/Liquid Systems (MCS) (5) 1 of 5

Description (Liquid/Liquid Distribution between solvent 1 + 2 Systems (MCS)) Temperature (Liquid/ Liquid Systems (MCS)) [°C]

Comment (Liquid/Liquid Systems (MCS))

pH dependence

Partner (Liquid/Liquid Systems (MCS))

1,2-dichloro-ethane; water

Deryabina, Maria A.; Hansen, Steen H.; Jensen, Henrik; Analytical Chemistry; vol. 80; nb. 1; (2008); p. 203 - 208, View in Reaxys 2 of 5

Description (Liquid/Liquid Distribution between solvent 1 + 2 Systems (MCS)) Temperature (Liquid/ Liquid Systems (MCS)) [°C]

Comment (Liquid/Liquid Systems (MCS))

pH dependence

Partner (Liquid/Liquid Systems (MCS))

1,2-dichloro-ethane; cholesterol; water

Deryabina, Maria A.; Hansen, Steen H.; Jensen, Henrik; Analytical Chemistry; vol. 80; nb. 1; (2008); p. 203 - 208, View in Reaxys

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3 of 5

Description (Liquid/Liquid Distribution between solvent 1 + 2 Systems (MCS)) Partner (Liquid/Liquid Systems (MCS))

octanol

Gulyaeva, Nellie; Zaslavsky, Alexander; Lechner, Pamela; Chlenov, Michael; McConnell, Oliver; Chait, Arnon; Kipnis, Victor; Zaslavsky, Boris; European Journal of Medicinal Chemistry; vol. 38; nb. 4; (2003); p. 391 - 396, View in Reaxys 4 of 5

Description (Liquid/Liquid Distribution between solvent 1 + 2 Systems (MCS)) Comment (Liquid/Liquid Systems (MCS))

in the presence of inorganic compounds

Partner (Liquid/Liquid Systems (MCS))

dextran-67; poly(ethylene glycol), MW 8000

Description (Liquid/Liquid Liquid/liquid phase diagram Systems (MCS)) Otero-Pastor; Otero-Aerelle; Anales de Quimica (1968-1979); vol. 71; (1975); p. 907,909, View in Reaxys

Liquid/Solid Systems (MCS) (3) 1 of 3

Description (Liquid/Solid Systems (MCS))

Phase transition temperature(s)

Temperature (Liquid/Solid Systems (MCS)) [°C]

3 - 22

Partner (Liquid/Solid Systems (MCS))

Poloxamer 407 poly(oxyethylene-b-oxypropylene-b-oxyethylene) tribock copolymer, Mw=12500, polyoxyethylene/polyoxypropylene=2:1; Poly(ethylene glycol), Mw = 400

Ricci; Bentley; Farah; Bretas; Marchetti; European Journal of Pharmaceutical Sciences; vol. 17; nb. 3; (2002); p. 161 - 167, View in Reaxys 2 of 3

Description (Liquid/Solid Systems (MCS))

Phase transition temperature(s)

Temperature (Liquid/Solid Systems (MCS)) [°C]

3 - 22

Comment (Liquid/Solid Systems (MCS))

in the presence of salts

Partner (Liquid/Solid Systems (MCS))

Poloxamer 407 poly(oxyethylene-b-oxypropylene-b-oxyethylene) tribock copolymer, Mw=12500, polyoxyethylene/polyoxypropylene=2:1

Ricci; Bentley; Farah; Bretas; Marchetti; European Journal of Pharmaceutical Sciences; vol. 17; nb. 3; (2002); p. 161 - 167, View in Reaxys 3 of 3

Description (Liquid/Solid Systems (MCS))

Liquid/solid phase diagram

Partner (Liquid/Solid Systems (MCS))

prilocaine hydrochloride

Brodin; Nyqvist-Mayer; Wadsten; Forslund; Broberg; Journal of Pharmaceutical Sciences; vol. 73; nb. 4; (1984); p. 481 484, View in Reaxys Mechanical & Physical Properties (MCS) (3) 1 of 3

Description (Mechanical & Physical Properties (MCS))

Apparent molal volume

Temperature (Mechanical & Physical Properties (MCS)) [°C]

24.99 - 36.99

Partner (Mechanical & Physical Properties (MCS))

H2O

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Torres, Daniel R.; Blanco, Luis H.; Martinez, Fleming; Vargas, Edgar F.; Journal of Chemical and Engineering Data; vol. 52; nb. 5; (2007); p. 1700 - 1703, View in Reaxys 2 of 3

Description (Mechanical & Physical Properties (MCS))

Partial molal volume

Partner (Mechanical & Physical Properties (MCS))

H2O

Iqbal; Asghar Jamal; Ahmed; Canadian Journal of Chemistry; vol. 72; nb. 4; (1994); p. 1076 - 1079, View in Reaxys 3 of 3

Description (Mechanical & Physical Properties (MCS))

Partial molal volume

Partner (Mechanical & Physical Properties (MCS))

ethanol

Iqbal; Asghar Jamal; Ahmed; Canadian Journal of Chemistry; vol. 72; nb. 4; (1994); p. 1076 - 1079, View in Reaxys Partition octan-1-ol/water (MCS) (5) 1 of 5

log POW

2.26

Zergiebel, Stephanie; Fleck, Christian; Arndt, Hans-Dieter; Enzensperger, Christoph; Seeling, Andreas; Drug Research; vol. 67; nb. 8; (2017); p. 466 - 475, View in Reaxys 2 of 5

log POW

-0.9

Uchida, Takashi; Yakumaru, Masafumi; Nishioka, Keisuke; Higashi, Yoshihiro; Sano, Tomohiko; Todo, Hiroaki; Sugibayashi, Kenji; Chemical and Pharmaceutical Bulletin; vol. 64; nb. 9; (2016); p. 1338 - 1346, View in Reaxys 3 of 5

log POW

2.43

Temperature (Partition octan-1-ol/water (MCS)) [°C]

Buyuktimkin, Tuba; Wurster, Dale Eric; Journal of Pharmaceutical Sciences; vol. 104; nb. 8; (2015); p. 2566 - 2573, View in Reaxys 4 of 5

log POW

2.3

Valenta; Cladera; O'Shea; Hadgraft; Journal of Pharmaceutical Sciences; vol. 90; nb. 4; (2001); p. 485 - 492, View in Reaxys 5 of 5

Partition Constant POW

6.19

Temperature (Partition octan-1-ol/water (MCS)) [°C]

Wu, Changhao; Clift, Paul; Fry, Christopher H.; Henry, John A.; Archives of Toxicology; vol. 70; nb. 12; (1996); p. 850 853, View in Reaxys Solubility (MCS) (5) 1 of 5

Comment (Solubility (MCS))

good solubility in 95percent ethanol; absolute ethanol did not provide sufficient solubility; dissolve in DMSO however deforms the membrane

Saturation

in solution

Temperature (Solubility (MCS)) [°C]

24.99

Solvent (Solubility (MCS))

water

Comment (Solubility (MCS))

Solubility: 62.42 weight percent

Torres, Daniel R.; Blanco, Luis H.; Vargas, Edgar F.; Martinez, Fleming; Journal of Chemical and Engineering Data; vol. 54; nb. 3; (2009); p. 786 - 790, View in Reaxys 3 of 5

Saturation

in solution

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Temperature (Solubility (MCS)) [°C]

29.99

Solvent (Solubility (MCS))

water

Comment (Solubility (MCS))

Solubility: 64.8 weight percent

Torres, Daniel R.; Blanco, Luis H.; Vargas, Edgar F.; Martinez, Fleming; Journal of Chemical and Engineering Data; vol. 54; nb. 3; (2009); p. 786 - 790, View in Reaxys 4 of 5

Saturation

in solution

Temperature (Solubility (MCS)) [°C]

34.99

Solvent (Solubility (MCS))

water

Comment (Solubility (MCS))

Solubility: 68.05 weight percent

Torres, Daniel R.; Blanco, Luis H.; Vargas, Edgar F.; Martinez, Fleming; Journal of Chemical and Engineering Data; vol. 54; nb. 3; (2009); p. 786 - 790, View in Reaxys 5 of 5

Saturation

in solution

Temperature (Solubility (MCS)) [°C]

39.99

Solvent (Solubility (MCS))

water

Comment (Solubility (MCS))

Solubility: 71.26 weight percent

Torres, Daniel R.; Blanco, Luis H.; Vargas, Edgar F.; Martinez, Fleming; Journal of Chemical and Engineering Data; vol. 54; nb. 3; (2009); p. 786 - 790, View in Reaxys Transport Phenomena (MCS) (1) 1 of 1

Description (Transport Phenomena (MCS))

Diffusion

Solvent (Transport Phenomena (MCS))

various solvent(s)

Partner (Transport Phenomena (MCS))

scopacryl

Gundermann; Dittgen; Jensch; Pharmazie; vol. 42; nb. 8; (1987); p. 553 - 554, View in Reaxys NMR Spectroscopy (10) 1 of 10

Description (NMR Spectroscopy)

Chemical shifts; Spectrum

Nucleus (NMR Spectroscopy)

Solvents (NMR Spectroscopy)

chloroform-d1

Badawi, Hassan M.; Förner, Wolfgang; Ali, Shaikh A.; Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy; vol. 152; (2016); p. 92 - 100, View in Reaxys 2 of 10

Description (NMR Spectroscopy)

Chemical shifts; Spectrum

Nucleus (NMR Spectroscopy)

13C

Solvents (NMR Spectroscopy)

chloroform-d1

Badawi, Hassan M.; Förner, Wolfgang; Ali, Shaikh A.; Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy; vol. 152; (2016); p. 92 - 100, View in Reaxys

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3 of 10

Description (NMR Spectroscopy)

Chemical shifts; Spectrum

Nucleus (NMR Spectroscopy)

Solvents (NMR Spectroscopy)

water-d2

Location

supporting information

Snchez-Leija; Pojman; Luna-Brcenas; Mota-Morales; Journal of Materials Chemistry B; vol. 2; nb. 43; (2014); p. 7495 7501, View in Reaxys 4 of 10

Description (NMR Spectroscopy)

Chemical shifts; Spectrum

Nucleus (NMR Spectroscopy)

35Cl

Frequency (NMR Spectro- 88.1 scopy) [MHz] Location

supporting information

Comment (NMR Spectroscopy)

neat (no solvent, solid phase)

Hamaed, Hiyam; Pawlowski, Jenna M.; Cooper, Benjamin F. T.; Fu, Riqiang; Eichhorn, S. Holger; Schurko, Robert W.; Journal of the American Chemical Society; vol. 130; nb. 33; (2008); p. 11056 - 11065, View in Reaxys 5 of 10

Description (NMR Spectroscopy)

MAS (Magic-Angle Spinning); Chemical shifts; Spectrum

Nucleus (NMR Spectroscopy)

35Cl

Frequency (NMR Spectro- 39.3 scopy) [MHz] Location

supporting information

Comment (NMR Spectroscopy)

neat (no solvent, solid phase)

Description (NMR Spectroscopy)

Spectrum

Nucleus (NMR Spectroscopy)

13C

Location

supporting information

Comment (NMR Spectroscopy)

neat (no solvent, solid phase)

Description (NMR Spectroscopy)

MAS (Magic-Angle Spinning); Chemical shifts; Spectrum

Nucleus (NMR Spectroscopy)

35Cl

Frequency (NMR Spectro- 88.1 scopy) [MHz] Location

supporting information

Comment (NMR Spectroscopy)

neat (no solvent, solid phase)

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8 of 10

Nucleus (NMR Spectroscopy)

Solvents (NMR Spectroscopy)

dimethylsulfoxide-d6; water-d2

Temperature (NMR Spectroscopy) [°C]

Patent; Saint Louis University; US6365590; (2002); (B1) English, View in Reaxys 9 of 10

Description (NMR Spectroscopy)

Spectrum

Nucleus (NMR Spectroscopy)

Solvents (NMR Spectroscopy)

D2O

Paris; Payard; Brecy; et al.; European Journal of Medicinal Chemistry; vol. 15; nb. 1; (1980); p. 55 - 62, View in Reaxys 10 of 10

Description (NMR Spectroscopy)

Chemical shifts

Nucleus (NMR Spectroscopy)

Solvents (NMR Spectroscopy)

D2O

Description (IR Spectroscopy)

ATR (attenuated total reflectance); Spectrum

Location

supporting information

Berton, Paula; Di Bona, Kristin R.; Yancey, Denise; Rizvi, Syed A. A.; Gray, Marquita; Gurau, Gabriela; Shamshina, Julia L.; Rasco, Jane F.; Rogers, Robin D.; ACS Medicinal Chemistry Letters; vol. 8; nb. 5; (2017); p. 498 - 503, View in Reaxys 2 of 5

Description (IR Spectroscopy)

Intensity of IR bands; Bands; Spectrum

Solvent (IR Spectroscopy)

potassium bromide

Badawi, Hassan M.; Förner, Wolfgang; Ali, Shaikh A.; Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy; vol. 152; (2016); p. 92 - 100, View in Reaxys 3 of 5

Description (IR Spectroscopy)

Spectrum

Description (IR Spectroscopy)

ATR (attenuated total reflectance); Bands; Spectrum

Snchez-Leija; Pojman; Luna-Brcenas; Mota-Morales; Journal of Materials Chemistry B; vol. 2; nb. 43; (2014); p. 7495 7501, View in Reaxys 5 of 5

Description (IR Spectroscopy)

Bands

Solvent (IR Spectroscopy)

CHCl3

Comment (IR Spectroscopy)

3270 - 1650 cm**(-1)

Description (UV/VIS Spectroscopy)

Spectrum

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Solvent (UV/VIS Spectroscopy)

water

Absorption Maxima (UV/ VIS) [nm]

197

Soni, Surbhi; Pal, Amalendu; Journal of Solution Chemistry; vol. 45; nb. 5; (2016); p. 665 - 674, View in Reaxys NQR Spectroscopy (1) Description (NQR References Spectroscopy) Nuclear quadrupole Buess, M. L.; Bray, P. J.; Organic Magnetic Resonance; vol. 22; nb. 4; (1984); p. 233 - 236, View in Reaxys resonance Raman Spectroscopy (1) Description (Ram- References an Spectroscopy) Spectrum; Bands

Badawi, Hassan M.; Förner, Wolfgang; Ali, Shaikh A.; Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy; vol. 152; (2016); p. 92 - 100, View in Reaxys

Fluorescence Spectroscopy (1) Description (Fluo- References rescence Spectroscopy) Spectrum Use (87) Use Pattern

Soni, Surbhi; Pal, Amalendu; Journal of Solution Chemistry; vol. 45; nb. 5; (2016); p. 665 - 674, View in Reaxys; Pal, Amalendu; Yadav, Alka; Journal of Molecular Liquids; vol. 222; (2016); p. 471 - 479, View in Reaxys Location

References

Page/Page column title page; 4-6

Patent; ISIFER AB; Edelstam, Greta; (4 pag.); US9849102; (2017); (B2) English, View in Reaxys

endometriosis in a Page/Page column person suffering title page; 4-6 from inflammation due to endometriosis and having an endometriosis implant, by reducing a cytokine MCP-1 related activity level of the endometriosis implant

Patent; ISIFER AB; Edelstam, Greta; (4 pag.); US9849102; (2017); (B2) English, View in Reaxys

Pharmaceuticals

Page/Page column title page

Patent; Zhejiang Esigma Animal Health Co.,Ltd.; Wu, Zhonghua; Zhang, Xiaopeng; Chen, Guicai; Xu, Tianhua; He, Qilei; Wen, Ming; (6 pag.); CN105294477; (2016); (A) Chinese, View in Reaxys

anesthetic

Page/Page column title page

Patent; Zhejiang Esigma Animal Health Co.,Ltd.; Wu, Zhonghua; Zhang, Xiaopeng; Chen, Guicai; Xu, Tianhua; He, Qilei; Wen, Ming; (6 pag.); CN105294477; (2016); (A) Chinese, View in Reaxys

Pharmaceuticals

Page/Page column title page; 7

Patent; PHARMACTİVE ILAÇ SANAYİ VE TİCARET A. Ş.; YILDIRIM, Ersin; IŞIK, Murat, Muhibbi; JAIN, Sandeep; SEZGIN, Asiye; KARAER, Özlem; KARASU, Tolga, Ramazan; YILMAZ, Koray; (11 pag.); WO2016/126217; (2016); (A1) English, View in Reaxys

local anesthetic drug

Page/Page column title page; 7

treatment of mouth Page/Page column ulcers in combina- title page; 7 tion with benzydamine hydrochloride and cetylpyridinium chloride and optionally a zinc salt

treatment of sore Page/Page column throats in combina- title page; 7 tion with benzydamine hydrochloride

Pharmaceuticals

13/467

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and cetylpyridinium chloride and optionally a zinc salt Pharmaceuticals

Page/Page column title page; 35-36

Patent; Loewi LLC; Mulvahill, Mark; US2015/359738; (2015); (A1) English, View in Reaxys

anesthetizing nerve tissue

Page/Page column title page; 35-36

Patent; Loewi LLC; Mulvahill, Mark; US2015/359738; (2015); (A1) English, View in Reaxys

anesthetizing nerve tissue in the trigeminal nerve pathway

Page/Page column title page; 35-36

Patent; Loewi LLC; Mulvahill, Mark; US2015/359738; (2015); (A1) English, View in Reaxys

local anesthetic

Patent; Anika Therapeutics, Inc.; US2005/136122; (2005); (A1) English, View in Reaxys; Patent; Takeda Pharmaceutical Company Limited; EP1595549; (2005); (A1) English, View in Reaxys; Patent; Southall, Michael; Liebel, Frank; US2006/142304; (2006); (A1) English, View in Reaxys; Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys

local anesthetic agent

Patent; Sato Pharmaceutical Co. Ltd.; EP1666024; (2006); (A1) English, View in Reaxys; Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys

analgesic agent

Patent; Wright Medical Technology, Inc.; US2006/88601; (2006); (A1) English, View in Reaxys; Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys

local anesthesia

Patent; CHI MEI FOUNDATION HOSPITAL; US2008/70939; (2008); (A1) English, View in Reaxys

in combination with dextrorotatory morphinan derivatives

Patent; CHI MEI FOUNDATION HOSPITAL; US2008/70939; (2008); (A1) English, View in Reaxys

jellyfish sting

Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys

insect sting

Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys

ant sting

Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys

wasp sting

Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys

painful or irritating skin condition

Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys

mosquito sting

Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys

skin rash

Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys

plant toxins

Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys

poison ivy

Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys

poison oak

Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys

contact dermatitis from allergic reactions

Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys

sunburn

Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys

chigger bite

Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys

fire ant bite

Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys

red bug bite

Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys

Trombicula alfreddugesi bite

Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys

Anti-inflammatory/ antipyretic/analgetic drug

Patent; BIOFARMITALIA S.p.A.; EP1911439; (2008); (A2) English, View in Reaxys

analgesic in composition comprising a hydroxycinnamic

Patent; LIPO CHEMICALS INC.; WO2008/73684; (2008); (A1) English, View in Reaxys

14/467

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acid or methoxycinnamic acid, or mixtures thereof, useful for the treating aging human skin to maintain or improve at least visible indicia of aging local anesthetic of preparation for iontophoresis

Patent; TEIKOKU SEIYAKU CO., LTD.; EP1949895; (2008); (A1) English, View in Reaxys

Anesthetic for throat

Patent; COMBE INCORPORATED; US2008/214664; (2008); (A1) English, View in Reaxys

anesthetic

Patent; Zasler, Nathan D.; Carpenter, Jeffrey; US2007/207193; (2007); (A1) English, View in Reaxys; Patent; Xylos Corporation; EP1849463; (2007); (A2) English, View in Reaxys; Patent; MED Institute, Inc; US2008/81829; (2008); (A1) English, View in Reaxys; Patent; AMCOL INTERNATIONAL CORPORATION; EP1140033; (2005); (B1) English, View in Reaxys

additive of an artificial bone mineral substitute material

Patent; Lidgren, Lars; Nilsson, Malin; US2007/41906; (2007); (A1) English, View in Reaxys

Bone formation

Patent; Lidgren, Lars; Nilsson, Malin; US2007/41906; (2007); (A1) English, View in Reaxys

Bone turnover

Patent; Lidgren, Lars; Nilsson, Malin; US2007/41906; (2007); (A1) English, View in Reaxys

Bone degradation

Patent; Lidgren, Lars; Nilsson, Malin; US2007/41906; (2007); (A1) English, View in Reaxys

Analgesic

Patent; Lidgren, Lars; Nilsson, Malin; US2007/41906; (2007); (A1) English, View in Reaxys

drug reservoir in electrode assembly

Patent; VYTERIS, INC.; WO2007/41475; (2007); (A2) English, View in Reaxys

sodium channel blocker

Patent; THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ALABAMA FOR AND ON BEHALF OF THE UNIVERSITY OF ALABAMA; WO2007/62186; (2007); (A2) English, View in Reaxys

neurodegeneration and neuronal loss associated with protein misfolding or aggregation

Patent; THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ALABAMA FOR AND ON BEHALF OF THE UNIVERSITY OF ALABAMA; WO2007/62186; (2007); (A2) English, View in Reaxys

neurodegenerative disease

Patent; THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ALABAMA FOR AND ON BEHALF OF THE UNIVERSITY OF ALABAMA; WO2007/62186; (2007); (A2) English, View in Reaxys

neurodegeneration and neuronal loss associated with reactive oxygen species

Patent; THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ALABAMA FOR AND ON BEHALF OF THE UNIVERSITY OF ALABAMA; WO2007/62186; (2007); (A2) English, View in Reaxys

Anesthetic

Patent; Mitragotri, Samir; Karande, Pankaj S.; Jain, Amit K.; US2007/269379; (2007); (A1) English, View in Reaxys

Anaesthetic agent

Patent; Shaw, Robert A.; Niculescu, Florin I.; US2007/264238; (2007); (A1) English, View in Reaxys

Prevents both the generation and conduction of the nerve impulse

Patent; Shaw, Robert A.; Niculescu, Florin I.; US2007/264238; (2007); (A1) English, View in Reaxys

reduce pain

Patent; Xylos Corporation; EP1849463; (2007); (A2) English, View in Reaxys

Infection

Patent; Xylos Corporation; EP1849463; (2007); (A2) English, View in Reaxys

wound dressing

Patent; Xylos Corporation; EP1849463; (2007); (A2) English, View in Reaxys

synthetic bone subsitute material

Patent; Wright Medical Technology, Inc.; US2006/88601; (2006); (A1) English, View in Reaxys

15/467

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component in antiitching compositions

Patent; Southall, Michael; Liebel, Frank; US2006/142304; (2006); (A1) English, View in Reaxys

an analgesic

Patent; Richelsoph, Kelly C.; Morris, Linda; Cole, Jantzen A.; US2006/188541; (2006); (A1) English, View in Reaxys

an anesthetic

Patent; Richelsoph, Kelly C.; Morris, Linda; Cole, Jantzen A.; US2006/188541; (2006); (A1) English, View in Reaxys

anaesthetic agent

Patent; ANIMAL ETHICS; WO2006/96913; (2006); (A1) English, View in Reaxys

anaesthesia

Patent; ANIMAL ETHICS; WO2006/96913; (2006); (A1) English, View in Reaxys

wound

Patent; ANIMAL ETHICS; WO2006/96913; (2006); (A1) English, View in Reaxys

laceration

Patent; ANIMAL ETHICS; WO2006/96913; (2006); (A1) English, View in Reaxys

surgical incision

Patent; ANIMAL ETHICS; WO2006/96913; (2006); (A1) English, View in Reaxys

ulcer

Patent; ANIMAL ETHICS; WO2006/96913; (2006); (A1) English, View in Reaxys

abrasion

Patent; ANIMAL ETHICS; WO2006/96913; (2006); (A1) English, View in Reaxys

burn

Patent; ANIMAL ETHICS; WO2006/96913; (2006); (A1) English, View in Reaxys

topical medicament

Patent; ANIMAL ETHICS; WO2006/96913; (2006); (A1) English, View in Reaxys

wound caused by mulesing

Patent; ANIMAL ETHICS; WO2006/96913; (2006); (A1) English, View in Reaxys

wound caused by castration

Patent; ANIMAL ETHICS; WO2006/96913; (2006); (A1) English, View in Reaxys

chemical mulesing

Patent; ANIMAL ETHICS; WO2006/96913; (2006); (A1) English, View in Reaxys

branding

Patent; ANIMAL ETHICS; WO2006/96913; (2006); (A1) English, View in Reaxys

Anestetic

Patent; ROXRO PHARMA, INC.; WO2006/71601; (2006); (A2) English, View in Reaxys

component comosition for the treating mammalian skin and hair

Patent; LIPO CHEMICALS, INC.; WO2006/36557; (2006); (A1) English, View in Reaxys

ear infections

Patent; Johnson, John Moore; US2006/57226; (2006); (A1) English, View in Reaxys

anesthetic agent

Patent; Johnson, John Moore; US2006/57226; (2006); (A1) English, View in Reaxys

analgesic agent

Page/Page column 10

Patent; CHUGAI SEIYAKU KABUSHIKI KAISHA; EP1634874; (2006); (A1) English, View in Reaxys

dermopharmaceutical active agent in a composition containing kukui nut oil

Patent; PHARMACIA and UPJOHN COMPANY; EP954278; (2005); (B1) English, View in Reaxys

pharmacologically active substance in ophthalmic insert

Patent; El Meski, Said; Tourrette, Philippe; Aiache, Jean-Marc; Di Battista, Marie; Serpin, Gilbert; US2005/118231; (2005); (A1) English, View in Reaxys

bioactive agent in crosslinked hyaluronic acid-based composition

Patent; Anika Therapeutics, Inc.; US2005/136122; (2005); (A1) English, View in Reaxys

active agent for the sustained release composition

Patent; Sojka, Milan; US2005/129759; (2005); (A1) English, View in Reaxys

sustained-release preparation

Patent; Takeda Pharmaceutical Company Limited; EP1595549; (2005); (A1) English, View in Reaxys

Local anesthetic for a composition

Patent; Showa Yakuhin Kako Co., Ltd; EP1582220; (2005); (A1) English, View in Reaxys

local anaesthetic for preparing the

Patent; Rippon, Mark Geoffrey; Meadows, John; US2005/64021; (2005); (A1) English, View in Reaxys

16/467

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wound dressing comprising poloxamer for an exudative wound topically active agent

Patent; AMCOL INTERNATIONAL CORPORATION; EP1140033; (2005); (B1) English, View in Reaxys

active agent controlled release compositions

Patent; AMCOL INTERNATIONAL CORPORATION; EP1140033; (2005); (B1) English, View in Reaxys

Soothing agent for eye drops

Patent; Senju Pharmaceutical Co., Ltd.; EP1457212; (2004); (A1) English, View in Reaxys

External analgesic

Patent; Le Roy II, Charles Richard; Le Roy, Deborah Gay; US2004/247707; (2004); (A1) English, View in Reaxys

Local anesthetics

Patent; J.B. Chemicals and Pharmaceuticals Ltd.; WO2004/253; (2003); (A1) English, View in Reaxys

Quantum Chemical Calculations (1) Calculated Proper- Method (Quantum ties Chemical Calculations)

Location

References

NMR shifts, sigDFT - density func- supporting informa- Badawi, Hassan M.; Förner, Wolfgang; Ali, Shaikh A.; Spectrochimica nals, intensities, tional methods tion Acta - Part A: Molecular and Biomolecular Spectroscopy; vol. 152; (2016); transition moments; p. 92 - 100, View in Reaxys Total energy Medchem (1220) 1 of 1220

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lignocaine HCl

Substance Dose

3.46000 µM

Measurement Parameter

Rate

Unit

µmol/x min/mg protein

Measurement Object

ALL

Quantitative value

2.85

Deviation

0.440000

Deacon; Lennard; Bax; British Journal of Clinical Pharmacology; vol. 12; nb. 3; (1981); p. 429 - 431, View in Reaxys 2 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Name

Spontaneous activity

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dosing Regimen

Single

Measurement Parameter

ED50

Unit

mg/kg

Quantitative value

2.65

17/467

2018-05-14 08:43:54

Cheng, Kuang-I; Shieh, Ja-Ping; Lin, Ching-Nan; Chu, Koung-Shing; Kwan, Aij-Lie; Hou, Chia-Hui; Wang, Jhi-Joung; Drug Development Research; vol. 67; nb. 12; (2006); p. 905 - 909, View in Reaxys 3 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Name

Spontaneous activity

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dosing Regimen

Single

Measurement Parameter

ED50

Unit

mg/kg

Quantitative value

2.31

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : CAT-2 induced neurodegeneration; effect onTarget : C. elegans, nematode Pdat-1::CAT-2Bioassay : Example 7; Lidocaine and meclofenamic acid protect against 6'OHDA through different mechanisms; To test whether meclofenamic acid or lidocaine can down-regulate DAT-I protein level independent of torsinA function, we used a transgenic line P<f&oslash;.;::GFP::DAT-l previously described

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

title compound incresed CAT-2 induced neurodegeneration by 7.9%

Measurement Parameter

qualitative

Patent; THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ALABAMA FOR AND ON BEHALF OF THE UNIVERSITY OF ALABAMA; WO2007/62186; (2007); (A2) English, View in Reaxys 5 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : DAT-1 protein level; effect onTarget : C. elegans, nematode Pdat-1::GFP::DAT-1Bioassay : Example 7; Lidocaine and meclofenamic acid protect against 6'OHDA through different mechanisms; To test whether meclofenamic acid or lidocaine can down-regulate DAT-I protein level independent of torsinA function, we used a transgenic line P<f&oslash;.;::GFP::DAT-l previously described

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

title compound (1.85 mmol/l) down-regulated level of DAT-1 protein (decreased fluorescence intensity from 1970 A.U. in the control to 1612 A.U. and decreased percentage neurons with cell body and dendritic/axonal GFP from 70% in the control to 30%)

Measurement Parameter

qualitative

Patent; THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ALABAMA FOR AND ON BEHALF OF THE UNIVERSITY OF ALABAMA; WO2007/62186; (2007); (A2) English, View in Reaxys 6 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : 6-hydroxydopamine (6-OHDA)-mediated neurodegeneration; effect onTarget : C. elegans, nematode Pdat-1::GFP + Pdat-1::torsinA + Pdat-1::torsinA(ΔE)Bioassay : Example 2; Neuroprotection of dopaminergic neurons in C. elegans by compounds identified from the Prestwick small molecule library; Previous studies have established that the "CEP" and "ADE" mechanosensory neurons in C. elegans undergo readily discernable neuronal degeneration after treatment with the

18/467

2018-05-14 08:43:54

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

title compound (0.5 mg/ml) significantly reduced 6-OHDA-mediated neurodegeneration; diagram given

Measurement Parameter

qualitative

Patent; THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ALABAMA FOR AND ON BEHALF OF THE UNIVERSITY OF ALABAMA; WO2007/62186; (2007); (A2) English, View in Reaxys 7 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : 6-hydroxydopamine (6-OHDA)-mediated neurodegeneration; effect onTarget : C. elegans, nematode Pdat-1::GFPBioassay : Example 2; Neuroprotection of dopaminergic neurons in C. elegans by compounds identified from the Prestwick small molecule library; Previous studies have established that the "CEP" and "ADE" mechanosensory neurons in C. elegans undergo readily discernable neuronal degeneration after treatment with the

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

title compound (0.5 mg/ml) significantly reduced 6-OHDA-mediated neurodegeneration; diagram given

Measurement Parameter

qualitative

Patent; THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ALABAMA FOR AND ON BEHALF OF THE UNIVERSITY OF ALABAMA; WO2007/62186; (2007); (A2) English, View in Reaxys 8 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

New Zealand White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

5.36000 µmol/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

heart rate

Unit

b.p.m

Measurement Object

Heart Rate

Quantitative value

231

Deviation

13.9000

Concomitants: Compound RN

24140824; 4284264

Concomitants: Compound name

Chloralose; Methohexital sodium

Concomitants: Compound role

ANA; ANA

Carlsson; Drews; Duker; Schiller-Linhardt; Journal of Pharmacology and Experimental Therapeutics; vol. 267; nb. 3; (1993); p. 1076 - 1080, View in Reaxys 9 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

New Zealand White (rabbit)

19/467

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Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

16 µmol/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

heart rate

Unit

b.p.m

Measurement Object

Heart Rate

Quantitative value

270

Deviation

12.8000

Concomitants: Compound RN

24140824; 4284264

Concomitants: Compound name

Chloralose; Methohexital sodium

Concomitants: Compound role

ANA; ANA

Carlsson; Drews; Duker; Schiller-Linhardt; Journal of Pharmacology and Experimental Therapeutics; vol. 267; nb. 3; (1993); p. 1076 - 1080, View in Reaxys 10 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

New Zealand White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

5.36000 µmol/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

QRS interval

Unit

Quantitative value

Deviation

3.40000

Concomitants: Compound RN

24140824; 4284264

Concomitants: Compound name

Chloralose; Methohexital sodium

Concomitants: Compound role

ANA; ANA

Carlsson; Drews; Duker; Schiller-Linhardt; Journal of Pharmacology and Experimental Therapeutics; vol. 267; nb. 3; (1993); p. 1076 - 1080, View in Reaxys 11 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

New Zealand White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

20/467

2018-05-14 08:43:54

Substance Dose

16 µmol/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

QRS interval

Unit

Quantitative value

Deviation

2.90000

Concomitants: Compound RN

24140824; 4284264

Concomitants: Compound name

Chloralose; Methohexital sodium

Concomitants: Compound role

ANA; ANA

Carlsson; Drews; Duker; Schiller-Linhardt; Journal of Pharmacology and Experimental Therapeutics; vol. 267; nb. 3; (1993); p. 1076 - 1080, View in Reaxys 12 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

New Zealand White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

5.36000 µmol/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

QT interval

Unit

Quantitative value

128

Deviation

7.60000

Concomitants: Compound RN

24140824; 4284264

Concomitants: Compound name

Chloralose; Methohexital sodium

Concomitants: Compound role

ANA; ANA

Carlsson; Drews; Duker; Schiller-Linhardt; Journal of Pharmacology and Experimental Therapeutics; vol. 267; nb. 3; (1993); p. 1076 - 1080, View in Reaxys 13 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

New Zealand White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

16 µmol/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

21/467

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Measurement Parameter

QT interval

Unit

Quantitative value

116

Deviation

8.40000

Concomitants: Compound RN

24140824; 4284264

Concomitants: Compound name

Chloralose; Methohexital sodium

Concomitants: Compound role

ANA; ANA

Carlsson; Drews; Duker; Schiller-Linhardt; Journal of Pharmacology and Experimental Therapeutics; vol. 267; nb. 3; (1993); p. 1076 - 1080, View in Reaxys 14 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

New Zealand White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

5.36000 µmol/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

heart rate decrease

Unit

b.p.m

Measurement Object

Maximum decrease of HR

Quantitative value

215

Deviation

15.5000

Statistical sgnificance (pvalue)

0.05

Concomitants: Compound RN

6318453; 8159235; 24140824; 4284264

Concomitants: Compound name

Methoxamine hydrochloride; Almokalant; Chloralose; Methohexital sodium

Concomitants: Compound role

OCV; IAV; ANA; ANA

Carlsson; Drews; Duker; Schiller-Linhardt; Journal of Pharmacology and Experimental Therapeutics; vol. 267; nb. 3; (1993); p. 1076 - 1080, View in Reaxys 15 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

New Zealand White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

16 µmol/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

heart rate decrease

22/467

2018-05-14 08:43:54

Unit

b.p.m

Measurement Object

Maximum decrease of HR

Quantitative value

229

Deviation

9.20000

Statistical sgnificance (Qualitative)

***

Statistical sgnificance (pvalue)

0.001

Concomitants: Compound RN

6318453; 8159235; 24140824; 4284264

Concomitants: Compound name

Methoxamine hydrochloride; Almokalant; Chloralose; Methohexital sodium

Concomitants: Compound role

OCV; IAV; ANA; ANA

Carlsson; Drews; Duker; Schiller-Linhardt; Journal of Pharmacology and Experimental Therapeutics; vol. 267; nb. 3; (1993); p. 1076 - 1080, View in Reaxys 16 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

New Zealand White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

5.36000 µmol/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

QT interval

Unit

Measurement Object

maximum prolongation of QT

Quantitative value

175

Deviation

15.9000

Statistical sgnificance (Qualitative)

***

Statistical sgnificance (pvalue)

0.001

Concomitants: Compound RN

6318453; 8159235; 24140824; 4284264

Concomitants: Compound name

Methoxamine hydrochloride; Almokalant; Chloralose; Methohexital sodium

Concomitants: Compound role

OCV; IAV; ANA; ANA

Carlsson; Drews; Duker; Schiller-Linhardt; Journal of Pharmacology and Experimental Therapeutics; vol. 267; nb. 3; (1993); p. 1076 - 1080, View in Reaxys 17 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

New Zealand White (rabbit)

Substance RN

3917968View in Reaxys

23/467

2018-05-14 08:43:54

Substance Name

Lidocaine

Substance Dose

16 µmol/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

QT interval

Unit

Measurement Object

maximum prolongation of QT

Quantitative value

159

Deviation

10.3000

Statistical sgnificance (Qualitative)

***

Statistical sgnificance (pvalue)

0.001

Concomitants: Compound RN

6318453; 8159235; 24140824; 4284264

Concomitants: Compound name

Methoxamine hydrochloride; Almokalant; Chloralose; Methohexital sodium

Concomitants: Compound role

OCV; IAV; ANA; ANA

Carlsson; Drews; Duker; Schiller-Linhardt; Journal of Pharmacology and Experimental Therapeutics; vol. 267; nb. 3; (1993); p. 1076 - 1080, View in Reaxys 18 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

New Zealand White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

12.8000 µmol/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

QT interval

Unit

Measurement Object

Time increase for onset of arrhytmia vs control group

Quantitative value

144

Deviation

5.10000

Concomitants: Compound RN

6318453; 8159235; 24140824; 4284264

Concomitants: Compound name

Methoxamine hydrochloride; Almokalant; Chloralose; Methohexital sodium

Concomitants: Compound role

OCV; IAV; ANA; ANA

Carlsson; Drews; Duker; Schiller-Linhardt; Journal of Pharmacology and Experimental Therapeutics; vol. 267; nb. 3; (1993); p. 1076 - 1080, View in Reaxys 19 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

24/467

2018-05-14 08:43:54

Biological Species/NCBI ID

New Zealand White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

12.8000 µmol/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

QT interval

Unit

Measurement Object

Time increase for onset of arrhytmia vs control group

Quantitative value

152

Deviation

6.10000

Concomitants: Compound RN

6318453; 8159235; 24140824; 4284264

Concomitants: Compound name

Methoxamine hydrochloride; Almokalant; Chloralose; Methohexital sodium

Concomitants: Compound role

OCV; IAV; ANA; ANA

Carlsson; Drews; Duker; Schiller-Linhardt; Journal of Pharmacology and Experimental Therapeutics; vol. 267; nb. 3; (1993); p. 1076 - 1080, View in Reaxys 20 of 1220

Target Name

voltage-gated sodium channel [Rattus norvegicus]

Target Synonyms

voltage-gated sodium channel

Target, Subunit, Species

voltage-gated sodium channel [Rattus norvegicus]

Target Mutant/Chimera Details

voltage-gated sodium channel [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Wistar rat

Organs/Tissues

heart right ventricle

Substance RN

3917968View in Reaxys

Substance Name

lignocaine

Substance Dose

0.000100000 M

Measurement Parameter

APA

Unit

Quantitative value

111

Deviation

Concomitants: Compound RN

24140898; 6552119

Concomitants: Compound name

Atropine sulfate; Guanethidine sulfate

Concomitants: Compound role

COM; COM

25/467

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21 of 1220

22 of 1220

Target Name

voltage-gated sodium channel [Rattus norvegicus]

Target Synonyms

voltage-gated sodium channel

Target, Subunit, Species

voltage-gated sodium channel [Rattus norvegicus]

Target Mutant/Chimera Details

voltage-gated sodium channel [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Wistar rat

Organs/Tissues

heart right ventricle

Substance RN

3917968View in Reaxys

Substance Name

lignocaine

Substance Dose

0.000100000 M

Measurement Parameter

Delta

Unit

Measurement Object

Threshold potential

Quantitative value

-80

Deviation

Concomitants: Compound RN

24140898; 6552119

Concomitants: Compound name

Atropine sulfate; Guanethidine sulfate

Concomitants: Compound role

COM; COM

Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Route of Adm.

subcutaneous administration

Substance Dosing Regimen

Single

Measurement Parameter

ED50

Unit

mg/kg

Measurement Object

anesthesic activity

Quantitative value

Patent; CHI MEI FOUNDATION HOSPITAL; US2008/70939; (2008); (A1) English, View in Reaxys 23 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Name

Lethality

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

26/467

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Substance Name

Lidocaine hydrochloride

Substance Route of Adm.

intraperitoneal administration

Substance Dosing Regimen

Single

Measurement Parameter

LD50

Unit

mg/kg

Measurement Object

Lethality

Quantitative value

196

Patent; CHI MEI FOUNDATION HOSPITAL; US2008/70939; (2008); (A1) English, View in Reaxys 24 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : skin penetration Bioassay : cadaver trunk skinExample 4 Transdermal delivery of Lidocaine by microbial cellulose in vitro using human cadaver skin diffusion cell study The study was carried out to test microbial cellulose containing a solution of 10% lidocaine HCl in water tested on two different skin donors using a finite dose in vitro cadaver

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Route of Adm.

transdermal administration

Qualitative Results

treatment with the title compound resulted to rate of penetration of 0.270-0.645 &micro;g/cm2/hr in an un-occuded chamber and 1.977-2.123 &micro;g/cm2/hr in an occuded chamber; higher transdermal penetration with microbial cellulose with 10% of the title

Measurement Parameter

qualitative

Patent; Xylos Corporation; EP1849463; (2007); (A2) English, View in Reaxys 25 of 1220

Substance Effect

Analgesic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : analgesicTo verify the applicational functionality of the solid composition obtained, an in vivo test is carried out: a film piece is deposited on the rear of the previously wetted forearm of 6 persons of female sex. This film piece is soaked with 1 ml of water then, while making rapid circular movements, complete

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

treatment with the title compound showed analgesic effect

Measurement Parameter

qualitative

Patent; BIOFARMITALIA S.p.A.; EP1911439; (2008); (A2) English, View in Reaxys 26 of 1220

Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

27/467

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Substance Dose

25 µM

Measurement Parameter

fu (unbound fraction)

Quantitative value

0.98 - 1.02

Wattanachai, Nitsupa; Tassaneeyakul, Wichittra; Rowland, Andrew; Elliot, David J.; Bowalgaha, Kushari; Knights, Kathleen M.; Miners, John O.; Drug Metabolism and Disposition; vol. 40; nb. 5; (2012); p. 982 - 989, View in Reaxys 27 of 1220

Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Escherichia coli

Cell Fraction

Membrane

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

25 µM

Measurement Parameter

fu (unbound fraction)

Quantitative value

0.98 - 1.02

Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

25 µM

Measurement Parameter

fu (unbound fraction)

Quantitative value

0.88

Deviation

0.0300000

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

25 µM

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Measurement Object

HIGH

Quantitative value

186

Deviation

28/467

2018-05-14 08:43:54

Measurement pX

3.73

Metabolite RN

2417108; 2208089

Metabolite name

Norlidocaine; Acetaminophen

Concomitants: Compound RN

24140787; 3885115

Concomitants: Compound name

Glucose-6-phosphate; NADP

Concomitants: Compound role

COM; COE

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

25 µM

Measurement Parameter

Vmax

Unit

pmol/min/mg protein

Measurement Object

HIGH

Quantitative value

978

Deviation

517

Metabolite RN

2417108; 2208089

Metabolite name

Norlidocaine; Acetaminophen

Concomitants: Compound RN

24140787; 3885115

Concomitants: Compound name

Glucose-6-phosphate; NADP

Concomitants: Compound role

COM; COE

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

25 µM

Measurement Parameter

Km (Michaelis constant)

Unit

µM

29/467

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Measurement Object

LOW

Quantitative value

1723

Deviation

318

Measurement pX

2.76

Metabolite RN

2417108; 2208089

Metabolite name

Norlidocaine; Acetaminophen

Concomitants: Compound RN

24140787; 3885115

Concomitants: Compound name

Glucose-6-phosphate; NADP

Concomitants: Compound role

COM; COE

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

25 µM

Measurement Parameter

Vmax

Unit

pmol/min/mg protein

Measurement Object

LOW

Quantitative value

4886

Deviation

1470

Metabolite RN

2417108; 2208089

Metabolite name

Norlidocaine; Acetaminophen

Concomitants: Compound RN

24140787; 3885115

Concomitants: Compound name

Glucose-6-phosphate; NADP

Concomitants: Compound role

COM; COE

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

30/467

2018-05-14 08:43:54

Substance Dose

25 µM

Measurement Parameter

CLint

Unit

µL/min/mg protein

Measurement Object

HIGH

Quantitative value

5.26

Metabolite RN

2417108; 2208089

Metabolite name

Norlidocaine; Acetaminophen

Concomitants: Compound RN

24140787; 3885115

Concomitants: Compound name

Glucose-6-phosphate; NADP

Concomitants: Compound role

COM; COE

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

25 µM

Measurement Parameter

CLint

Unit

µL/min/mg protein

Measurement Object

LOW

Quantitative value

2.84

Metabolite RN

2417108; 2208089

Metabolite name

Norlidocaine; Acetaminophen

Concomitants: Compound RN

24140787; 3885115

Concomitants: Compound name

Glucose-6-phosphate; NADP

Concomitants: Compound role

COM; COE

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

31/467

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Substance Dose

25 µM

Measurement Parameter

CLint

Unit

µL/min/mg protein

Measurement Object

HIGH

Quantitative value

18.4

Metabolite RN

2417108; 2208089

Metabolite name

Norlidocaine; Acetaminophen

Concomitants: Compound RN

24140787; 3885115

Concomitants: Compound name

Glucose-6-phosphate; NADP

Concomitants: Compound role

COM; COE

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

25 µM

Measurement Parameter

CLint

Unit

µL/min/mg protein

Measurement Object

LOW

Quantitative value

3.41

Metabolite RN

2417108; 2208089

Metabolite name

Norlidocaine; Acetaminophen

Concomitants: Compound RN

24140787; 3885115

Concomitants: Compound name

Glucose-6-phosphate; NADP

Concomitants: Compound role

COM; COE

Target Name

Cytochrome P450 1A2 [human]

Target Synonyms

cholesterol 25-hydroxylase; cyp1a2; cypia2; cytochrome p(3)450; cytochrome p450 1a2; cytochrome p450 4; cytochrome p450-p3

Target Uniprot ID

p05177

Target PDB ID

2hi4

Target, Subunit, Species

Cytochrome P450 1A2 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild

32/467

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Target Species (Bioactivity)

human

Target Transfection

Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

Escherichia coli

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

25 µM

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Quantitative value

4940

Deviation

204

Measurement pX

2.31

Metabolite RN

2417108; 2208089

Metabolite name

Norlidocaine; Acetaminophen

Concomitants: Compound RN

24140787; 3885115

Concomitants: Compound name

Glucose-6-phosphate; NADP

Concomitants: Compound role

COM; COE

Target Name

Cytochrome P450 1A2 [human]

Target Synonyms

cholesterol 25-hydroxylase; cyp1a2; cypia2; cytochrome p(3)450; cytochrome p450 1a2; cytochrome p450 4; cytochrome p450-p3

Target Uniprot ID

p05177

Target PDB ID

2hi4

Target, Subunit, Species

Cytochrome P450 1A2 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

Escherichia coli

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

25 µM

Measurement Parameter

Vmax

Unit

pmol/min/pmol target

Quantitative value

274

33/467

2018-05-14 08:43:54

Deviation

Metabolite RN

2417108; 2208089

Metabolite name

Norlidocaine; Acetaminophen

Concomitants: Compound RN

24140787; 3885115

Concomitants: Compound name

Glucose-6-phosphate; NADP

Concomitants: Compound role

COM; COE

Target Name

Cytochrome P450 1A2 [human]

Target Synonyms

cholesterol 25-hydroxylase; cyp1a2; cypia2; cytochrome p(3)450; cytochrome p450 1a2; cytochrome p450 4; cytochrome p450-p3

Target Uniprot ID

p05177

Target PDB ID

2hi4

Target, Subunit, Species

Cytochrome P450 1A2 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

Escherichia coli

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

25 µM

Measurement Parameter

CLint

Unit

µL/min/pmol target

Quantitative value

0.0555

Metabolite RN

2417108; 2208089

Metabolite name

Norlidocaine; Acetaminophen

Concomitants: Compound RN

24140787; 3885115

Concomitants: Compound name

Glucose-6-phosphate; NADP

Concomitants: Compound role

COM; COE

Target Name

Cytochrome P450 1A2 [human]

Target Synonyms

cholesterol 25-hydroxylase; cyp1a2; cypia2; cytochrome p(3)450; cytochrome p450 1a2; cytochrome p450 4; cytochrome p450-p3

Target Uniprot ID

p05177

Target PDB ID

2hi4

Target, Subunit, Species

Cytochrome P450 1A2 [human]

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Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

Escherichia coli

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

25 µM

Measurement Parameter

CLint

Unit

µL/min/pmol target

Quantitative value

0.23

Metabolite RN

2417108; 2208089

Metabolite name

Norlidocaine; Acetaminophen

Concomitants: Compound RN

24140787; 3885115

Concomitants: Compound name

Glucose-6-phosphate; NADP

Concomitants: Compound role

COM; COE

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

25 µM

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Measurement Object

HIGH

Quantitative value

63.4

Deviation

37.8000

Measurement pX

4.2

Metabolite RN

2417108; 2208089

Metabolite name

Norlidocaine; Acetaminophen

Concomitants: Compound RN

24140787; 3885115

Concomitants: Compound name

Glucose-6-phosphate; NADP

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Concomitants: Compound role

COM; COE

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

25 µM

Measurement Parameter

Vmax

Unit

pmol/min/mg protein

Measurement Object

HIGH

Quantitative value

1165

Deviation

873

Metabolite RN

2417108; 2208089

Metabolite name

Norlidocaine; Acetaminophen

Concomitants: Compound RN

24140787; 3885115

Concomitants: Compound name

Glucose-6-phosphate; NADP

Concomitants: Compound role

COM; COE

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

25 µM

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Measurement Object

LOW

Quantitative value

1504

Deviation

373

Measurement pX

2.82

Metabolite RN

2417108; 2208089

Metabolite name

Norlidocaine; Acetaminophen

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Concomitants: Compound RN

24140787; 3885115

Concomitants: Compound name

Glucose-6-phosphate; NADP

Concomitants: Compound role

COM; COE

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

25 µM

Measurement Parameter

Vmax

Unit

pmol/min/mg protein

Measurement Object

LOW

Quantitative value

5127

Deviation

1697

Metabolite RN

2417108; 2208089

Metabolite name

Norlidocaine; Acetaminophen

Concomitants: Compound RN

24140787; 3885115

Concomitants: Compound name

Glucose-6-phosphate; NADP

Concomitants: Compound role

COM; COE

Target Name

Cytochrome P450 1A2 [human]

Target Synonyms

cholesterol 25-hydroxylase; cyp1a2; cypia2; cytochrome p(3)450; cytochrome p450 1a2; cytochrome p450 4; cytochrome p450-p3

Target Uniprot ID

p05177

Target PDB ID

2hi4

Target, Subunit, Species

Cytochrome P450 1A2 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

Escherichia coli

Substance RN

3917968View in Reaxys

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Substance Name

lidocaine

Substance Dose

25 µM

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Quantitative value

822

Deviation

Measurement pX

3.09

Metabolite RN

2417108; 2208089

Metabolite name

Norlidocaine; Acetaminophen

Concomitants: Compound RN

24140787; 3885115

Concomitants: Compound name

Glucose-6-phosphate; NADP

Concomitants: Compound role

COM; COE

Target Name

Cytochrome P450 1A2 [human]

Target Synonyms

cholesterol 25-hydroxylase; cyp1a2; cypia2; cytochrome p(3)450; cytochrome p450 1a2; cytochrome p450 4; cytochrome p450-p3

Target Uniprot ID

p05177

Target PDB ID

2hi4

Target, Subunit, Species

Cytochrome P450 1A2 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

Escherichia coli

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

25 µM

Measurement Parameter

Vmax

Unit

pmol/min/pmol target

Quantitative value

189

Deviation

Metabolite RN

2417108; 2208089

Metabolite name

Norlidocaine; Acetaminophen

Concomitants: Compound RN

24140787; 3885115

Concomitants: Compound name

Glucose-6-phosphate; NADP

Concomitants: Compound role

COM; COE

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Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

rectal absorption in Sprague-Dawley rat: plot

Measurement Parameter

qualitative

Nishihata; Rytting; Higuchi; Journal of Pharmaceutical Sciences; vol. 71; nb. 8; (1982); p. 865 - 868, View in Reaxys 48 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : |transport Target : human dura-arachnoid membraneBioassay : membrane obtained post mortem; diffusion of title comp. through the membrane in pH 7.4 and 4.0 phosphate-buffered saline (PBS); diffusion cell divided with the membrane; UV-spectrometry at 287 nm

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

50 mg/L

Qualitative Results

permeability for title comp. were significantly greater at pH 7.4 than at 4.0; graphical representation

Measurement Parameter

qualitative

Grouls, Rene; Korsten, Erik; Ackerman, Eric; Hellebrekers, Ludo; Van Zundert, Andre; Breimer, Douwe; European Journal of Pharmaceutical Sciences; vol. 12; nb. 2; (2000); p. 125 - 131, View in Reaxys 49 of 1220

Substance Effect

Hemodynamic

Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Target : New Zealand white rabbitBioassay : effects of title comp. in anestgetized rabbits; mean arterial pressure (MAP), heart rate (HR, electrocardiography), and title comp. levels in plama (GC) measured during perfusion

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

0.800000 mM

Substance Route of Adm.

intracerebroventricular administration

Qualitative Results

dose-dependently increased MAP; 0.8 and 4 mmol/l significantly increased HR, higher doses did not; plasma level of title comp. was 0.31 μg/ml after 10 min perfusion with 16 mmol/l

Measurement Parameter

qualitative

Bernards, Christopher M.; European Journal of Pharmacology; vol. 307; nb. 1; (1996); p. 33 - 39, View in Reaxys 50 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

pharmacokinetics: delivery from the drug-dosed electrode (kinetics of dosing and washout phases, absorption data) for alone and in combination with tolazoline*HCl and norepinephrine (isolated perfused porcine skin flap, 1.45-31.6percent concentrations)

Measurement Parameter

qualitative

Williams; Riviere; Journal of Pharmaceutical Sciences; vol. 82; nb. 11; (1993); p. 1080 - 1084, View in Reaxys 51 of 1220

Bioassay Category

In Vitro (Efficacy)

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Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

inhibitory effect on carbachol-induced catecholamine release from chromaffin cells IC50 = 210 μM

Measurement Parameter

qualitative

Kawabata; Sumikawa; Kamibayashi; Fukumitsu; Hayashi; Takada; Yoshiya; Journal of Pharmacy and Pharmacology; vol. 45; nb. 7; (1993); p. 632 - 635, View in Reaxys 52 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

in vivo local anesthetic activity (corneal anesthesia in rabbit and mouse tail anesthesia: IC50 = 1.6*10-2 mol/L)

Measurement Parameter

qualitative

Caliendo; Greco; Grieco; Mattace Raso; Meli; Novellino; Perissutti; Santagada; European Journal of Medicinal Chemistry; vol. 31; nb. 2; (1996); p. 99 - 104, View in Reaxys 53 of 1220

54 of 1220

Target Name

enzyme

Target Synonyms

enzyme

Target, Subunit, Species

enzyme

Target Mutant/Chimera Details

enzyme:Wild

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : |enzyme; inhib. of Bioassay : control: untreated cells; PMA: 4ω-phorbol 12-myristate 13-acetate; PBut (phosphatidylbutanol) accumulation, index of phospholipase D activity <3H>oleic acidlabeled, differentiated cells preincubated with title comp., 30 min; cytochalasin B added for last 5 min of incub.; stimulated with PMA at 37 deg C in presence of butanol; lipids extracted; separated by TLC; <3H>PBut levels detd. by LSC

Biological Species/NCBI ID

human

Cells/Cell Lines

HL-60 cell line

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

0.000500000 M

Qualitative Results

title comp. significantly suppressed the PMA-induced phospholipase D activation; diagram

Measurement Parameter

qualitative

Substance Effect

Neuroregulatoric

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Bioassay : aCSF: artifical cerebrospinal fluid; control: vehicle firing activity of multiple prefrontal cortex neurons was recorded simultaneously using array of 12 tetrodes; rats were freely moving; activity was determined at baseline, during final 5 min of each title comp. exposure period, and after 30-min washout

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Name

178204

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Qualitative Results

title comp. reduced neuronal firing activity only at 74 mmol/l; effect was variable among individual neurons; title comp. abolished firing in 15% neurons; activity partially recovered after washout, but was lower than baseline

Measurement Parameter

qualitative

Van Duuren; Van Der Plasse; Van Der Blom; Joosten; Mulder; Pennartz; Feenstra, Matthijs G. P.; Journal of Pharmacology and Experimental Therapeutics; vol. 323; nb. 1; (2007); p. 61 - 69, View in Reaxys 55 of 1220

Substance Effect

Myocontractant

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Target : Wistar albino rat phrenic nerve diaphragmBioassay : indirect stimulation: through nerve, pulse duration 0.05 ms, voltage supramaximum ca. 2-3 V; t1/2: time to 50 percent inhibition of twitch amplitude; SLS: sodium lauryl sulfate, 5.0E-4 mol/l rib end of diaphragm preparation put into suspension fork with two electrodes; twitch amplitude inhibited by SLS during indirect stimulation; tendinous end of muscle connected to force transducer

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

0.000210000 M

Qualitative Results

title comp. increased t1/2 of SLS from 12.0 to 16.0 min

Measurement Parameter

qualitative

Herlofson, Bente Brokstad; Brodin, Pal; Roed, Asbjorn; Pharmacology and Toxicology; vol. 79; nb. 5; (1996); p. 217 - 224, View in Reaxys 56 of 1220

Target Name

Cytochrome P450 3A4 [human]

Target Synonyms

1,8-cineole 2-exo-monooxygenase; albendazole monooxygenase; albendazole sulfoxidase; cholesterol 25-hydroxylase; cyp3a3; cyp3a4; cypiiia3; cypiiia4; cytochrome p450 3a3; cytochrome p450 3a4; cytochrome p450 hlp; cytochrome p450 nf-25; cytochrome p450-pcn1; nifedipine oxidase; quinine 3-monooxygenase; taurochenodeoxycholate 6-alpha-hydroxylase

Target Uniprot ID

p08684

Target PDB ID

1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

CLint

Unit

µL/min/mg protein

Quantitative value

3.974

Metabolite RN

2417108; 2127970

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58 of 1220

Metabolite name

MEGX; 3-OH-lidocaine

Concomitants: Compound RN

77547; 77911

Concomitants: Compound name

Troleandomycin; NADPH

Concomitants: Compound role

COM; COE

Target Name

Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p08684

Target PDB ID

1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

CLint

Unit

µL/min/mg protein

Quantitative value

70.07

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Concomitants: Compound RN

77547; 77911

Concomitants: Compound name

Troleandomycin; NADPH

Concomitants: Compound role

COM; COE

Target Name

Cytochrome P450 1A2 [human]

Target Synonyms

cholesterol 25-hydroxylase; cyp1a2; cypia2; cytochrome p(3)450; cytochrome p450 1a2; cytochrome p450 4; cytochrome p450-p3

Target Uniprot ID

p05177

Target PDB ID

2hi4

Target, Subunit, Species

Cytochrome P450 1A2 [human]

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Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

CLint

Unit

µL/min/mg protein

Quantitative value

2.275

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Concomitants: Compound RN

8150336; 77911

Concomitants: Compound name

Furafylline; NADPH

Concomitants: Compound role

COM; COE

Target Name

Cytochrome P450 1A2 [human]

Target Synonyms

cholesterol 25-hydroxylase; cyp1a2; cypia2; cytochrome p(3)450; cytochrome p450 1a2; cytochrome p450 4; cytochrome p450-p3

Target Uniprot ID

p05177

Target PDB ID

2hi4

Target, Subunit, Species

Cytochrome P450 1A2 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

CLint

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61 of 1220

Unit

µL/min/mg protein

Quantitative value

7.765

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Concomitants: Compound RN

8150336; 77911

Concomitants: Compound name

Furafylline; NADPH

Concomitants: Compound role

COM; COE

Target Name

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Synonyms

cholesterol 25-hydroxylase; cyp1a2; cypia2; cytochrome p(3)450; cytochrome p450 1a2; cytochrome p450 4; cytochrome p450-p3 + 1,8-cineole 2-exo-monooxygenase; albendazole monooxygenase; albendazole sulfoxidase; cholesterol 25-hydroxylase; cyp3a3; cyp3a4; cypiiia3; cypiiia4; cytochrome p450 3a3; cytochrome p450 3a4; cytochrome p450 hlp; cytochrome p450 nf-25; cytochrome p450-pcn1; nifedipine oxidase; quinine 3-monooxygenase; taurochenodeoxycholate 6-alpha-hydroxylase

Target Uniprot ID

p05177 + p08684

Target PDB ID

2hi4 + 1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild; Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human; human

Target Transfection

Non Transfected; Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

Vmax

Unit

nmol/min/mg protein

Measurement Object

HIGH

Quantitative value

3.82

Metabolite RN

2417108

Metabolite name

MEGX

Target Name

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p05177 + p08684

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Target PDB ID

2hi4 + 1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild; Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human; human

Target Transfection

Non Transfected; Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Measurement Object

HIGH

Quantitative value

228

Measurement pX

3.64

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Target Name

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p05177 + p08684

Target PDB ID

2hi4 + 1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild; Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human; human

Target Transfection

Non Transfected; Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

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64 of 1220

Substance Dose

0 µM

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Measurement Object

HIGH

Quantitative value

6395

Measurement pX

2.19

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Target Name

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p05177 + p08684

Target PDB ID

2hi4 + 1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild; Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human; human

Target Transfection

Non Transfected; Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

Vmax

Unit

nmol/min/mg protein

Measurement Object

LOW

Quantitative value

2.3

Metabolite RN

2417108

Metabolite name

MEGX

Target Name

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p05177 + p08684

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Target PDB ID

2hi4 + 1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild; Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human; human

Target Transfection

Non Transfected; Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Measurement Object

LOW

Quantitative value

134

Measurement pX

3.87

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Target Name

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p05177 + p08684

Target PDB ID

2hi4 + 1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild; Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human; human

Target Transfection

Non Transfected; Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

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66 of 1220

67 of 1220

Substance Dose

0 µM

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Measurement Object

LOW

Quantitative value

813

Measurement pX

3.09

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Target Name

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p05177 + p08684

Target PDB ID

2hi4 + 1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild; Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human; human

Target Transfection

Non Transfected; Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

Vmax

Unit

pmol/min/mg protein

Measurement Object

HIGH

Quantitative value

Metabolite RN

2127970

Metabolite name

3-OH-lidocaine

Target Name

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p05177 + p08684

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68 of 1220

Target PDB ID

2hi4 + 1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild; Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human; human

Target Transfection

Non Transfected; Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

Vmax

Unit

pmol/min/mg protein

Measurement Object

LOW

Quantitative value

Metabolite RN

2127970

Metabolite name

3-OH-lidocaine

Target Name

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p05177 + p08684

Target PDB ID

2hi4 + 1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild; Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human; human

Target Transfection

Non Transfected; Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

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69 of 1220

70 of 1220

Measurement Parameter

CLint

Unit

µL/min/mg protein

Measurement Object

HIGH

Quantitative value

0.00203

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Target Name

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p05177 + p08684

Target PDB ID

2hi4 + 1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild; Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human; human

Target Transfection

Non Transfected; Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

CLint

Unit

µL/min/mg protein

Measurement Object

HIGH

Quantitative value

16.8

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Target Name

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p05177 + p08684

Target PDB ID

2hi4 + 1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

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71 of 1220

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild; Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human; human

Target Transfection

Non Transfected; Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

CLint

Unit

µL/min/mg protein

Measurement Object

LOW

Quantitative value

0.216

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Target Name

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p05177 + p08684

Target PDB ID

2hi4 + 1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild; Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human; human

Target Transfection

Non Transfected; Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

CLint

Unit

µL/min/mg protein

51/467

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72 of 1220

73 of 1220

Measurement Object

LOW

Quantitative value

2.83

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Target Name

Cytochrome P450 1A2 [human]

Target Synonyms

cholesterol 25-hydroxylase; cyp1a2; cypia2; cytochrome p(3)450; cytochrome p450 1a2; cytochrome p450 4; cytochrome p450-p3

Target Uniprot ID

p05177

Target PDB ID

2hi4

Target, Subunit, Species

Cytochrome P450 1A2 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild

Target Species (Bioactivity)

human

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Cells/Cell Lines

BTI-Tn-5B1-4 cell line

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

100 µM

Measurement Parameter

Rate

Unit

pmol/min/pmol target

Quantitative value

0.42

Metabolite RN

2417108; 2127970

Metabolite name

Norlidocaine; 3-OH-lidocaine

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

Target Name

Cytochrome P450 1A2 [human]

Target Synonyms

cholesterol 25-hydroxylase; cyp1a2; cypia2; cytochrome p(3)450; cytochrome p450 1a2; cytochrome p450 4; cytochrome p450-p3

Target Uniprot ID

p05177

Target PDB ID

2hi4

Target, Subunit, Species

Cytochrome P450 1A2 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild

Target Species (Bioactivity)

human

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Cells/Cell Lines

BTI-Tn-5B1-4 cell line

Cell Fraction

Microsome

52/467

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74 of 1220

75 of 1220

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

100 µM

Measurement Parameter

Rate

Unit

pmol/min/pmol target

Quantitative value

29.46

Metabolite RN

2417108; 2127970

Metabolite name

Norlidocaine; 3-OH-lidocaine

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

Target Name

Cytochrome P450 2C9 [human]

Target Synonyms

(r)-limonene 6-monooxygenase; (s)-limonene 6-monooxygenase; (s)-limonene 7-monooxygenase; cholesterol 25-hydroxylase; cyp2c10; cyp2c9; cypiic9; cytochrome p-450mp; cytochrome p450 2c9; cytochrome p450 mp-4; cytochrome p450 mp-8; cytochrome p450 pb-1; s-mephenytoin 4-hydroxylase

Target Uniprot ID

p11712

Target PDB ID

1og2; 1og5; 1r9o; 4nz2; 5a5i; 5a5j

Target, Subunit, Species

Cytochrome P450 2C9 [human]

Target Mutant/Chimera Details

Cytochrome P450 2C9 [human]:Wild

Target Species (Bioactivity)

human

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Cells/Cell Lines

BTI-Tn-5B1-4 cell line

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

100 µM

Measurement Parameter

Rate

Unit

pmol/min/pmol target

Quantitative value

0.31

Metabolite RN

2417108

Metabolite name

Norlidocaine

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

Target Name

Cytochrome P450 3A4 [human]

Target Synonyms

1,8-cineole 2-exo-monooxygenase; albendazole monooxygenase; albendazole sulfoxidase; cholesterol 25-hydroxylase; cyp3a3; cyp3a4; cypiiia3; cypiiia4; cytochrome p450 3a3; cytochrome p450

53/467

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3a4; cytochrome p450 hlp; cytochrome p450 nf-25; cytochrome p450-pcn1; nifedipine oxidase; quinine 3-monooxygenase; taurochenodeoxycholate 6-alpha-hydroxylase

76 of 1220

Target Uniprot ID

p08684

Target PDB ID

1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Cells/Cell Lines

BTI-Tn-5B1-4 cell line

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

100 µM

Measurement Parameter

Rate

Unit

pmol/min/pmol target

Quantitative value

0.01

Metabolite RN

2417108; 2127970

Metabolite name

Norlidocaine; 3-OH-lidocaine

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

Target Name

Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p08684

Target PDB ID

1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Cells/Cell Lines

BTI-Tn-5B1-4 cell line

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

100 µM

54/467

2018-05-14 08:43:54

77 of 1220

78 of 1220

Measurement Parameter

Rate

Unit

pmol/min/pmol target

Quantitative value

31.99

Metabolite RN

2417108; 2127970

Metabolite name

Norlidocaine; 3-OH-lidocaine

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

Target Name

Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p08684

Target PDB ID

1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Cells/Cell Lines

BTI-Tn-5B1-4 cell line

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

CLint

Unit

µL/min/pmol target

Quantitative value

0.25

Metabolite RN

2417108

Metabolite name

MEGX

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

Target Name

Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p08684

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Target PDB ID

79 of 1220

1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Cells/Cell Lines

BTI-Tn-5B1-4 cell line

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

CLint

Unit

nL/min/pmol target

Quantitative value

0.21

Metabolite RN

2127970

Metabolite name

3-OH-lidocaine

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

Target Name

Cytochrome P450 1A2 [human]

Target Synonyms

cholesterol 25-hydroxylase; cyp1a2; cypia2; cytochrome p(3)450; cytochrome p450 1a2; cytochrome p450 4; cytochrome p450-p3

Target Uniprot ID

p05177

Target PDB ID

2hi4

Target, Subunit, Species

Cytochrome P450 1A2 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild

Target Species (Bioactivity)

human

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Cells/Cell Lines

BTI-Tn-5B1-4 cell line

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

CLint

Unit

µL/min/pmol target

Quantitative value

0.23

Metabolite RN

2417108

56/467

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80 of 1220

81 of 1220

Metabolite name

MEGX

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

Target Name

Cytochrome P450 1A2 [human]

Target Synonyms

cholesterol 25-hydroxylase; cyp1a2; cypia2; cytochrome p(3)450; cytochrome p450 1a2; cytochrome p450 4; cytochrome p450-p3

Target Uniprot ID

p05177

Target PDB ID

2hi4

Target, Subunit, Species

Cytochrome P450 1A2 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild

Target Species (Bioactivity)

human

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Cells/Cell Lines

BTI-Tn-5B1-4 cell line

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

CLint

Unit

nL/min/pmol target

Quantitative value

3.3

Metabolite RN

2127970

Metabolite name

3-OH-lidocaine

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

Target Name

Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p08684

Target PDB ID

1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human

57/467

2018-05-14 08:43:54

82 of 1220

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Cells/Cell Lines

BTI-Tn-5B1-4 cell line

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Quantitative value

1032

Measurement pX

2.99

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

Target Name

Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p08684

Target PDB ID

1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Cells/Cell Lines

BTI-Tn-5B1-4 cell line

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Quantitative value

1435

Measurement pX

2.84

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

58/467

2018-05-14 08:43:54

83 of 1220

84 of 1220

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

Target Name

Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p08684

Target PDB ID

1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Cells/Cell Lines

BTI-Tn-5B1-4 cell line

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

Vmax

Unit

pmol/min/pmol target

Quantitative value

0.3

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

Target Name

Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p08684

Target PDB ID

1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human

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Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Cells/Cell Lines

BTI-Tn-5B1-4 cell line

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

Vmax

Unit

pmol/min/pmol target

Quantitative value

254

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

Target Name

Cytochrome P450 1A2 [human]

Target Synonyms

cholesterol 25-hydroxylase; cyp1a2; cypia2; cytochrome p(3)450; cytochrome p450 1a2; cytochrome p450 4; cytochrome p450-p3

Target Uniprot ID

p05177

Target PDB ID

2hi4

Target, Subunit, Species

Cytochrome P450 1A2 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild

Target Species (Bioactivity)

human

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Cells/Cell Lines

BTI-Tn-5B1-4 cell line

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Quantitative value

810

Measurement pX

3.09

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

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87 of 1220

COE

Target Name

Cytochrome P450 1A2 [human]

Target Synonyms

cholesterol 25-hydroxylase; cyp1a2; cypia2; cytochrome p(3)450; cytochrome p450 1a2; cytochrome p450 4; cytochrome p450-p3

Target Uniprot ID

p05177

Target PDB ID

2hi4

Target, Subunit, Species

Cytochrome P450 1A2 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild

Target Species (Bioactivity)

human

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Cells/Cell Lines

BTI-Tn-5B1-4 cell line

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Quantitative value

818

Measurement pX

3.09

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

Target Name

Cytochrome P450 1A2 [human]

Target Synonyms

cholesterol 25-hydroxylase; cyp1a2; cypia2; cytochrome p(3)450; cytochrome p450 1a2; cytochrome p450 4; cytochrome p450-p3

Target Uniprot ID

p05177

Target PDB ID

2hi4

Target, Subunit, Species

Cytochrome P450 1A2 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild

Target Species (Bioactivity)

human

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Cells/Cell Lines

BTI-Tn-5B1-4 cell line

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

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Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

Vmax

Unit

pmol/min/pmol target

Quantitative value

190

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

Target Name

Cytochrome P450 1A2 [human]

Target Synonyms

cholesterol 25-hydroxylase; cyp1a2; cypia2; cytochrome p(3)450; cytochrome p450 1a2; cytochrome p450 4; cytochrome p450-p3

Target Uniprot ID

p05177

Target PDB ID

2hi4

Target, Subunit, Species

Cytochrome P450 1A2 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild

Target Species (Bioactivity)

human

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Cells/Cell Lines

BTI-Tn-5B1-4 cell line

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

Vmax

Unit

pmol/min/pmol target

Quantitative value

2.7

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

Target Name

Histamine H2 receptor [guinea pig]

Target Synonyms

gastric receptor i; h2r; hh2r; histamine h2 receptor; hrh2

Target Uniprot ID

p47747

Target, Subunit, Species

Histamine H2 receptor [guinea pig]

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Target Mutant/Chimera Details

Histamine H2 receptor [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig

Target Transfection

Non Transfected

Substance Action on Target

Agonist

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Organ contraction

Biological Species/NCBI ID

guinea pig

Organs/Tissues

duodenal longitudinal muscle

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Measurement Parameter

pIC50

Quantitative value

4.33

Deviation

0.0900000

Measurement pX

4.33

Concomitants: Compound RN

269019; 1764436; 6071707

Concomitants: Compound name

Pyrilamine; Acetylcholine; Famotidine

Concomitants: Compound role

COM; IND; COM

Target Name

Histamine H2 receptor [guinea pig]

Target Synonyms

gastric receptor i; h2r; hh2r; histamine h2 receptor; hrh2

Target Uniprot ID

p47747

Target, Subunit, Species

Histamine H2 receptor [guinea pig]

Target Mutant/Chimera Details

Histamine H2 receptor [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig

Target Transfection

Non Transfected

Substance Action on Target

Agonist

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Organ contraction

Biological Species/NCBI ID

guinea pig

Organs/Tissues

duodenal longitudinal muscle

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Measurement Parameter

pIC50

Quantitative value

3.11

Deviation

0.170000

Measurement pX

3.11

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Concomitants: Compound RN

8137362; 269019; 6071707

Concomitants: Compound name

KCl; Pyrilamine; Famotidine

Concomitants: Compound role

IND; COM; COM

Target Name

Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p08684

Target PDB ID

1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

Vmax

Unit

nmol/min/mg protein

Quantitative value

8.96

Deviation

5.59000

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Concomitants: Compound RN

77547; 77911

Concomitants: Compound name

Troleandomycin; NADPH

Concomitants: Compound role

COM; COE

Target Name

Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p08684

Target PDB ID

1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

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Target, Subunit, Species

Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

Vmax

Unit

nmol/min/mg protein

Quantitative value

Deviation

4.24000

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Concomitants: Compound RN

77547; 77911

Concomitants: Compound name

Troleandomycin; NADPH

Concomitants: Compound role

COM; COE

Target Name

Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p08684

Target PDB ID

1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

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Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Quantitative value

2254.5

Deviation

2153.14

Measurement pX

2.65

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Concomitants: Compound RN

77547; 77911

Concomitants: Compound name

Troleandomycin; NADPH

Concomitants: Compound role

COM; COE

Target Name

Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p08684

Target PDB ID

1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Quantitative value

342.5

Deviation

191.600

Measurement pX

3.46

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Concomitants: Compound RN

77547; 77911

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Concomitants: Compound name

Troleandomycin; NADPH

Concomitants: Compound role

COM; COE

Target Name

Cytochrome P450 1A2 [human]

Target Synonyms

cholesterol 25-hydroxylase; cyp1a2; cypia2; cytochrome p(3)450; cytochrome p450 1a2; cytochrome p450 4; cytochrome p450-p3

Target Uniprot ID

p05177

Target PDB ID

2hi4

Target, Subunit, Species

Cytochrome P450 1A2 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

Vmax

Unit

nmol/min/mg protein

Quantitative value

7.26

Deviation

7.01000

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Concomitants: Compound RN

8150336; 77911

Concomitants: Compound name

Furafylline; NADPH

Concomitants: Compound role

COM; COE

Target Name

Cytochrome P450 1A2 [human]

Target Synonyms

cholesterol 25-hydroxylase; cyp1a2; cypia2; cytochrome p(3)450; cytochrome p450 1a2; cytochrome p450 4; cytochrome p450-p3

Target Uniprot ID

p05177

Target PDB ID

2hi4

Target, Subunit, Species

Cytochrome P450 1A2 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

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Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

Vmax

Unit

nmol/min/mg protein

Quantitative value

18.5

Deviation

6.40000

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Concomitants: Compound RN

8150336; 77911

Concomitants: Compound name

Furafylline; NADPH

Concomitants: Compound role

COM; COE

Target Name

Cytochrome P450 1A2 [human]

Target Synonyms

cholesterol 25-hydroxylase; cyp1a2; cypia2; cytochrome p(3)450; cytochrome p450 1a2; cytochrome p450 4; cytochrome p450-p3

Target Uniprot ID

p05177

Target PDB ID

2hi4

Target, Subunit, Species

Cytochrome P450 1A2 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Quantitative value

3191.5

Deviation

2945.10

Measurement pX

2.5

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99 of 1220

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Concomitants: Compound RN

8150336; 77911

Concomitants: Compound name

Furafylline; NADPH

Concomitants: Compound role

COM; COE

Target Name

Cytochrome P450 1A2 [human]

Target Synonyms

cholesterol 25-hydroxylase; cyp1a2; cypia2; cytochrome p(3)450; cytochrome p450 1a2; cytochrome p450 4; cytochrome p450-p3

Target Uniprot ID

p05177

Target PDB ID

2hi4

Target, Subunit, Species

Cytochrome P450 1A2 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0 µM

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Quantitative value

2382.5

Deviation

531.040

Measurement pX

2.62

Metabolite RN

2417108; 2127970

Metabolite name

MEGX; 3-OH-lidocaine

Concomitants: Compound RN

8150336; 77911

Concomitants: Compound name

Furafylline; NADPH

Concomitants: Compound role

COM; COE

Substance Effect

Analgesic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Bioassay : paw withdrawal latency (PWL) to radiant heat tested 5 min after intraplantar inj. of title comp. into one hindpaw, normal tissue

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Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

profound antinociceptive effect (PWL: 19.0 s vs. 8.8 s)

Measurement Parameter

qualitative

Jackson; Graff; Richardson; Hargreaves; European Journal of Pharmacology; vol. 284; nb. 3; (1995); p. 321 - 325, View in Reaxys 100 of 1220 Target Name

enzyme

Target Synonyms

enzyme

Target, Subunit, Species

enzyme

Target Mutant/Chimera Details

enzyme:Wild

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : |enzyme; examination of Bioassay : CSF: artificial cerebrospinal fluid; TTX: tetrodotoxin, 1 μmol/l; FAK: focal adhesion kinase slices incubated in CSF at 37 deg C and then with CaCl2 (1 mmol/l) and title comp. for 5 min in presence of TTX; immunoblotting with both antiphosphotyrosine SL2 and rabbit anti-Y397FAK phosphospecific antibody; phosphorylated PP125FAK determined

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

4.20000E-09 M

Measurement Parameter

EC50

Unit

µM

Quantitative value

0.39

Measurement pX

6.41

101 of 1220 Target Name

enzyme

Target Synonyms

enzyme

Target, Subunit, Species

enzyme

Target Mutant/Chimera Details

enzyme:Wild

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : |enzyme; examination of Bioassay : TTX: tetrodotoxin, 1 μmol/l; FAK: focal adhesion kinase; further invest. with N-methyl-D-aspartate receptor antagonist dizocilpine (MK-801), blockers of protein kinase C RO-318220, GF 109203X and chelerythrin and blocker of Ca(2+) release dantrolene slices incubated at 37 deg C with CaCl2 (1 mmol/l) and title comp. for 5 min in presence of TTX; immunoblotting with both antiphosphotyrosine SL2 and rabbit anti-Y397FAK phosphospecific antibody; phosphorylated PP125FAK determined

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

4.20000E-09 M

Measurement Parameter

EC50

Unit

µM

Quantitative value

0.39

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Measurement pX 102 of 1220 Target Name

6.41 sodium channel

Target Synonyms

sodium channel; sodium channel activity

Target, Subunit, Species

sodium channel

Target Mutant/Chimera Details

sodium channel:Wild

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Binding

Organs/Tissues

brain cortex

Cells/Cell Lines

cells

Cell Fraction

Membrane

Substance RN

3917968View in Reaxys

Substance Name

lidocaine.HCl

Measurement Parameter

IC50

Unit

Quantitative value

0.00023

Measurement pX

3.64

Concomitants: Compound RN

78875; 24140984

Concomitants: Compound name

Veratridine; [3H]-Batrachotoxin; BSA; Scorpion venom (Leiurus quinquestriatus)

Concomitants: Compound role

NSB; RAD; COM; COM

103 of 1220 Target Name

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]

Target Synonyms

hyperpolarization-activated cyclic nucleotide gated channel (hcn1)

Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]

Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Xenopus laevis

Cells/Cell Lines

oocyte

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

100 µM

Measurement Parameter

% Inhibition

Unit

Measurement Object

Current amplitude

Quantitative value

35.5

Deviation

4.90000

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Measurement pX 104 of 1220 Target Name

3.74 Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]

Target Synonyms

hyperpolarization-activated cyclic nucleotide gated channel (hcn2)

Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]

Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Xenopus laevis

Cells/Cell Lines

oocyte

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

100 µM

Measurement Parameter

% Inhibition

Unit

Measurement Object

Current amplitude

Quantitative value

32.5

Deviation

9.50000

Measurement pX

3.68

105 of 1220 Target Name

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus];+Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]

Target Synonyms

hyperpolarization-activated cyclic nucleotide gated channel (hcn2) + hyperpolarization-activated cyclic nucleotide gated channel (hcn1)

Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]; Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]

Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]:Wild + Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Xenopus laevis

Cells/Cell Lines

oocyte

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

100 µM

Measurement Parameter

% Inhibition

Unit

Measurement Object

Current amplitude

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Quantitative value

31.7

Deviation

5.80000

Measurement pX

3.67

106 of 1220 Target Name

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]

Target Synonyms

hyperpolarization-activated cyclic nucleotide gated channel (hcn1)

Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]

Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

Target Transfection

Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

HEK293 cell line

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

100 µM

Measurement Parameter

% Inhibition

Unit

Measurement Object

Current amplitude

Quantitative value

30.9

Deviation

5.20000

Measurement pX

3.65

Concomitants: Compound RN

24141025

Concomitants: Compound name

Mg-ATP

Concomitants: Compound role

COM

107 of 1220 Target Name

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]

Target Synonyms

hyperpolarization-activated cyclic nucleotide gated channel (hcn1)

Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]

Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

Target Transfection

Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

HEK293 cell line

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

73/467

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Substance Dose

100 µM

Measurement Parameter

Delta

Unit

Measurement Object

V0.5 (activation)

Quantitative value

-11.8

Deviation

0.300000

Concomitants: Compound RN

24141025

Concomitants: Compound name

Mg-ATP

Concomitants: Compound role

COM

108 of 1220 Target Name

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]

Target Synonyms

hyperpolarization-activated cyclic nucleotide gated channel (hcn2)

Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]

Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

Target Transfection

Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

HEK293 cell line

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

100 µM

Measurement Parameter

% Inhibition

Unit

Measurement Object

Current amplitude

Quantitative value

46.6

Deviation

4.20000

Measurement pX

3.94

Concomitants: Compound RN

24141025

Concomitants: Compound name

Mg-ATP

Concomitants: Compound role

COM

109 of 1220 Target Name Target Synonyms

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus] hyperpolarization-activated cyclic nucleotide gated channel (hcn2)

Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]

Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

74/467

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Target Transfection

Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

HEK293 cell line

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

100 µM

Measurement Parameter

Delta

Unit

Measurement Object

V0.5 (activation)

Quantitative value

-3.2

Deviation

1.50000

Concomitants: Compound RN

24141025

Concomitants: Compound name

Mg-ATP

Concomitants: Compound role

COM

110 of 1220 Target Name

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus];+Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]

Target Synonyms

hyperpolarization-activated cyclic nucleotide gated channel (hcn1) + hyperpolarization-activated cyclic nucleotide gated channel (hcn2)

Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]; Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]

Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]:Wild + Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

Target Transfection

Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

HEK293 cell line

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

100 µM

Measurement Parameter

% Inhibition

Unit

Measurement Object

Current amplitude

Quantitative value

38.7

Deviation

3.20000

Measurement pX

3.8

Concomitants: Compound RN

24141025

75/467

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Concomitants: Compound name

Mg-ATP

Concomitants: Compound role

COM

111 of 1220 Target Name

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus];+Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]

Target Synonyms

hyperpolarization-activated cyclic nucleotide gated channel (hcn1) + hyperpolarization-activated cyclic nucleotide gated channel (hcn2)

Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]; Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]

Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]:Wild + Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

Target Transfection

Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

HEK293 cell line

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

100 µM

Measurement Parameter

Delta

Unit

Measurement Object

V0.5 (activation)

Quantitative value

-10.1

Deviation

Concomitants: Compound RN

24141025

Concomitants: Compound name

Mg-ATP

Concomitants: Compound role

COM

112 of 1220 Target Name

Hyperpolarization-activated cyclic nucleotide gated channel (HCN4) [Mus musculus]

Target Synonyms

hyperpolarization-activated cyclic nucleotide gated channel (hcn4)

Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN4) [Mus musculus]

Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN4) [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

Target Transfection

Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

HEK293 cell line

Substance RN

3917968View in Reaxys

76/467

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Substance Name

lidocaine

Substance Dose

100 µM

Measurement Parameter

% Inhibition

Unit

Measurement Object

Current amplitude

Quantitative value

30.4

Deviation

4.20000

Measurement pX

3.64

Concomitants: Compound RN

24141025

Concomitants: Compound name

Mg-ATP

Concomitants: Compound role

COM

113 of 1220 Target Name

Hyperpolarization-activated cyclic nucleotide gated channel (HCN4) [Mus musculus]

Target Synonyms

hyperpolarization-activated cyclic nucleotide gated channel (hcn4)

Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN4) [Mus musculus]

Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN4) [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

Target Transfection

Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

HEK293 cell line

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

100 µM

Measurement Parameter

Delta

Unit

Measurement Object

V0.5 (activation)

Quantitative value

-2.6

Deviation

0.900000

Concomitants: Compound RN

24141025

Concomitants: Compound name

Mg-ATP

Concomitants: Compound role

COM

114 of 1220 Target Name

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]

Target Synonyms

hyperpolarization-activated cyclic nucleotide gated channel (hcn1)

Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]

Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]:Wild

77/467

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Target Species (Bioactivity)

Mus musculus

Target Transfection

Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

HEK293 cell line

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

100 µM

Measurement Parameter

% Inhibition

Unit

Measurement Object

tonic

Quantitative value

45.7

Measurement pX

3.93

Concomitants: Compound RN

9321248; 24141025

Concomitants: Compound name

CsCl; Mg-ATP

Concomitants: Compound role

IND; COM

115 of 1220 Target Name

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]

Target Synonyms

hyperpolarization-activated cyclic nucleotide gated channel (hcn2)

Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]

Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

Target Transfection

Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

HEK293 cell line

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

100 µM

Measurement Parameter

% Inhibition

Unit

Measurement Object

tonic

Quantitative value

54.3

Measurement pX

4.07

Concomitants: Compound RN

9321248; 24141025

78/467

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Concomitants: Compound name

CsCl; Mg-ATP

Concomitants: Compound role

IND; COM

116 of 1220 Target Name

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus];+Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]

Target Synonyms

hyperpolarization-activated cyclic nucleotide gated channel (hcn1) + hyperpolarization-activated cyclic nucleotide gated channel (hcn2)

Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]; Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]

Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]:Wild + Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

Target Transfection

Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

HEK293 cell line

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

100 µM

Measurement Parameter

% Inhibition

Unit

Measurement Object

tonic

Quantitative value

53.3

Measurement pX

4.06

Concomitants: Compound RN

9321248; 24141025

Concomitants: Compound name

CsCl; Mg-ATP

Concomitants: Compound role

IND; COM

117 of 1220 Target Name

Hyperpolarization-activated cyclic nucleotide gated channel (HCN4) [Mus musculus]

Target Synonyms

hyperpolarization-activated cyclic nucleotide gated channel (hcn4)

Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN4) [Mus musculus]

Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN4) [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

Target Transfection

Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

HEK293 cell line

Substance RN

3917968View in Reaxys

79/467

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Substance Name

lidocaine

Substance Dose

100 µM

Measurement Parameter

% Inhibition

Unit

Measurement Object

tonic

Quantitative value

4.6

Measurement pX

Concomitants: Compound RN

9321248; 24141025

Concomitants: Compound name

CsCl; Mg-ATP

Concomitants: Compound role

IND; COM

118 of 1220 Target Name

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]

Target Synonyms

hyperpolarization-activated cyclic nucleotide gated channel (hcn1)

Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]

Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

Target Transfection

Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

HEK293 cell line

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

100 µM

Measurement Parameter

% Inhibition

Unit

Measurement Object

tonic

Quantitative value

Deviation

6.80000

Measurement pX

4.91

Concomitants: Compound RN

9321248; 24141025

Concomitants: Compound name

CsCl; Mg-ATP

Concomitants: Compound role

IND; COM

119 of 1220 Target Name

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]

Target Synonyms

hyperpolarization-activated cyclic nucleotide gated channel (hcn2)

Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]

Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]:Wild

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Target Species (Bioactivity)

Mus musculus

Target Transfection

Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

HEK293 cell line

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

100 µM

Measurement Parameter

% Inhibition

Unit

Measurement Object

tonic

Quantitative value

60.3

Deviation

6.20000

Measurement pX

4.18

Concomitants: Compound RN

9321248; 24141025

Concomitants: Compound name

CsCl; Mg-ATP

Concomitants: Compound role

IND; COM

120 of 1220 Target Name

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]

Target Synonyms

hyperpolarization-activated cyclic nucleotide gated channel (hcn1)

Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]

Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Xenopus laevis

Cells/Cell Lines

oocyte

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Measurement Parameter

IC50

Unit

µM

Quantitative value

67.6

Deviation

9.60000

Measurement pX

4.17

121 of 1220 Target Name Target Synonyms

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus] hyperpolarization-activated cyclic nucleotide gated channel (hcn2)

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Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]

Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Xenopus laevis

Cells/Cell Lines

oocyte

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Measurement Parameter

IC50

Unit

µM

Quantitative value

66.8

Deviation

15.3000

Measurement pX

4.18

122 of 1220 Target Name

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus];+Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]

Target Synonyms

hyperpolarization-activated cyclic nucleotide gated channel (hcn2) + hyperpolarization-activated cyclic nucleotide gated channel (hcn1)

Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]; Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]

Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]:Wild + Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Xenopus laevis

Cells/Cell Lines

oocyte

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Measurement Parameter

IC50

Unit

µM

Quantitative value

51.6

Deviation

9.50000

Measurement pX

4.29

123 of 1220 Target Name

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]

Target Synonyms

hyperpolarization-activated cyclic nucleotide gated channel (hcn1)

Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]

82/467

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Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Xenopus laevis

Cells/Cell Lines

oocyte

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Measurement Parameter

Emax

Unit

Quantitative value

43.8

Deviation

3.50000

124 of 1220 Target Name

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]

Target Synonyms

hyperpolarization-activated cyclic nucleotide gated channel (hcn2)

Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]

Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Xenopus laevis

Cells/Cell Lines

oocyte

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Measurement Parameter

Emax

Unit

Quantitative value

41.7

Deviation

5.20000

125 of 1220 Target Name

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus];+Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]

Target Synonyms

hyperpolarization-activated cyclic nucleotide gated channel (hcn2) + hyperpolarization-activated cyclic nucleotide gated channel (hcn1)

Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]; Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]

Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]:Wild + Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

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Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Xenopus laevis

Cells/Cell Lines

oocyte

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Measurement Parameter

Emax

Unit

Quantitative value

32.4

Deviation

126 of 1220 Target Name

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]

Target Synonyms

hyperpolarization-activated cyclic nucleotide gated channel (hcn1)

Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]

Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Xenopus laevis

Cells/Cell Lines

oocyte

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

100 µM

Measurement Parameter

Delta

Unit

Measurement Object

V0.5 (activation)

Quantitative value

-12.9

Deviation

1.50000

127 of 1220 Target Name

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]

Target Synonyms

hyperpolarization-activated cyclic nucleotide gated channel (hcn2)

Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]

Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

84/467

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Biological Species/NCBI ID

Xenopus laevis

Cells/Cell Lines

oocyte

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

100 µM

Measurement Parameter

Delta

Unit

Measurement Object

V0.5 (activation)

Quantitative value

-3.9

Deviation

128 of 1220 Target Name

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus];+Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]

Target Synonyms

hyperpolarization-activated cyclic nucleotide gated channel (hcn2) + hyperpolarization-activated cyclic nucleotide gated channel (hcn1)

Target, Subunit, Species

Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]; Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]

Target Mutant/Chimera Details

Hyperpolarization-activated cyclic nucleotide gated channel (HCN2) [Mus musculus]:Wild + Hyperpolarization-activated cyclic nucleotide gated channel (HCN1) [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Xenopus laevis

Cells/Cell Lines

oocyte

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

100 µM

Measurement Parameter

Delta

Unit

Measurement Object

V0.5 (activation)

Quantitative value

-11.3

Deviation

0.700000

129 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

human

Population State

Non Smoker

Organs/Tissues

liver

Cell Fraction

Microsome (pooled)

Substance RN

3917968View in Reaxys

Substance Name

Lignocaine

Substance Dose

200 µM

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Measurement Parameter

fu (unbound fraction)

Quantitative value

0.37

Deviation

0.0100000

McLure, James A.; Birkett, Donald J.; Elliot, David J.; Williams, J. Andrew; Rowland, Andrew; Miners, John O.; Drug Metabolism and Disposition; vol. 39; nb. 9; (2011); p. 1711 - 1717, View in Reaxys 130 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

human

Population State

Non Smoker

Organs/Tissues

liver

Cell Fraction

Microsome (pooled)

Substance RN

3917968View in Reaxys

Substance Name

Lignocaine

Substance Dose

500 µM

Measurement Parameter

fu (unbound fraction)

Quantitative value

0.37

Deviation

0.0800000

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

human

Population State

Non Smoker

Organs/Tissues

liver

Cell Fraction

Microsome (pooled)

Substance RN

3917968View in Reaxys

Substance Name

Lignocaine

Substance Dose

100 µM

Measurement Parameter

fu (unbound fraction)

Quantitative value

0.29

Deviation

0.110000

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

Effect on reserpine-induced ptosis and hypothermia (mice), effect on 5-hydroxytryptophan syndrome (mice), effect on haloperidol-induced catalepsy (rat)

Measurement Parameter

qualitative

Hirotsu; Kihara; Nakamura; Hattori; Hatta; Kitakaze; Takahama; Hashimoto; Miyata; Ishihara; Satoh; ArzneimittelForschung/Drug Research; vol. 38; nb. 10; (1988); p. 1398 - 1409, View in Reaxys 133 of 1220 Bioassay Category

In Vitro (Efficacy)

86/467

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Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

Effect on isolated urinary bladder (g. pig) no change

Measurement Parameter

qualitative

Hirotsu; Kihara; Hattori; Hatta; Hirose; Ishihara; Satoh; Arzneimittel-Forschung/Drug Research; vol. 38; nb. 10; (1988); p. 1410 - 1416, View in Reaxys 134 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

LD50 = 37 mg/kg (mice)

Measurement Parameter

qualitative

Glushkov, R. G.; Sizova, O. S.; Azimov, A. V.; Trubitsyna, T. K.; Denisov, A. V.; et al.; Pharmaceutical Chemistry Journal; vol. 23; nb. 7; (1989); p. 570 - 575; Khimiko-Farmatsevticheskii Zhurnal; vol. 23; nb. 7; (1989); p. 820 - 824, View in Reaxys 135 of 1220 Substance Effect

Analgesic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Bioassay : Degree of Anesthesia and Sensation of Iontophoresis with the Lidocaine/Epinephrine PatchThe present Example addressed the issues of drug concentration and charge density in order to determine the optimal conditions for the iontophoresis of lidocaine HCl and epinephrine. A maximal charge density of 3.4

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

The degree of analgesia determined by cannulation pain (VAS) after treatment with the title compound (10%) patch iontophoretic device was 37.50 and 35.20 at charge densities of 2.5 and 3.4 mA*min/cm2, respectively (placebo - 50.35).

Measurement Parameter

qualitative

Patent; VYTERIS, INC.; WO2007/41475; (2007); (A2) English, View in Reaxys 136 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : edema; effect onBioassay : Degree of Anesthesia and Sensation of Iontophoresis with the Lidocaine/Epinephrine PatchThe present Example addressed the issues of drug concentration and charge density in order to determine the optimal conditions for the iontophoresis of lidocaine HCl and epinephrine. A maximal charge density of 3.4

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

At anode and cathode sites, there were no statistically significant differences in the average edema scores among the six treatments where a current was applied to the title compound (10 %) patch for Time 0 and Time 24 at charge densities of 2.5 and

Measurement Parameter

qualitative

Patent; VYTERIS, INC.; WO2007/41475; (2007); (A2) English, View in Reaxys 137 of 1220 Bioassay Category Bioassay Name

In Vitro (Efficacy) In Vitro (others)

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Bioassay Details

Effect : erythema; effect onBioassay : Degree of Anesthesia and Sensation of Iontophoresis with the Lidocaine/Epinephrine PatchThe present Example addressed the issues of drug concentration and charge density in order to determine the optimal conditions for the iontophoresis of lidocaine HCl and epinephrine. A maximal charge density of 3.4

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

For the 5 treatments where a current was applied to the title compound (10 %) patch, the average scores were not statistically significantly different at charge densities of 2.5 and 3.4mA*min/cm2. At Time 24, the average score at both the anode and

Measurement Parameter

qualitative

Patent; VYTERIS, INC.; WO2007/41475; (2007); (A2) English, View in Reaxys 138 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : sensation of iontophoresis; effect onBioassay : Degree of Anesthesia and Sensation of Iontophoresis with the Lidocaine/Epinephrine PatchThe present Example addressed the issues of drug concentration and charge density in order to determine the optimal conditions for the iontophoresis of lidocaine HCl and epinephrine. A maximal charge density of 3.4

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

The sensation of iontophoresis with title compound patch (10 %) was evaluated using the SIS and the Hedonic scale: SIS score - 7.40 and 6.15, Hedonic score - -0.95 and -1.05 at charge densities of 2.5 and 3.4mA*min/cm2, respectively (SIS score - 1.65,

Measurement Parameter

qualitative

Patent; VYTERIS, INC.; WO2007/41475; (2007); (A2) English, View in Reaxys 139 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

antiarrhythmic activity in conscious dogs

Measurement Parameter

qualitative

Wilkerson; Henderson; Journal of Medicinal Chemistry; vol. 23; nb. 11; (1980); p. 1255 - 1258, View in Reaxys 140 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

antiarrhytmic activity in mice ED50= 29 mg/kg

Measurement Parameter

qualitative

Miyano; Sumoto; Satoh; Shima; Hayashimatsu; Morita; Aisaka; Noguchi; Journal of Medicinal Chemistry; vol. 28; nb. 6; (1985); p. 714 - 717, View in Reaxys 141 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : motor blockade; effect onTarget : land-race pigBioassay : scale: normal stability and strength (0), faint legs (1) and total paralysis of legs (2); control: placebo poloxamer gel, physiological saline and title comp. HCl-saline solution (2 percent) pigs administered with title comp.; motor

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function testing (motor blockade) performed by letting pig stand and walk on even surface; response measured on three-point scale Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

title comp. treatment resulted in maximum motor blockade of hind legs which lasted for 90 min longer than control (title comp. solution); fig.

Measurement Parameter

qualitative

Paavola, Anne; Tarkkila, Pekka; Xu, Mei; Wahlstroem, Torsten; Yliruusi, Jouko; Rosenberg, Per; Pharmaceutical Research; vol. 15; nb. 3; (1998); p. 482 - 487, View in Reaxys 142 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : |pharmacokinetics Target : land-race pigBioassay : control: placebo poloxamer gel, physiological saline and title comp. HCl-saline solution (2 percent) pigs administered with title comp.; venous blood samples collected 5-240 minutes post-dose; plasma concentration of title comp. determined by HPLC; pharmacokinetic parameters calculated

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

Cmax value (0.94 μg/ml) of title comp. was reached 20 min post-dose; t1/2 and MRT values were significantly longer; AUC value of title comp. was 200 μg/ml/min; fig., table

Measurement Parameter

qualitative

Paavola, Anne; Tarkkila, Pekka; Xu, Mei; Wahlstroem, Torsten; Yliruusi, Jouko; Rosenberg, Per; Pharmaceutical Research; vol. 15; nb. 3; (1998); p. 482 - 487, View in Reaxys 143 of 1220 Substance Effect

Analgesic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Target : land-race pigBioassay : scale: normal stability and strength (0), faint legs (1) and total paralysis of legs (2); control: placebo poloxamer gel, physiological saline and title comp. HCl-saline solution (2 percent); RC: reflex contraction pigs administered with title comp.; toe clamped at border of nail and skin; response graded as instantaneous withdrawal (0), visible RC or delayed withdrawal (1) and no withdrawal of legs or visible RC of muscles (2); nociceptive response determined

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

antinociceptive response of title comp. administration lasted 60 min longer and was more effective over time compared to control (title comp. solution); sensory blockade was not observed in forelegs

Measurement Parameter

qualitative

Paavola, Anne; Tarkkila, Pekka; Xu, Mei; Wahlstroem, Torsten; Yliruusi, Jouko; Rosenberg, Per; Pharmaceutical Research; vol. 15; nb. 3; (1998); p. 482 - 487, View in Reaxys 144 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : K(1+) current; effect onTarget : rat spinal dorsal horn neuroneBioassay : HP: holding potential intact neurones were patch-clamped in external choline-Cl solution at HP -80 mV by 200 ms voltage step to +20 mV following 150 ms prepulse to -60 mV in presence of title comp.; relative amplitudes of delayed-rectifier K(1+) currents recorded

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

1.00000E-06 M

Qualitative Results

1 - 100 μmol/l title comp. enhanced delayed-rectifier K(1+) current but at higher concentrations (> 100 μmol/l) induced partial blocking effect (figure)

Measurement Parameter

qualitative

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Olschewski, Andrea; Wolff, Matthias; Braeu, Michael E.; Hempelmann, Gunter; Vogel, Werner; Safronov, Boris V.; British Journal of Pharmacology; vol. 136; nb. 4; (2002); p. 540 - 549, View in Reaxys 145 of 1220 Target Name

Cytochrome P450 [human]

Target Synonyms

cyp1a2; cyp1b1; cyp2a6v2; cyp2b6; cyp2c19; cyp2j2; cyp3a4; cyp3a43; cyp3a43/cyp3a4; cyp4f2; cytochrome p450

Target Uniprot ID

a0n0x8; a4f4k4; c1kde6; c1kde7; c1kde8; d0ezn6; d0ezn7; d0ezn8; e7emt5; o95743; q0vhd5; q13120; q53g23; q5j9b1; q6nwu3; q767a3; q7z2g5; q7z446; q7z447; q7z448; q86sk2; q86sk3; q96rx4; q9unx8

Target, Subunit, Species

Cytochrome P450 [human]

Target Mutant/Chimera Details

Cytochrome P450 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Quantitative value

363.43

Measurement pX

3.44

Metabolite RN

2417108

Metabolite name

Monoethylglycinexylidide

Concomitants: Compound RN

24140787; 3885115

Concomitants: Compound name

Glucose-6-phosphate; NADP

Concomitants: Compound role

COM; COE

146 of 1220 Target Name

Cytochrome P450 [Rattus norvegicus]

Target Synonyms

cyp1a1; cyp1b1; cytochrome p450

Target Uniprot ID

a7tud9; q64590; q80ue2; q9esw3

Target, Subunit, Species

Cytochrome P450 [Rattus norvegicus]

Target Mutant/Chimera Details

Cytochrome P450 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

Long Evans rat

Organs/Tissues

liver

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Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Quantitative value

304.33

Measurement pX

3.52

Metabolite RN

2417108

Metabolite name

Monoethylglycinexylidide

Concomitants: Compound RN

24140787; 3885115

Concomitants: Compound name

Glucose-6-phosphate; NADP

Concomitants: Compound role

COM; COE

147 of 1220 Target Name

Cytochrome P450 [Rattus norvegicus]

Target Synonyms

cyp1a1; cyp1b1; cytochrome p450

Target Uniprot ID

a7tud9; q64590; q80ue2; q9esw3

Target, Subunit, Species

Cytochrome P450 [Rattus norvegicus]

Target Mutant/Chimera Details

Cytochrome P450 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

Long Evans rat

Organs/Tissues

turbinate

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Quantitative value

156.77

Measurement pX

3.8

Metabolite RN

2417108

Metabolite name

Monoethylglycinexylidide

Concomitants: Compound RN

24140787; 3885115

Concomitants: Compound name

Glucose-6-phosphate; NADP

Concomitants: Compound role

COM; COE

148 of 1220 Target Name Target Synonyms

Cytochrome P450 [Rattus norvegicus] cyp1a1; cyp1b1; cytochrome p450

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Target Uniprot ID

a7tud9; q64590; q80ue2; q9esw3

Target, Subunit, Species

Cytochrome P450 [Rattus norvegicus]

Target Mutant/Chimera Details

Cytochrome P450 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

Long Evans rat

Organs/Tissues

nose mucosa

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Quantitative value

505.23

Measurement pX

3.3

Metabolite RN

2417108

Metabolite name

Monoethylglycinexylidide

Concomitants: Compound RN

24140787; 3885115

Concomitants: Compound name

Glucose-6-phosphate; NADP

Concomitants: Compound role

COM; COE

149 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

LD50 270 mg/kg (white mice)

Measurement Parameter

qualitative

Daukshas, V. K.; Ramanauskas, Yu. Yu.; Udrenaite, E. B.; Brukshtus, A. B.; Yautakene, I. Yu.; et al.; Pharmaceutical Chemistry Journal; vol. 24; nb. 5; (1990); p. 362 - 365; Khimiko-Farmatsevticheskii Zhurnal; vol. 24; nb. 5; (1990); p. 37 - 39, View in Reaxys 150 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

duration of action of the anaesthetic tested as 0.5percent W/V solution in the guinea-pig intradermal wheal test: 1-1.5

Measurement Parameter

qualitative

Al-Saadi; Sneader; Arzneimittel-Forschung/Drug Research; vol. 41; nb. 2; (1991); p. 115 - 118, View in Reaxys 151 of 1220 Bioassay Category Bioassay Name

In Vitro (Efficacy) In Vitro (others)

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Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

in vitro effect on the water permeability of negatively charged liposomes induced by hypertonic osmotic shock

Measurement Parameter

qualitative

Shimooka; Seto; Terada; Chemical and Pharmaceutical Bulletin; vol. 40; nb. 7; (1992); p. 1880 - 1882, View in Reaxys 152 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

local anaesthetic activity in vitro (sciatic nerve of the frog)

Measurement Parameter

qualitative

Geronikaki; Theophilidis; European Journal of Medicinal Chemistry; vol. 27; nb. 7; (1992); p. 709 - 716, View in Reaxys 153 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

Local anesthetic activity in male Hartley guinea pigs (surface anesthesia, the loss of corneal reflex). ED(50) = 0.22 (w/v percent); Relative potency: 5.8

Measurement Parameter

qualitative

Yamamoto; Nakamura; Nagasaka; Asai; Chemical and Pharmaceutical Bulletin; vol. 35; nb. 8; (1987); p. 3419 - 3424, View in Reaxys 154 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : skin penetrationTarget : cadaver trunk skin of humanBioassay : Example 4 Transdermal delivery of Lidocaine by microbial cellulose in vitro using human cadaver skin diffusion cell study The study was carried out to test microbial cellulose containing a solution of 10% lidocaine HCl in water tested on two different skin donors using a finite dose in vitro cadaver

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Route of Adm.

transdermal administration

Qualitative Results

Measurement Parameter

qualitative

Patent; Serafica, Gonzalo; Mink, Richard; Hoon, Russell; Damien, Christopher; EP1849463; (A2); (2007), View in Reaxys 155 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : |biotransformation Bioassay : (14C)-radiolabeled chemical liver perfusion in a oncethrough fashion with red-blood-cell-free Krebs-Henseleit buffer containing 0-2 percent bovine serum albumine; effluent perfusate HPLC analysis

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

metabolites: hydroxymonoethyl glycine xylidide, hydroxylignocaine, monoethylglycine xylidide

Measurement Parameter

qualitative

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Mellick, George D.; Roberts, Michael S.; Journal of Pharmacy and Pharmacology; vol. 49; nb. 10; (1997); p. 1008 - 1018, View in Reaxys 156 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : |pharmacokinetics Bioassay : (14C)-radiolabeled chemical; normal and retrograde flow directions with perfusate flow rates of 20-30 mL/min liver perfusion in a once-through fashion with red-blood-cell-free Krebs-Henseleit buffer containing 0-2 percent bovine serum albumine; twocompartment dispersion model

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

outflow-concentration-time profile: 0.35; hepatic availability: 0.42; mean transit time: 75.80 s

Measurement Parameter

qualitative

Mellick, George D.; Roberts, Michael S.; Journal of Pharmacy and Pharmacology; vol. 49; nb. 10; (1997); p. 1008 - 1018, View in Reaxys 157 of 1220 Substance Effect

Toxic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : immobilizationBioassay : protozoan of the 1630/1W strain, Culture Centre of Algae and Protozoa, National Environment Research Council, Cumbria, UK in culture medium containing proteose peptone powder, yeast extract, Ca(2+), Mg(2+) and K(1+); incubated at 30 deg C for 45 min; effect on the swimming speed examined

Biological Species/NCBI ID

Tetrahymena pyriformis

Substance RN

3917968View in Reaxys

Substance Name

178204

Measurement Parameter

IC50

Unit

Quantitative value

85.73

Measurement pX

1.07

Darcy; Kelly; Leonard; Henry; Toxicology Letters; vol. 128; nb. 1-3; (2002); p. 207 - 214, View in Reaxys 158 of 1220 Substance Effect

Toxic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Biological Species/NCBI ID

Tetrahymena pyriformis

Substance RN

3917968View in Reaxys

Substance Name

178204

Measurement Parameter

EC50

Unit

Quantitative value

57.21

Measurement pX

1.24

Darcy; Kelly; Leonard; Henry; Toxicology Letters; vol. 128; nb. 1-3; (2002); p. 207 - 214, View in Reaxys

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159 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

penetration into the optic nerve fibers, effect of additive (cats)

Measurement Parameter

qualitative

Hemo; Touitou; Zauberman; Journal of Pharmaceutical Sciences; vol. 76; nb. 9; (1987); p. 692 - 694, View in Reaxys 160 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

cross-reactivity of procainamide antibody: concentration for 50percent inhibition of binding, M x 10-5 > 800

Measurement Parameter

qualitative

Mojaverian; Chase; Journal of Pharmaceutical Sciences; vol. 69; nb. 6; (1980); p. 721 - 724, View in Reaxys 161 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

Voltage clamp measurements on the frog node of Raniver, on the sheep cardiac Purkinje fibres and rat phrenic nerve diaphragm

Measurement Parameter

qualitative

Mitolo-Chieppa; Carratu; Dubois; Mugelli; Amerine; Conte-Camerino; Siro-Brigiani; Journal of Pharmacy and Pharmacology; vol. 37; nb. 1; (1985); p. 68 - 70, View in Reaxys 162 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : |transport Target : human abdominal skinBioassay : SC: stratum corneum; DC: donor compartment; IC: intrinsic conductivity full-thickness epidermal membranes mounted between two glass half-cells with SC facing DC; exposed to donor soln. contg. title comp.; receptor volume removed at 15-60 min; epidermal transport of title comp. detd.; specific conductance measured; IC detd.

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

1 nM

Qualitative Results

title comp. IC and mobility were 79.9/773 μS/cm and 0.83/0.80 cm2/ohm/F at 1/10 nmol/l, respectively; table

Measurement Parameter

qualitative

Lai, Pamela M.; Roberts, Michael S.; Pharmaceutical Research; vol. 15; nb. 10; (1998); p. 1579 - 1588, View in Reaxys 163 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

cardiomyopathy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

90 mg/h

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Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration (parameters)

Unit

µg/mL

Quantitative value

3.9

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Maeda, Yorinobu; Funakoshi, Sachiyo; Nakamura, Mamoru; Fukuzawa, Masataka; Kugaya, Yukimasa; Yamasaki, Miho; Tsukiai, Satsuki; Murakami, Teruo; Takano, Mikihisa; Clinical Pharmacology and Therapeutics; vol. 71; nb. 5; (2002); p. 389 - 397, View in Reaxys 164 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

cardiomyopathy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

90 mg/h

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration (parameters)

Unit

µg/mL

Quantitative value

4.53

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

cardiomyopathy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

60 mg/h

Substance Route of Adm.

intravenous administration

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Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration (parameters)

Unit

µg/mL

Quantitative value

3.19

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

cardiomyopathy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

120 mg/h

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration (parameters)

Unit

µg/mL

Quantitative value

6.84

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

cardiomyopathy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

78 mg/h

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

97/467

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Measurement Parameter

concentration (parameters)

Unit

µg/mL

Quantitative value

5.7

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

cardiomyopathy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

42 mg/h

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration (parameters)

Unit

µg/mL

Quantitative value

2.71

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

cardiomyopathy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

42 mg/h

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration (parameters)

Unit

µg/mL

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Quantitative value

2.71

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

cardiomyopathy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

90 mg/h

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration (parameters)

Unit

h/L

Measurement Object

Dose-Corrected

Quantitative value

4.3

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

cardiomyopathy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

90 mg/h

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration (parameters)

Unit

h/L

Measurement Object

Dose-Corrected

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Quantitative value

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

cardiomyopathy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

60 mg/h

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration (parameters)

Unit

h/L

Measurement Object

Dose-Corrected

Quantitative value

5.3

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

cardiomyopathy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

120 mg/h

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration (parameters)

Unit

h/L

Measurement Object

Dose-Corrected

100/467

2018-05-14 08:43:54

Quantitative value

5.7

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

cardiomyopathy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

78 mg/h

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration (parameters)

Unit

h/L

Measurement Object

Dose-Corrected

Quantitative value

7.3

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

cardiomyopathy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

42 mg/h

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration (parameters)

Unit

h/L

Measurement Object

Dose-Corrected

101/467

2018-05-14 08:43:54

Quantitative value

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

cardiomyopathy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

42 mg/h

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration (parameters)

Unit

h/L

Measurement Object

Dose-Corrected

Quantitative value

6.5

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

C[lambda1]

Unit

µg/mL

Quantitative value

5.7

Deviation

1.40000

102/467

2018-05-14 08:43:54

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

C[lambda2]

Unit

µg/mL

Quantitative value

Deviation

0.700000

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

lambda1

Unit

h-1

Quantitative value

12.6

Deviation

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

103/467

2018-05-14 08:43:54

Measurement Parameter

lambda2

Unit

h-1

Quantitative value

0.7

Deviation

0.100000

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

k12

Unit

h-1

Quantitative value

6.1

Deviation

1.80000

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

k21

Unit

h-1

Quantitative value

5.6

Deviation

1.30000

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

104/467

2018-05-14 08:43:54

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Kel

Unit

h-1

Quantitative value

1.6

Deviation

0.100000

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

Deviation

0.100000

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Vdss

Unit

L/kg

Quantitative value

2.7

Deviation

0.700000

Metabolism/Transport Binding

105/467

2018-05-14 08:43:54

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

CL (0-inf)

Unit

L/h/kg

Quantitative value

2.1

Deviation

0.400000

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-inf)

Unit

µg.h/mL

Quantitative value

5.9

Deviation

1.10000

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Vc (central volume of distribution)

Unit

L/kg

Quantitative value

1.3

Deviation

0.300000

106/467

2018-05-14 08:43:54

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

V2 (second compartment)

Unit

L/kg

Quantitative value

1.4

Deviation

0.400000

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

C[lambda1]

Unit

µg/mL

Quantitative value

5.7

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

C[lambda2]

107/467

2018-05-14 08:43:54

Unit

µg/mL

Quantitative value

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

lambda1

Unit

h-1

Quantitative value

12.6

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

lambda2

Unit

h-1

Quantitative value

0.7

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

108/467

2018-05-14 08:43:54

Measurement Parameter

k12

Unit

h-1

Quantitative value

6.1

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

k21

Unit

h-1

Quantitative value

5.6

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Kel

Unit

h-1

Quantitative value

1.6

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

109/467

2018-05-14 08:43:54

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Vdss

Unit

L/kg

Quantitative value

2.7

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

CL (0-inf)

Unit

L/h/kg

Quantitative value

2.1

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

110/467

2018-05-14 08:43:54

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-inf)

Unit

µg.h/mL

Quantitative value

5.9

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Vc (central volume of distribution)

Unit

L/kg

Quantitative value

1.3

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

V2 (second compartment)

Unit

L/kg

Quantitative value

1.4

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

111/467

2018-05-14 08:43:54

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

kel i/kel

Quantitative value

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el i/t1/2 el

Quantitative value

1.1

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Vdss i/Vdss

Quantitative value

0.815

112/467

2018-05-14 08:43:54

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

CL i/CL (0-inf)

Quantitative value

0.762

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC i/AUC (0-inf)

Quantitative value

1.288

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

113/467

2018-05-14 08:43:54

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Vc i/Vc

Quantitative value

0.769

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

fu (unbound fraction)

Quantitative value

0.78

Deviation

0.0700000

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

114/467

2018-05-14 08:43:54

Substance Dosing Regimen

Single

Measurement Parameter

fu (unbound fraction)

Quantitative value

0.78

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

fu i/fu

Quantitative value

1.0513

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

31.2000 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Kp (tissue-to-plasma ratio)

Quantitative value

2.1

Deviation

0.400000

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

Japanese White (rabbit)

115/467

2018-05-14 08:43:54

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

31.2000 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Kp (tissue-to-plasma ratio)

Quantitative value

2.2

Deviation

0.500000

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

31.2000 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Kp (tissue-to-plasma ratio)

Quantitative value

8.9

Deviation

0.600000

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

31.2000 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Kp (tissue-to-plasma ratio)

Quantitative value

15.9

Deviation

1.20000

Pharmacokinetic Pharmacokinetic

116/467

2018-05-14 08:43:54

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

31.2000 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

brain/plasma ratio

Quantitative value

2.5

Deviation

0.100000

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

31.2000 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Kp (tissue-to-plasma ratio)

Quantitative value

15.9

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

31.2000 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Kp (tissue-to-plasma ratio)

Quantitative value

2.1

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

Japanese White (rabbit)

117/467

2018-05-14 08:43:54

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

31.2000 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Kp (tissue-to-plasma ratio)

Quantitative value

2.2

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

31.2000 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Kp (tissue-to-plasma ratio)

Quantitative value

8.9

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

31.2000 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

brain/plasma ratio

Quantitative value

2.5

In Vivo (Animal models)

Bioassay Name

Blood bleeding/clotting

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

118/467

2018-05-14 08:43:54

Substance Name

lidocaine hydrochloride

Substance Dose

33.5000 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

activated partial thromboplastin time

Unit

second

Measurement Object

Activated partial thromboplastin time (aPTT)

Quantitative value

27.9

Inglis, Anne Marie L; Sheth, Sunita B; Hursting, Marcie J; Tenero, David M; Graham, Alison M; DiCicco, Robert A; American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists; vol. 59; nb. 13; (2002); p. 1258 - 1266, View in Reaxys 223 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

C[lambda1]

Unit

µg/mL

Quantitative value

7.3

Deviation

0.600000

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

C[lambda2]

Unit

µg/mL

119/467

2018-05-14 08:43:54

Quantitative value

4.5

Deviation

0.300000

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

lambda1

Unit

h-1

Quantitative value

12.6

Deviation

7.30000

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

lambda2

Unit

h-1

Quantitative value

0.7

Deviation

0.100000

120/467

2018-05-14 08:43:54

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

k12

Unit

h-1

Quantitative value

6.5

Deviation

4.60000

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

k21

Unit

h-1

Quantitative value

5.1

Deviation

2.60000

Concomitants: Compound RN

4209895

121/467

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Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Kel

Unit

h-1

Quantitative value

1.6

Deviation

0.200000

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

1.1

Deviation

0.100000

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

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Concomitants: Compound role

ICP

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Vdss

Unit

L/kg

Quantitative value

2.2

Deviation

0.300000

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

CL (0-inf)

Unit

L/h/kg

Quantitative value

1.6

Deviation

0.200000

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

123/467

2018-05-14 08:43:54

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-inf)

Unit

µg.h/mL

Quantitative value

7.6

Deviation

0.800000

Statistical sgnificance (pvalue)

0.05

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Vc (central volume of distribution)

Unit

L/kg

Quantitative value

Deviation

0.100000

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

124/467

2018-05-14 08:43:54

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

V2 (second compartment)

Unit

L/kg

Quantitative value

1.2

Deviation

0.300000

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

10 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

fu (unbound fraction)

Quantitative value

0.82

Deviation

0.0500000

Concomitants: Compound RN

4209895

Concomitants: Compound name

Mexiletine hydrochloride

Concomitants: Compound role

ICP

Pharmacokinetic

125/467

2018-05-14 08:43:54

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

31.2000 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Kp (tissue-to-plasma ratio)

Quantitative value

10.7

Deviation

1.50000

Statistical sgnificance (pvalue)

0.05

Concomitants: Compound RN

2092205

Concomitants: Compound name

Mexiletine

Concomitants: Compound role

ICP

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

31.2000 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Kp (tissue-to-plasma ratio)

Quantitative value

6.6

Deviation

0.600000

Statistical sgnificance (pvalue)

0.05

Concomitants: Compound RN

2092205

Concomitants: Compound name

Mexiletine

Concomitants: Compound role

ICP

Pharmacokinetic Pharmacokinetic

126/467

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Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

31.2000 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Kp (tissue-to-plasma ratio)

Quantitative value

2.6

Deviation

0.300000

Concomitants: Compound RN

2092205

Concomitants: Compound name

Mexiletine

Concomitants: Compound role

ICP

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

31.2000 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Kp (tissue-to-plasma ratio)

Quantitative value

2.3

Deviation

0.300000

Concomitants: Compound RN

2092205

Concomitants: Compound name

Mexiletine

Concomitants: Compound role

ICP

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

Japanese White (rabbit)

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

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Substance Dose

31.2000 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

brain/plasma ratio

Quantitative value

2.8

Deviation

0.700000

Concomitants: Compound RN

2092205

Concomitants: Compound name

Mexiletine

Concomitants: Compound role

ICP

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p05177 + p08684

Target PDB ID

2hi4 + 1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild; Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human; human

Target Transfection

Non Transfected; Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

Human Caucasian

Population State

Healthy

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

0 mM

Measurement Parameter

Vmax

Unit

pmol/min/mg protein

Measurement Object

LOW

Quantitative value

31.5

Metabolite RN

2417108; 2127970

Metabolite name

Norlidocaine; 3-Hydroxylidocaine

128/467

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Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

243 of 1220 Target Name

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p05177 + p08684

Target PDB ID

2hi4 + 1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild; Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human; human

Target Transfection

Non Transfected; Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

Human Caucasian

Population State

Healthy

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

0 mM

Measurement Parameter

Vmax

Unit

pmol/min/mg protein

Measurement Object

LOW

Quantitative value

3840

Metabolite RN

2417108; 2127970

Metabolite name

Norlidocaine; 3-Hydroxylidocaine

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

244 of 1220 Target Name Target Synonyms

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human] cholesterol 25-hydroxylase; cyp1a2; cypia2; cytochrome p(3)450; cytochrome p450 1a2; cytochrome p450 4; cytochrome p450-p3 + 1,8-cineole 2-exo-monooxygenase; albendazole monooxygenase; albendazole sulfoxidase; cholesterol 25-hydroxylase; cyp3a3; cyp3a4; cypiiia3; cypiiia4; cytochrome p450 3a3; cytochrome p450 3a4; cytochrome p450 hlp; cytochrome p450 nf-25; cyto-

129/467

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chrome p450-pcn1; nifedipine oxidase; quinine 3-monooxygenase; taurochenodeoxycholate 6-alpha-hydroxylase Target Uniprot ID

p05177 + p08684

Target PDB ID

2hi4 + 1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild; Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human; human

Target Transfection

Non Transfected; Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

Human Caucasian

Population State

Healthy

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

0 mM

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Measurement Object

LOW

Quantitative value

1530

Measurement pX

2.82

Metabolite RN

2417108; 2127970

Metabolite name

Norlidocaine; 3-Hydroxylidocaine

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

245 of 1220 Target Name

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p05177 + p08684

Target PDB ID

2hi4 + 1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild; Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human; human

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Target Transfection

Non Transfected; Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

Human Caucasian

Population State

Healthy

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

0 mM

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Measurement Object

LOW

Quantitative value

1570

Measurement pX

2.8

Metabolite RN

2417108; 2127970

Metabolite name

Norlidocaine; 3-Hydroxylidocaine

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

246 of 1220 Target Name

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p05177 + p08684

Target PDB ID

2hi4 + 1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild; Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human; human

Target Transfection

Non Transfected; Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

Human Caucasian

Population State

Healthy

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

131/467

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Substance Name

Lidocaine hydrochloride

Substance Dose

0 mM

Measurement Parameter

Vmax

Unit

pmol/min/mg protein

Measurement Object

HIGH

Quantitative value

17.5

Metabolite RN

2417108; 2127970

Metabolite name

Norlidocaine; 3-Hydroxylidocaine

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

247 of 1220 Target Name

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p05177 + p08684

Target PDB ID

2hi4 + 1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild; Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human; human

Target Transfection

Non Transfected; Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

Human Caucasian

Population State

Healthy

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

0 mM

Measurement Parameter

Vmax

Unit

pmol/min/mg protein

Measurement Object

HIGH

Quantitative value

600

Metabolite RN

2417108; 2127970

Metabolite name

Norlidocaine; 3-Hydroxylidocaine

Concomitants: Compound RN

77911

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Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

248 of 1220 Target Name

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p05177 + p08684

Target PDB ID

2hi4 + 1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild; Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human; human

Target Transfection

Non Transfected; Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

Human Caucasian

Population State

Healthy

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

0 mM

Measurement Parameter

S50

Unit

µM

Measurement Object

HIGH

Quantitative value

103

Metabolite RN

2417108

Metabolite name

Norlidocaine

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

249 of 1220 Target Name

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p05177 + p08684

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Target PDB ID

2hi4 + 1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild; Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human; human

Target Transfection

Non Transfected; Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

Human Caucasian

Population State

Healthy

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

0 mM

Measurement Parameter

nH (Hill coefficient)

Measurement Object

HIGH

Quantitative value

1.57

Metabolite RN

2417108

Metabolite name

Norlidocaine

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

250 of 1220 Target Name

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p05177 + p08684

Target PDB ID

2hi4 + 1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild; Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human; human

Target Transfection

Non Transfected; Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

Human Caucasian

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Population State

Healthy

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

0 mM

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Measurement Object

HIGH

Quantitative value

155

Measurement pX

3.81

Metabolite RN

2127970

Metabolite name

3-Hydroxylidocaine

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

251 of 1220 Target Name

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p05177 + p08684

Target PDB ID

2hi4 + 1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild; Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human; human

Target Transfection

Non Transfected; Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

Human Caucasian

Population State

Healthy

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

0 mM

Measurement Parameter

Ksi

Unit

µM

135/467

2018-05-14 08:43:54

Measurement Object

HIGH

Quantitative value

0.002

Metabolite RN

2127970

Metabolite name

3-Hydroxylidocaine

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

252 of 1220 Target Name

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p05177 + p08684

Target PDB ID

2hi4 + 1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild; Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human; human

Target Transfection

Non Transfected; Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

Human Caucasian

Population State

Healthy

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

0 mM

Measurement Parameter

CLint

Unit

µL/min/mg protein

Measurement Object

LOW

Quantitative value

0.0206

Metabolite RN

2417108; 2127970

Metabolite name

Norlidocaine; 3-Hydroxylidocaine

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

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253 of 1220 Target Name

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p05177 + p08684

Target PDB ID

2hi4 + 1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild; Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human; human

Target Transfection

Non Transfected; Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

Human Caucasian

Population State

Healthy

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

0 mM

Measurement Parameter

CLint

Unit

µL/min/mg protein

Measurement Object

LOW

Quantitative value

2.45

Metabolite RN

2417108; 2127970

Metabolite name

Norlidocaine; 3-Hydroxylidocaine

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

254 of 1220 Target Name

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p05177 + p08684

Target PDB ID

2hi4 + 1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 1A2 [human]; Cytochrome P450 3A4 [human]

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Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild; Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human; human

Target Transfection

Non Transfected; Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

Human Caucasian

Population State

Healthy

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

0 mM

Measurement Parameter

CLint

Unit

µL/min/mg protein

Measurement Object

HIGH

Quantitative value

0.113

Metabolite RN

2127970

Metabolite name

3-Hydroxylidocaine

Concomitants: Compound RN

77911

Concomitants: Compound name

NADPH

Concomitants: Compound role

COE

255 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Biological Species/NCBI ID

Tuck Ordinary mouse

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Route of Adm.

subcutaneous administration

Substance Dosing Regimen

Repeated

Measurement Parameter

ED50

Unit

mg/kg

Measurement Object

against abdominal constriction responses

Quantitative value

93.3

Concomitants: Compound RN

1764436

Concomitants: Compound name

Acetylcholine

Concomitants: Compound role

IAV

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Collier; Dinneen; Johnson; Schneider; British journal of pharmacology and chemotherapy; vol. 32; nb. 2; (1968); p. 295 - 310, View in Reaxys 256 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

Spontaneous activity

Biological Species/NCBI ID

Tuck Ordinary mouse

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Route of Adm.

subcutaneous administration

Substance Dosing Regimen

Single

Measurement Parameter

ED50

Unit

mg/kg

Measurement Object

to cause fall from the surface of a drum rotating at 1rev/min

Quantitative value

55.9

Collier; Dinneen; Johnson; Schneider; British journal of pharmacology and chemotherapy; vol. 32; nb. 2; (1968); p. 295 - 310, View in Reaxys 257 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Flux transport

Bioassay Details

Effect : |transport Target : ear skin of rabbitBioassay : In vitro permeation experiments through rabbit ear skin The in vitro permeation of a drug from patches prepared in example 1a) was analysed using a vertical Franz diffusion cell and a barrier consisting of rabbit ear skin, in accordance with the protocol described by Cristina Padula et al, in Journal

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

title compound permeation was higher after application of patch with protective layer than after application of patch without protection layer; figure is given

Measurement Parameter

qualitative

Patent; LABORATORIO ITALIANO BIOCHIMICO FARMACEUTICO LISAPHARMA S.P.A.; WO2006/8320; (2006); (A2) English, View in Reaxys 258 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

antinociceptive-, spontaneous motor-, anticonvulsive activity (mice, rats).

Measurement Parameter

qualitative

Karttunen; Mannisto; Lahovaara; Havas; Arzneimittel-Forschung/Drug Research; vol. 38; nb. 4 A; (1988); p. 605 - 608, View in Reaxys 259 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

antitussives properties (guinea-pigs), effect on lung mechanics

Measurement Parameter

qualitative

Salonen; Arzneimittel-Forschung/Drug Research; vol. 38; nb. 4 A; (1988); p. 609 - 612, View in Reaxys 260 of 1220 Bioassay Category

In Vitro (Efficacy)

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Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

antitussives properties; effect on platelet aggregation in human platelet-rich plasma

Measurement Parameter

qualitative

Kangasaho; Arzneimittel-Forschung/Drug Research; vol. 38; nb. 4 A; (1988); p. 613 - 616, View in Reaxys 261 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : on electrical fibrillation thresholdBioassay : control: title comp. not applied (6 animals); EFT: electrical fibrillation treshold 8 animals, ca. 6 weeks old, 22-28 kg; anesthetized; thoracotomized; left anterior descending coronary artery occluded for 30-150s; after each occlusion EFT measured using trains of diastolic stimuli with intensity increasing in 0.5-1.0 mA increments

Biological Species/NCBI ID

pig

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Route of Adm.

intravenous administration

Qualitative Results

title comp. did not affect EFT after 30 s ischemia, after ischemia periods >=60s title comp. induced greater fall of EFT as compared to controls (diagram)

Measurement Parameter

qualitative

Aupetit, Jean-Francois; Loufoua-Moundanga, Joseph; Faucon, Georges; Timour, Quadiri; British Journal of Pharmacology; vol. 120; nb. 3; (1997); p. 523 - 529, View in Reaxys 262 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : on fibrillation onsetBioassay : control: title comp. not applied (6 animals); MAP: monophasic action potential 8 animals, ca. 6 weeks old, 22-28 kg; anesthetized; thoracotomized; left anterior descending coronary artery occluded for 30-150s; number of animals at which occured spontaneous fibrillation after ischemia period recorded

Biological Species/NCBI ID

pig

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Route of Adm.

intravenous administration

Qualitative Results

title comp. induced increased incidence of fibrillations after ischemia periods >=90 s as compared to controls (table)

Measurement Parameter

qualitative

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : on monophasic action potential durationBioassay : control: title comp. not applied (6 animals); MAP: monophasic action potential 8 animals, ca. 6 weeks old, 22-28 kg; anesthetized; thoracotomized; left anterior descending coronary artery occluded for 30-150s; MAP was continuously monitored through electrode implanted in subepicardial area subjected to ischemia

Biological Species/NCBI ID

pig

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Route of Adm.

intravenous administration

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Qualitative Results

after 60 s and 90 s ischemia periods title comp. induced shortening of MAP duration as compared to controls (table)

Measurement Parameter

qualitative

Antiarrhytmic

Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Bioassay : control: title comp. not applied 8 animals, ca. 6 weeks old, 22-28 kg; anesthetized; thoracotomized; electrical fibrillation treshold (EFT) measured using trains of diastolic stimuli with intensity increasing in 1.0 mA increments

Biological Species/NCBI ID

pig

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Route of Adm.

intravenous administration

Qualitative Results

title comp. significantly increased the EFT

Measurement Parameter

qualitative

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : neurotransmitter uptake; inhibition ofTarget : COS cellsBioassay : reference comp.: cocaine; NE: norepinephrine cells expressing rat NE transporter; title comp. effect on <3H>NE uptake determined; incubation with 10 nmol/l <3H>NE (10 min, 37 deg C); radioactivity measured by liquid scintillation counting

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

1 µM

Qualitative Results

title comp. inhibited <3H>NE uptake in dose-dependent manner; title comp. was less potent than cocaine (figure)

Measurement Parameter

qualitative

Sato, Tomoyuki; Kitayama, Shigeo; Mitsuhata, Chieko; Ikeda, Tetsurou; Morita, Katsuya; Dohi, Toshihiro; NaunynSchmiedeberg's Archives of Pharmacology; vol. 361; nb. 2; (2000); p. 214 - 220, View in Reaxys 266 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : neurotransmitter uptake; inhibition ofTarget : COS cellsBioassay : reference comp.: cocaine; 5-HT: serotonin cells expressing rat 5-HT transporter; title comp. effect on <3H>5-HT uptake determined; incubation with 10 nmol/l <3H>5-HT (10 min, 37 deg C); radioactivity measured by liquid scintillation counting

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

1 µM

Qualitative Results

title comp. inhibited <3H>5-HT uptake in dose-dependent manner; title comp. was less potent than cocaine (figure)

Measurement Parameter

qualitative

In Vitro (Efficacy)

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Bioassay Name

In Vitro (others)

Bioassay Details

Effect : neurotransmitter uptake; inhibition ofTarget : COS cellsBioassay : reference comp.: cocaine, had no effect up to 1 mmol/l; GAT: GABA transporter cells expressing mouse GAT; title comp. effect on <3H>GABA uptake determined; incubation with 10 nmol/l <3H>GABA (10 min, 37 deg C); radioactivity measured by liquid scintillation counting

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

1 mM

Measurement Parameter

qualitative

Qualitative value

Measurement pX

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : binding; inhibition ofTarget : COS cellsBioassay : reference comp.: cocaine (IC50 = 0.22 μmol/l); DA: dopamine; CFT: 2-ω-carbomethoxy-3-ω-(4-fluorophenyl)tropane, cocaine analogue cells expressing rat DA transporter; title comp. effect on <3H>CFT binding determined; incubation with 4 nmol/l <3H>CFT (2 h, on ice); radioactivity measured by liquid scintillation counting

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

0.0100000 µM

Measurement Parameter

IC50

Unit

µM

Quantitative value

1000

Measurement pX

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : neurotransmitter uptake; inhibition ofTarget : COS cellsBioassay : reference comp.: cocaine (IC50 = 0.68 μmol/l); DA: dopamine cells expressing rat DA transporter; title comp. effect on <3H>DA uptake determined; incubation with 10 nmol/l <3H>DA (10 min, 37 deg C); radioactivity measured by liquid scintillation counting

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

0.0100000 µM

Measurement Parameter

IC50

Unit

µM

Quantitative value

1000

Measurement pX

In Vitro (Efficacy)

Bioassay Name

Flux transport

Bioassay Details

Effect : |transport Target : Sprague-Dawley rat abdominal skinBioassay : chambers: donor (D) and receptor (R); acute renal failure (ARF) induced by glycerol (50 percent v/v, i.m.); PBS: phosphate buffered saline; control: normal rat skin treated with 0.9 percent saline and title comp.; permeability

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coefficient of control: 4.08 cm/s*1E6 ARF rat skin sandwiched between D and R; title comp. or PBS introduced into D and R, resp.; microdialysis probe inserted into R and perfused with PBS (3 μl/min, pH 7.4); permeation study done at 37 deg C; dialysate analyzed by HPLC; in vitro Substance RN

3917968View in Reaxys

Substance Name

178204

Measurement Parameter

qualitative

Qualitative value

Measurement pX

Lili, Cui; Shibata, Nobuhito; Yoshikawa, Yukako; Takada, Kanji; Biological and Pharmaceutical Bulletin; vol. 26; nb. 8; (2003); p. 1150 - 1154, View in Reaxys 271 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : |pharmacokinetics Bioassay : acute renal failure (ARF) induced by glycerol (50 percent v/v, i.m.); control: normal rats admin. with 0.9 percent saline and title comp.; dialysate collected every 1 h for 10 h; blood samples collected at 0.5 to 9.5 h after starting dialysis ARF rats anaesthetized; microdialysis probe inserted into abdominal skin; Tyrode solution perfused at 3 μl/min; title comp. added to the reservoir; dialysate and blood samples collected; analyzed by HPLC; in vivo

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Route of Adm.

transdermal administration

Qualitative Results

title comp. showed significantly increased AUC values in plasma of ARF rats compared to control (from 2.18 to 4.87 μg*h/ml); no significant difference in AUC values of skin dialysate in ARF (41.88 μg*h/ml) and control (43.07 μg*h/ml) rats;

Measurement Parameter

qualitative

Lili, Cui; Shibata, Nobuhito; Yoshikawa, Yukako; Takada, Kanji; Biological and Pharmaceutical Bulletin; vol. 26; nb. 8; (2003); p. 1150 - 1154, View in Reaxys 272 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : |pharmacokinetics Bioassay : acute renal failure (ARF) induced by glycerol (50 percent v/v, i.m.); control: normal rats administered with 0.9 percent saline and title comp.; pharmacokinetic parameters studied: Vd (l/kg), K (l/h), CLt (l/h/kg), and CSS (μg/ml) ARF rats anaesthetized; title comp. administered; blood samples collected from 0.5 to 6 h after start of infusion; conc. of title comp. in plasma analyzed by HPLC; pharmacokinetics parameters determined

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

5 mg/kg

Substance Route of Adm.

intravenous administration

Qualitative Results

title comp. showed decreased volume of distribution (Vd) and clearance (CLt) in ARF rats and showed plasma conc. of 1.47 μg/ml; values of Vd: 1.91 l/kg, K: 1.29 l/h, CLt: 5.40 l/h/kg, CSS: 1.24

Measurement Parameter

qualitative

Lili, Cui; Shibata, Nobuhito; Yoshikawa, Yukako; Takada, Kanji; Biological and Pharmaceutical Bulletin; vol. 26; nb. 8; (2003); p. 1150 - 1154, View in Reaxys 273 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : |transport Bioassay : acute renal failure (ARF) induced by glycerol (50 percent v/v, i.m.); FITC: ω-D-glucopyranosyl fluorescein isothiocyanate; control: normal rats admin. with 0.9 percent

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saline and title comp. ARF rats admin. with title comp.; FITC-albumin (10 mg/kg, i.v.) injected; sacrificed after 1 h; abdominal skin and muscle tissue removed; homogenized and centrifuged; fluorescence intensity of supernatant measured spectrophotometrically at 520 nm Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Route of Adm.

intravenous administration

Qualitative Results

title comp. exhibited significantly increased blood vessel permeability in abdominal muscle tissue in ARF rat compared to control, but not in case of epidermis; table

Measurement Parameter

qualitative

Lili, Cui; Shibata, Nobuhito; Yoshikawa, Yukako; Takada, Kanji; Biological and Pharmaceutical Bulletin; vol. 26; nb. 8; (2003); p. 1150 - 1154, View in Reaxys 274 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : |protein binding Target : Sprague-Dawley rat plasmaBioassay : acute renal failure (ARF) induced by glycerol (50 percent v/v, i.m.); control: with normal rats administered with 0.9 percent saline and title comp. in vitro protein binding study; blood samples collected from ARF rats; plasma separated and treated with title comp.; concentrated and centrifuged for 10 min, 37 deg C; conc. of title comp. and percent protein binding determined

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

0.500000 mg/L

Qualitative Results

title comp. exhibited an significantly increased plasma protein-binding of 74.2 percent in ARF rats compared to control of 56.6 percent; table

Measurement Parameter

qualitative

Lili, Cui; Shibata, Nobuhito; Yoshikawa, Yukako; Takada, Kanji; Biological and Pharmaceutical Bulletin; vol. 26; nb. 8; (2003); p. 1150 - 1154, View in Reaxys 275 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

concentration (parameters)

Unit

ng/mL

Quantitative value

53.4

Deviation

15.8000

Metabolite RN

24194177

Metabolite name

Methylhydroxy-Lidocaine

Sotaniemi; Rautio; Backstrom; Arvela; Pelkonen; British Journal of Clinical Pharmacology; vol. 39; nb. 1; (1995); p. 71 - 76, View in Reaxys 276 of 1220 Bioassay Category

Pharmacokinetic

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Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

liver fibrosis

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

concentration (parameters)

Unit

ng/mL

Quantitative value

4.6

Deviation

Statistical sgnificance (pvalue)

0.001

Metabolite RN

24194177

Metabolite name

Methylhydroxy-Lidocaine

Sotaniemi; Rautio; Backstrom; Arvela; Pelkonen; British Journal of Clinical Pharmacology; vol. 39; nb. 1; (1995); p. 71 - 76, View in Reaxys 277 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

liver fibrosis

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

concentration (parameters)

Unit

ng/mL

Quantitative value

19.1

Deviation

11.6000

Statistical sgnificance (pvalue)

0.001

Metabolite RN

24194177

Metabolite name

Methylhydroxy-Lidocaine

Sotaniemi; Rautio; Backstrom; Arvela; Pelkonen; British Journal of Clinical Pharmacology; vol. 39; nb. 1; (1995); p. 71 - 76, View in Reaxys 278 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

liver fibrosis

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Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

concentration (parameters)

Unit

ng/mL

Quantitative value

32.8

Deviation

14.2000

Statistical sgnificance (pvalue)

0.001

Metabolite RN

24194177

Metabolite name

Methylhydroxy-Lidocaine

Sotaniemi; Rautio; Backstrom; Arvela; Pelkonen; British Journal of Clinical Pharmacology; vol. 39; nb. 1; (1995); p. 71 - 76, View in Reaxys 279 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

chronic kidney failure

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

concentration (parameters)

Unit

ng/mL

Quantitative value

56.5

Deviation

26.1000

Metabolite RN

24194177

Metabolite name

Methylhydroxy-Lidocaine

Sotaniemi; Rautio; Backstrom; Arvela; Pelkonen; British Journal of Clinical Pharmacology; vol. 39; nb. 1; (1995); p. 71 - 76, View in Reaxys 280 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

epilepsy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

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Measurement Parameter

concentration (parameters)

Unit

ng/mL

Quantitative value

Deviation

14.1000

Statistical sgnificance (pvalue)

0.01

Metabolite RN

24194177

Metabolite name

Methylhydroxy-Lidocaine

Sotaniemi; Rautio; Backstrom; Arvela; Pelkonen; British Journal of Clinical Pharmacology; vol. 39; nb. 1; (1995); p. 71 - 76, View in Reaxys 281 of 1220 Target Name

calcium channel [Leporidae]

Target Synonyms

calcium channel

Target, Subunit, Species

calcium channel [Leporidae]

Target Mutant/Chimera Details

calcium channel [Leporidae]:Wild

Target Species (Bioactivity)

Leporidae

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Binding

Biological Species/NCBI ID

New Zealand White (rabbit)

Organs/Tissues

cardiac muscle

Cells/Cell Lines

cardiac muscle cell

Cell Fraction

Membrane

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Measurement Parameter

IC50

Unit

µM

Qualitative value

Quantitative value

1000

Measurement pX

Concomitants: Compound RN

498823; 498823

Concomitants: Compound name

Nitrendipine; [3H]-Nitrendipine

Concomitants: Compound role

NSB; RAD

Sanfilippo; Urbanski; Press; Dubinsky; Moore Jr.; Journal of Medicinal Chemistry; vol. 31; nb. 11; (1988); p. 2221 - 2227, View in Reaxys 282 of 1220 Target Name

calcium channel [dog]

Target Synonyms

calcium channel

Target, Subunit, Species

calcium channel [dog]

Target Mutant/Chimera Details

calcium channel [dog]:Wild

Target Species (Bioactivity)

dog

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Target Transfection

Non Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Organ contraction

Biological Species/NCBI ID

dog

Organs/Tissues

trachea muscle

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

10 µM

Measurement Parameter

% Inhibition

Unit

Qualitative value

Quantitative value

10000

Measurement pX

6.28

Concomitants: Compound RN

8137362

Concomitants: Compound name

KCl

Concomitants: Compound role

IND

Sanfilippo; Urbanski; Press; Dubinsky; Moore Jr.; Journal of Medicinal Chemistry; vol. 31; nb. 11; (1988); p. 2221 - 2227, View in Reaxys 283 of 1220 Substance Effect

Anaesthesic

Bioassay Category

In Vivo (Animal models)

Bioassay Name

Inverted Screen

Biological Species/NCBI ID

CD-1 mouse

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Route of Adm.

intramuscular administration

Substance Dosing Regimen

Single

Measurement Parameter

concentration (parameters)

Unit

% (w/v)

Measurement Object

lowest concentration causing local anesthesic activity

Quantitative value

Sanfilippo; Urbanski; Press; Dubinsky; Moore Jr.; Journal of Medicinal Chemistry; vol. 31; nb. 11; (1988); p. 2221 - 2227, View in Reaxys 284 of 1220 Substance Effect

Anaesthesic

Bioassay Category

In Vivo (Animal models)

Bioassay Name

Inverted Screen

Biological Species/NCBI ID

CD-1 mouse

Substance RN

3917968View in Reaxys

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Substance Name

lidocaine

Substance Route of Adm.

intramuscular administration

Substance Dosing Regimen

Single

Measurement Parameter

concentration (parameters)

Unit

% (w/v)

Measurement Object

lowest concentration causing local anesthesic activity

Quantitative value

Sanfilippo; Urbanski; Press; Dubinsky; Moore Jr.; Journal of Medicinal Chemistry; vol. 31; nb. 11; (1988); p. 2221 - 2227, View in Reaxys 285 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : anesthetic ability ability; effect onTarget : Swiss-Webster mouseBioassay : The rat tail flick test is used to determine the local anesthetic ability of lidocaine docusate compared with lidocaine hydrochloride. The rat is immobilized in a restraining sock, so that the tail is only exposed. The tail is dipped into hot water and the number of times the rat flicks its tail is

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

title compound showed lower and shorter anesthetic ability than lidocaine docusate at 1mM and 100 mM concentrations; figures are given

Measurement Parameter

qualitative

Patent; Rogers, Robin D.; Daly, Daniel T.; Swatloski, Richard P.; Hough, Whitney L.; Davis, James Hilliard; Smiglak, Marcin; Pernak, Juliusz; Spear, Scott K.; US2007/93462; (2007); (A1) English, View in Reaxys 286 of 1220 Target Name

voltage-gated sodium channel [Rattus norvegicus]

Target Synonyms

voltage-gated sodium channel

Target, Subunit, Species

voltage-gated sodium channel [Rattus norvegicus]

Target Mutant/Chimera Details

voltage-gated sodium channel [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Wistar rat

Organs/Tissues

prefrontal cortex

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

320 µM

Measurement Parameter

% Inhibition

Unit

Measurement Object

input resistance

Qualitative value

Quantitative value

Measurement pX

3.13

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287 of 1220 Target Name

voltage-gated sodium channel [Rattus norvegicus]

Target Synonyms

voltage-gated sodium channel

Target, Subunit, Species

voltage-gated sodium channel [Rattus norvegicus]

Target Mutant/Chimera Details

voltage-gated sodium channel [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Wistar rat

Organs/Tissues

prefrontal cortex

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

160 µM

Measurement Parameter

block time constant

Unit

Quantitative value

Deviation

288 of 1220 Target Name

voltage-gated sodium channel [Rattus norvegicus]

Target Synonyms

voltage-gated sodium channel

Target, Subunit, Species

voltage-gated sodium channel [Rattus norvegicus]

Target Mutant/Chimera Details

voltage-gated sodium channel [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Wistar rat

Organs/Tissues

prefrontal cortex

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

160 µM

Measurement Parameter

block time constant

Unit

Quantitative value

Deviation

3.40000

289 of 1220 Target Name Target Synonyms

voltage-gated sodium channel [Rattus norvegicus] voltage-gated sodium channel

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Target, Subunit, Species

voltage-gated sodium channel [Rattus norvegicus]

Target Mutant/Chimera Details

voltage-gated sodium channel [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Wistar rat

Organs/Tissues

prefrontal cortex

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

160 µM

Measurement Parameter

block time constant

Unit

Quantitative value

Deviation

0.400000

290 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

skin permeability from EtOH/panasate 800 (40/60), parameters - in vitro (female mouse), in vivo (Wistar rat): perm. rate (percent/h) - 2.3, 3.2; perm. percent (percent of dose at 12 h) - 19.4, 33.1; lag time (h) - 3.8, 0.5; residual percent (percent

Measurement Parameter

qualitative

Cheon Koo Lee; Uchida; Kitagawa; Yagi; Kim; Goto; Journal of Pharmaceutical Sciences; vol. 83; nb. 4; (1994); p. 562 565, View in Reaxys 291 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

penetration across isolated human epidermis at pH 3.67, the permeability coefficient (cm/h) (percent): 0.00032

Measurement Parameter

qualitative

Singh; Roberts; Journal of Pharmaceutical Sciences; vol. 83; nb. 6; (1994); p. 774 - 782, View in Reaxys 292 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

pharmacokinetics afer dermal application in male Wistar rats, effects of phenylephrine

Measurement Parameter

qualitative

Singh; Roberts; Journal of Pharmaceutical Sciences; vol. 83; nb. 6; (1994); p. 783 - 791, View in Reaxys 293 of 1220 Bioassay Category

In Vitro (Efficacy)

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Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

protecting action against maximal electroshock (ED 50: 19.0 mg/kg, mouse)

Measurement Parameter

qualitative

Fischer; Muller; Pharmazie; vol. 42; nb. 6; (1987); p. 420 - 421, View in Reaxys 294 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

anti-arrhytmic activity in mice at a dose 50 mg/kg ip; no anesthetic activity on guinea pig

Measurement Parameter

qualitative

Laguerre; Boyer; Carpy; Leger; Panconi; Vaugien; Cognic; European Journal of Medicinal Chemistry; vol. 28; nb. 1; (1993); p. 77 - 80, View in Reaxys 295 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

anaesthetic activity: 80 min of anaesthetic activity in rat sciatic nerve block test (male Wistar rats, in vivo); acute toxicity, LD50: 5.24E-2 M (male Swiss mice, i.p.); therapeutic index (LD50/IC50): 11.9 mg/Kg (mouse tail test)

Measurement Parameter

qualitative

Vazzana; Boido; Sparatore; Di Carlo; Raso; Pacilio; Farmaco; vol. 52; nb. 3; (1997); p. 131 - 139, View in Reaxys 296 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : chigger; bites releifBioassay : Example 22: Effect of 4% Lidocaine Formulation on Chigger BitesThe subject for this example had substantial experience with chigger bites, with typical symptoms including intense and prolonged (days to weeks) itching associated with the bites. Subject was provided with a solution of 4% lidocaine and

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Route of Adm.

cutaneous administration

Qualitative Results

test compound at concentration 4% ceased itching within minutes of application with no further symptoms

Measurement Parameter

qualitative

Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys 297 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : fire ant; bites releifBioassay : Example 23: Effect of 4% Lidocaine Formulation on Fire Ant Bites The subject for this example had substantial experience with fire ant bites, with general symptoms of blistering, itching, pain associated with the bites. Subject was provided with a solution of 4% lidocaine and water (carrier). Subject

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

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Substance Name

178204

Substance Route of Adm.

cutaneous administration

Qualitative Results

applying test compound at concentration 4% about 15 minutes after the bites occurred, complete relief from pain and itching after application was observed; typical blisters did not form

Measurement Parameter

qualitative

Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys 298 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : jellyfish; sting releifBioassay : Example 20: Effect of 4% Lidocaine on Time to Pain ReleifIn this example a composition of 4% lidocaine hydrochloride in water was tested according to the procedures set forth in Example 2 above. It was found that initial pain relief could be felt at around one minute after application, with complete

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Route of Adm.

cutaneous administration

Qualitative Results

initial pain relief could be felt at around one minute after application of test compound at concentration 4% , with complete or nearly complete relief at round 4.5 to 5 minutes from application; figure is given

Measurement Parameter

qualitative

Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys 299 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : sea nettle; sting releifBioassay : Example 12: Effects of Urea on PerformanceTwo formulations were tested to determine the effects of urea on the efficacy of formulations of the present disclosure. 10% lidocaine in water <n="37"/>10% lidocaine in water + 10% ureaStinging jellyfish: sea nettle with 4" bell diameter Results:There was

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Route of Adm.

cutaneous administration

Qualitative Results

test compound at concentration 10-15 % provided relief within about 10-60 sec., and pain and redness diminished over time much faster than in untreated stings; extended relief from irritation was observed

Measurement Parameter

qualitative

Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys 300 of 1220 Substance Effect

Analgesic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Bioassay : To verify the applicational functionality of the solid composition obtained, an in vivo test is carried out: a film piece is deposited on the rear of the previously wetted forearm of 6 persons of female sex. This film piece is soaked with 1 ml of water then, while making rapid circular movements, complete

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Name

178204

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Qualitative Results

treatment with the title compound showed analgesic effect

Measurement Parameter

qualitative

Patent; Lombardo, Paola; EP1911439; (A2); (2008), View in Reaxys 301 of 1220 Substance Effect

Toxic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : protozoan motililty inhibitionBioassay : organisms strain 1630/1W; phosphate-saline buffer, pH 7.4; swimming speed measurement

Biological Species/NCBI ID

Tetrahymena pyriformis

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

0.0100000 mM

Measurement Parameter

IC50

Unit

Quantitative value

16.8

Measurement pX

1.77

Wu, Changhao; Clift, Paul; Fry, Christopher H.; Henry, John A.; Archives of Toxicology; vol. 70; nb. 12; (1996); p. 850 853, View in Reaxys 302 of 1220 Substance Effect

Toxic : Subchronic

Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Target : Lewis rat pupsBioassay : newborn rat pups received with title compound in combination with cocaine, vehicle, saline, animals euthanized, blood, brain, liver, spleen removed, homogenized, lymphocytes and neutrophil counts performed, serum immunoglobulin M (IgM) measured, HPLC

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

20 mg/kg

Substance Route of Adm.

oral administration

Qualitative Results

significantly decreased serum IgM conc., ca. 39 percent lower than control, did not display significant reduction in slpeen wt. or blood cell populations

Measurement Parameter

qualitative

Barat, Stephen A.; Turkall, Rita M.; Toxicology Letters; vol. 89; nb. 3; (1996); p. 201 - 206, View in Reaxys 303 of 1220 Substance Effect

Toxic : Subchronic

Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Target : Lewis rat pupsBioassay : newborn rat pups, vehicle, saline, animals euthanized, blood, brain, liver, spleen removed, homogenized, lymphocytes and neutrophil counts performed, serum immunoglobulin M (IgM) measured, HPLC

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

20 mg/kg

Substance Route of Adm.

oral administration

Measurement Parameter

qualitative

Qualitative value

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Measurement pX

Barat, Stephen A.; Turkall, Rita M.; Toxicology Letters; vol. 89; nb. 3; (1996); p. 201 - 206, View in Reaxys 304 of 1220 Substance Effect

Antifungal

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Target : Candida albicans 731Bioassay : antifungal index was calculated as mean diameter of corresponding inhibition zone (in millimeters)/minimal title comp. amount resulting in growth inhibition (in micrograms); indices< 0.2 mm/μg were considered negligible; control: vehicle yeast suspension was applied on YEPD agar plates containing 25 μg/ml fluconazole or without it; then cellulose disks impregnated with title comp. were placed on agar; incubation for 48 h at 35 deg C; diameters of growth inhibition areas were recorded

Substance RN

3917968View in Reaxys

Substance Name

178204

Measurement Parameter

qualitative

Qualitative value

Measurement pX

Marchetti; Moreillon; Glauser; Bille; Sanglard; Antimicrobial Agents and Chemotherapy; vol. 44; nb. 9; (2000); p. 2373 2381, View in Reaxys 305 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : |transport Bioassay : skin samples were obtained from abdominal sites of Caucasian females (46-48 years); phosphate buffer (PB) in vitro; skin samples mounted in diffusion cells were treated with 50 μl of methanol and left for 12 h; title comp. solution was applied from donor side and PB (pH 3.5) was used as acceptor side; study was conducted for 24 and 48 h; HPLC

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

at pH 7.0 cumulative amount of title comp. transported across skin after 24 h was equal to 3196 μg/ cm2 ; at pH 4.0 cumulative amounts of transported title comp. after 24 and 48 h were equal to 39 and 78 μg/cm2; diagrams

Measurement Parameter

qualitative

Valenta; Cladera; O'Shea; Hadgraft; Journal of Pharmaceutical Sciences; vol. 90; nb. 4; (2001); p. 485 - 492, View in Reaxys 306 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : |Accumulation Target : Long-Evans rat sciatic nerveBioassay : nerve of anesthetized rats placed in bathing chamber and incubated with <14C>labeled title comp. for 7, 20 and 60 min; uptake and distribution of title comp. determined using liquid scintillation counter

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

0.400000 mM

Qualitative Results

rapid uptake of title comp. was observed from 0 to 7 min, steady state reached in about 20 min (diagram)

Measurement Parameter

qualitative

Anaesthesic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

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Bioassay Details

Target : Long-Evans rat sciatic nerve nociceptive Aω-fibersBioassay : control: in the absence of title comp. tissue of anesthetized rats placed in bathing chamber, superfused with title comp.; electrical stimulation performed via subdermal recording electrodes; phasic action determined using 5-Hz and 10-Hz bursts stimulation (10 stimuli in each burst)

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

0.100000 mM

Measurement Parameter

qualitative

Qualitative value

Measurement pX

Anaesthesic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Target : Long-Evans rat sciatic nerve nociceptive C-fibersBioassay : control: in the absence of title comp. tissue of anesthetized rats placed in bathing chamber, superfused with title comp.; electrical stimulation performed via subdermal recording electrodes; phasic action determined using 5-Hz and 10-Hz bursts stimulation (10 stimuli in each burst)

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

0.100000 mM

Measurement Parameter

qualitative

Qualitative value

Measurement pX

Anaesthesic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Target : Long-Evans rat sciatic nerve mechanosensitive Aω-fibersBioassay : control: in the absence of title comp.; functional subgroups rapidly (RA) and slowly (SA) adapting mechanoreceptive afferents and muscle (M) afferents of Aω fibers investigated tissue of anesthetized rats placed in bathing chamber, superfused with title comp.; electrical stimulation performed via subdermal recording electrodes; phasic action determined using 200-Hz burst stimulation; use- and activity-dependent block evaluated

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

0.100000 mM

Measurement Parameter

IC50

Unit

Quantitative value

0.28

Measurement pX

3.55

Anaesthesic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

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Bioassay Details

Target : Long-Evans rat sciatic nerve mechanosensitive Aω-fibersBioassay : tonic susceptibility: determination of resting conduction velocity, blocking conc., normalized latency increase; control: in the absence of title comp.; Aω subgroups: RA (rapid), SA (slow) adapting mechanoreceptive, M (muscle) afferents investigated tissue of anesthetized rats placed in bathing chamber, superfused with title comp.; electrical stimulation performed via subdermal recording electrodes; tonic action determined using infrequent stimuli (1 Hz) at steady state; susceptibility evaluated

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

0.100000 mM

Measurement Parameter

IC50

Unit

Quantitative value

0.41

Measurement pX

3.39

Anaesthesic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Target : Long-Evans rat sciatic nerve nociceptive Aω-fibersBioassay : tonic susceptibility: determination of resting conduction velocity, title comp. blocking conc., normalized latency increase; control: in the absence of title comp. tissue of anesthetized rats placed in bathing chamber, superfused with title comp.; electrical stimulation performed via subdermal recording electrodes; tonic action determined using infrequent stimuli (0.2 Hz) at steady state; susceptibility evaluated

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

0.100000 mM

Measurement Parameter

IC50

Unit

Quantitative value

0.32

Measurement pX

3.49

Anaesthesic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Target : Long-Evans rat sciatic nerve nociceptive C-fibersBioassay : tonic susceptibility: determination of resting conduction velocity, title comp. blocking conc., normalized latency increase; control: in the absence of title comp. tissue of anesthetized rats placed in bathing chamber, superfused with title comp.; electrical stimulation performed via subdermal recording electrodes; tonic action determined using infrequent stimuli (0.2 Hz) at steady state; susceptibility evaluated

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

0.100000 mM

Measurement Parameter

IC50

Unit

Quantitative value

0.8

Measurement pX

3.1

Huang, Jason Haitao; Thalhammer, Johann G.; Raymond, Stephen A.; Strichartz, Gary R.; Journal of Pharmacology and Experimental Therapeutics; vol. 282; nb. 2; (1997); p. 802 - 811, View in Reaxys

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313 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : |transport Bioassay : permeability coefficient (P) calculated by flux healthy nail tip piece (ca. 350 nm) hydrated for a day and mounted in side-by-side diffusion cell at 37 deg C; title comp. added to dorsal side, ventral side filled with water; title comp. measured in ventral side solution by HPLC at 5-17 days

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

title comp. P = 0.031E-7 cm/s

Measurement Parameter

qualitative

In Vitro (Efficacy)

Bioassay Name

Flux transport

Bioassay Details

Effect : |transport Bioassay : further investigation with P-glycoprotein (Pgp) inhibitors (verapamil or digoxin) rat anaesthetized, jejunum cannulated and perfused with title comp. (37 deg C); outlet perfusate collected at 45-105 min; title comp. effective permeability (Peff) determined using high performance liquid chromatography with UV-detection

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

0.500000 µM

Qualitative Results

title comp. Peff was ca. 7E-5 - 10E-5 cm/s with/without Pgp inhibitors, resp. (figure)

Measurement Parameter

qualitative

Berggren, Sofia; Hoogstraate, Janet; Fagerholm, Urban; Lennernaes, Hans; European Journal of Pharmaceutical Sciences; vol. 21; nb. 4; (2004); p. 553 - 560, View in Reaxys 315 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : |transport Bioassay : pH 7.4 in S compartment and pH 7.4 or 6.5 in M compartment; extra: with P-glycoprotein (Pgp) inhibitors (verapamil or digoxin); KBR: Krebs buffered Ringer solution; Papp: apparent permeability; M: mucosal side; S: serosal side; S-M/M-S: efflux ratio jejunum free from Payer's patches and serosa layer moved in Ussing chamber; title comp. - donor, KBR - receiver, 37 deg C; M-S and S-M Peff tested; donor samples taken at <=3 h after the start; high performance liquid chromatography with UV-detection

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

500 µM

Qualitative Results

title comp. Papp was similar with/without Pgp inhibitors; title comp. S-M/M-S was 7.5 and 1.8 at apical pH 6.5 and 7.4, resp. (figure)

Measurement Parameter

qualitative

Berggren, Sofia; Hoogstraate, Janet; Fagerholm, Urban; Lennernaes, Hans; European Journal of Pharmaceutical Sciences; vol. 21; nb. 4; (2004); p. 553 - 560, View in Reaxys 316 of 1220 Bioassay Category Bioassay Name

In Vitro (Efficacy) In Vitro (others)

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Bioassay Details

Effect : accumulation; induction ofTarget : Caco-2VCR25 cellsBioassay : cyclosporin A used as positive control calcein AM extrusion assay performed in presence of title comp. using vincristine resistant (VCR) cells

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

10 µM

Qualitative Results

title comp. caused retention of calcein in cells of 3.5 times that of control compared to 10 times for positive control

Measurement Parameter

qualitative

Berggren, Sofia; Hoogstraate, Janet; Fagerholm, Urban; Lennernaes, Hans; European Journal of Pharmaceutical Sciences; vol. 21; nb. 4; (2004); p. 553 - 560, View in Reaxys 317 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : electrophysiology; effect onTarget : Sprague-Dawley rat brain slicesBioassay : membrane electrical properties and action potential firing of neurones of ventral posterolateral (VPL) nucleus of thalamus investigated using whole cell recording techniques

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

0.600000 µM

Qualitative Results

low conc. shunted tonic and burst firing in VPL neurones by decreasing input resistance (Ri); higher conc. (>=300 μM) elevated voltage threshold for firing and reduced dV/dtmax of spikes in conc.dependent fashion without decrease in

Measurement Parameter

qualitative

Schwarz, Stephan K. W.; Puil, Ernest; British Journal of Pharmacology; vol. 124; nb. 8; (1998); p. 1633 - 1642, View in Reaxys 318 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : |transport Bioassay : standard: title comp. marketed gel (2 w/w%) excised skin mounted between receptor and donor compartments; title comp. added to donor side; receptor side filled with PBS (37 deg C); at predetermined intervals, samples taken from receptor side; assayed for title comp. using UV spectrophotometer

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

title comp. flux increased by the concentration and molecular weight of chitosan; by increasing title comp. concentration in gels from 2% in standard to 4% in gel, the flux of title comp. increased significantly; table

Measurement Parameter

qualitative

Varshosaz, Jaleh; Jaffari, Fariba; Karimzadeh, Sara; Scientia Pharmaceutica; vol. 74; nb. 4; (2006); p. 209 - 223, View in Reaxys 319 of 1220 Substance Effect

Analgesic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Bioassay : standard: title comp. marketed gel (2 w/w%) mice admin. with title comp.; after 30 min, pain behavior quantified using paw formalin assay over 30 min using 5 min bins; two phases of spontaneous licking behavior observed (phase I: 0-5 min, phase II: 15-30 min)

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

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Substance Name

178204

Qualitative Results

title comp. produced greater suppression of formalin-induced nociceptive behavior with longer duration of action; maximal response was about 52% and 36% analgesia in second phase for title comp. formulation and standard, resp. compared to control; fig.

Measurement Parameter

qualitative

Varshosaz, Jaleh; Jaffari, Fariba; Karimzadeh, Sara; Scientia Pharmaceutica; vol. 74; nb. 4; (2006); p. 209 - 223, View in Reaxys 320 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : |antagonist Target : bovine tracheal smooth muscle membranesBioassay : competition binding assay to ω adrenoceptors; 240 pmol/l <125I>cyanopindolol as radioligand, Tris-HCl, pH 7.4, 37 deg C, incubation 60 min; after termination by rapid filtration remaining radioactivity quantified by gamma counter

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

1.00000E-06 M

Measurement Parameter

qualitative

Qualitative value

Measurement pX

Nakahara; Kubota; Sakamato; Moriuchi; Yunoki; Ishii; Naunyn-Schmiedeberg's Archives of Pharmacology; vol. 364; nb. 5; (2001); p. 409 - 413, View in Reaxys 321 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lignocaine

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-inf)

Unit

µg.min/mL

Quantitative value

Bax; Tucker; Lennard; Woods; British Journal of Clinical Pharmacology; vol. 19; nb. 5; (1985); p. 597 - 603, View in Reaxys 322 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lignocaine

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

160/467

2018-05-14 08:43:54

Measurement Parameter

t1/2 el

Unit

minute

Quantitative value

103

Bax; Tucker; Lennard; Woods; British Journal of Clinical Pharmacology; vol. 19; nb. 5; (1985); p. 597 - 603, View in Reaxys 323 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lignocaine

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Cmax

Unit

ng/mL

Quantitative value

502

Bax; Tucker; Lennard; Woods; British Journal of Clinical Pharmacology; vol. 19; nb. 5; (1985); p. 597 - 603, View in Reaxys 324 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lignocaine

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

tmax

Unit

minute

Quantitative value

Bax; Tucker; Lennard; Woods; British Journal of Clinical Pharmacology; vol. 19; nb. 5; (1985); p. 597 - 603, View in Reaxys 325 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lignocaine

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

161/467

2018-05-14 08:43:54

Measurement Parameter

AUC i/AUC (0-inf)

Quantitative value

2.02

Concomitants: Compound RN

4164259

Concomitants: Compound name

Propranolol hydrochloride

Concomitants: Compound role

ICP

Bax; Tucker; Lennard; Woods; British Journal of Clinical Pharmacology; vol. 19; nb. 5; (1985); p. 597 - 603, View in Reaxys 326 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lignocaine

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el i/t1/2 el

Quantitative value

1.21

Concomitants: Compound RN

4164259

Concomitants: Compound name

Propranolol hydrochloride

Concomitants: Compound role

ICP

Bax; Tucker; Lennard; Woods; British Journal of Clinical Pharmacology; vol. 19; nb. 5; (1985); p. 597 - 603, View in Reaxys 327 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lignocaine

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Cmax i/Cmax

Quantitative value

1.74

Concomitants: Compound RN

4164259

Concomitants: Compound name

Propranolol hydrochloride

Concomitants: Compound role

ICP

162/467

2018-05-14 08:43:54

Bax; Tucker; Lennard; Woods; British Journal of Clinical Pharmacology; vol. 19; nb. 5; (1985); p. 597 - 603, View in Reaxys 328 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Drug Free

Substance RN

3917968View in Reaxys

Substance Name

Lignocaine hydrochlorid monohydrate

Substance Dose

400 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-4 h)

Unit

µmol.min/L

Quantitative value

707

Deviation

352

Perucca; Hedges; Makki; Richens; British Journal of Clinical Pharmacology; vol. 10; nb. 5; (1980); p. 491 - 497, View in Reaxys 329 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Drug Free

Substance RN

3917968View in Reaxys

Substance Name

Lignocaine hydrochlorid monohydrate

Substance Dose

400 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

CL (0-4 h)

Unit

L/h/kg

Quantitative value

2.5

Deviation

1.20000

Perucca; Hedges; Makki; Richens; British Journal of Clinical Pharmacology; vol. 10; nb. 5; (1980); p. 491 - 497, View in Reaxys 330 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Drug Free

Substance RN

3917968View in Reaxys

Substance Name

Lignocaine hydrochlorid monohydrate

Substance Dose

400 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

163/467

2018-05-14 08:43:54

Measurement Parameter

t1/2 el

Unit

minute

Quantitative value

Deviation

Perucca; Hedges; Makki; Richens; British Journal of Clinical Pharmacology; vol. 10; nb. 5; (1980); p. 491 - 497, View in Reaxys 331 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

Urine biochemistry

Biological Species/NCBI ID

human

Population State

Drug Free

Substance RN

3917968View in Reaxys

Substance Name

Lignocaine hydrochlorid monohydrate

Substance Dose

400 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

amount

Unit

µmol/x h/kg

Measurement Object

of D-Glucaric acid

Quantitative value

0.12

Deviation

0.0400000

Perucca; Hedges; Makki; Richens; British Journal of Clinical Pharmacology; vol. 10; nb. 5; (1980); p. 491 - 497, View in Reaxys 332 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

epilepsy

Substance RN

3917968View in Reaxys

Substance Name

Lignocaine hydrochlorid monohydrate

Substance Dose

400 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-4 h)

Unit

µmol.min/L

Quantitative value

353

Deviation

235

Perucca; Hedges; Makki; Richens; British Journal of Clinical Pharmacology; vol. 10; nb. 5; (1980); p. 491 - 497, View in Reaxys 333 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

epilepsy

164/467

2018-05-14 08:43:54

Substance RN

3917968View in Reaxys

Substance Name

Lignocaine hydrochlorid monohydrate

Substance Dose

400 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

CL (0-4 h)

Unit

L/h/kg

Quantitative value

Deviation

4.80000

Perucca; Hedges; Makki; Richens; British Journal of Clinical Pharmacology; vol. 10; nb. 5; (1980); p. 491 - 497, View in Reaxys 334 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

epilepsy

Substance RN

3917968View in Reaxys

Substance Name

Lignocaine hydrochlorid monohydrate

Substance Dose

400 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

minute

Quantitative value

Deviation

Perucca; Hedges; Makki; Richens; British Journal of Clinical Pharmacology; vol. 10; nb. 5; (1980); p. 491 - 497, View in Reaxys 335 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

epilepsy

Substance RN

3917968View in Reaxys

Substance Name

Lignocaine hydrochlorid monohydrate

Substance Dose

400 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

amount

Unit

µmol/x h/kg

Measurement Object

of D-Glucaric acid

Quantitative value

178

Deviation

1.20000

165/467

2018-05-14 08:43:54

Perucca; Hedges; Makki; Richens; British Journal of Clinical Pharmacology; vol. 10; nb. 5; (1980); p. 491 - 497, View in Reaxys 336 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Drug Free

Substance RN

3917968View in Reaxys

Substance Name

Lignocaine hydrochlorid monohydrate

Substance Dose

400 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

CL (drug clearance)

Unit

mL/h/kg

Quantitative value

Deviation

Perucca; Hedges; Makki; Richens; British Journal of Clinical Pharmacology; vol. 10; nb. 5; (1980); p. 491 - 497, View in Reaxys 337 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

CL (drug clearance)

Unit

mL/min

Quantitative value

1060.5

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 338 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

166/467

2018-05-14 08:43:54

Measurement Parameter

Vdss

Unit

Quantitative value

156

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 339 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Kel

Unit

min-1

Quantitative value

0.005875

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 340 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

t1/2 el

Unit

minute

Quantitative value

122.5

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 341 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

167/467

2018-05-14 08:43:54

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

CL (drug clearance)

Unit

mL/min

Quantitative value

1060.5

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 342 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Vdss

Unit

Quantitative value

156

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 343 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Kel

Unit

min-1

Quantitative value

0.005875

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 344 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

168/467

2018-05-14 08:43:54

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

t1/2 el

Unit

minute

Quantitative value

122.5

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 345 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

CL (drug clearance)

Unit

mL/min

Quantitative value

1060.5

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 346 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Vdss

Unit

Quantitative value

156

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 347 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

169/467

2018-05-14 08:43:54

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Kel

Unit

min-1

Quantitative value

0.005875

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 348 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

t1/2 el

Unit

minute

Quantitative value

122.5

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 349 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

CL i/CL

Quantitative value

0.846

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

170/467

2018-05-14 08:43:54

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 350 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Vdss i/Vdss

Quantitative value

0.788

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 351 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

kel i/kel

Quantitative value

1.08

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 352 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

171/467

2018-05-14 08:43:54

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

t1/2 el i/t1/2 el

Quantitative value

1.03

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 353 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

CL i/CL

Quantitative value

1.09

Concomitants: Compound RN

4327819

Concomitants: Compound name

Ranitidine

Concomitants: Compound role

ICP

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 354 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

172/467

2018-05-14 08:43:54

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Vdss i/Vdss

Quantitative value

1.12

Concomitants: Compound RN

4327819

Concomitants: Compound name

Ranitidine

Concomitants: Compound role

ICP

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 355 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

kel i/kel

Quantitative value

0.962

Concomitants: Compound RN

4327819

Concomitants: Compound name

Ranitidine

Concomitants: Compound role

ICP

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 356 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

t1/2 el i/t1/2 el

Quantitative value

0.914

Concomitants: Compound RN

4327819

173/467

2018-05-14 08:43:54

Concomitants: Compound name

Ranitidine

Concomitants: Compound role

ICP

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 357 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocïne HCl

Substance Dose

25 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

1.81

Deviation

0.410000

Abernethy; Schwartz; Todd; Clinical pharmacology and therapeutics; vol. 38; nb. 3; (1985); p. 342 - 349, View in Reaxys 358 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocïne HCl

Substance Dose

25 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Vd (volume of distribution)

Unit

L/kg

Quantitative value

1.77

Deviation

0.660000

Abernethy; Schwartz; Todd; Clinical pharmacology and therapeutics; vol. 38; nb. 3; (1985); p. 342 - 349, View in Reaxys 359 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocïne HCl

Substance Dose

25 mg

174/467

2018-05-14 08:43:54

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

CL (drug clearance)

Unit

mL/min

Quantitative value

665

Deviation

216

Abernethy; Schwartz; Todd; Clinical pharmacology and therapeutics; vol. 38; nb. 3; (1985); p. 342 - 349, View in Reaxys 360 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocïne HCl

Substance Dose

25 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

1.81

Abernethy; Schwartz; Todd; Clinical pharmacology and therapeutics; vol. 38; nb. 3; (1985); p. 342 - 349, View in Reaxys 361 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocïne HCl

Substance Dose

25 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Vd (volume of distribution)

Unit

L/kg

Quantitative value

1.77

Abernethy; Schwartz; Todd; Clinical pharmacology and therapeutics; vol. 38; nb. 3; (1985); p. 342 - 349, View in Reaxys 362 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocïne HCl

175/467

2018-05-14 08:43:54

Substance Dose

25 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

CL (drug clearance)

Unit

mL/min

Quantitative value

665

Abernethy; Schwartz; Todd; Clinical pharmacology and therapeutics; vol. 38; nb. 3; (1985); p. 342 - 349, View in Reaxys 363 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocïne HCl

Substance Dose

25 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el i/t1/2 el

Quantitative value

1.35

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Abernethy; Schwartz; Todd; Clinical pharmacology and therapeutics; vol. 38; nb. 3; (1985); p. 342 - 349, View in Reaxys 364 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocïne HCl

Substance Dose

25 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Vd i/Vd

Quantitative value

1.12

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

176/467

2018-05-14 08:43:54

Abernethy; Schwartz; Todd; Clinical pharmacology and therapeutics; vol. 38; nb. 3; (1985); p. 342 - 349, View in Reaxys 365 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocïne HCl

Substance Dose

25 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

CL i/CL

Quantitative value

0.792

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Abernethy; Schwartz; Todd; Clinical pharmacology and therapeutics; vol. 38; nb. 3; (1985); p. 342 - 349, View in Reaxys 366 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine HCl

Substance Dose

3600 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

heart rate

Unit

b.p.m

Measurement Object

supine resting heart rate

Quantitative value

Deviation

Schneck; Luderer; Davis; Vary; Clinical Pharmacology and Therapeutics; vol. 36; nb. 5; (1984); p. 584 - 587, View in Reaxys 367 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine HCl

Substance Dose

3600 mg

177/467

2018-05-14 08:43:54

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration (parameters)

Unit

µg/mL

Quantitative value

2.1

Deviation

0.200000

Schneck; Luderer; Davis; Vary; Clinical Pharmacology and Therapeutics; vol. 36; nb. 5; (1984); p. 584 - 587, View in Reaxys 368 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine HCl

Substance Dose

3600 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

CL (drug clearance)

Unit

mL/min

Quantitative value

1030

Deviation

Schneck; Luderer; Davis; Vary; Clinical Pharmacology and Therapeutics; vol. 36; nb. 5; (1984); p. 584 - 587, View in Reaxys 369 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine HCl

Substance Dose

3600 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

EH (hepatic extraction ratio)

Unit

Quantitative value

0.86

Deviation

0.0600000

Schneck; Luderer; Davis; Vary; Clinical Pharmacology and Therapeutics; vol. 36; nb. 5; (1984); p. 584 - 587, View in Reaxys 370 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

178/467

2018-05-14 08:43:54

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine HCl

Substance Dose

3600 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration (parameters)

Unit

µg/mL

Quantitative value

2.1

Schneck; Luderer; Davis; Vary; Clinical Pharmacology and Therapeutics; vol. 36; nb. 5; (1984); p. 584 - 587, View in Reaxys 371 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine HCl

Substance Dose

3600 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

CL (drug clearance)

Unit

mL/min

Quantitative value

1030

Schneck; Luderer; Davis; Vary; Clinical Pharmacology and Therapeutics; vol. 36; nb. 5; (1984); p. 584 - 587, View in Reaxys 372 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine HCl

Substance Dose

3600 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

EH (hepatic extraction ratio)

Unit

Quantitative value

0.86

Schneck; Luderer; Davis; Vary; Clinical Pharmacology and Therapeutics; vol. 36; nb. 5; (1984); p. 584 - 587, View in Reaxys 373 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

179/467

2018-05-14 08:43:54

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine HCl

Substance Dose

3600 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration (parameters)

Unit

µg/mL

Quantitative value

2.1

Schneck; Luderer; Davis; Vary; Clinical Pharmacology and Therapeutics; vol. 36; nb. 5; (1984); p. 584 - 587, View in Reaxys 374 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine HCl

Substance Dose

3600 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

CL (drug clearance)

Unit

mL/min

Quantitative value

1030

Schneck; Luderer; Davis; Vary; Clinical Pharmacology and Therapeutics; vol. 36; nb. 5; (1984); p. 584 - 587, View in Reaxys 375 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine HCl

Substance Dose

3600 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

EH (hepatic extraction ratio)

Unit

Quantitative value

0.86

Schneck; Luderer; Davis; Vary; Clinical Pharmacology and Therapeutics; vol. 36; nb. 5; (1984); p. 584 - 587, View in Reaxys 376 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

180/467

2018-05-14 08:43:54

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine HCl

Substance Dose

3600 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration i/concentration

Quantitative value

1.19

Concomitants: Compound RN

987417

Concomitants: Compound name

Propranolol

Concomitants: Compound role

ICP

Schneck; Luderer; Davis; Vary; Clinical Pharmacology and Therapeutics; vol. 36; nb. 5; (1984); p. 584 - 587, View in Reaxys 377 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine HCl

Substance Dose

3600 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

CL i/CL

Quantitative value

0.841

Concomitants: Compound RN

987417

Concomitants: Compound name

Propranolol

Concomitants: Compound role

ICP

Schneck; Luderer; Davis; Vary; Clinical Pharmacology and Therapeutics; vol. 36; nb. 5; (1984); p. 584 - 587, View in Reaxys 378 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine HCl

Substance Dose

3600 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration i/concentration

181/467

2018-05-14 08:43:54

Quantitative value

1.29

Concomitants: Compound RN

2059000

Concomitants: Compound name

Nadolol

Concomitants: Compound role

ICP

Schneck; Luderer; Davis; Vary; Clinical Pharmacology and Therapeutics; vol. 36; nb. 5; (1984); p. 584 - 587, View in Reaxys 379 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine HCl

Substance Dose

3600 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

CL i/CL

Quantitative value

0.825

Concomitants: Compound RN

2059000

Concomitants: Compound name

Nadolol

Concomitants: Compound role

ICP

Schneck; Luderer; Davis; Vary; Clinical Pharmacology and Therapeutics; vol. 36; nb. 5; (1984); p. 584 - 587, View in Reaxys 380 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine HCl

Substance Dose

3600 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration (parameters)

Unit

µg/mL

Quantitative value

1.95

Deviation

0.200000

Schneck; Luderer; Davis; Vary; Clinical Pharmacology and Therapeutics; vol. 36; nb. 5; (1984); p. 584 - 587, View in Reaxys 381 of 1220 Bioassay Category Bioassay Name

Pharmacokinetic Pharmacokinetic

182/467

2018-05-14 08:43:54

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine HCl

Substance Dose

3600 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration (parameters)

Unit

µg/mL

Quantitative value

1.98

Deviation

0.300000

Schneck; Luderer; Davis; Vary; Clinical Pharmacology and Therapeutics; vol. 36; nb. 5; (1984); p. 584 - 587, View in Reaxys 382 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

1.71

Deviation

0.190000

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 383 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

CL (drug clearance)

Unit

mL/min/kg

Quantitative value

183/467

2018-05-14 08:43:54

Deviation

7.99000

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 384 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

1.71

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 385 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

CL (drug clearance)

Unit

mL/min/kg

Quantitative value

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 386 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

184/467

2018-05-14 08:43:54

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

1.71

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 387 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

1.78

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 388 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

CL (drug clearance)

Unit

mL/min/kg

Quantitative value

10.84

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 389 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

185/467

2018-05-14 08:43:54

Substance Dosing Regimen

Single

Measurement Parameter

CL (drug clearance)

Unit

mL/min/kg

Quantitative value

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 390 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

F (drug bioavailability)

Unit

Measurement Object

AUC

Quantitative value

29.1

Deviation

5.20000

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 391 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

F (drug bioavailability)

Unit

Quantitative value

29.1

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 392 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

186/467

2018-05-14 08:43:54

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

F (drug bioavailability)

Unit

Quantitative value

29.1

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 393 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

1.78

Deviation

0.210000

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 394 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

CL (drug clearance)

Unit

mL/min/kg

Quantitative value

10.84

Deviation

1.41000

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 395 of 1220 Bioassay Category

Pharmacokinetic

187/467

2018-05-14 08:43:54

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Vdss

Unit

L/kg

Quantitative value

1.58

Deviation

0.190000

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 396 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

1.78

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 397 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

CL (drug clearance)

Unit

mL/min/kg

Quantitative value

10.84

188/467

2018-05-14 08:43:54

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 398 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Vdss

Unit

L/kg

Quantitative value

1.58

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 399 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Vdss

Unit

L/kg

Quantitative value

1.58

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 400 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el i/t1/2 el

189/467

2018-05-14 08:43:54

Quantitative value

1.13

Concomitants: Compound RN

2739235

Concomitants: Compound name

Atenolol

Concomitants: Compound role

ICP

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 401 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

CL i/CL

Quantitative value

1.05

Concomitants: Compound RN

2739235

Concomitants: Compound name

Atenolol

Concomitants: Compound role

ICP

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 402 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el i/t1/2 el

Quantitative value

1.11

Concomitants: Compound RN

3917968; 1117585

Concomitants: Compound name

Lidocaine hydrochloride; Metoprolol

190/467

2018-05-14 08:43:54

Concomitants: Compound role

ICP; ICP

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 403 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el i/t1/2 el

Quantitative value

1.13

Concomitants: Compound RN

3917968; 1117585

Concomitants: Compound name

Lidocaine hydrochloride; Metoprolol

Concomitants: Compound role

ICP; ICP

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 404 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

CL i/CL

Quantitative value

0.861

Concomitants: Compound RN

3917968; 1117585

Concomitants: Compound name

Lidocaine hydrochloride; Metoprolol

Concomitants: Compound role

ICP; ICP

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 405 of 1220 Bioassay Category Bioassay Name

Pharmacokinetic Pharmacokinetic

191/467

2018-05-14 08:43:54

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

CL i/CL

Quantitative value

0.989

Concomitants: Compound RN

3917968; 1117585

Concomitants: Compound name

Lidocaine hydrochloride; Metoprolol

Concomitants: Compound role

ICP; ICP

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 406 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el i/t1/2 el

Quantitative value

0.994

Concomitants: Compound RN

2739235

Concomitants: Compound name

Atenolol

Concomitants: Compound role

ICP

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 407 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

192/467

2018-05-14 08:43:54

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

CL i/CL

Quantitative value

0.937

Concomitants: Compound RN

2739235

Concomitants: Compound name

Atenolol

Concomitants: Compound role

ICP

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 408 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Vdss i/Vdss

Quantitative value

0.962

Concomitants: Compound RN

2739235

Concomitants: Compound name

Atenolol

Concomitants: Compound role

ICP

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 409 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Vdss i/Vdss

Quantitative value

0.987

193/467

2018-05-14 08:43:54

Concomitants: Compound RN

3917968; 1117585

Concomitants: Compound name

Lidocaine hydrochloride; Metoprolol

Concomitants: Compound role

ICP; ICP

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 410 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

CL (drug clearance)

Unit

mL/min

Quantitative value

766

Deviation

Feely; Wilkinson; McAllister; Wood; Annals of Internal Medicine; vol. 96; nb. 5; (1982); p. 592 - 594, View in Reaxys 411 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

1.8

Deviation

0.200000

Feely; Wilkinson; McAllister; Wood; Annals of Internal Medicine; vol. 96; nb. 5; (1982); p. 592 - 594, View in Reaxys 412 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

194/467

2018-05-14 08:43:54

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration (parameters)

Unit

µg/mL

Quantitative value

1.7

Deviation

0.200000

Feely; Wilkinson; McAllister; Wood; Annals of Internal Medicine; vol. 96; nb. 5; (1982); p. 592 - 594, View in Reaxys 413 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Cmax

Unit

µg/mL

Quantitative value

Deviation

0.200000

Feely; Wilkinson; McAllister; Wood; Annals of Internal Medicine; vol. 96; nb. 5; (1982); p. 592 - 594, View in Reaxys 414 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Vd (volume of distribution)

Unit

Quantitative value

Deviation

Feely; Wilkinson; McAllister; Wood; Annals of Internal Medicine; vol. 96; nb. 5; (1982); p. 592 - 594, View in Reaxys 415 of 1220 Bioassay Category Bioassay Name

Metabolism/Transport Binding

195/467

2018-05-14 08:43:54

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Vdss

Unit

Quantitative value

Deviation

Feely; Wilkinson; McAllister; Wood; Annals of Internal Medicine; vol. 96; nb. 5; (1982); p. 592 - 594, View in Reaxys 416 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

fu (unbound fraction)

Quantitative value

0.344

Deviation

0.0100000

Feely; Wilkinson; McAllister; Wood; Annals of Internal Medicine; vol. 96; nb. 5; (1982); p. 592 - 594, View in Reaxys 417 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

CL (drug clearance)

Unit

mL/min

Quantitative value

766

Concomitants: Compound RN

9406848

196/467

2018-05-14 08:43:54

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Feely; Wilkinson; McAllister; Wood; Annals of Internal Medicine; vol. 96; nb. 5; (1982); p. 592 - 594, View in Reaxys 418 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

1.8

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Feely; Wilkinson; McAllister; Wood; Annals of Internal Medicine; vol. 96; nb. 5; (1982); p. 592 - 594, View in Reaxys 419 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration (parameters)

Unit

µg/mL

Quantitative value

1.7

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Feely; Wilkinson; McAllister; Wood; Annals of Internal Medicine; vol. 96; nb. 5; (1982); p. 592 - 594, View in Reaxys

197/467

2018-05-14 08:43:54

420 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Cmax

Unit

µg/mL

Quantitative value

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Feely; Wilkinson; McAllister; Wood; Annals of Internal Medicine; vol. 96; nb. 5; (1982); p. 592 - 594, View in Reaxys 421 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Vd (volume of distribution)

Unit

Quantitative value

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Feely; Wilkinson; McAllister; Wood; Annals of Internal Medicine; vol. 96; nb. 5; (1982); p. 592 - 594, View in Reaxys 422 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

human

Population State

Non Smoker

198/467

2018-05-14 08:43:54

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Vdss

Unit

Quantitative value

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Feely; Wilkinson; McAllister; Wood; Annals of Internal Medicine; vol. 96; nb. 5; (1982); p. 592 - 594, View in Reaxys 423 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

fu (unbound fraction)

Quantitative value

0.344

Feely; Wilkinson; McAllister; Wood; Annals of Internal Medicine; vol. 96; nb. 5; (1982); p. 592 - 594, View in Reaxys 424 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration (parameters)

Unit

mg/dL

Measurement Object

of alpha 1 acid glycoprotein

Quantitative value

Deviation

199/467

2018-05-14 08:43:54

Feely; Wilkinson; McAllister; Wood; Annals of Internal Medicine; vol. 96; nb. 5; (1982); p. 592 - 594, View in Reaxys 425 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

human

Population State

Healthy

Organs/Tissues

plasma

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

0.900000 µg/mL

Measurement Parameter

fu (unbound fraction)

Quantitative value

0.399

Deviation

0.0300000

Feely; Wilkinson; McAllister; Wood; Annals of Internal Medicine; vol. 96; nb. 5; (1982); p. 592 - 594, View in Reaxys 426 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

50 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

1.98

Blyden; Greenblatt; LeDuc; Scavone; European journal of clinical pharmacology; vol. 35; nb. 4; (1988); p. 413 - 417, View in Reaxys 427 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

50 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

CL (drug clearance)

Unit

mL/min/kg

Quantitative value

200/467

2018-05-14 08:43:54

Blyden; Greenblatt; LeDuc; Scavone; European journal of clinical pharmacology; vol. 35; nb. 4; (1988); p. 413 - 417, View in Reaxys 428 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

50 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Vd (volume of distribution)

Unit

L/kg

Quantitative value

2.56

Blyden; Greenblatt; LeDuc; Scavone; European journal of clinical pharmacology; vol. 35; nb. 4; (1988); p. 413 - 417, View in Reaxys 429 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

50 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

1.98

Blyden; Greenblatt; LeDuc; Scavone; European journal of clinical pharmacology; vol. 35; nb. 4; (1988); p. 413 - 417, View in Reaxys 430 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

50 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

CL (drug clearance)

201/467

2018-05-14 08:43:54

Unit

mL/min/kg

Quantitative value

13.5

Blyden; Greenblatt; LeDuc; Scavone; European journal of clinical pharmacology; vol. 35; nb. 4; (1988); p. 413 - 417, View in Reaxys 431 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

50 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Vd (volume of distribution)

Unit

L/kg

Quantitative value

2.56

Blyden; Greenblatt; LeDuc; Scavone; European journal of clinical pharmacology; vol. 35; nb. 4; (1988); p. 413 - 417, View in Reaxys 432 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

50 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

t1/2 el i/t1/2 el

Quantitative value

1.2

Concomitants: Compound RN

157775

Concomitants: Compound name

Antipyrine

Concomitants: Compound role

ICP

Blyden; Greenblatt; LeDuc; Scavone; European journal of clinical pharmacology; vol. 35; nb. 4; (1988); p. 413 - 417, View in Reaxys 433 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

202/467

2018-05-14 08:43:54

Substance Name

lidocaine HCl

Substance Dose

50 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

CL i/CL

Quantitative value

Concomitants: Compound RN

157775

Concomitants: Compound name

Antipyrine

Concomitants: Compound role

ICP

Blyden; Greenblatt; LeDuc; Scavone; European journal of clinical pharmacology; vol. 35; nb. 4; (1988); p. 413 - 417, View in Reaxys 434 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

50 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Vd i/Vd

Quantitative value

1.07

Concomitants: Compound RN

157775

Concomitants: Compound name

Antipyrine

Concomitants: Compound role

ICP

Blyden; Greenblatt; LeDuc; Scavone; European journal of clinical pharmacology; vol. 35; nb. 4; (1988); p. 413 - 417, View in Reaxys 435 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Cl/F

203/467

2018-05-14 08:43:54

Unit

L/h/kg

Quantitative value

3.31

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 436 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

F (drug bioavailability)

Unit

Quantitative value

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 437 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Cl/F

Unit

L/h/kg

Quantitative value

2.53

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 438 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

F (drug bioavailability)

204/467

2018-05-14 08:43:54

Unit

Quantitative value

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 439 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

75 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

CL (drug clearance)

Unit

L/h/kg

Quantitative value

0.75

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 440 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

75 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Vdss

Unit

L/kg

Quantitative value

1.51

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 441 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

75 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

205/467

2018-05-14 08:43:54

Unit

hour

Quantitative value

1.4

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 442 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

75 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

CL (drug clearance)

Unit

L/h/kg

Quantitative value

0.86

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 443 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

75 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Vdss

Unit

L/kg

Quantitative value

2.45

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 444 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

75 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

206/467

2018-05-14 08:43:54

Unit

hour

Quantitative value

2.1

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 445 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Cl/F

Unit

L/h/kg

Quantitative value

2.92

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 446 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

F (drug bioavailability)

Unit

Quantitative value

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 447 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

75 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

CL (drug clearance)

207/467

2018-05-14 08:43:54

Unit

L/h/kg

Quantitative value

0.8

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 448 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

75 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Vdss

Unit

L/kg

Quantitative value

1.98

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 449 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

75 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

1.74

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 450 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

75 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

CL (drug clearance)

208/467

2018-05-14 08:43:54

Unit

L/h/kg

Quantitative value

0.8

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 451 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

75 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Vdss

Unit

L/kg

Quantitative value

1.98

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 452 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

75 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

1.74

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 453 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Cl/F

209/467

2018-05-14 08:43:54

Unit

L/h/kg

Quantitative value

2.92

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 454 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

F (drug bioavailability)

Unit

Quantitative value

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 455 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

75 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

CL i/CL

Quantitative value

0.788

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 456 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

75 mg

210/467

2018-05-14 08:43:54

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Vdss i/Vdss

Quantitative value

0.798

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 457 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

75 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el i/t1/2 el

Quantitative value

1.02

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 458 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

CL/F i/CL/F

Quantitative value

0.579

Concomitants: Compound RN

9406848

211/467

2018-05-14 08:43:54

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 459 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lignocaine

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-inf)

Unit

µg.min/mL

Quantitative value

117

Deviation

Statistical sgnificance (pvalue)

0.005

Concomitants: Compound RN

4164259

Concomitants: Compound name

Propranolol hydrochloride

Concomitants: Compound role

ICP

Bax; Tucker; Lennard; Woods; British Journal of Clinical Pharmacology; vol. 19; nb. 5; (1985); p. 597 - 603, View in Reaxys 460 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lignocaine

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

minute

Quantitative value

125

Deviation

Statistical sgnificance (pvalue)

0.05

212/467

2018-05-14 08:43:54

Concomitants: Compound RN

4164259

Concomitants: Compound name

Propranolol hydrochloride

Concomitants: Compound role

ICP

Bax; Tucker; Lennard; Woods; British Journal of Clinical Pharmacology; vol. 19; nb. 5; (1985); p. 597 - 603, View in Reaxys 461 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lignocaine

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Cmax

Unit

ng/mL

Quantitative value

875

Deviation

250

Statistical sgnificance (pvalue)

0.025

Concomitants: Compound RN

4164259

Concomitants: Compound name

Propranolol hydrochloride

Concomitants: Compound role

ICP

Bax; Tucker; Lennard; Woods; British Journal of Clinical Pharmacology; vol. 19; nb. 5; (1985); p. 597 - 603, View in Reaxys 462 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lignocaine

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

tmax

Unit

minute

Quantitative value

Deviation

213/467

2018-05-14 08:43:54

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

4164259

Concomitants: Compound name

Propranolol hydrochloride

Concomitants: Compound role

ICP

Bax; Tucker; Lennard; Woods; British Journal of Clinical Pharmacology; vol. 19; nb. 5; (1985); p. 597 - 603, View in Reaxys 463 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

CL (drug clearance)

Unit

mL/min

Quantitative value

897

Deviation

214

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 464 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Vdss

Unit

Quantitative value

123

Deviation

214/467

2018-05-14 08:43:54

Statistical sgnificance (pvalue)

0.02

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 465 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Kel

Unit

min-1

Quantitative value

0.00633

Deviation

0.000880000

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 466 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

t1/2 el

Unit

minute

Quantitative value

126

Deviation

215/467

2018-05-14 08:43:54

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 467 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

CL (drug clearance)

Unit

mL/min

Quantitative value

1155

Deviation

225

Concomitants: Compound RN

4327819

Concomitants: Compound name

Ranitidine

Concomitants: Compound role

ICP

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 468 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Vdss

Unit

Quantitative value

174

Deviation

Concomitants: Compound RN

4327819

216/467

2018-05-14 08:43:54

Concomitants: Compound name

Ranitidine

Concomitants: Compound role

ICP

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 469 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Kel

Unit

min-1

Quantitative value

0.00565

Deviation

0.000870000

Concomitants: Compound RN

4327819

Concomitants: Compound name

Ranitidine

Concomitants: Compound role

ICP

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 470 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

Lidocaïne HCl

Substance Dose

2 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

t1/2 el

Unit

minute

Quantitative value

112

Deviation

Concomitants: Compound RN

4327819

Concomitants: Compound name

Ranitidine

217/467

2018-05-14 08:43:54

Concomitants: Compound role

ICP

Jackson; Bentley; Glass; Fukui; Gandolfi; Plachetka; Clinical Pharmacology and Therapeutics; vol. 37; nb. 5; (1985); p. 544 - 548, View in Reaxys 471 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocïne HCl

Substance Dose

25 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

2.44

Deviation

0.420000

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Abernethy; Schwartz; Todd; Clinical pharmacology and therapeutics; vol. 38; nb. 3; (1985); p. 342 - 349, View in Reaxys 472 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocïne HCl

Substance Dose

25 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Vd (volume of distribution)

Unit

L/kg

Quantitative value

1.99

Deviation

0.810000

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

218/467

2018-05-14 08:43:54

Concomitants: Compound role

ICP

Abernethy; Schwartz; Todd; Clinical pharmacology and therapeutics; vol. 38; nb. 3; (1985); p. 342 - 349, View in Reaxys 473 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocïne HCl

Substance Dose

25 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

CL (drug clearance)

Unit

mL/min

Quantitative value

527

Deviation

134

Statistical sgnificance (pvalue)

0.05

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Abernethy; Schwartz; Todd; Clinical pharmacology and therapeutics; vol. 38; nb. 3; (1985); p. 342 - 349, View in Reaxys 474 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine HCl

Substance Dose

3600 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration (parameters)

Unit

µg/mL

Quantitative value

2.5

Deviation

0.300000

Statistical sgnificance (pvalue)

0.05

Concomitants: Compound RN

987417

219/467

2018-05-14 08:43:54

Concomitants: Compound name

Propranolol

Concomitants: Compound role

ICP

Schneck; Luderer; Davis; Vary; Clinical Pharmacology and Therapeutics; vol. 36; nb. 5; (1984); p. 584 - 587, View in Reaxys 475 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine HCl

Substance Dose

3600 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

CL (drug clearance)

Unit

mL/min

Quantitative value

866

Deviation

Statistical sgnificance (pvalue)

0.05

Concomitants: Compound RN

987417

Concomitants: Compound name

Propranolol

Concomitants: Compound role

ICP

Schneck; Luderer; Davis; Vary; Clinical Pharmacology and Therapeutics; vol. 36; nb. 5; (1984); p. 584 - 587, View in Reaxys 476 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine HCl

Substance Dose

3600 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

EH (hepatic extraction ratio)

Unit

Quantitative value

0.9

Deviation

0.0600000

Concomitants: Compound RN

987417

220/467

2018-05-14 08:43:54

Concomitants: Compound name

Propranolol

Concomitants: Compound role

ICP

Schneck; Luderer; Davis; Vary; Clinical Pharmacology and Therapeutics; vol. 36; nb. 5; (1984); p. 584 - 587, View in Reaxys 477 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine HCl

Substance Dose

3600 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration (parameters)

Unit

µg/mL

Quantitative value

2.7

Deviation

0.400000

Statistical sgnificance (pvalue)

0.05

Concomitants: Compound RN

2059000

Concomitants: Compound name

Nadolol

Concomitants: Compound role

ICP

Schneck; Luderer; Davis; Vary; Clinical Pharmacology and Therapeutics; vol. 36; nb. 5; (1984); p. 584 - 587, View in Reaxys 478 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine HCl

Substance Dose

3600 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

CL (drug clearance)

Unit

mL/min

Quantitative value

850

Deviation

Statistical sgnificance (pvalue)

0.05

221/467

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Concomitants: Compound RN

2059000

Concomitants: Compound name

Nadolol

Concomitants: Compound role

ICP

Schneck; Luderer; Davis; Vary; Clinical Pharmacology and Therapeutics; vol. 36; nb. 5; (1984); p. 584 - 587, View in Reaxys 479 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine HCl

Substance Dose

3600 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

EH (hepatic extraction ratio)

Unit

Quantitative value

0.91

Deviation

0.0500000

Concomitants: Compound RN

2059000

Concomitants: Compound name

Nadolol

Concomitants: Compound role

ICP

Schneck; Luderer; Davis; Vary; Clinical Pharmacology and Therapeutics; vol. 36; nb. 5; (1984); p. 584 - 587, View in Reaxys 480 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

1.94

Deviation

0.100000

Concomitants: Compound RN

2739235

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Concomitants: Compound name

Atenolol

Concomitants: Compound role

ICP

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 481 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

CL (drug clearance)

Unit

mL/min/kg

Quantitative value

47.18

Deviation

7.17000

Concomitants: Compound RN

2739235

Concomitants: Compound name

Atenolol

Concomitants: Compound role

ICP

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 482 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

1.93

Deviation

0.110000

Concomitants: Compound RN

3917968; 1117585

Concomitants: Compound name

Lidocaine hydrochloride; Metoprolol

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Concomitants: Compound role

ICP; ICP

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 483 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

1.98

Deviation

0.210000

Concomitants: Compound RN

3917968; 1117585

Concomitants: Compound name

Lidocaine hydrochloride; Metoprolol

Concomitants: Compound role

ICP; ICP

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 484 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

CL (drug clearance)

Unit

mL/min/kg

Quantitative value

44.51

Deviation

9.60000

Concomitants: Compound RN

3917968; 1117585

Concomitants: Compound name

Lidocaine hydrochloride; Metoprolol

Concomitants: Compound role

ICP; ICP

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Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 485 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

CL (drug clearance)

Unit

mL/min/kg

Quantitative value

9.33

Deviation

0.990000

Concomitants: Compound RN

3917968; 1117585

Concomitants: Compound name

Lidocaine hydrochloride; Metoprolol

Concomitants: Compound role

ICP; ICP

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 486 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

F (drug bioavailability)

Unit

Quantitative value

23.9

Deviation

3.90000

Concomitants: Compound RN

2739235

Concomitants: Compound name

Atenolol

Concomitants: Compound role

ICP

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys

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487 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

F (drug bioavailability)

Unit

Quantitative value

28.2

Deviation

6.30000

Concomitants: Compound RN

3917968; 1117585

Concomitants: Compound name

Lidocaine hydrochloride; Metoprolol

Concomitants: Compound role

ICP; ICP

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 488 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

1.77

Deviation

0.150000

Concomitants: Compound RN

2739235

Concomitants: Compound name

Atenolol

Concomitants: Compound role

ICP

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 489 of 1220 Bioassay Category

Pharmacokinetic

226/467

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Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

CL (drug clearance)

Unit

mL/min/kg

Quantitative value

10.16

Deviation

0.980000

Concomitants: Compound RN

2739235

Concomitants: Compound name

Atenolol

Concomitants: Compound role

ICP

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 490 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Vdss

Unit

L/kg

Quantitative value

1.52

Deviation

0.130000

Concomitants: Compound RN

2739235

Concomitants: Compound name

Atenolol

Concomitants: Compound role

ICP

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 491 of 1220 Bioassay Category Bioassay Name

Pharmacokinetic Pharmacokinetic

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Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lignocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Vdss

Unit

L/kg

Quantitative value

1.56

Deviation

0.180000

Concomitants: Compound RN

3917968; 1117585

Concomitants: Compound name

Lidocaine hydrochloride; Metoprolol

Concomitants: Compound role

ICP; ICP

Miners; Wing; Lillywhite; Smith; British Journal of Clinical Pharmacology; vol. 18; nb. 6; (1984); p. 853 - 860, View in Reaxys 492 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

CL (drug clearance)

Unit

mL/min

Quantitative value

576

Deviation

Statistical sgnificance (pvalue)

0.05

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Feely; Wilkinson; McAllister; Wood; Annals of Internal Medicine; vol. 96; nb. 5; (1982); p. 592 - 594, View in Reaxys 493 of 1220 Bioassay Category Bioassay Name

Metabolism/Transport Binding

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Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

2.5

Deviation

0.400000

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Feely; Wilkinson; McAllister; Wood; Annals of Internal Medicine; vol. 96; nb. 5; (1982); p. 592 - 594, View in Reaxys 494 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

concentration (parameters)

Unit

µg/mL

Quantitative value

2.5

Deviation

0.200000

Statistical sgnificance (pvalue)

0.05

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Feely; Wilkinson; McAllister; Wood; Annals of Internal Medicine; vol. 96; nb. 5; (1982); p. 592 - 594, View in Reaxys 495 of 1220 Bioassay Category Bioassay Name

Metabolism/Transport Binding

229/467

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Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Cmax

Unit

µg/mL

Quantitative value

Deviation

0.500000

Statistical sgnificance (pvalue)

0.05

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Feely; Wilkinson; McAllister; Wood; Annals of Internal Medicine; vol. 96; nb. 5; (1982); p. 592 - 594, View in Reaxys 496 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Vd (volume of distribution)

Unit

Quantitative value

Deviation

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Feely; Wilkinson; McAllister; Wood; Annals of Internal Medicine; vol. 96; nb. 5; (1982); p. 592 - 594, View in Reaxys 497 of 1220 Bioassay Category Bioassay Name

Metabolism/Transport Binding

230/467

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Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Vdss

Unit

Quantitative value

Deviation

Statistical sgnificance (pvalue)

0.05

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Feely; Wilkinson; McAllister; Wood; Annals of Internal Medicine; vol. 96; nb. 5; (1982); p. 592 - 594, View in Reaxys 498 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

human

Population State

Non Smoker

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

fu (unbound fraction)

Quantitative value

0.374

Deviation

0.0200000

Statistical sgnificance (pvalue)

0.05

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Feely; Wilkinson; McAllister; Wood; Annals of Internal Medicine; vol. 96; nb. 5; (1982); p. 592 - 594, View in Reaxys 499 of 1220 Bioassay Category Bioassay Name

Pharmacokinetic Pharmacokinetic

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Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

50 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

2.38

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

157775

Concomitants: Compound name

Antipyrine

Concomitants: Compound role

ICP

Blyden; Greenblatt; LeDuc; Scavone; European journal of clinical pharmacology; vol. 35; nb. 4; (1988); p. 413 - 417, View in Reaxys 500 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

50 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

CL (drug clearance)

Unit

mL/min/kg

Quantitative value

13.5

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

157775

Concomitants: Compound name

Antipyrine

Concomitants: Compound role

ICP

Blyden; Greenblatt; LeDuc; Scavone; European journal of clinical pharmacology; vol. 35; nb. 4; (1988); p. 413 - 417, View in Reaxys 501 of 1220 Bioassay Category Bioassay Name

Pharmacokinetic Pharmacokinetic

232/467

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Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

50 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

Vd (volume of distribution)

Unit

L/kg

Quantitative value

2.73

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

157775

Concomitants: Compound name

Antipyrine

Concomitants: Compound role

ICP

Blyden; Greenblatt; LeDuc; Scavone; European journal of clinical pharmacology; vol. 35; nb. 4; (1988); p. 413 - 417, View in Reaxys 502 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

75 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

CL (drug clearance)

Unit

L/h/kg

Quantitative value

0.63

Statistical sgnificance (pvalue)

0.001

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 503 of 1220 Bioassay Category Bioassay Name

Pharmacokinetic Pharmacokinetic

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Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

75 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Vdss

Unit

L/kg

Quantitative value

1.58

Statistical sgnificance (pvalue)

0.05

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 504 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

75 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

1.78

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 505 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

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Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Cl/F

Unit

L/h/kg

Quantitative value

1.69

Statistical sgnificance (pvalue)

0.001

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 506 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

lidocaine HCl

Substance Dose

200 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

F (drug bioavailability)

Unit

Quantitative value

Statistical sgnificance (pvalue)

0.001

Concomitants: Compound RN

9406848

Concomitants: Compound name

Cimetidine

Concomitants: Compound role

ICP

Wing; Miners; Birkett; et al.; Clinical Pharmacology and Therapeutics; vol. 35; nb. 5; (1984); p. 695 - 701, View in Reaxys 507 of 1220 Substance Effect

Antiproliferative

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : TF-1 cells proliferation; inhibition ofBioassay : TF-1 (CD34+ erythroleukemic cell line) cells stimulated with erythropoietin (EPO)5. Example 5: A Cell Based Screening Assay For Identifying Inhibitors ofEosinophil Proliferation244. The purpose of this study was to identify potential

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drug candidates for asthma. Eosinophils are white blood cells which contribute to the pathology of asthma. Lidocaine inhibits interleukin-5 (IL-5) Substance RN

3917968View in Reaxys

Substance Name

19; 21

Measurement Parameter

IC50

Unit

µM

Quantitative value

276

Measurement pX

3.56

Patent; WAGNER, Lori, A.; SZARDENINGS, Katrin; GLEICH, Gerald, J.; HASSAN, Tarek, Aboul-Fadl, Mohamed; (117 pag.); WO2007/136707; (A2); (2007), View in Reaxys 508 of 1220 Substance Effect

Antiproliferative

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : TF-1 cells proliferation; inhibition ofBioassay : TF-1 (CD34+ erythroleukemic cell line) cells stimulated with interleukin-5 (IL5)5. Example 5: A Cell Based Screening Assay For Identifying Inhibitors ofEosinophil Proliferation244. The purpose of this study was to identify potential drug candidates for asthma. Eosinophils are white blood cells which contribute to the pathology of asthma. Lidocaine inhibits interleukin-5 (IL-5)

Substance RN

3917968View in Reaxys

Substance Name

19; 21

Measurement Parameter

IC50

Unit

µM

Quantitative value

Measurement pX

4.08

Patent; WAGNER, Lori, A.; SZARDENINGS, Katrin; GLEICH, Gerald, J.; HASSAN, Tarek, Aboul-Fadl, Mohamed; (117 pag.); WO2007/136707; (A2); (2007), View in Reaxys 509 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : chigger; bites releif Example 22: Effect of 4% Lidocaine Formulation on Chigger BitesThe subject for this example had substantial experience with chigger bites, with typical symptoms including intense and prolonged (days to weeks) itching associated with the bites. Subject was provided with a solution of 4% lidocaine and

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Route of Adm.

cutaneous administration

Qualitative Results

test compound at concentration 4% ceased itching within minutes of application with no further symptoms

Measurement Parameter

qualitative

Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys 510 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : fire ant; bites releif Example 23: Effect of 4% Lidocaine Formulation on Fire Ant Bites The subject for this example had substantial experience with fire ant bites, with general symptoms of blistering, itching, pain associated with the bites. Subject was provided with a solution of 4% lidocaine and water (carrier). Subject

Biological Species/NCBI ID

human

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Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Route of Adm.

cutaneous administration

Qualitative Results

applying test compound at concentration 4% about 15 minutes after the bites occurred, complete relief from pain and itching after application was observed; typical blisters did not form

Measurement Parameter

qualitative

Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys 511 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : jellyfish; sting releif Example 20: Effect of 4% Lidocaine on Time to Pain ReleifIn this example a composition of 4% lidocaine hydrochloride in water was tested according to the procedures set forth in Example 2 above. It was found that initial pain relief could be felt at around one minute after application, with complete

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Route of Adm.

cutaneous administration

Qualitative Results

Measurement Parameter

qualitative

Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys 512 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : sea nettle; sting releif Example 12: Effects of Urea on PerformanceTwo formulations were tested to determine the effects of urea on the efficacy of formulations of the present disclosure. 10% lidocaine in water <n="37"/>10% lidocaine in water + 10% ureaStinging jellyfish: sea nettle with 4" bell diameter Results:There was

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Route of Adm.

cutaneous administration

Qualitative Results

Measurement Parameter

qualitative

Patent; COASTAL SOLUTIONS, INC.; WO2008/36912; (2008); (A2) English, View in Reaxys 513 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

a dose-dependent decreases the electrically driven ventricle strips in vitro, 2 - 20 μg/ml, (WistarCPB rats); a dose-dependent decreases the heart rate and contraction force in vitro, 2 - 20 μg/ml, (guinea pig atria)

Measurement Parameter

qualitative

Zwagemakers; Claassen; Arzneimittel-Forschung/Drug Research; vol. 30; nb. 9; (1980); p. 1526 - 1534, View in Reaxys

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514 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

antispasmodic activity on the smooth musculature of the urinary tract of male Wistar rats (pD2, 2.83-3.14)

Measurement Parameter

qualitative

Schiantarelli; Murmann; Arzneimittel-Forschung/Drug Research; vol. 30; nb. 7; (1980); p. 1102 - 1109, View in Reaxys 515 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

in vitro electrophysiology in canine Purkinje fibers and canine ventricular muscle strips; intraduodenal bioavailability (dog); antiarrhythmic efficacy (dog)

Measurement Parameter

qualitative

Morgan Jr.; Lis; Marisca; Argentieri; Sullivan; Wong; Journal of Medicinal Chemistry; vol. 30; nb. 12; (1987); p. 2259 2269, View in Reaxys 516 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

LD 50: 158 mg/kg (mouse, intraperitoneally); surface anesthetic activity in rabbits (cornea of eye) at a min. dose of 5.0E-2 M

Measurement Parameter

qualitative

Oelschlager; Ueberall; Paradeiser; Kummer; Archiv der Pharmazie; vol. 321; nb. 2; (1988); p. 115 - 118, View in Reaxys 517 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : |Accumulation Bioassay : 5 rats/group; rats housed in 25 deg C tissue distribution study; animals killed 5, 10 and 15 min after injection; brain, liver and heart samples collected; HPLC

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

5 mg/kg

Substance Route of Adm.

intravenous administration

Qualitative Results

title comp. distribution (μg/g wet tissue): brain - 1.0, 0.4, 0.3, liver - 1.3, 0.8, 1.9, heart - 5.3, 1.8, 2.0 at 5, 10 and 15 min post-injection, resp.

Measurement Parameter

qualitative

Barat, Stephen A.; Ahdel-Rahman, Mohamed S.; Journal of Applied Toxicology; vol. 18; nb. 4; (1998); p. 227 - 232, View in Reaxys 518 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : |toxicokinetics Bioassay : 6-8 rats/group; rats housed in 25 deg C plasma time-course study; blood samples collected at 1, 5, 15, 30, 45 min and 1, 1.5, 2, 3, 4, 5 and 6 h; one-compartment model of elimination; half-live of elimination determined; HPLC

Biological Species/NCBI ID

Rattus norvegicus

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Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

5 mg/kg

Substance Route of Adm.

intravenous administration

Qualitative Results

diagram

Measurement Parameter

qualitative

Barat, Stephen A.; Ahdel-Rahman, Mohamed S.; Journal of Applied Toxicology; vol. 18; nb. 4; (1998); p. 227 - 232, View in Reaxys 519 of 1220 Substance Effect

Behavioural Symptoms

Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Bioassay : 5 rats/group; rats housed in 25 deg C locomotor activity study; in saline (control); mean horizontal counts per minute were taken at 5, 15, 30, 45, 60 and 90 min post-injection

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

5 mg/kg

Substance Route of Adm.

intravenous administration

Measurement Parameter

qualitative

Qualitative value

Measurement pX

Barat, Stephen A.; Ahdel-Rahman, Mohamed S.; Journal of Applied Toxicology; vol. 18; nb. 4; (1998); p. 227 - 232, View in Reaxys 520 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : |pharmacokinetics Bioassay : group 3, ETT cuffs filled with title comp.(30 mg)+NaHCO3 8.4 percent; group 4, title comp.(20 mg)+NaHCO3 8.4 percent; group 5, title comp.(20 mg) and water; anaesthetic time: 159 min; plasma lidocain concentration were determined using a reversedphase HPLC method 15 adults, smoker patients (43+/-5 years, 171+/-11 cm, 74+/-8 kg, 25+/-5 cigarettes/day for at least 8 years)patients randomly assigned to 5 groups: in group 1: endotracheal tube (ETT) cuffs inflated with air; group 2: title comp.(40 mg)+NaHCO3 (8.4 percent)

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Route of Adm.

intraspinal administration

Qualitative Results

improved tolerance (decreased pain scores) in the rank order: air group<<title comp. group<alkalinized title comp. group; increased spontaneous ventillation time: 28+/-13 min for groups 2, 3, 4; 12+/-3 min for group 5; 3+/-2 min for control

Measurement Parameter

qualitative

Dollo, Gilles; Estebe, Jean-Pierre; Le Corre, Pascal; Chevanne, Francois; Ecoffey, Claude; Le Verge, Roger; European Journal of Pharmaceutical Sciences; vol. 13; nb. 3; (2001); p. 319 - 323, View in Reaxys 521 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : |transport Target : endotracheal tubeBioassay : 2 percent title comp. with water; title comp. (20, 30 or 40 mg) with sodium bicarbonate (8.4 percent); title comp. base conc. measured continuously at 205 nm every 15 min using Uvikon spectrophotometer in vitro release of title comp. from endotracheal tube (ETT) cuffs filled with different formulations (base form, HCl form or alkali-

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nized HCl); ETT immersed in release medium consisting phosphate buffer at 37 deg C; 0.2 percent title comp. base in water Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

dramatic increase in percent title comp. base released (65.1 percent released after 6 h) compared to title comp. (1.1 percent after 6 h); only hydrophobic neutral base form of title comp. was able to diffuse; alkalinization of title comp. no lag time

Measurement Parameter

qualitative

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

cardiovascular and ventilator effects (rats, guinea-pigs)

Measurement Parameter

qualitative

Paakkari; Svartstrom-Fraser; Arzneimittel-Forschung/Drug Research; vol. 38; nb. 4 A; (1988); p. 617 - 619, View in Reaxys 523 of 1220 Substance Effect

Analgesic

Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Bioassay : photochemically induced nerve ischaemia model (Gazelius model); 1 week after injury, behavioural testing by two methods: mechanical stimulation (von Frey hair stimulation) and cold stimulation (spraying ethyl chloride); observation up to 60 min

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

10 mg/kg

Substance Route of Adm.

intraperitoneal administration

Measurement Parameter

qualitative

Qualitative value

Measurement pX

Erichsen, Helle Kirstein; Hao, Jing-Xia; Xu, Xiao-Jun; Blackburn-Munro, Gordon; European Journal of Pharmacology; vol. 458; nb. 3; (2003); p. 275 - 282, View in Reaxys 524 of 1220 Substance Effect

Analgesic

Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Bioassay : spared nerve injury model; 1 week after injury, behavioural testing by three methods: mechanical stimulation (von Frey hair stimulation), cold stimulation (spraying ethyl chloride), pin prick test (for mechanical hyperalgesia); observation up to 60 min

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

10 mg/kg

Substance Route of Adm.

intraperitoneal administration

Measurement Parameter

qualitative

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Qualitative value

Measurement pX

Erichsen, Helle Kirstein; Hao, Jing-Xia; Xu, Xiao-Jun; Blackburn-Munro, Gordon; European Journal of Pharmacology; vol. 458; nb. 3; (2003); p. 275 - 282, View in Reaxys 525 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

mongrel dog

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

117 µg/min/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

time

Unit

Measurement Object

His-Purkinje conduction time (HV interval)

Quantitative value

19.6

Deviation

0.700000

Concomitants: Compound RN

987417; 24141036

Concomitants: Compound name

Propranolol; Pentobarbital sodium

Concomitants: Compound role

OCV; ANA

Dise; Stolfi; Clarkson; Pickoff; Journal of Pharmacology and Experimental Therapeutics; vol. 259; nb. 2; (1991); p. 535 - 542, View in Reaxys 526 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

mongrel dog

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

117 µg/min/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

time

Unit

Measurement Object

His-Purkinje conduction time (HV interval)

Quantitative value

19.8

Deviation

0.700000

Concomitants: Compound RN

987417; 24141036

Concomitants: Compound name

Propranolol; Pentobarbital sodium

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Concomitants: Compound role

OCV; ANA

Dise; Stolfi; Clarkson; Pickoff; Journal of Pharmacology and Experimental Therapeutics; vol. 259; nb. 2; (1991); p. 535 - 542, View in Reaxys 527 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

mongrel dog

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

117 µg/min/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

time

Unit

Measurement Object

His-Purkinje conduction time (HV interval)

Quantitative value

20.5

Deviation

0.700000

Concomitants: Compound RN

987417; 24141036

Concomitants: Compound name

Propranolol; Pentobarbital sodium

Concomitants: Compound role

OCV; ANA

Dise; Stolfi; Clarkson; Pickoff; Journal of Pharmacology and Experimental Therapeutics; vol. 259; nb. 2; (1991); p. 535 - 542, View in Reaxys 528 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

mongrel dog

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

117 µg/min/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

time

Unit

Measurement Object

His-Purkinje conduction time (HV interval)

Quantitative value

22.2

Deviation

0.800000

Concomitants: Compound RN

987417; 24141036

Concomitants: Compound name

Propranolol; Pentobarbital sodium

Concomitants: Compound role

OCV; ANA

242/467

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Dise; Stolfi; Clarkson; Pickoff; Journal of Pharmacology and Experimental Therapeutics; vol. 259; nb. 2; (1991); p. 535 - 542, View in Reaxys 529 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

mongrel dog

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

117 µg/min/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

time

Unit

Measurement Object

His-Purkinje conduction time (HV interval)

Quantitative value

23.4

Deviation

1.10000

Concomitants: Compound RN

987417; 24141036

Concomitants: Compound name

Propranolol; Pentobarbital sodium

Concomitants: Compound role

OCV; ANA

Dise; Stolfi; Clarkson; Pickoff; Journal of Pharmacology and Experimental Therapeutics; vol. 259; nb. 2; (1991); p. 535 - 542, View in Reaxys 530 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

mongrel dog

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

117 µg/min/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

time

Unit

Measurement Object

Pacing spike to ventricle interval (SV interval)

Quantitative value

19.2

Deviation

0.800000

Concomitants: Compound RN

987417; 24141036

Concomitants: Compound name

Propranolol; Pentobarbital sodium

Concomitants: Compound role

OCV; ANA

Dise; Stolfi; Clarkson; Pickoff; Journal of Pharmacology and Experimental Therapeutics; vol. 259; nb. 2; (1991); p. 535 - 542, View in Reaxys

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531 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

mongrel dog

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

117 µg/min/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

time

Unit

Measurement Object

Pacing spike to ventricle interval (SV interval)

Quantitative value

20.2

Deviation

Concomitants: Compound RN

987417; 24141036

Concomitants: Compound name

Propranolol; Pentobarbital sodium

Concomitants: Compound role

OCV; ANA

Dise; Stolfi; Clarkson; Pickoff; Journal of Pharmacology and Experimental Therapeutics; vol. 259; nb. 2; (1991); p. 535 - 542, View in Reaxys 532 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

mongrel dog

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

117 µg/min/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

time

Unit

Measurement Object

Pacing spike to ventricle interval (SV interval)

Quantitative value

21.3

Deviation

1.10000

Concomitants: Compound RN

987417; 24141036

Concomitants: Compound name

Propranolol; Pentobarbital sodium

Concomitants: Compound role

OCV; ANA

Dise; Stolfi; Clarkson; Pickoff; Journal of Pharmacology and Experimental Therapeutics; vol. 259; nb. 2; (1991); p. 535 - 542, View in Reaxys 533 of 1220 Bioassay Category

In Vivo (Animal models)

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Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

mongrel dog

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

117 µg/min/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

time

Unit

Measurement Object

Pacing spike to ventricle interval (SV interval)

Quantitative value

22.9

Deviation

1.20000

Concomitants: Compound RN

987417; 24141036

Concomitants: Compound name

Propranolol; Pentobarbital sodium

Concomitants: Compound role

OCV; ANA

Dise; Stolfi; Clarkson; Pickoff; Journal of Pharmacology and Experimental Therapeutics; vol. 259; nb. 2; (1991); p. 535 - 542, View in Reaxys 534 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

mongrel dog

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

117 µg/min/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

time

Unit

Measurement Object

Pacing spike to ventricle interval (SV interval)

Quantitative value

24.3

Deviation

1.10000

Concomitants: Compound RN

987417; 24141036

Concomitants: Compound name

Propranolol; Pentobarbital sodium

Concomitants: Compound role

OCV; ANA

Dise; Stolfi; Clarkson; Pickoff; Journal of Pharmacology and Experimental Therapeutics; vol. 259; nb. 2; (1991); p. 535 - 542, View in Reaxys 535 of 1220 Bioassay Category Bioassay Name

In Vivo (Animal models) Electrocardiogram : ECG

245/467

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Biological Species/NCBI ID

mongrel dog

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

117 µg/min/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

time

Unit

Measurement Object

Pacing spike to ventricle interval (SV interval)

Quantitative value

27.7

Deviation

1.30000

Concomitants: Compound RN

987417; 24141036

Concomitants: Compound name

Propranolol; Pentobarbital sodium

Concomitants: Compound role

OCV; ANA

Dise; Stolfi; Clarkson; Pickoff; Journal of Pharmacology and Experimental Therapeutics; vol. 259; nb. 2; (1991); p. 535 - 542, View in Reaxys 536 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

mongrel dog

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

117 µg/min/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

time

Unit

Measurement Object

Pacing spike to ventricle interval (SV interval)

Quantitative value

30.4

Deviation

2.60000

Concomitants: Compound RN

987417; 24141036

Concomitants: Compound name

Propranolol; Pentobarbital sodium

Concomitants: Compound role

OCV; ANA

Dise; Stolfi; Clarkson; Pickoff; Journal of Pharmacology and Experimental Therapeutics; vol. 259; nb. 2; (1991); p. 535 - 542, View in Reaxys 537 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

mongrel dog

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Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

117 µg/min/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

time

Unit

Measurement Object

His-Purkinje conduction time of extrastimulated beat (S2V2 interval)

Quantitative value

19.3

Deviation

0.800000

Concomitants: Compound RN

987417; 24141036

Concomitants: Compound name

Propranolol; Pentobarbital sodium

Concomitants: Compound role

OCV; ANA

Dise; Stolfi; Clarkson; Pickoff; Journal of Pharmacology and Experimental Therapeutics; vol. 259; nb. 2; (1991); p. 535 - 542, View in Reaxys 538 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

mongrel dog

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

117 µg/min/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

time

Unit

Measurement Object

His-Purkinje conduction time of extrastimulated beat (S2V2 interval)

Quantitative value

19.8

Deviation

0.900000

Concomitants: Compound RN

987417; 24141036

Concomitants: Compound name

Propranolol; Pentobarbital sodium

Concomitants: Compound role

OCV; ANA

Dise; Stolfi; Clarkson; Pickoff; Journal of Pharmacology and Experimental Therapeutics; vol. 259; nb. 2; (1991); p. 535 - 542, View in Reaxys 539 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

mongrel dog

Substance RN

3917968View in Reaxys

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Substance Name

Lidocaine

Substance Dose

117 µg/min/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

time

Unit

Measurement Object

His-Purkinje conduction time of extrastimulated beat (S2V2 interval)

Quantitative value

19.6

Deviation

0.900000

Concomitants: Compound RN

987417; 24141036

Concomitants: Compound name

Propranolol; Pentobarbital sodium

Concomitants: Compound role

OCV; ANA

Dise; Stolfi; Clarkson; Pickoff; Journal of Pharmacology and Experimental Therapeutics; vol. 259; nb. 2; (1991); p. 535 - 542, View in Reaxys 540 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

mongrel dog

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

117 µg/min/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

time

Unit

Measurement Object

His-Purkinje conduction time of extrastimulated beat (S2V2 interval)

Quantitative value

19.8

Deviation

0.800000

Concomitants: Compound RN

987417; 24141036

Concomitants: Compound name

Propranolol; Pentobarbital sodium

Concomitants: Compound role

OCV; ANA

Dise; Stolfi; Clarkson; Pickoff; Journal of Pharmacology and Experimental Therapeutics; vol. 259; nb. 2; (1991); p. 535 - 542, View in Reaxys 541 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

mongrel dog

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

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Substance Dose

117 µg/min/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

time

Unit

Measurement Object

His-Purkinje conduction time of extrastimulated beat (S2V2 interval)

Quantitative value

Deviation

Concomitants: Compound RN

987417; 24141036

Concomitants: Compound name

Propranolol; Pentobarbital sodium

Concomitants: Compound role

OCV; ANA

Dise; Stolfi; Clarkson; Pickoff; Journal of Pharmacology and Experimental Therapeutics; vol. 259; nb. 2; (1991); p. 535 - 542, View in Reaxys 542 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

mongrel dog

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

117 µg/min/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

time

Unit

Measurement Object

His-Purkinje conduction time of extrastimulated beat (S2V2 interval)

Quantitative value

20.6

Deviation

0.900000

Concomitants: Compound RN

987417; 24141036

Concomitants: Compound name

Propranolol; Pentobarbital sodium

Concomitants: Compound role

OCV; ANA

Dise; Stolfi; Clarkson; Pickoff; Journal of Pharmacology and Experimental Therapeutics; vol. 259; nb. 2; (1991); p. 535 - 542, View in Reaxys 543 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

mongrel dog

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

117 µg/min/kg

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Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

time

Unit

Measurement Object

His-Purkinje conduction time of extrastimulated beat (S2V2 interval)

Quantitative value

21.5

Deviation

0.800000

Concomitants: Compound RN

987417; 24141036

Concomitants: Compound name

Propranolol; Pentobarbital sodium

Concomitants: Compound role

OCV; ANA

Dise; Stolfi; Clarkson; Pickoff; Journal of Pharmacology and Experimental Therapeutics; vol. 259; nb. 2; (1991); p. 535 - 542, View in Reaxys 544 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

mongrel dog

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

117 µg/min/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

time

Unit

Measurement Object

His-Purkinje conduction time of extrastimulated beat (S2V2 interval)

Quantitative value

22.3

Deviation

0.900000

Concomitants: Compound RN

987417; 24141036

Concomitants: Compound name

Propranolol; Pentobarbital sodium

Concomitants: Compound role

OCV; ANA

Dise; Stolfi; Clarkson; Pickoff; Journal of Pharmacology and Experimental Therapeutics; vol. 259; nb. 2; (1991); p. 535 - 542, View in Reaxys 545 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

mongrel dog

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

117 µg/min/kg

Substance Route of Adm.

intravenous administration

250/467

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Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

time

Unit

Measurement Object

His-Purkinje conduction time of extrastimulated beat (S2V2 interval)

Quantitative value

23.3

Deviation

1.10000

Concomitants: Compound RN

987417; 24141036

Concomitants: Compound name

Propranolol; Pentobarbital sodium

Concomitants: Compound role

OCV; ANA

Dise; Stolfi; Clarkson; Pickoff; Journal of Pharmacology and Experimental Therapeutics; vol. 259; nb. 2; (1991); p. 535 - 542, View in Reaxys 546 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

mongrel dog

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

117 µg/min/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

time

Unit

Measurement Object

His-Purkinje conduction time of extrastimulated beat (S2V2 interval)

Quantitative value

25.4

Deviation

1.20000

Concomitants: Compound RN

987417; 24141036

Concomitants: Compound name

Propranolol; Pentobarbital sodium

Concomitants: Compound role

OCV; ANA

Dise; Stolfi; Clarkson; Pickoff; Journal of Pharmacology and Experimental Therapeutics; vol. 259; nb. 2; (1991); p. 535 - 542, View in Reaxys 547 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

mongrel dog

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

117 µg/min/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

251/467

2018-05-14 08:43:54

Measurement Parameter

time

Unit

Measurement Object

His-Purkinje conduction time of extrastimulated beat (S2V2 interval)

Quantitative value

Deviation

1.90000

Concomitants: Compound RN

987417; 24141036

Concomitants: Compound name

Propranolol; Pentobarbital sodium

Concomitants: Compound role

OCV; ANA

Dise; Stolfi; Clarkson; Pickoff; Journal of Pharmacology and Experimental Therapeutics; vol. 259; nb. 2; (1991); p. 535 - 542, View in Reaxys 548 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

Electrocardiogram : ECG

Biological Species/NCBI ID

mongrel dog

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

117 µg/min/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

time

Unit

Measurement Object

His-Purkinje conduction time of extrastimulated beat (S2V2 interval)

Quantitative value

34.4

Deviation

2.90000

Concomitants: Compound RN

987417; 24141036

Concomitants: Compound name

Propranolol; Pentobarbital sodium

Concomitants: Compound role

OCV; ANA

Dise; Stolfi; Clarkson; Pickoff; Journal of Pharmacology and Experimental Therapeutics; vol. 259; nb. 2; (1991); p. 535 - 542, View in Reaxys 549 of 1220 Substance Effect

Antiarrhytmic

Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Biological Species/NCBI ID

Swiss Webster mouse

Bioassay Pathology

heart arrhythmia

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine HCl

Substance Dose

30 mg/kg

Substance Route of Adm.

intravenous administration

252/467

2018-05-14 08:43:54

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

time

Unit

second

Measurement Object

Onset of initial arrhytmia

Quantitative value

191

Deviation

Statistical sgnificance (pvalue)

0.01

Concomitants: Compound RN

24147515; 24141036

Concomitants: Compound name

Aconitine; Pentobarbital sodium

Concomitants: Compound role

IAV; ANA

Nwangwu; Holcslaw; Stohs; Archives Internationales de Pharmacodynamie et de Therapie; vol. 229; nb. 2; (1977); p. 219 226, View in Reaxys 550 of 1220 Substance Effect

Antiarrhytmic

Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Biological Species/NCBI ID

Swiss Webster mouse

Bioassay Pathology

tachycardia

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine HCl

Substance Dose

30 mg/kg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Perfused/Infused

Measurement Parameter

time

Unit

second

Measurement Object

Onset of ventricular tachycardia

Quantitative value

225

Deviation

Statistical sgnificance (pvalue)

0.01

Concomitants: Compound RN

24147515; 24141036

Concomitants: Compound name

Aconitine; Pentobarbital sodium

Concomitants: Compound role

IAV; ANA

Nwangwu; Holcslaw; Stohs; Archives Internationales de Pharmacodynamie et de Therapie; vol. 229; nb. 2; (1977); p. 219 226, View in Reaxys 551 of 1220 Target Name Target Synonyms

Sodium channel protein type 10 subunit alpha [Rattus norvegicus]; Sodium channel subunit beta-1 [Rattus norvegicus] peripheral nerve sodium channel 3; pn3; scn10a; sensory neuron sodium channel; sns; sodium channel protein type 10 subunit alpha; sodium channel protein type x subunit alpha; voltage-gated sodium channel subunit alpha nav1.8 + scn1b; sodium channel subunit beta-1

253/467

2018-05-14 08:43:54

Target Uniprot ID

q62968 + q00954

Target, Subunit, Species

Sodium channel protein type 10 subunit alpha [Rattus norvegicus]; Sodium channel subunit beta-1 [Rattus norvegicus]

Target Mutant/Chimera Details

Sodium channel protein type 10 subunit alpha [Rattus norvegicus]:Wild; Sodium channel subunit beta-1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus; Rattus norvegicus

Target Transfection

Transfected; Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

ND7/23 cell line

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Measurement Parameter

IC50

Unit

µM

Quantitative value

319

Deviation

Measurement pX

3.5

Concomitants: Compound RN

24140929

Concomitants: Compound name

Tetrodotoxin

Concomitants: Compound role

COM

552 of 1220 Target Name

Sodium channel protein type 10 subunit alpha [Rattus norvegicus]; Sodium channel subunit beta-1 [Rattus norvegicus]

Target Synonyms

peripheral nerve sodium channel 3; pn3; scn10a; sensory neuron sodium channel; sns; sodium channel protein type 10 subunit alpha; sodium channel protein type x subunit alpha; voltage-gated sodium channel subunit alpha nav1.8 + scn1b; sodium channel subunit beta-1

Target Uniprot ID

q62968 + q00954

Target, Subunit, Species

Sodium channel protein type 10 subunit alpha [Rattus norvegicus]; Sodium channel subunit beta-1 [Rattus norvegicus]

Target Mutant/Chimera Details

Sodium channel protein type 10 subunit alpha [Rattus norvegicus]:Wild; Sodium channel subunit beta-1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus; Rattus norvegicus

Target Transfection

Transfected; Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

ND7/23 cell line

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Measurement Parameter

nH (Hill coefficient)

Quantitative value

1.02

254/467

2018-05-14 08:43:54

Deviation

0.0200000

Concomitants: Compound RN

24140929

Concomitants: Compound name

Tetrodotoxin

Concomitants: Compound role

COM

553 of 1220 Target Name

Sodium channel protein type 10 subunit alpha [Rattus norvegicus]; Sodium channel subunit beta-1 [Rattus norvegicus]

Target Synonyms

Target Uniprot ID

q62968 + q00954

Target, Subunit, Species

Sodium channel protein type 10 subunit alpha [Rattus norvegicus]; Sodium channel subunit beta-1 [Rattus norvegicus]

Target Mutant/Chimera Details

Sodium channel protein type 10 subunit alpha [Rattus norvegicus]:Wild; Sodium channel subunit beta-1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus; Rattus norvegicus

Target Transfection

Transfected; Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

ND7/23 cell line

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Measurement Parameter

IC50

Unit

µM

Quantitative value

164

Deviation

Measurement pX

3.79

Concomitants: Compound RN

24140929

Concomitants: Compound name

Tetrodotoxin

Concomitants: Compound role

COM

554 of 1220 Target Name

Sodium channel protein type 10 subunit alpha [Rattus norvegicus]; Sodium channel subunit beta-1 [Rattus norvegicus]

Target Synonyms

Target Uniprot ID

q62968 + q00954

Target, Subunit, Species

Sodium channel protein type 10 subunit alpha [Rattus norvegicus]; Sodium channel subunit beta-1 [Rattus norvegicus]

Target Mutant/Chimera Details

Sodium channel protein type 10 subunit alpha [Rattus norvegicus]:Wild; Sodium channel subunit beta-1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus; Rattus norvegicus

255/467

2018-05-14 08:43:54

Target Transfection

Transfected; Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

ND7/23 cell line

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Measurement Parameter

nH (Hill coefficient)

Quantitative value

1.11

Deviation

0.0600000

Concomitants: Compound RN

24140929

Concomitants: Compound name

Tetrodotoxin

Concomitants: Compound role

COM

555 of 1220 Target Name

Voltage-gated sodium channel, TTX-Sensitive [Rattus norvegicus]; Sodium channel subunit beta-1 [Rattus norvegicus]

Target Synonyms

voltage-gated sodium channel, ttx-sensitive + scn1b; sodium channel subunit beta-1

Target Uniprot ID

q00954

Target, Subunit, Species

Voltage-gated sodium channel, TTX-Sensitive [Rattus norvegicus]; Sodium channel subunit beta-1 [Rattus norvegicus]

Target Mutant/Chimera Details

Voltage-gated sodium channel, TTX-Sensitive [Rattus norvegicus]:Wild; Sodium channel subunit beta-1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus; Rattus norvegicus

Target Transfection

Non Transfected; Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

ND7/23 cell line

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Measurement Parameter

IC50

Unit

µM

Quantitative value

517

Deviation

Measurement pX

3.29

556 of 1220 Target Name

Voltage-gated sodium channel, TTX-Sensitive [Rattus norvegicus]; Sodium channel subunit beta-1 [Rattus norvegicus]

Target Synonyms

voltage-gated sodium channel, ttx-sensitive + scn1b; sodium channel subunit beta-1

Target Uniprot ID

q00954

Target, Subunit, Species

Voltage-gated sodium channel, TTX-Sensitive [Rattus norvegicus]; Sodium channel subunit beta-1 [Rattus norvegicus]

256/467

2018-05-14 08:43:54

Target Mutant/Chimera Details

Voltage-gated sodium channel, TTX-Sensitive [Rattus norvegicus]:Wild; Sodium channel subunit beta-1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus; Rattus norvegicus

Target Transfection

Non Transfected; Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

ND7/23 cell line

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Measurement Parameter

nH (Hill coefficient)

Quantitative value

0.96

Deviation

0.0400000

557 of 1220 Target Name

Voltage-gated sodium channel, TTX-Sensitive [Rattus norvegicus]; Sodium channel subunit beta-1 [Rattus norvegicus]

Target Synonyms

voltage-gated sodium channel, ttx-sensitive + scn1b; sodium channel subunit beta-1

Target Uniprot ID

q00954

Target, Subunit, Species

Voltage-gated sodium channel, TTX-Sensitive [Rattus norvegicus]; Sodium channel subunit beta-1 [Rattus norvegicus]

Target Mutant/Chimera Details

Voltage-gated sodium channel, TTX-Sensitive [Rattus norvegicus]:Wild; Sodium channel subunit beta-1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus; Rattus norvegicus

Target Transfection

Non Transfected; Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

ND7/23 cell line

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Measurement Parameter

IC50

Unit

µM

Quantitative value

Deviation

Measurement pX

4.52

558 of 1220 Target Name

Voltage-gated sodium channel, TTX-Sensitive [Rattus norvegicus]; Sodium channel subunit beta-1 [Rattus norvegicus]

Target Synonyms

voltage-gated sodium channel, ttx-sensitive + scn1b; sodium channel subunit beta-1

Target Uniprot ID

q00954

Target, Subunit, Species

Voltage-gated sodium channel, TTX-Sensitive [Rattus norvegicus]; Sodium channel subunit beta-1 [Rattus norvegicus]

Target Mutant/Chimera Details

Voltage-gated sodium channel, TTX-Sensitive [Rattus norvegicus]:Wild; Sodium channel subunit beta-1 [Rattus norvegicus]:Wild

257/467

2018-05-14 08:43:54

Target Species (Bioactivity)

Rattus norvegicus; Rattus norvegicus

Target Transfection

Non Transfected; Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

ND7/23 cell line

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Measurement Parameter

nH (Hill coefficient)

Quantitative value

1.03

Deviation

0.0500000

559 of 1220 Target Name

acid-sensing ion channel (ASIC2a);+acid-sensing ion channel (ASIC1a)

Target Synonyms

acid-sensing ion channel (asic2a) + acid-sensing ion channel (asic1a)

Target, Subunit, Species

acid-sensing ion channel (ASIC1a); acid-sensing ion channel (ASIC2a)

Target Mutant/Chimera Details

acid-sensing ion channel (ASIC2a):Wild + acid-sensing ion channel (ASIC1a):Wild

Target Transfection

Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

CHO cell line

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

30 mM

Measurement Parameter

% Inhibition

Unit

Quantitative value

Measurement pX

2.48

560 of 1220 Target Name

acid-sensing ion channel (ASIC2a);+acid-sensing ion channel (ASIC1a)

Target Synonyms

acid-sensing ion channel (asic2a) + acid-sensing ion channel (asic1a)

Target, Subunit, Species

acid-sensing ion channel (ASIC1a); acid-sensing ion channel (ASIC2a)

Target Mutant/Chimera Details

acid-sensing ion channel (ASIC2a):Wild + acid-sensing ion channel (ASIC1a):Wild

Target Transfection

Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

CHO cell line

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

1 mM

258/467

2018-05-14 08:43:54

Measurement Parameter

% Inhibition

Unit

Quantitative value

15.67

Deviation

2.96000

Measurement pX

561 of 1220 Target Name

acid-sensing ion channel (ASIC2a);+acid-sensing ion channel (ASIC1a)

Target Synonyms

acid-sensing ion channel (asic2a) + acid-sensing ion channel (asic1a)

Target, Subunit, Species

acid-sensing ion channel (ASIC1a); acid-sensing ion channel (ASIC2a)

Target Mutant/Chimera Details

acid-sensing ion channel (ASIC2a):Wild + acid-sensing ion channel (ASIC1a):Wild

Target Transfection

Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

CHO cell line

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Measurement Parameter

IC50

Unit

Quantitative value

11.79

Deviation

1.74000

Measurement pX

1.93

562 of 1220 Target Name

acid-sensing ion channel (ASIC2a);+acid-sensing ion channel (ASIC1a)

Target Synonyms

acid-sensing ion channel (asic2a) + acid-sensing ion channel (asic1a)

Target, Subunit, Species

acid-sensing ion channel (ASIC1a); acid-sensing ion channel (ASIC2a)

Target Mutant/Chimera Details

acid-sensing ion channel (ASIC2a):Wild + acid-sensing ion channel (ASIC1a):Wild

Target Transfection

Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

CHO cell line

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Measurement Parameter

nH (Hill coefficient)

Quantitative value

2.7

Deviation

0.500000

563 of 1220 Target Name

acid-sensing ion channel (ASIC2a);+acid-sensing ion channel (ASIC1a)

Target Synonyms

acid-sensing ion channel (asic2a) + acid-sensing ion channel (asic1a)

Target, Subunit, Species

acid-sensing ion channel (ASIC1a); acid-sensing ion channel (ASIC2a)

Target Mutant/Chimera Details

acid-sensing ion channel (ASIC2a):Wild + acid-sensing ion channel (ASIC1a):Wild

259/467

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Target Transfection

Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

CHO cell line

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

1 mM

Measurement Parameter

% Inhibition

Unit

Quantitative value

17.28

Deviation

2.25000

Measurement pX

564 of 1220 Target Name

acid-sensing ion channel (ASIC2a);+acid-sensing ion channel (ASIC1a)

Target Synonyms

acid-sensing ion channel (asic2a) + acid-sensing ion channel (asic1a)

Target, Subunit, Species

acid-sensing ion channel (ASIC1a); acid-sensing ion channel (ASIC2a)

Target Mutant/Chimera Details

acid-sensing ion channel (ASIC2a):Wild + acid-sensing ion channel (ASIC1a):Wild

Target Transfection

Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

CHO cell line

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

1 mM

Measurement Parameter

% Inhibition

Unit

Quantitative value

11.46

Deviation

0.690000

Measurement pX

565 of 1220 Substance Effect

Antiproliferative

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Target : TF-1 (CD34+ erythroleukemic cell line) cells stimulated with erythropoietin (EPO)Bioassay : 5. Example 5: A Cell Based Screening Assay For Identifying Inhibitors ofEosinophil Proliferation244. The purpose of this study was to identify potential drug candidates for asthma. Eosinophils are white blood cells which contribute to the pathology of asthma. Lidocaine inhibits interleukin-5 (IL-5)

Substance RN

3917968View in Reaxys

Substance Name

178204

Measurement Parameter

IC50

Unit

µM

260/467

2018-05-14 08:43:54

Quantitative value

276

Measurement pX

3.56

Patent; UNIVERSITY OF UTAH RESEARCH FOUNDATION; WO2007/136707; (2007); (A2) English, View in Reaxys 566 of 1220 Substance Effect

Antiproliferative

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Target : TF-1 (CD34+ erythroleukemic cell line) cells stimulated with interleukin-5 (IL5)Bioassay : 5. Example 5: A Cell Based Screening Assay For Identifying Inhibitors ofEosinophil Proliferation244. The purpose of this study was to identify potential drug candidates for asthma. Eosinophils are white blood cells which contribute to the pathology of asthma. Lidocaine inhibits interleukin-5 (IL-5)

Substance RN

3917968View in Reaxys

Substance Name

178204

Measurement Parameter

IC50

Unit

µM

Quantitative value

Measurement pX

4.08

Patent; UNIVERSITY OF UTAH RESEARCH FOUNDATION; WO2007/136707; (2007); (A2) English, View in Reaxys 567 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

LD 50: 131 mg/kg, i.p., (male Swiss Webster mice)

Measurement Parameter

qualitative

Vidrio; Mena; Hong; Arzneimittel-Forschung/Drug Research; vol. 30; nb. 1; (1980); p. 12 - 17, View in Reaxys 568 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

local anesthetic (guinea pigs, ED 50: 0.31percent) and cardiac membrane stabilizing effect (in isolated guinea pigs left atria, ED 40: 0.013 mg/ml)

Measurement Parameter

qualitative

Aisaka; Hidaka; Inomata; Hamasaki; Ishihara; Morita; Arzneimittel-Forschung/Drug Research; vol. 35; nb. 8; (1985); p. 1239 - 1245, View in Reaxys 569 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

decreasing effect on force of contraction of guinea-pig left atria and papillary muscles, EC 50 256.1 (pH 7.4), 104.8 (pH 9) and 76.2 (pH 7.4), 56.0 μmol/l (pH 9), respectively

Measurement Parameter

qualitative

Schlieper; Arzneimittel-Forschung/Drug Research; vol. 34; nb. 7; (1984); p. 759 - 761, View in Reaxys 570 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

261/467

2018-05-14 08:43:54

Substance Name

178204

Qualitative Results

effects on tracheal ciliary movement in unanesthetized pigeons at 0.3 and 3.0 mg/kg i.v.

Measurement Parameter

qualitative

Fukuda; Saito; Yoshidomi; Ito; Arzneimittel-Forschung/Drug Research; vol. 34; nb. 7; (1984); p. 816 - 818, View in Reaxys 571 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

local-anaesthetic activity (g/percent), EC 50: 0.075, EC 100: 0.15 (3.9 min, i.c., guinea pig)

Measurement Parameter

qualitative

May, H. J.; Kretzschmar, R.; Neumann, W.; Gries, J.; Arzneimittel Forschung; vol. 30; nb. 9; (1980); p. 1486 - 1493, View in Reaxys 572 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

dose-dependent inhib. of proliferation of human keratinocytes (HaCaT cell line)

Measurement Parameter

qualitative

Haupenthal; Moll; Pharmazie; vol. 53; nb. 10; (1998); p. 690 - 694, View in Reaxys 573 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

effect on transmembrane action potentials in isolated cardiac cells

Measurement Parameter

qualitative

Librowski, Tomasz; Filipek, Barbara; Czarnecki, Ryszard; Beresewicz; Karwatowska-Prokopczuk; Acta Poloniae Pharmaceutica - Drug Research; vol. 55; nb. 3; (1998); p. 243 - 247, View in Reaxys 574 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

CNS toxicity (dogs, iv, cum dose 0.27 +/- 0.15)

Measurement Parameter

qualitative

Tenthorey; Ronfeld; Feldman; Sandberg; McMaster; Smith; Journal of Medicinal Chemistry; vol. 24; nb. 1; (1981); p. 47 53, View in Reaxys 575 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

antiarrhythmic activity (ED50 for protection, sc, mice)

Measurement Parameter

qualitative

McMaster; Byrnes; Block; Tenthorey; Journal of Medicinal Chemistry; vol. 24; nb. 1; (1981); p. 53 - 58, View in Reaxys 576 of 1220 Target Name Target Synonyms

Natriuretic peptide (IPR:IPR000663) natriuretic peptide (ipr:ipr000663)

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Target, Subunit, Species

Natriuretic peptide (IPR:IPR000663)

Target Mutant/Chimera Details

Natriuretic peptide (IPR:IPR000663):Wild

Target Transfection

Non Transfected

Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : atrial natriuretic peptide releasingBioassay : further investigations on mechanism of action by measuring electrocardiography, ventricular and aortic pressures, cardiac output, plasma and urine Na(+) and K(+) conc. dogs (24 kg) fasted 23 h prior to study; atrial natriuretic peptides (ANP) in plasma and urine measured 5 min after title comp. administration; long-acting ANP (LANP), vessel dilator, and atrial natriuretic factor (ANF) monitored by radioimmunoassay

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Route of Adm.

intravenous administration

Qualitative Results

title comp. raised plasma LANP and ANF, increased urinary LANP and ANF; no change in plasma or urine vessel dilator observed (table, diagram); by mechanisms other than cardiodepression and/or vasodilation

Measurement Parameter

qualitative

Wyeth, Richard P.; Soulsby, Michael E.; Vesely, David L.; Kennedy, Richard H.; Life Sciences; vol. 60; nb. 7; (1997); p. 473 - 477, View in Reaxys 577 of 1220 Substance Effect

Anaesthesic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Bioassay : incubation of cells in media containing title comp. at 37 deg C for 15 min; influx of <14C>lidocaine: incubation with PBS containing 10.5 mM title comp. and 1.85 MBq/ml 14C comp. for 30 s, 5, 15, 30, or 60 min at 37 deg C change in shape of human red blood cells observed by scanning electron microscopy; radio ligand assay; radioactivity measured by scintillation counter

Biological Species/NCBI ID

human

Cells/Cell Lines

erythrocyte

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

title comp. induced reversible transformation from discocytes to stomatocytes; change in shape depends on title comp. concn. and incubation period; influx of 22Na decreased with increasing concn. of title comp.

Measurement Parameter

qualitative

Nishiguchi; Hamada; Shindo; European Journal of Pharmacology; vol. 286; nb. 1; (1995); p. 1 - 8, View in Reaxys 578 of 1220 Target Name

voltage-gated sodium channel [guinea pig]

Target Synonyms

voltage-gated sodium channel

Target, Subunit, Species

voltage-gated sodium channel [guinea pig]

Target Mutant/Chimera Details

voltage-gated sodium channel [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Binding

263/467

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Biological Species/NCBI ID

Hartley guinea pig

Organs/Tissues

brain cortex

Cell Fraction

Membrane: vesicle

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Measurement Parameter

IC50

Unit

µM

Quantitative value

240

Measurement pX

3.62

Concomitants: Compound RN

24140929; 78875; 24144495

Concomitants: Compound name

Tetrodotoxin; Veratridine; [3H]-BTX-B; Scorpion venom (Leiurus quinquestriatus)

Concomitants: Compound role

COM; NSB; RAD; COM

579 of 1220 Target Name

voltage-gated sodium channel [guinea pig]

Target Synonyms

voltage-gated sodium channel

Target, Subunit, Species

voltage-gated sodium channel [guinea pig]

Target Mutant/Chimera Details

voltage-gated sodium channel [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Binding

Biological Species/NCBI ID

Hartley guinea pig

Organs/Tissues

brain cortex

Cell Fraction

Membrane: vesicle

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

10 µM

Measurement Parameter

% Inhibition

Unit

Quantitative value

9.8

Deviation

1.10000

Measurement pX

Concomitants: Compound RN

24140929; 78875; 24144495

Concomitants: Compound name

Tetrodotoxin; Veratridine; [3H]-BTX-B; Scorpion venom (Leiurus quinquestriatus)

Concomitants: Compound role

COM; NSB; RAD; COM

580 of 1220 Target Name Target Synonyms

voltage-gated sodium channel [guinea pig] voltage-gated sodium channel

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Target, Subunit, Species

voltage-gated sodium channel [guinea pig]

Target Mutant/Chimera Details

voltage-gated sodium channel [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Binding

Biological Species/NCBI ID

Hartley guinea pig

Organs/Tissues

brain cortex

Cell Fraction

Membrane: vesicle

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

100 µM

Measurement Parameter

% Inhibition

Unit

Quantitative value

31.4

Deviation

4.70000

Measurement pX

3.66

Concomitants: Compound RN

24140929; 78875; 24144495

Concomitants: Compound name

Tetrodotoxin; Veratridine; [3H]-BTX-B; Scorpion venom (Leiurus quinquestriatus)

Concomitants: Compound role

COM; NSB; RAD; COM

581 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

50 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 [lambda1]

Unit

minute

Quantitative value

10.4

Deviation

11.0500

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 582 of 1220 Bioassay Category Bioassay Name

Pharmacokinetic Pharmacokinetic

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Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

100 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 [lambda1]

Unit

minute

Quantitative value

12.57

Deviation

8.55000

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 583 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

50 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

minute

Quantitative value

49.33

Deviation

25.7900

Metabolite RN

2417108

Metabolite name

Norlidocaine

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 584 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

100 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

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Unit

minute

Quantitative value

Deviation

31.1900

Metabolite RN

2417108

Metabolite name

Norlidocaine

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 585 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

100 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

minute

Quantitative value

106.27

Deviation

62.3500

Metabolite RN

2417108

Metabolite name

Norlidocaine

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 586 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

50 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

minute

Quantitative value

127.73

Deviation

89.9300

Metabolite RN

2417108

Metabolite name

Norlidocaine

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys

267/467

2018-05-14 08:43:54

587 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

50 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

CL (drug clearance)

Unit

mL/min/kg

Quantitative value

15.53

Deviation

1.90000

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 588 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

100 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

CL (drug clearance)

Unit

mL/min/kg

Quantitative value

15.73

Deviation

2.11000

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 589 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

100 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Vc (central volume of distribution)

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Unit

L/kg

Quantitative value

0.9

Deviation

0.680000

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 590 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

50 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Vc (central volume of distribution)

Unit

L/kg

Quantitative value

1.15

Deviation

1.22000

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 591 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

50 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Vd (volume of distribution)

Unit

L/kg

Quantitative value

2.73

Deviation

1.60000

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 592 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

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Substance Dose

100 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Vd (volume of distribution)

Unit

L/kg

Quantitative value

2.52

Deviation

1.66000

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 593 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

100 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Vdss

Unit

L/kg

Quantitative value

Deviation

1.43000

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 594 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride

Substance Dose

50 mg

Substance Route of Adm.

intravenous administration

Substance Dosing Regimen

Single

Measurement Parameter

Vdss

Unit

L/kg

Quantitative value

2.4

Deviation

1.63000

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 595 of 1220 Bioassay Category Bioassay Name

Pharmacokinetic Pharmacokinetic

270/467

2018-05-14 08:43:54

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride monohydrate

Substance Dose

100 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

tmax

Unit

minute

Quantitative value

37.5

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 596 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride monohydrate

Substance Dose

300 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

tmax

Unit

minute

Quantitative value

37.5

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 597 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride monohydrate

Substance Dose

500 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

tmax

Unit

minute

Quantitative value

37.5

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys

271/467

2018-05-14 08:43:54

598 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride monohydrate

Substance Dose

500 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

F (drug bioavailability)

Unit

Quantitative value

30.2

Deviation

11.7000

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 599 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride monohydrate

Substance Dose

300 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

F (drug bioavailability)

Unit

Quantitative value

31.3

Deviation

13.9000

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 600 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride monohydrate

Substance Dose

100 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

F (drug bioavailability)

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Unit

Quantitative value

29.4

Deviation

7.30000

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 601 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride monohydrate

Substance Dose

500 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

tlag

Unit

minute

Quantitative value

11.38

Deviation

4.17000

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 602 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride monohydrate

Substance Dose

300 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

tlag

Unit

minute

Quantitative value

13.3

Deviation

4.37000

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 603 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride monohydrate

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Substance Dose

100 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

tlag

Unit

minute

Quantitative value

14.77

Deviation

5.08000

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 604 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride monohydrate

Substance Dose

500 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 abs

Unit

minute

Quantitative value

20.98

Deviation

17.6300

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 605 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride monohydrate

Substance Dose

300 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 abs

Unit

minute

Quantitative value

36.53

Deviation

25.1400

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 606 of 1220 Bioassay Category Bioassay Name

Pharmacokinetic Pharmacokinetic

274/467

2018-05-14 08:43:54

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride monohydrate

Substance Dose

100 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 abs

Unit

minute

Quantitative value

13.76

Deviation

9.02000

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 607 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride monohydrate

Substance Dose

100 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-inf)

Unit

mg.min/L

Quantitative value

76.1

Deviation

24.6000

Metabolite RN

2417108

Metabolite name

Norlidocaine

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 608 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride monohydrate

Substance Dose

100 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-inf)

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Unit

mg.min/L

Quantitative value

33.9

Deviation

8.30000

Metabolite RN

2417108

Metabolite name

Norlidocaine

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 609 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride monohydrate

Substance Dose

300 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Repeated

Measurement Parameter

AUC (0-8 h)

Unit

mg.min/L

Quantitative value

94.1

Deviation

47.9000

Metabolite RN

2417108

Metabolite name

Norlidocaine

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 610 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride monohydrate

Substance Dose

300 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Repeated

Measurement Parameter

AUC (0-8 h)

Unit

mg.min/L

Quantitative value

36.1

Deviation

9.10000

Metabolite RN

2417108

Metabolite name

Norlidocaine

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys

276/467

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611 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride monohydrate

Substance Dose

300 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Repeated

Measurement Parameter

Cavg ss

Unit

mg/L

Quantitative value

0.0752

Metabolite RN

2417108

Metabolite name

Norlidocaine

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 612 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine hydrochloride monohydrate

Substance Dose

300 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Repeated

Measurement Parameter

Cavg ss

Unit

mg/L

Quantitative value

0.196

Metabolite RN

2417108

Metabolite name

Norlidocaine

Bennett; Aarons; Bending; Steiner; Rowland; Journal of Pharmacokinetics and Biopharmaceutics; vol. 10; nb. 3; (1982); p. 265 - 281, View in Reaxys 613 of 1220 Target Name

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Synonyms

anktm1; ankyrin-like with transmembrane domains protein 1; transient receptor potential cation channel subfamily a member 1; trpa1

Target Uniprot ID

q6ri86

Target, Subunit, Species

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

277/467

2018-05-14 08:43:54

Substance Action on Target

Activator

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

substantia nigra

Cells/Cell Lines

nerve cell

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

5 mM

Measurement Parameter

stimulation percentage

Unit

Measurement Object

frequency of EPSC

Quantitative value

132

Measurement pX

3.58

614 of 1220 Target Name

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Synonyms

anktm1; ankyrin-like with transmembrane domains protein 1; transient receptor potential cation channel subfamily a member 1; trpa1

Target Uniprot ID

q6ri86

Target, Subunit, Species

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Substance Action on Target

Activator

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

substantia nigra

Cells/Cell Lines

nerve cell

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

5 mM

Measurement Parameter

stimulation percentage

Unit

Measurement Object

amplitude of EPSP

Quantitative value

Measurement pX

615 of 1220 Target Name

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Synonyms

anktm1; ankyrin-like with transmembrane domains protein 1; transient receptor potential cation channel subfamily a member 1; trpa1

Target Uniprot ID

q6ri86

278/467

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Target, Subunit, Species

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Substance Action on Target

Activator

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

substantia nigra

Cells/Cell Lines

nerve cell

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

5 mM

Measurement Parameter

stimulation percentage

Unit

Measurement Object

frequency of EPSC

Quantitative value

206

Measurement pX

3.58

616 of 1220 Target Name

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Synonyms

anktm1; ankyrin-like with transmembrane domains protein 1; transient receptor potential cation channel subfamily a member 1; trpa1

Target Uniprot ID

q6ri86

Target, Subunit, Species

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Substance Action on Target

Activator

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

substantia nigra

Cells/Cell Lines

nerve cell

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

5 mM

Measurement Parameter

stimulation percentage

Unit

Measurement Object

amplitude of EPSP

279/467

2018-05-14 08:43:54

Quantitative value

Measurement pX

617 of 1220 Target Name

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Synonyms

anktm1; ankyrin-like with transmembrane domains protein 1; transient receptor potential cation channel subfamily a member 1; trpa1

Target Uniprot ID

q6ri86

Target, Subunit, Species

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Substance Action on Target

Activator

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

substantia nigra

Cells/Cell Lines

nerve cell

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

5 mM

Measurement Parameter

stimulation percentage

Unit

Measurement Object

frequency of EPSC

Quantitative value

226

Measurement pX

3.58

618 of 1220 Target Name

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Synonyms

anktm1; ankyrin-like with transmembrane domains protein 1; transient receptor potential cation channel subfamily a member 1; trpa1

Target Uniprot ID

q6ri86

Target, Subunit, Species

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Substance Action on Target

Activator

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

substantia nigra

Cells/Cell Lines

nerve cell

280/467

2018-05-14 08:43:54

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

5 mM

Measurement Parameter

stimulation percentage

Unit

Measurement Object

amplitude of EPSP

Quantitative value

Measurement pX

619 of 1220 Target Name

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Synonyms

anktm1; ankyrin-like with transmembrane domains protein 1; transient receptor potential cation channel subfamily a member 1; trpa1

Target Uniprot ID

q6ri86

Target, Subunit, Species

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Substance Action on Target

Activator

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

substantia nigra

Cells/Cell Lines

nerve cell

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

5 mM

Measurement Parameter

stimulation percentage

Unit

Measurement Object

frequency of EPSC

Quantitative value

152

Measurement pX

3.58

Concomitants: Compound RN

24140929

Concomitants: Compound name

Tetrodotoxin

Concomitants: Compound role

COM

620 of 1220 Target Name

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Synonyms

anktm1; ankyrin-like with transmembrane domains protein 1; transient receptor potential cation channel subfamily a member 1; trpa1

Target Uniprot ID

q6ri86

Target, Subunit, Species

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

281/467

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Target Mutant/Chimera Details

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Substance Action on Target

Activator

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

substantia nigra

Cells/Cell Lines

nerve cell

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

5 mM

Measurement Parameter

stimulation percentage

Unit

Measurement Object

amplitude of EPSP

Quantitative value

Measurement pX

Concomitants: Compound RN

24140929

Concomitants: Compound name

Tetrodotoxin

Concomitants: Compound role

COM

621 of 1220 Target Name

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Synonyms

anktm1; ankyrin-like with transmembrane domains protein 1; transient receptor potential cation channel subfamily a member 1; trpa1

Target Uniprot ID

q6ri86

Target, Subunit, Species

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Substance Action on Target

Activator

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

substantia nigra

Cells/Cell Lines

cells

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

282/467

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Substance Dose

5 mM

Measurement Parameter

stimulation percentage

Unit

Measurement Object

frequency of EPSC

Quantitative value

145

Measurement pX

3.58

Concomitants: Compound RN

7047754

Concomitants: Compound name

Capsazepine

Concomitants: Compound role

IND

622 of 1220 Target Name

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Synonyms

anktm1; ankyrin-like with transmembrane domains protein 1; transient receptor potential cation channel subfamily a member 1; trpa1

Target Uniprot ID

q6ri86

Target, Subunit, Species

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Substance Action on Target

Activator

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

substantia nigra

Cells/Cell Lines

cells

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

5 mM

Measurement Parameter

stimulation percentage

Unit

Measurement Object

amplitude of EPSP

Quantitative value

Measurement pX

Concomitants: Compound RN

7047754

Concomitants: Compound name

Capsazepine

Concomitants: Compound role

IND

623 of 1220 Target Name Target Synonyms

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus] anktm1; ankyrin-like with transmembrane domains protein 1; transient receptor potential cation channel subfamily a member 1; trpa1

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Target Uniprot ID

q6ri86

Target, Subunit, Species

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Substance Action on Target

Activator

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

substantia nigra

Cells/Cell Lines

cells

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

5 mM

Measurement Parameter

stimulation percentage

Unit

Measurement Object

frequency of EPSC

Quantitative value

Measurement pX

Concomitants: Compound RN

24146002

Concomitants: Compound name

Ruthenium red

Concomitants: Compound role

IND

624 of 1220 Target Name

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Synonyms

anktm1; ankyrin-like with transmembrane domains protein 1; transient receptor potential cation channel subfamily a member 1; trpa1

Target Uniprot ID

q6ri86

Target, Subunit, Species

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Substance Action on Target

Activator

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

substantia nigra

Cells/Cell Lines

cells

284/467

2018-05-14 08:43:54

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

5 mM

Measurement Parameter

stimulation percentage

Unit

Measurement Object

amplitude of EPSP

Quantitative value

-6

Measurement pX

Concomitants: Compound RN

24146002

Concomitants: Compound name

Ruthenium red

Concomitants: Compound role

IND

625 of 1220 Target Name

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Synonyms

anktm1; ankyrin-like with transmembrane domains protein 1; transient receptor potential cation channel subfamily a member 1; trpa1

Target Uniprot ID

q6ri86

Target, Subunit, Species

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Substance Action on Target

Activator

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

substantia nigra

Cells/Cell Lines

nerve cell

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

5 mM

Measurement Parameter

Frequency

Unit

Measurement Object

frequency of EPSC

Quantitative value

13.7

Deviation

0.300000

626 of 1220 Target Name

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Synonyms

anktm1; ankyrin-like with transmembrane domains protein 1; transient receptor potential cation channel subfamily a member 1; trpa1

Target Uniprot ID

q6ri86

Target, Subunit, Species

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

285/467

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Target Mutant/Chimera Details

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Substance Action on Target

Activator

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

substantia nigra

Cells/Cell Lines

nerve cell

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

2 mM

Measurement Parameter

Frequency

Unit

Measurement Object

frequency of EPSC

Quantitative value

Deviation

0.800000

627 of 1220 Target Name

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Synonyms

anktm1; ankyrin-like with transmembrane domains protein 1; transient receptor potential cation channel subfamily a member 1; trpa1

Target Uniprot ID

q6ri86

Target, Subunit, Species

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Substance Action on Target

Activator

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

substantia nigra

Cells/Cell Lines

nerve cell

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

1 mM

Measurement Parameter

Frequency

Unit

Measurement Object

frequency of EPSC

Quantitative value

14.1

286/467

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Deviation 628 of 1220 Target Name

1 Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Synonyms

anktm1; ankyrin-like with transmembrane domains protein 1; transient receptor potential cation channel subfamily a member 1; trpa1

Target Uniprot ID

q6ri86

Target, Subunit, Species

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Substance Action on Target

Activator

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

substantia nigra

Cells/Cell Lines

nerve cell

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

5 mM

Measurement Parameter

Current

Unit

Measurement Object

amplitude of EPSP

Quantitative value

13.9

Deviation

1.60000

629 of 1220 Target Name

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Synonyms

anktm1; ankyrin-like with transmembrane domains protein 1; transient receptor potential cation channel subfamily a member 1; trpa1

Target Uniprot ID

q6ri86

Target, Subunit, Species

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Substance Action on Target

Activator

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

substantia nigra

Cells/Cell Lines

nerve cell

Substance RN

3917968View in Reaxys

287/467

2018-05-14 08:43:54

Substance Name

lidocaine

Substance Dose

1 mM

Measurement Parameter

Current

Unit

Measurement Object

amplitude of EPSP

Quantitative value

13.6

Deviation

1.90000

630 of 1220 Target Name

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Synonyms

anktm1; ankyrin-like with transmembrane domains protein 1; transient receptor potential cation channel subfamily a member 1; trpa1

Target Uniprot ID

q6ri86

Target, Subunit, Species

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Substance Action on Target

Activator

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

substantia nigra

Cells/Cell Lines

nerve cell

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

2 mM

Measurement Parameter

Current

Unit

Measurement Object

amplitude of EPSP

Quantitative value

12.9

Deviation

2.10000

631 of 1220 Target Name

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Synonyms

anktm1; ankyrin-like with transmembrane domains protein 1; transient receptor potential cation channel subfamily a member 1; trpa1

Target Uniprot ID

q6ri86

Target, Subunit, Species

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Substance Action on Target

Activator

Bioassay Category

In Vitro (Efficacy)

288/467

2018-05-14 08:43:54

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

substantia nigra

Cells/Cell Lines

nerve cell

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

5 mM

Measurement Parameter

Frequency

Unit

Measurement Object

frequency of EPSC

Quantitative value

12.6

Deviation

632 of 1220 Target Name

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Synonyms

anktm1; ankyrin-like with transmembrane domains protein 1; transient receptor potential cation channel subfamily a member 1; trpa1

Target Uniprot ID

q6ri86

Target, Subunit, Species

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Transient receptor potential cation channel subfamily A member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Substance Action on Target

Activator

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

substantia nigra

Cells/Cell Lines

nerve cell

Substance RN

3917968View in Reaxys

Substance Name

lidocaine

Substance Dose

5 mM

Measurement Parameter

Current

Unit

Measurement Object

amplitude of EPSP

Quantitative value

12.7

Deviation

1.90000

633 of 1220 Target Name

voltage-gated sodium channel [Mus musculus]

Target Synonyms

voltage-gated sodium channel

Target, Subunit, Species

voltage-gated sodium channel [Mus musculus]

Target Mutant/Chimera Details

voltage-gated sodium channel [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

289/467

2018-05-14 08:43:54

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Organ contraction

Biological Species/NCBI ID

Mus musculus

Organs/Tissues

extensor digitorum longus muscle

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

5 g/L

Measurement Parameter

number

Measurement Object

Mean number of stimuli

Quantitative value

245

Deviation

Concomitants: Compound RN

3898737

Concomitants: Compound name

Tubocurarine

Concomitants: Compound role

COM

634 of 1220 Target Name

voltage-gated sodium channel [Mus musculus]

Target Synonyms

voltage-gated sodium channel

Target, Subunit, Species

voltage-gated sodium channel [Mus musculus]

Target Mutant/Chimera Details

voltage-gated sodium channel [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Organ contraction

Biological Species/NCBI ID

Mus musculus

Organs/Tissues

extensor digitorum longus muscle

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

10 g/L

Measurement Parameter

number

Measurement Object

Mean number of stimuli

Quantitative value

240

Deviation

Concomitants: Compound RN

3898737

Concomitants: Compound name

Tubocurarine

Concomitants: Compound role

COM

635 of 1220 Target Name

voltage-gated sodium channel [Mus musculus]

290/467

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Target Synonyms

voltage-gated sodium channel

Target, Subunit, Species

voltage-gated sodium channel [Mus musculus]

Target Mutant/Chimera Details

voltage-gated sodium channel [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Organ contraction

Biological Species/NCBI ID

Mus musculus

Organs/Tissues

extensor digitorum longus muscle

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

2.50000 g/L

Measurement Parameter

number

Measurement Object

Mean number of stimuli

Quantitative value

Deviation

Concomitants: Compound RN

3898737

Concomitants: Compound name

Tubocurarine

Concomitants: Compound role

COM

636 of 1220 Target Name

Cytochrome P450 2D6 [human]

Target Synonyms

cholesterol 25-hydroxylase; cyp2d6; cyp2dl1; cypiid6; cytochrome p450 2d6; cytochrome p450db1; debrisoquine 4-hydroxylase

Target Uniprot ID

p10635

Target PDB ID

2f9q; 3qm4; 3tbg; 3tda; 4wnt; 4wnu; 4wnv; 4wnw; 4xry; 4xrz; 5tft; 5tfu

Target, Subunit, Species

Cytochrome P450 2D6 [human]

Target Mutant/Chimera Details

Cytochrome P450 2D6 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology inhibition

Cell Fraction

Membrane

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

0.0230000 µM

Measurement Parameter

IC50

Unit

µM

Qualitative value

Quantitative value

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Measurement pX

Metabolite RN

22541978

Metabolite name

AHMC

Concomitants: Compound RN

741857; 11841397; 77911

Concomitants: Compound name

Acetonitrile; 3-[2-(N,N-diethyl-N-methylamino]-ethyl)-7-Methoxy-4-methylcoumarin; NADPH

Concomitants: Compound role

SLV; SUB; COE

637 of 1220 Target Name

Cytochrome P450 2D6 [human]

Target Synonyms

cholesterol 25-hydroxylase; cyp2d6; cyp2dl1; cypiid6; cytochrome p450 2d6; cytochrome p450db1; debrisoquine 4-hydroxylase

Target Uniprot ID

p10635

Target PDB ID

2f9q; 3qm4; 3tbg; 3tda; 4wnt; 4wnu; 4wnv; 4wnw; 4xry; 4xrz; 5tft; 5tfu

Target, Subunit, Species

Cytochrome P450 2D6 [human]

Target Mutant/Chimera Details

Cytochrome P450 2D6 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Cell Fraction

Membrane

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

1 µM

Measurement Parameter

CLint

Unit

µL/min/pmol target

Measurement Object

ALL

Qualitative value

Quantitative value

0.2

Concomitants: Compound RN

741857; 77911

Concomitants: Compound name

Acetonitrile; NADPH

Concomitants: Compound role

SLV; COE

638 of 1220 Target Name

Acetylcholine receptor subunit alpha [Mus musculus];+Acetylcholine receptor subunit delta [Mus musculus];+Acetylcholine receptor subunit epsilon [Mus musculus];+Acetylcholine receptor subunit beta [Mus musculus]

Target Synonyms

acetylcholine receptor subunit alpha; acra; chrna1 + acetylcholine receptor subunit delta; acrd; chrnd + acetylcholine receptor subunit epsilon; acre; chrne + acetylcholine receptor subunit beta; acrb; chrnb1

Target Uniprot ID

p04756 + p02716 + p20782 + p09690

Target PDB ID

2qc1; 5hbv

Target, Subunit, Species

Acetylcholine receptor subunit alpha [Mus musculus]; Acetylcholine receptor subunit beta [Mus musculus]; Acetylcholine receptor subunit delta [Mus musculus]; Acetylcholine receptor subunit epsilon [Mus musculus]

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Target Mutant/Chimera Details

Acetylcholine receptor subunit alpha [Mus musculus]:Wild + Acetylcholine receptor subunit delta [Mus musculus]:Wild + Acetylcholine receptor subunit epsilon [Mus musculus]:Wild + Acetylcholine receptor subunit beta [Mus musculus]:Wild

Target Species (Bioactivity)

Mus musculus

Target Transfection

Transfected

Substance Action on Target

Antagonist

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Cells/Cell Lines

HEK293 cell line

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Measurement Parameter

IC50

Unit

µM

Quantitative value

11.1

Measurement pX

4.95

Concomitants: Compound RN

1764436

Concomitants: Compound name

Acetylcholine

Concomitants: Compound role

AGO

639 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

first-pass clearance in healthy volunteers and epileptic patients compared

Measurement Parameter

qualitative

Colburn; Journal of Pharmaceutical Sciences; vol. 70; nb. 8; (1981); p. 969 - 971, View in Reaxys 640 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

increases the calcium-induced contractions of chick oesophagus

Measurement Parameter

qualitative

Mishra; Raviprakash; Journal of Pharmacy and Pharmacology; vol. 32; nb. 10; (1980); p. 716 - 717, View in Reaxys 641 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

reduced the positive chronotropic response without markedly altering the basal rate (rat)

Measurement Parameter

qualitative

Algate; Rashid; Waterfall; Journal of Pharmacy and Pharmacology; vol. 33; nb. 4; (1981); p. 236 - 239, View in Reaxys 642 of 1220 Bioassay Category

In Vitro (Efficacy)

293/467

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Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

growth inhibition of Saccharomyces cerevisiae (IC50 = 100 mg/l) (alternative test method of acute toxicity)

Measurement Parameter

qualitative

Koch; Pharmazie; vol. 47; nb. 7; (1992); p. 531 - 537, View in Reaxys 643 of 1220 Substance Effect

Dopaminergic

Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Bioassay : levels of dopamine (DA) and its metabolites 3-methoxytyramine (3-MT) and dihydroxyphenylacetic acid (DOPAC) in the striatum (STR), nucleus accumbens (NAcc) and prefrontal cortex PFC) rats weighing 185 to 310 g; food and water ad libitum; 12 h light-dark cycle; sacrificed; time course study; reverse-phase HPLC with electrochemical detection and gas chromatographymass spectrometry

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

223 µmol/kg

Substance Route of Adm.

intraperitoneal administration

Measurement Parameter

qualitative

Qualitative value

Measurement pX

Graham III; Maher; Robinson; Journal of Pharmacology and Experimental Therapeutics; vol. 274; nb. 2; (1995); p. 707 - 717, View in Reaxys 644 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : cAMP accumulation; induction ofTarget : bovine tracheal smooth muscle segmentBioassay : further invest.: salbutamol/forskolin added after title comp. for 10 min; IBMX: 3-isobutyl-1methylxanthine muscle exposed to methacholine and IBMX (15 min), then to title comp. (15 min); cAMP content determined by radioimmunoassay kit

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

100 µM

Qualitative Results

title comp. sign. increased basal and salbutamol-/forskolin-induced cAMP accumulation (figure)

Measurement Parameter

qualitative

Nakahara, Tsutomu; Yunoki, Motonari; Moriuchi, Hiroshi; Sakamato, Kenji; Ishii, Kunio; Naunyn-Schmiedeberg's Archives of Pharmacology; vol. 361; nb. 6; (2000); p. 605 - 609, View in Reaxys 645 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : |drug interaction Target : bovine tracheal smooth muscle segmentBioassay : IBMX: 3-isobutyl-1-methylxanthine muscle tension recorded isometrically; after precontraction with methacholine title comp. added for 15 min, then salbutamol/forskolin/IBMX/diltiazem added cumulatively

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

10 µM

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Qualitative Results

100 μmol/l of title comp. sign. shifted conc.-response curves to left for salbutamol, forskolin, IBMX and had no effect on diltiazem curve (figure); 10 μmol/l of title comp. had no effect

Measurement Parameter

qualitative

Myorelaxant

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Target : bovine tracheal smooth muscle segmentBioassay : muscle tension recorded isometrically; effect of title comp. on tension developed by 0.3 μmol/l methacholine examined

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

3 µM

Measurement Parameter

IC50

Unit

µM

Quantitative value

210

Measurement pX

3.68

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : |drug interaction Bioassay : right hindlimbs served as controls; title comp. alone and dextromethorphan used as reference comp.; AUC: areas under the curves title comp. with dextromethorphan (at dose of ED50) injected into sciatic notch of the left hindlimbs; evaluations of motor function, proprioception and nociception performed; time courses of effects constructed; AUCs obtained

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

title comp. with dextromethorphan produced an additive effect on the sciatic nerve blockades

Measurement Parameter

qualitative

Hou, Chia-Hui; Tzeng, Jann-Inn; Chen, Yu-Wen; Lin, Ching-Nan; Lin, Mao-Tsun; Tu, Chieh-Hsien; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 544; nb. 1-3; (2006); p. 10 - 16, View in Reaxys 648 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : |drug interaction Bioassay : right hindlimbs served as controls; title comp. alone and dextrorphan used as reference comp.; AUC: areas under the curves title comp. with dextrorphan (at dose of ED50) injected into sciatic notch of the left hindlimbs; evaluations of motor function, proprioception and nociception conducted; time courses of effects constructed; AUCs obtained

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

title comp. with dextrorphan produced an additive effect on the sciatic nerve blockades

Measurement Parameter

qualitative

Hou, Chia-Hui; Tzeng, Jann-Inn; Chen, Yu-Wen; Lin, Ching-Nan; Lin, Mao-Tsun; Tu, Chieh-Hsien; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 544; nb. 1-3; (2006); p. 10 - 16, View in Reaxys

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649 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : |drug interaction Bioassay : right hindlimbs served as controls; title comp. alone and 3-methoxymorphinan used as reference comp.; AUC: areas under the curves title comp. with 3-methoxymorphinan (at the dose of ED50) injected into sciatic notch of the left hindlimbs; evaluations of motor function, proprioception and nociception conducted; time courses of effects constructed; AUCs obtained

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

title comp. with 3-methoxymorphinan produced an additive effect on the sciatic nerve blockades

Measurement Parameter

qualitative

Clastogenic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Target : Syrian hamster embryo cellsBioassay : control: without title comp.; PBS(-): Ca(2+)-and Mg(2+)-free phosphate-buffered saline 5E5 cells treated with different conc. of title comp. for 24 h; 3 h before harvest colcemid (0.2 μg/ml) administered; harvested with 0.1 percent trypsin; chromosome aberrations and mitotic index determined

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

370 µM

Qualitative Results

title comp. failed to induce chromosome aberrations in cells and decreased mitotic indices in concentration-dependent manner; table

Measurement Parameter

qualitative

Hagiwara, Makoto; Watanabe, Eiko; Barrett, J. Carl; Tsutsui, Takeki; Mutation Research - Genetic Toxicology and Environmental Mutagenesis; vol. 603; nb. 2; (2006); p. 111 - 120, View in Reaxys 651 of 1220 Substance Effect

Clastogenic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Target : Syrian hamster embryo cellsBioassay : control: without title comp.; PMS: rat liver postmitochondrial supernatant; PBS(-): Ca (2+)-and Mg(2+)-free phosphate-buffered saline 5E5 cells treated with title comp. for 3 h in 5 percent PMS mixture; washed twice with PBS(-) and incubated with fresh medium for 21 h; chromosome aberrations and mitotic index determined

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

111 µM

Qualitative Results

title comp. had little effect on mitotic indices and chromosome aberrations; table

Measurement Parameter

qualitative

Cytotoxic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Target : Syrian hamster embryo cellsBioassay : control: without title comp.; PBS(-): Ca(2+)-and Mg(2+)-free phosphate-buffered saline 5E5 cells treated with different conc. of title comp. for 24 h;

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after harvesting with 0.1 percent trypsin cells replated and incubated for 7 d; cytotoxicity determined by colony forming efficiency Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

370 µM

Qualitative Results

colony-forming efficiency of cells decreased with increasing conc. of title comp.; control cells: 11.5 percent; table

Measurement Parameter

qualitative

Cytotoxic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Target : Syrian hamster embryo cellsBioassay : control: without title comp.; PMS: rat liver postmitochondrial supernatant; PBS(-): Ca (2+)-and Mg(2+)-free phosphate-buffered saline 5E5 cells treated with different conc. of title comp. for 3 h in 5 percent PMS mixture; cells washed twice with PBS(-) and incubated with fresh medium for 21 h; cytotoxicity determined by colony-forming efficiency

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

111 µM

Measurement Parameter

qualitative

Qualitative value

Measurement pX

Myorelaxant

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Target : pig coronary smooth muscleBioassay : artery strips were precontracted in Tyrode's soln. by 1E-5 - 2E-5 mol/l PGF2ω, addn. of 3E-5 mol/l tetrodotoxin and title comp., isometric tension was measured

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

1.00000E-06 M

Measurement Parameter

pIC50

Quantitative value

2.36

Measurement pX

2.36

Tanaka, Yoshio; Kamibayashi, Makoto; Yamashita, Yoko; Imai, Toshiyasu; Tanaka, Hikaru; Nakahara, Tsutomu; Ishii, Kunio; Shigenobu, Koki; Naunyn-Schmiedeberg's Archives of Pharmacology; vol. 365; nb. 1; (2002); p. 56 - 66, View in Reaxys 655 of 1220 Substance Effect

Myorelaxant

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Target : pig coronary smooth muscleBioassay : artery strips were precontracted in Tyrode's soln. by 80 mmol/l KCl, addn. of 20 mmol/l CaCl2 and title comp., isometric tension was measured

Substance RN

3917968View in Reaxys

Substance Name

178204

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Substance Dose

1.00000E-06 M

Measurement Parameter

pIC50

Quantitative value

2.28

Measurement pX

2.28

Myorelaxant

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Target : pig coronary smooth muscleBioassay : artery strips were precontracted in Tyrode's soln. by 80 mmol/l KCl, addn. of 3E-5 mol/l tetrodotoxin and title comp., isometric tension was measured

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

1.00000E-06 M

Measurement Parameter

pIC50

Quantitative value

2.71

Measurement pX

2.71

Myorelaxant

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Target : pig coronary smooth muscleBioassay : artery strips were precontracted in Tyrode's soln. by 30 - 80 mmol/l KCl; title comp. was added, isometric tension was measured

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

1.00000E-06 M

Measurement Parameter

pIC50

Quantitative value

2.62 - 2.85

Measurement pX

2.85

Anaesthesic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Bioassay : control: placebo prospective, single centre, randomised, double-blind phase III study; patients with sore throat received single title comp. dose during 2-h stationary phase and up to 6 lozenges per 24 h for 2 days; pain intensity det. on 100 mm Visual Analogue Scale

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

8 mg

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Qualitative Results

title comp. superior in pain relief, minimum pain intensity, meaningful pain relief and time of onset of meaningful pain relief than placebo; good tolerability and low number of adverse effects observed; fig.

Measurement Parameter

qualitative

Wonnemann, Meinolf; Helm, Ilka; Stauss-Grabo, Manuela; Roettger-Luer, Patricia; Tran, Cam-Tuan; Canenbley, Rainer; Donath, Frank; Nowak, Horst; Schug, Barbara S.; Blume, Henning H.; Arzneimittel-Forschung/Drug Research; vol. 57; nb. 11; (2007); p. 689 - 697, View in Reaxys 659 of 1220 Target Name

Transient receptor potential cation channel subfamily V member 1 [Rattus norvegicus]

Target Synonyms

capsaicin receptor; osm-9-like trp channel 1; otrpc1; transient receptor potential cation channel subfamily v member 1; trpv1; vanilloid receptor 1; vanilloid receptor type 1-like; vr1; vr1l

Target Uniprot ID

o35433

Target PDB ID

2nyj; 2pnn; 3j5p; 3j5q; 3j5r; 3j9j; 3sui; 5irx; 5irz; 5is0

Target, Subunit, Species

Transient receptor potential cation channel subfamily V member 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Transient receptor potential cation channel subfamily V member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Substance Action on Target

Antagonist

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Xenopus laevis

Cells/Cell Lines

oocyte

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

100 nM

Measurement Parameter

% Inhibition

Unit

Quantitative value

Measurement pX

Concomitants: Compound RN

2816484

Concomitants: Compound name

Capsaicin

Concomitants: Compound role

AGO

660 of 1220 Target Name

Transient receptor potential cation channel subfamily V member 1 [Rattus norvegicus]

Target Synonyms

capsaicin receptor; osm-9-like trp channel 1; otrpc1; transient receptor potential cation channel subfamily v member 1; trpv1; vanilloid receptor 1; vanilloid receptor type 1-like; vr1; vr1l

Target Uniprot ID

o35433

Target PDB ID

2nyj; 2pnn; 3j5p; 3j5q; 3j5r; 3j9j; 3sui; 5irx; 5irz; 5is0

Target, Subunit, Species

Transient receptor potential cation channel subfamily V member 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Transient receptor potential cation channel subfamily V member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Substance Action on Target

Antagonist

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Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Xenopus laevis

Cells/Cell Lines

oocyte

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

10 µM

Measurement Parameter

% Inhibition

Unit

Quantitative value

Measurement pX

5.37

Concomitants: Compound RN

2816484

Concomitants: Compound name

Capsaicin

Concomitants: Compound role

AGO

661 of 1220 Target Name

Transient receptor potential cation channel subfamily V member 1 [Rattus norvegicus]

Target Synonyms

capsaicin receptor; osm-9-like trp channel 1; otrpc1; transient receptor potential cation channel subfamily v member 1; trpv1; vanilloid receptor 1; vanilloid receptor type 1-like; vr1; vr1l

Target Uniprot ID

o35433

Target PDB ID

2nyj; 2pnn; 3j5p; 3j5q; 3j5r; 3j9j; 3sui; 5irx; 5irz; 5is0

Target, Subunit, Species

Transient receptor potential cation channel subfamily V member 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Transient receptor potential cation channel subfamily V member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Substance Action on Target

Antagonist

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Xenopus laevis

Cells/Cell Lines

oocyte

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Measurement Parameter

IC50

Unit

Quantitative value

Deviation

Measurement pX

7.09

Concomitants: Compound RN

2816484

Concomitants: Compound name

Capsaicin

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Concomitants: Compound role 662 of 1220 Target Name

AGO Transient receptor potential cation channel subfamily V member 1 [Rattus norvegicus]

Target Synonyms

capsaicin receptor; osm-9-like trp channel 1; otrpc1; transient receptor potential cation channel subfamily v member 1; trpv1; vanilloid receptor 1; vanilloid receptor type 1-like; vr1; vr1l

Target Uniprot ID

o35433

Target PDB ID

2nyj; 2pnn; 3j5p; 3j5q; 3j5r; 3j9j; 3sui; 5irx; 5irz; 5is0

Target, Subunit, Species

Transient receptor potential cation channel subfamily V member 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Transient receptor potential cation channel subfamily V member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Substance Action on Target

Antagonist

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Xenopus laevis

Cells/Cell Lines

oocyte

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Measurement Parameter

nH (Hill coefficient)

Quantitative value

0.7

Deviation

0.500000

Concomitants: Compound RN

2816484

Concomitants: Compound name

Capsaicin

Concomitants: Compound role

AGO

663 of 1220 Target Name

Transient receptor potential cation channel subfamily V member 1 [Rattus norvegicus]

Target Synonyms

capsaicin receptor; osm-9-like trp channel 1; otrpc1; transient receptor potential cation channel subfamily v member 1; trpv1; vanilloid receptor 1; vanilloid receptor type 1-like; vr1; vr1l

Target Uniprot ID

o35433

Target PDB ID

2nyj; 2pnn; 3j5p; 3j5q; 3j5r; 3j9j; 3sui; 5irx; 5irz; 5is0

Target, Subunit, Species

Transient receptor potential cation channel subfamily V member 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Transient receptor potential cation channel subfamily V member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Substance Action on Target

Antagonist

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Xenopus laevis

Cells/Cell Lines

oocyte

Substance RN

3917968View in Reaxys

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Substance Name

Lidocaine

Measurement Parameter

% Inhibition

Qualitative value

Concomitants: Compound RN

2816484

Concomitants: Compound name

Capsaicin

Concomitants: Compound role

AGO

664 of 1220 Target Name

voltage-gated sodium channel [Rattus norvegicus]

Target Synonyms

voltage-gated sodium channel

Target, Subunit, Species

voltage-gated sodium channel [Rattus norvegicus]

Target Mutant/Chimera Details

voltage-gated sodium channel [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Binding

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

brain cortex

Cells/Cell Lines

cells

Cell Fraction

Synaptosome

Substance RN

3917968View in Reaxys

Substance Name

Lignocaine

Measurement Parameter

pIC50

Quantitative value

4.26

Deviation

0.200000

Measurement pX

4.26

Concomitants: Compound RN

24140984; 24140929

Concomitants: Compound name

[3H]-Batrachotoxin; Tetrodotoxin; Scorpion venom (Leiurus quinquestriatus)

Concomitants: Compound role

RAD; COM; COM

665 of 1220 Target Name

voltage-gated sodium channel [Rattus norvegicus]

Target Synonyms

voltage-gated sodium channel

Target, Subunit, Species

voltage-gated sodium channel [Rattus norvegicus]

Target Mutant/Chimera Details

voltage-gated sodium channel [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Binding

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Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

brain cortex

Cells/Cell Lines

cells

Cell Fraction

Membrane

Substance RN

3917968View in Reaxys

Substance Name

Lignocaine

Measurement Parameter

pKi

Quantitative value

4.48

Deviation

0.410000

Measurement pX

4.48

Concomitants: Compound RN

13439294

Concomitants: Compound name

Lifarizine; BSA; [3H]-Lifarizine

Concomitants: Compound role

NSB; COM; RAD

666 of 1220 Target Name

voltage-gated sodium channel [Rattus norvegicus]

Target Synonyms

voltage-gated sodium channel

Target, Subunit, Species

voltage-gated sodium channel [Rattus norvegicus]

Target Mutant/Chimera Details

voltage-gated sodium channel [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Binding

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

brain cortex

Cells/Cell Lines

cells

Cell Fraction

Membrane

Substance RN

3917968View in Reaxys

Substance Name

Lignocaine

Measurement Parameter

nH (Hill coefficient)

Quantitative value

0.98

Deviation

0.0900000

Concomitants: Compound RN

13439294

Concomitants: Compound name

Lifarizine; BSA; [3H]-Lifarizine

Concomitants: Compound role

NSB; COM; RAD

667 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : acute bronchospasm; stimulation ofTarget : asthmatic patients of humanBioassay : EXAMPLE 4 Lidocaine Solution forInhalation used for Treatment of Asthma Patients This example de-

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scribes a clinical trial with inhalable lidocaine (10 and 40 mg) for treatment of asthma patients, some of whom were also treated with albuterol.The clinical trial was performed in a double blinded, placebo Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Route of Adm.

inhalational administration

Measurement Parameter

qualitative

Qualitative value

Measurement pX

Patent; CORUS PHARMA; BAKER, William, R.; WO2005/44233; (2005); (A1) English, View in Reaxys 668 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : asthma; effect onBioassay : EXAMPLE 4 Lidocaine Solution forInhalation used for Treatment of Asthma Patients This example describes a clinical trial with inhalable lidocaine (10 and 40 mg) for treatment of asthma patients, some of whom were also treated with albuterol.The clinical trial was performed in a double blinded, placebo

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Route of Adm.

inhalational administration

Qualitative Results

title compound caused improvement of airway susceptibility and asthma in tolerating environmental airway challenges like smoke, dust, pollution, allergens, etc.

Measurement Parameter

qualitative

Patent; CORUS PHARMA; BAKER, William, R.; WO2005/44233; (2005); (A1) English, View in Reaxys 669 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : cough; effect onBioassay : EXAMPLE 5Clinical Case This example describes a clinical study for treatment of cough using 1% of lidocaine.A 38 year old, otherwise healthy male patient had experienced postnasal drip and persistent cough for two weeks, after having had an upper respiratory infection. Cough episodes were occurring

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Route of Adm.

inhalational administration

Qualitative Results

title compound (25 mg) greatly diminished patients' cough and the patient remained essentially free of cough for the following 2 w

Measurement Parameter

qualitative

Patent; CORUS PHARMA; BAKER, William, R.; WO2005/44233; (2005); (A1) English, View in Reaxys 670 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : neurogenic inflammation; reduction ofTarget : Albino CD-1 mouseBioassay : Eight Albino male CD-1 mice per group, 7-9 weeks old, were used. Induction of neurogenic inflammation in the mouse ear was based on known methods (Inoue H, et al., Br J Pharmacol. 110:1614-1620, 1993). A 20-μl volume of Resiniferatoxin (0.05%) prepared in acetone was applied to the left ears (8 mice

Substance RN

3917968View in Reaxys

Substance Name

178204

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Qualitative Results

28.7 % inhibition of induced ear edema was observed 30 min after application of title compound in 0.5% w/v solution

Measurement Parameter

qualitative

Patent; Southall, Michael; Liebel, Frank; US2006/142304; (2006); (A1) English, View in Reaxys 671 of 1220 Target Name

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Synonyms

voltage-gated sodium channel + voltage-gated calcium channel

Target, Subunit, Species

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Mutant/Chimera Details

voltage-gated sodium channel [guinea pig]:Wild; voltage-gated calcium channel [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig; guinea pig

Target Transfection

Non Transfected; Non Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

guinea pig

Organs/Tissues

right ventricular papillary muscle

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

3 µM

Measurement Parameter

RMP

Unit

Quantitative value

-91

Deviation

672 of 1220 Target Name

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Synonyms

voltage-gated sodium channel + voltage-gated calcium channel

Target, Subunit, Species

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Mutant/Chimera Details

voltage-gated sodium channel [guinea pig]:Wild; voltage-gated calcium channel [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig; guinea pig

Target Transfection

Non Transfected; Non Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

guinea pig

Organs/Tissues

right ventricular papillary muscle

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

10 µM

Measurement Parameter

RMP

Unit

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Quantitative value

-91

Deviation

673 of 1220 Target Name

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Synonyms

voltage-gated sodium channel + voltage-gated calcium channel

Target, Subunit, Species

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Mutant/Chimera Details

voltage-gated sodium channel [guinea pig]:Wild; voltage-gated calcium channel [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig; guinea pig

Target Transfection

Non Transfected; Non Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

guinea pig

Organs/Tissues

right ventricular papillary muscle

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

30 µM

Measurement Parameter

RMP

Unit

Quantitative value

-91

Deviation

674 of 1220 Target Name

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Synonyms

voltage-gated sodium channel + voltage-gated calcium channel

Target, Subunit, Species

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Mutant/Chimera Details

voltage-gated sodium channel [guinea pig]:Wild; voltage-gated calcium channel [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig; guinea pig

Target Transfection

Non Transfected; Non Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

guinea pig

Organs/Tissues

right ventricular papillary muscle

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

100 µM

Measurement Parameter

RMP

Unit

Quantitative value

-90

Deviation

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675 of 1220 Target Name

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Synonyms

voltage-gated sodium channel + voltage-gated calcium channel

Target, Subunit, Species

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Mutant/Chimera Details

voltage-gated sodium channel [guinea pig]:Wild; voltage-gated calcium channel [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig; guinea pig

Target Transfection

Non Transfected; Non Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

guinea pig

Organs/Tissues

right ventricular papillary muscle

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

3 µM

Measurement Parameter

overshoot potential

Unit

Quantitative value

Deviation

676 of 1220 Target Name

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Synonyms

voltage-gated sodium channel + voltage-gated calcium channel

Target, Subunit, Species

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Mutant/Chimera Details

voltage-gated sodium channel [guinea pig]:Wild; voltage-gated calcium channel [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig; guinea pig

Target Transfection

Non Transfected; Non Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

guinea pig

Organs/Tissues

right ventricular papillary muscle

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

10 µM

Measurement Parameter

overshoot potential

Unit

Quantitative value

Deviation

677 of 1220 Target Name Target Synonyms

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig] voltage-gated sodium channel + voltage-gated calcium channel

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Target, Subunit, Species

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Mutant/Chimera Details

voltage-gated sodium channel [guinea pig]:Wild; voltage-gated calcium channel [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig; guinea pig

Target Transfection

Non Transfected; Non Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

guinea pig

Organs/Tissues

right ventricular papillary muscle

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

30 µM

Measurement Parameter

overshoot potential

Unit

Quantitative value

Deviation

678 of 1220 Target Name

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Synonyms

voltage-gated sodium channel + voltage-gated calcium channel

Target, Subunit, Species

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Mutant/Chimera Details

voltage-gated sodium channel [guinea pig]:Wild; voltage-gated calcium channel [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig; guinea pig

Target Transfection

Non Transfected; Non Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

guinea pig

Organs/Tissues

right ventricular papillary muscle

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

100 µM

Measurement Parameter

overshoot potential

Unit

Quantitative value

Deviation

679 of 1220 Target Name

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Synonyms

voltage-gated sodium channel + voltage-gated calcium channel

Target, Subunit, Species

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

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Target Mutant/Chimera Details

voltage-gated sodium channel [guinea pig]:Wild; voltage-gated calcium channel [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig; guinea pig

Target Transfection

Non Transfected; Non Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

guinea pig

Organs/Tissues

right ventricular papillary muscle

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

3 µM

Measurement Parameter

APD30

Unit

Measurement Object

30% of repolarization

Quantitative value

178

Deviation

680 of 1220 Target Name

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Synonyms

voltage-gated sodium channel + voltage-gated calcium channel

Target, Subunit, Species

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Mutant/Chimera Details

voltage-gated sodium channel [guinea pig]:Wild; voltage-gated calcium channel [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig; guinea pig

Target Transfection

Non Transfected; Non Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

guinea pig

Organs/Tissues

right ventricular papillary muscle

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

10 µM

Measurement Parameter

APD30

Unit

Measurement Object

30% of repolarization

Quantitative value

168

Deviation

681 of 1220 Target Name

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Synonyms

voltage-gated sodium channel + voltage-gated calcium channel

Target, Subunit, Species

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

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Target Mutant/Chimera Details

voltage-gated sodium channel [guinea pig]:Wild; voltage-gated calcium channel [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig; guinea pig

Target Transfection

Non Transfected; Non Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

guinea pig

Organs/Tissues

right ventricular papillary muscle

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

30 µM

Measurement Parameter

APD30

Unit

Measurement Object

30% of repolarization

Quantitative value

161

Deviation

682 of 1220 Target Name

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Synonyms

voltage-gated sodium channel + voltage-gated calcium channel

Target, Subunit, Species

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Mutant/Chimera Details

voltage-gated sodium channel [guinea pig]:Wild; voltage-gated calcium channel [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig; guinea pig

Target Transfection

Non Transfected; Non Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

guinea pig

Organs/Tissues

right ventricular papillary muscle

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

100 µM

Measurement Parameter

APD30

Unit

Measurement Object

30% of repolarization

Quantitative value

150

Deviation

683 of 1220 Target Name

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Synonyms

voltage-gated sodium channel + voltage-gated calcium channel

Target, Subunit, Species

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

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Target Mutant/Chimera Details

voltage-gated sodium channel [guinea pig]:Wild; voltage-gated calcium channel [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig; guinea pig

Target Transfection

Non Transfected; Non Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

guinea pig

Organs/Tissues

right ventricular papillary muscle

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

3 µM

Measurement Parameter

APD90

Unit

Measurement Object

90% of repolarization

Quantitative value

250

Deviation

684 of 1220 Target Name

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Synonyms

voltage-gated sodium channel + voltage-gated calcium channel

Target, Subunit, Species

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Mutant/Chimera Details

voltage-gated sodium channel [guinea pig]:Wild; voltage-gated calcium channel [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig; guinea pig

Target Transfection

Non Transfected; Non Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

guinea pig

Organs/Tissues

right ventricular papillary muscle

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

10 µM

Measurement Parameter

APD90

Unit

Measurement Object

90% of repolarization

Quantitative value

242

Deviation

685 of 1220 Target Name

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Synonyms

voltage-gated sodium channel + voltage-gated calcium channel

Target, Subunit, Species

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

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Target Mutant/Chimera Details

voltage-gated sodium channel [guinea pig]:Wild; voltage-gated calcium channel [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig; guinea pig

Target Transfection

Non Transfected; Non Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

guinea pig

Organs/Tissues

right ventricular papillary muscle

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

30 µM

Measurement Parameter

APD90

Unit

Measurement Object

90% of repolarization

Quantitative value

235

Deviation

686 of 1220 Target Name

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Synonyms

voltage-gated sodium channel + voltage-gated calcium channel

Target, Subunit, Species

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Mutant/Chimera Details

voltage-gated sodium channel [guinea pig]:Wild; voltage-gated calcium channel [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig; guinea pig

Target Transfection

Non Transfected; Non Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

guinea pig

Organs/Tissues

right ventricular papillary muscle

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

100 µM

Measurement Parameter

APD90

Unit

Measurement Object

90% of repolarization

Quantitative value

223

Deviation

687 of 1220 Target Name

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Synonyms

voltage-gated sodium channel + voltage-gated calcium channel

Target, Subunit, Species

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

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Target Mutant/Chimera Details

voltage-gated sodium channel [guinea pig]:Wild; voltage-gated calcium channel [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig; guinea pig

Target Transfection

Non Transfected; Non Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

guinea pig

Organs/Tissues

right ventricular papillary muscle

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

3 µM

Measurement Parameter

overshoot potential

Unit

Measurement Object

overshoot of slow action potential

Quantitative value

Deviation

Concomitants: Compound RN

1209229

Concomitants: Compound name

BaCl2

Concomitants: Compound role

IND

688 of 1220 Target Name

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Synonyms

voltage-gated sodium channel + voltage-gated calcium channel

Target, Subunit, Species

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Mutant/Chimera Details

voltage-gated sodium channel [guinea pig]:Wild; voltage-gated calcium channel [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig; guinea pig

Target Transfection

Non Transfected; Non Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

guinea pig

Organs/Tissues

right ventricular papillary muscle

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

10 µM

Measurement Parameter

overshoot potential

Unit

Measurement Object

overshoot of slow action potential

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Quantitative value

Deviation

Concomitants: Compound RN

1209229

Concomitants: Compound name

BaCl2

Concomitants: Compound role

IND

689 of 1220 Target Name

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Synonyms

voltage-gated sodium channel + voltage-gated calcium channel

Target, Subunit, Species

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Mutant/Chimera Details

voltage-gated sodium channel [guinea pig]:Wild; voltage-gated calcium channel [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig; guinea pig

Target Transfection

Non Transfected; Non Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

guinea pig

Organs/Tissues

right ventricular papillary muscle

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

30 µM

Measurement Parameter

overshoot potential

Unit

Measurement Object

overshoot of slow action potential

Quantitative value

Deviation

Concomitants: Compound RN

1209229

Concomitants: Compound name

BaCl2

Concomitants: Compound role

IND

690 of 1220 Target Name

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Synonyms

voltage-gated sodium channel + voltage-gated calcium channel

Target, Subunit, Species

voltage-gated sodium channel [guinea pig]; voltage-gated calcium channel [guinea pig]

Target Mutant/Chimera Details

voltage-gated sodium channel [guinea pig]:Wild; voltage-gated calcium channel [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig; guinea pig

Target Transfection

Non Transfected; Non Transfected

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

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Bioassay Name

Electrophysiology

Biological Species/NCBI ID

guinea pig

Organs/Tissues

right ventricular papillary muscle

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Substance Dose

100 µM

Measurement Parameter

overshoot potential

Unit

Measurement Object

overshoot of slow action potential

Quantitative value

Deviation

Concomitants: Compound RN

1209229

Concomitants: Compound name

BaCl2

Concomitants: Compound role

IND

691 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : in rectal tissue; amount ofBioassay : [Test Example 2] [Determination of Amount of Drug in Rectal Tissue] The suppository of Example 1 or the suppository of Comparative example 1 was administered to a rat and the concentration of drugs (lidocaine hydrochloride) in the rat rectal tissue after predetermined time was evaluated.[Test Method]

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

Sixty minutes after the administration or later, the suppository of Example 1 (consisting of H.P.CL) exhibited higher concentration of test compound in the rectal tissue than that of the suppository of Comparative example 1 (consisting of P.E.G 6000)

Measurement Parameter

qualitative

Patent; Sato Pharmaceutical Co. Ltd.; EP1666024; (2006); (A1) English, View in Reaxys 692 of 1220 Substance Effect

Antidyspeptic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Target : spontaneously hypertensive ratBioassay : arterial pulse pressure (AP) and mean arterial pressure (MAP) measured in cannulated right femoral vein; heart rate (HR) detnd. by tachograph; brains removed and sectioned (50 μm), histological examination performed with microscope 18-22 week old rats propofol-anesthetized, tracheotomized; right kidney exposed, renal nerve activity measured by silver electrode; insular cortex (IC) exposed; conscious group also studied

Substance RN

3917968View in Reaxys

Substance Name

178204

Measurement Parameter

qualitative

Qualitative value

Measurement pX

Butcher; Cechetto; American Journal of Physiology - Regulatory Integrative and Comparative Physiology; vol. 268; nb. 1 37-1; (1995); p. R214-R222, View in Reaxys

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693 of 1220 Substance Effect

Cardiovascular

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Bioassay : arterial pulse pressure (AP) and mean arterial pressure (MAP) measured in cannulated right femoral vein; heart rate (HR) detnd. by tachograph; brains removed and sectioned (50 μm), histological examination performed with microscope 18-22 wk old rats propofol-anesthetized, tracheotomized; right kidney exposed, renal nerve activity measured by silver electrode; insular cortex (IC) exposed; conscious group also studied

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

anesthetized: no effect; conscious: increase in MAP, HR

Measurement Parameter

qualitative

Butcher; Cechetto; American Journal of Physiology - Regulatory Integrative and Comparative Physiology; vol. 268; nb. 1 37-1; (1995); p. R214-R222, View in Reaxys 694 of 1220 Substance Effect

Apoptotic

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Name

Apoptosis

Bioassay Details

Target : thymocytes of Wistar ratBioassay : cells incubated with title comp. for 3 h; DNA stained with propidium iodide (PI); observed by laser scanning microscope

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

10 mM

Qualitative Results

title comp. at 30 mM increased population of cells with decreased forward scatter (dead shrunken cells), indicating early stage of apoptosis; figures

Measurement Parameter

qualitative

Nishimura, Yumiko; Kanada, Aimi; Yamaguchi, Jun-Ya; Horimoto, Kanna; Kobayashi, Masako; Tatsuishi, Tomoko; Kanemaru, Kaori; Ueno, Shin-Ya; Oyama, Yasuo; Toxicology; vol. 218; nb. 1; (2006); p. 48 - 57, View in Reaxys 695 of 1220 Substance Effect

Apoptotic

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Name

Apoptosis

Bioassay Details

Target : thymocytes of Wistar ratBioassay : cells incubated with title comp. alone or with calcium ionophor A23187 for 3 h; stained with FM-1-43; FM-1-43 fluorescence measured by flow cytometry; population of cells stained with FM-1-43 (marker for early stage of apoptosis) determined

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

30 mM

Measurement Parameter

qualitative

Qualitative value

Measurement pX

Cytotoxic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

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Bioassay Details

Target : thymocytes of Wistar ratBioassay : cells incubated with title comp. for 3 h; propidium iodide added; dead cells as propidium fluorescence measured by flow cytometer with argon laser with excitation at 488 nm and emission at 600 nm

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

3 mM

Qualitative Results

title comp. greatly increased population of propidium-stained dead cells only at 30 mM; therefore, threshold conc. of title comp. to induce cell death were between 10 and 30 mM; figure

Measurement Parameter

qualitative

Cytotoxic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Target : thymocytes of Wistar ratBioassay : PI: propidium iodide; P: cells stained with PI; P-AN: annexin V positive living cells stained with PI; FC: flow cytometry; further invest. of 30 mM title comp. in presence of calcium ionophore A23187 without/with caspase inhibitor Z-VAD-FMK cells incubated with title comp. for 3 h; stained with PI and annexin V-FITC in order to classify cell population of intact (N), annexin V-positive (apoptotic) living (AN) and two types of dead cells (P and P-AN); PI and FITC fluorescence measured by FC

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

10 mM

Qualitative Results

title comp. had no effect on N cells, at 30 (but not at 10) mM reduced number of AN cells, and increased number of dead (P and P-AN) cells; title comp. in presence of A23187 further greatly increased number of P cells: caspase was not involved; figures

Measurement Parameter

qualitative

Genotoxic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Target : thymocytes of Wistar ratBioassay : cells incubated with title comp. for 3 h; DNA stained with propidium iodide (PI); fluorescence measured by flow cytometer at 600 nm; population of cells with hypodiplopial DNA estimated

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

10 mM

Measurement Parameter

qualitative

Qualitative value

Measurement pX

In Vitro (Efficacy)

Bioassay Name

Binding

Bioassay Details

Effect : |receptor blocking agent Target : CHO cell membranes expressing human muscarinic M1 receptorBioassay : CHO: Chinese hamster ovary; nonspecific binding determined with 1 μmol/l atropine competition binding assay; membranes incubated with 143 pmol/l <3H>N-methyl scopolamine and various concentrations of title comp.; scintillation counting after filtration

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Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

1.00000E-06 M

Measurement Parameter

pKi

Quantitative value

3.75

Measurement pX

3.75

Yunoki, Motonari; Nakahara, Tsutomu; Mitani, Akiko; Maruko, Takeshi; Kubota, Yuko; Sakamoto, Kenji; Ishii, Kunio; European Journal of Pharmacology; vol. 470; nb. 1-2; (2003); p. 65 - 71, View in Reaxys 700 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Binding

Bioassay Details

Effect : |receptor blocking agent Target : CHO cell membranes expressing human muscarinic M2 receptorBioassay : CHO: Chinese hamster ovary; nonspecific binding determined with 1 μmol/l atropine competition binding assay; membranes incubated with 143 pmol/l <3H>N-methyl scopolamine and various concentrations of title comp.; scintillation counting after filtration

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

1.00000E-06 M

Measurement Parameter

pKi

Quantitative value

4.22

Measurement pX

4.22

In Vitro (Efficacy)

Bioassay Name

Binding

Bioassay Details

Effect : |receptor blocking agent Target : CHO cell membranes expressing human muscarinic M3 receptorBioassay : CHO: Chinese hamster ovary; nonspecific binding determined with 1 μmol/l atropine competition binding assay; membranes incubated with 143 pmol/l <3H>N-methyl scopolamine and various concentrations of title comp.; scintillation counting after filtration

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

1.00000E-06 M

Measurement Parameter

pKi

Quantitative value

3.65

Measurement pX

3.65

In Vitro (Efficacy)

Bioassay Name

Binding

Bioassay Details

Effect : |receptor blocking agent Target : CHO cell membranes expressing human muscarinic M4 receptorBioassay : CHO: Chinese hamster ovary; nonspecific binding determined with 1 μmol/l atropine competition binding assay; membranes incubated with 143 pmol/l <3H>N-methyl scopolamine and various concentrations of title comp.; scintillation counting after filtration

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

1.00000E-06 M

Measurement Parameter

pKi

Quantitative value

3.57

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Measurement pX

3.57

In Vitro (Efficacy)

Bioassay Name

Binding

Bioassay Details

Effect : |receptor blocking agent Target : CHO cell membranes expressing human muscarinic M5 receptorBioassay : CHO: Chinese hamster ovary; nonspecific binding determined with 1 μmol/l atropine competition binding assay; membranes incubated with 143 pmol/l <3H>N-methyl scopolamine and various concentrations of title comp.; scintillation counting after filtration

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

1.00000E-06 M

Measurement Parameter

pKi

Quantitative value

3.33

Measurement pX

3.33

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : cAMP accumulation; induction ofTarget : bovine tracheal smooth muscle segmentBioassay : further investigation with methacholine; 8-CPT-cAMP: 8-(4-chlorophenylthio)adenosine 3',5'cyclic monophosphate muscles treated with title comp. 15 min after 3-isobutyl-1-methylxanthine (300 μmol/l) addition; 15 min later forskolin (1 μmol/l) added; tissues homogenized; cAMP accumulation in supernatant measured by radioimmunoassay

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

100 µM

Qualitative Results

in presence of methacholine title comp. enhanced both basal and forskolin-stimulated cAMP accumulation; neither basal nor forskolin-stimulated cAMP accumulation was affected by title comp. in absence of methacholine

Measurement Parameter

qualitative

Myorelaxant

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Target : bovine tracheal smooth muscle segmentBioassay : 8-CPT-cAMP: 8-(4-chlorophenylthio)adenosine 3',5'-cyclic monophosphate Krebs-Ringer bicarbonate buffer gassed with 95 percent CO2/5 percent 02 at 37 deg C; muscles contracted with histamine (100 μmol/l) or 40 mmol/l KCl treated with title comp.; 15 min later forskolin added; muscle tensions recorded isometrically

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

100 µM

Qualitative Results

title comp. attenuated 40 mmol/l KCl-induced contractions; title comp. did not affect relaxant responses to forskolin

Measurement Parameter

qualitative

Myorelaxant

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Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Target : bovine tracheal smooth muscle segmentBioassay : 8-CPT-cAMP: 8-(4-chlorophenylthio)adenosine 3',5'-cyclic monophosphate muscles contracted with methacholine (0.3 μmol/l) treated with title comp.; 15 min later forskolin (0.001 - 10 μmol/l) or 8-CPT-cAMP (1 - 300 μmol/l) added; muscle tensions recorded isometrically

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

100 µM

Qualitative Results

title comp. attenuated methacholine-induced tensions and shifted concentration-response curves for forskolin-induced relaxation to left (figures); title comp. did not affect relaxant responses to 8-CPTcAMP

Measurement Parameter

qualitative

Solute carrier family 22 member 2 [human]

Target Synonyms

hoct2; oct2; organic cation transporter 2; slc22a2; solute carrier family 22 member 2

Target Uniprot ID

o15244

Target, Subunit, Species

Solute carrier family 22 member 2 [human]

Target Mutant/Chimera Details

Solute carrier family 22 member 2 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

Substance Action on Target

Inhibitor

Bioassay Category

Metabolism/Transport

Bioassay Name

Flux uptake

Biological Species/NCBI ID

human

Cells/Cell Lines

liver cell

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Measurement Parameter

IC50

Unit

µM

Quantitative value

294

Measurement pX

3.53

Concomitants: Compound RN

606492

Concomitants: Compound name

[14C]-Metformin

Concomitants: Compound role

SUB

708 of 1220 Target Name

Solute carrier family 22 member 1 [Rattus norvegicus]

Target Synonyms

oct1; organic cation transporter 1; roct1; slc22a1; solute carrier family 22 member 1

Target Uniprot ID

q63089

Target, Subunit, Species

Solute carrier family 22 member 1 [Rattus norvegicus]

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Target Mutant/Chimera Details

Solute carrier family 22 member 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Substance Action on Target

Inhibitor

Bioassay Category

Metabolism/Transport

Bioassay Name

Flux uptake

Biological Species/NCBI ID

Rattus norvegicus

Cells/Cell Lines

liver cell

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Measurement Parameter

IC50

Unit

µM

Quantitative value

57.4

Measurement pX

4.24

Concomitants: Compound RN

606492

Concomitants: Compound name

[14C]-Metformin

Concomitants: Compound role

SUB

709 of 1220 Target Name

Solute carrier family 22 member 2 [Rattus norvegicus]

Target Synonyms

oct2; organic cation transporter 2; roct2; slc22a2; solute carrier family 22 member 2

Target Uniprot ID

q9r0w2

Target, Subunit, Species

Solute carrier family 22 member 2 [Rattus norvegicus]

Target Mutant/Chimera Details

Solute carrier family 22 member 2 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Substance Action on Target

Inhibitor

Bioassay Category

Metabolism/Transport

Bioassay Name

Flux uptake

Biological Species/NCBI ID

Rattus norvegicus

Cells/Cell Lines

liver cell

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine

Measurement Parameter

IC50

Unit

µM

Qualitative value

Quantitative value

1000

Measurement pX

321/467

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Concomitants: Compound RN

606492

Concomitants: Compound name

[14C]-Metformin

Concomitants: Compound role

SUB

710 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : |drug interaction Bioassay : EXAMPLE 2:[0044] This example provides a description of a phase I clinical study (a double- blind, randomized 4- way crossover) carried out to determine, i.a., if the presence of lidocaine hydrochloride in nasally administered formulations of ketorolac has any adverse effect on the PK profile of ketorolac.

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Route of Adm.

intranasal administration

Qualitative Results

title compound at concentrations higher than 4% reduced time to Cmax of ketorolac tromethamine

Measurement Parameter

qualitative

Patent; ROXRO PHARMA, INC.; WO2006/71601; (2006); (A2) English, View in Reaxys 711 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

increases the effective refractory period up to 80 min of the bioelectric activity in the sympathetic nerves of the heart (dose 8 mg/kg, i. v., cat); increase the electric fibrillatory threshold up to ca. 200percent (dose 5 mg/kg, i. v., cat)

Measurement Parameter

qualitative

Kaverina; Berdjajev; Darinskij; Pharmazie; vol. 40; nb. 12; (1985); p. 840 - 844, View in Reaxys 712 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

local anesthetic activity

Measurement Parameter

qualitative

Shafiee; Hedayati; Salimi; Faghihi; Journal of Pharmaceutical Sciences; vol. 72; nb. 2; (1983); p. 198 - 202, View in Reaxys 713 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : |receptor; binding activity Target : Wistar rat ventricular cardiocytesBioassay : determination of <125I>HEAT bound ( percent of control) versus time and dose; bound (fmol/mg protein) versus <125I>HEAT (pM) in vitro; ventricles from the neonatal rats (2-d-old); add. of (+/-)-ω(<125I>iodo-4-hydroxyphenyl)-ethyl-aminomethyl-tetralone (<125I>HEAT, 2200 Ci/mmol); radioimmunoassay; add. of l-norepinephrine (NE, 1 μM)

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

0.0100000 mM

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Qualitative Results

title comp. dose- and time-dependent manner increased the binding of <125I>HEAT and this effect was also observed in the presence of NE; <125I>HEAT binding was 128 percent of control at conc. 0.1 mM for 2 days

Measurement Parameter

qualitative

Mizuki; Kobayashi; Nakashima; Kuroiwa; Izumi; European Journal of Pharmacology; vol. 277; nb. 2-3; (1995); p. 133 - 137, View in Reaxys 714 of 1220 Substance Effect

Antiviral

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Bioassay : in vitro; 37 deg C African Green Monkey kidney Vero cell cultures; 2 h-preinfection with 5 percent CO2; 118 h-postincubation without compound; incident light microscopy

Biological Species/NCBI ID

Human alphaherpesvirus 1

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

800 ppm

Measurement Parameter

qualitative

Qualitative value

Measurement pX

Hill; Dawson; Pharmaceutical Sciences; vol. 2; nb. 10; (1996); p. 457 - 459, View in Reaxys 715 of 1220 Substance Effect

Antiviral

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Bioassay : in vitro; 37 deg C 2 h drug pretreatment of extracellular HSV-1; African Green Monkey kidney Vero cell cultures infection; 24-120 h-incubation; incident light microscopy

Biological Species/NCBI ID

Human alphaherpesvirus 1

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

5000 ppm

Measurement Parameter

qualitative

Qualitative value

Measurement pX

Hill; Dawson; Pharmaceutical Sciences; vol. 2; nb. 10; (1996); p. 457 - 459, View in Reaxys 716 of 1220 Substance Effect

Antiarrhytmic

Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : lethalityBioassay : chest opened by a left thoracotomy; pericardium opened; heart exteriorized; coronary artery connected with ligature-5/0 braided silk suture; dysrhythmias produced; ligature tied; after 5 min of coronary occlusion reperfusion obtained by cutting suture rats anesthetized, fixed and dissected; indwelling polyethylene catheters inserted into a common carotid artery (connected with transducer) and into a femoral vein (drug admin.); trachea cannulated, animals ventilated; lead II ECG recorded

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

5 mg/kg

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Substance Route of Adm.

intravenous administration

Qualitative Results

title compd. (injected 10 min before occlusion) prevented reperfusion syndrome: ventricular tachycardia and fibrillation; decreased lethality

Measurement Parameter

qualitative

Guarini, Salvatore; Martini, Maria Cristina; Bertolini, Alfio; Life Sciences; vol. 57; nb. 10; (1995); p. 967 - 972, View in Reaxys 717 of 1220 Substance Effect

Antiarrhytmic

Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Bioassay : determination of arteriar blood pressure, ECG, HR, ventricular fibrillation (VF) rats (ca. 250 g); carotid arteria was cannulated; ischemia was induced by left coronary arteria ligation and reperfusion was achived ( after 5 min period of ischemia) by removing the ligature; title comp. administered before 5 min occlusion

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

1 mg/kg

Substance Route of Adm.

intravenous administration

Qualitative Results

title comp. did not reduce significally the incidence of reperfusion-induced arrhythmias

Measurement Parameter

qualitative

Manning; Bruyninckx; Ramboux; Chatelain; Journal of Cardiovascular Pharmacology; vol. 26; nb. 3; (1995); p. 453 - 461, View in Reaxys 718 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : |drug delivery system Target : healthy humanBioassay : DPPC: L-ω-dipalmitoylphosphatidyl choline; DCP: dicetyl phosphate; SPB: saline phosphate buffer; HPMC: hydroxypropyl-methylcellulose 6 volunteers, wt 60-80 kg, 30-45 years old; pin prick test; title comp. encapsulated in liposomal delivery systems of var. mixtures of DPPC, cholesterol with or without DCP, stearylamine; swelling at 53 deg C up to 48 h, SPB, pH 7.4; HPMC gel

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Route of Adm.

cutaneous administration

Qualitative Results

delayed onset, localized and prolonged duration of action; percentage of drug entrapped increased with swelling time, negative charge of liposomes, increasing cholesterol content

Measurement Parameter

qualitative

El-Ridy; Khalil; Pharmazie; vol. 54; nb. 9; (1999); p. 682 - 684, View in Reaxys 719 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

in vivo rabbit corneal and IC50 = 1.6*10-2 mol/l for male mice tail anesthetic activities; in vivo duration of local anesthetic activity (male rat sciatic nerve block); therapeutic index

Measurement Parameter

qualitative

Caliendo; Di Carlo; Greco; Grieco; Meli; Novellino; Perissutti; Santagada; European Journal of Medicinal Chemistry; vol. 30; nb. 7-8; (1995); p. 603 - 608, View in Reaxys 720 of 1220 Bioassay Category Bioassay Name

In Vitro (Efficacy) In Vitro (others)

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Substance RN

3917968View in Reaxys

Substance Name

178204

Qualitative Results

surface anesthetic activity (IC 50: 0.86percent, conjuctival sac administration) and infiltration anesthetic activity (IC 50: 0.36percent, intradermal administration into the conscius) in guinea-pigs

Measurement Parameter

qualitative

Malawska; Filipek; Stadnicka; Ciechanowicz-Rutkowska; Archiv der Pharmazie; vol. 328; nb. 6; (1995); p. 541 - 546, View in Reaxys 721 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : |secretion inhibition Bioassay : effect on release of periplasmic pertussis toxin (PTX); control: without title comp. wild type strain BP338 grown on Bordet-Gengou agar containing 15 percent sheep's blood; incubation with title comp. at 37 deg C for 2 or 24 h; amount of secreted pertussis toxin from culture supernatants dialyzed against phosphate-buffered saline measured

Biological Species/NCBI ID

Bordetella pertussis

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

40 g/L

Qualitative Results

title comp. significantly reduced secretion of PTX after 2 and 24 h (table)

Measurement Parameter

qualitative

Craig-Mylius, Kathleen A.; Weiss, Alison A.; Antimicrobial Agents and Chemotherapy; vol. 44; nb. 5; (2000); p. 1383 - 1386, View in Reaxys 722 of 1220 Substance Effect

Antibiotic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Bioassay : wild type strain BP338 grown on Bordet-Gengou agar containing 15 percent sheep's blood; incubation with title comp. at 37 deg C for 24 h; bacterial growth was monitored by optical density at 600 nm; viability determined; control: without title comp.

Biological Species/NCBI ID

Bordetella pertussis

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

40 g/L

Qualitative Results

title comp. reduced growth and viability to 27 percent and 1 percent of control, respectively

Measurement Parameter

qualitative

Craig-Mylius, Kathleen A.; Weiss, Alison A.; Antimicrobial Agents and Chemotherapy; vol. 44; nb. 5; (2000); p. 1383 - 1386, View in Reaxys 723 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Bioassay Details

Effect : Ih current; blocking ofTarget : rat dorsal root ganglion neuronesBioassay : Ih: hyperpolarization-activated inward current; control: currents before application of title comp.; expt. done at 22-24 deg C; averaged I-V plots for Ih currents measured as difference between steady-state and instantaneous currents slices of neurones from 6-12 d old rats prepared; Ih currents were activated from holding potential of -80 to -160 mV in 10 mV steps; perfused extracellular with title comp., 4-5 min; whole-cell Ih currents recorded

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

100 µM

Qualitative Results

Ih was reversibly blocked by title comp.; diagram

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Measurement Parameter

qualitative

Bischoff, Ulrike; Braeu, Michael E.; Vogel, Werner; Hempelmann, Gunter; Olschewski, Andrea; British Journal of Pharmacology; vol. 139; nb. 7; (2003); p. 1273 - 1280, View in Reaxys 724 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Bioassay Details

Effect : Ih current; blocking ofTarget : rat dorsal root ganglion neuronesBioassay : Ih: hyperpolarization-activated inward current; control: currents before application of title comp.; expt. done at 22-24 deg C; averaged I-V plots for Ih currents measured as difference between steady-state and instantaneous currents slices of neurones from 6-12 d old rats prepared; Ih currents activated from holding potential of -80 mV in hyperpolarizing 60 mV steps to -140 mV; perfused extracellular with title comp., 4-5 min; Ih currents detd.

Substance RN

3917968View in Reaxys

Substance Name

178204

Substance Dose

3 µM

Measurement Parameter

IC50

Unit

µM

Quantitative value

Measurement pX

Sodium channel protein type 9 subunit alpha [Rattus norvegicus];+Sodium channel subunit beta-1 [Rattus norvegicus]

Target Synonyms

peripheral sodium channel 1; pn1; scn9a; sodium channel protein type 9 subunit alpha; sodium channel protein type ix subunit alpha; voltage-gated sodium channel subunit alpha nav1.7 + scn1b; sodium channel subunit beta-1

Target Uniprot ID

o08562 + q00954

Target, Subunit, Species

Sodium channel protein type 9 subunit alpha [Rattus norvegicus]; Sodium channel subunit beta-1 [Rattus norvegicus]

Target Mutant/Chimera Details

Sodium channel protein type 9 subunit alpha [Rattus norvegicus]:Wild + Sodium channel subunit beta-1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Concentration required to inhibit [3H]BTX binding to Na+ channel of rat brain using 5 nM [3H]BTX as radioligand and 5mM HEPES buffer incubated for 90 min at 25 degree C

Biological Species/NCBI ID

Rattus norvegicus

Organs/Tissues

brain

Substance RN

3917968View in Reaxys

Measurement Parameter

IC50

Unit

Qualitative value

Quantitative value

56000

Measurement pX

4.25

Concomitants: Compound name

[3H]Batrachotoxin

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Concomitants: Compound role 726 of 1220 Bioassay Category

RAD In Vivo (Animal models)

Bioassay Details

Infiltration EC50 of the compound which produced loss of response to painful stimuli in wheals of guinea pig at the time of peak action (5 min following intradermal injection)

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intradermal administration

Qualitative Results

RA not calculated

Measurement Parameter

qualitative

Measurement Object

Regan; Galysh; Morris; Journal of medicinal chemistry; vol. 10; nb. 4; (1967); p. 649 - 652, View in Reaxys 727 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Relative activity was determined in mice at a duration 27.5min relative to lidocaine

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Measurement Object

relative activity

Quantitative value

Tsatsas; Sandris; Kontonassios; Zaroslinski; Browne; Possley; Journal of medicinal chemistry; vol. 10; nb. 2; (1967); p. 235 - 242, View in Reaxys 728 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Details

Local anesthetic activity of the compound was in mice determined 30 min after injection of equieffective concentration of 0.5 g/100ml

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Measurement Parameter

Activity

Unit

Qualitative value

Quantitative value

A. M. ROE; R. A. BURTON; G. L. WILLEY; M. W. BAINES; A. C. RASMUSSEN; Journal of medicinal chemistry; vol. 11; nb. 4; (1968); p. 814 - 819, View in Reaxys 729 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was evaluated for the local anesthetic activity 30 min after injection of equieffective concentration of 0.5g/ml

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Measurement Parameter

Activity

Unit

Qualitative value

327/467

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Quantitative value

A. M. ROE; R. A. BURTON; G. L. WILLEY; M. W. BAINES; A. C. RASMUSSEN; Journal of medicinal chemistry; vol. 11; nb. 4; (1968); p. 814 - 819, View in Reaxys 730 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Activity(infiltration) relative to lidocaine that abolishes corneal reflex in guinea pig tested 5 min after injection of 2 or 3 drops

Biological Species/NCBI ID

guinea pig

Cells/Cell Lines

cornea cell

Substance RN

3917968View in Reaxys

Qualitative Results

RA not calculated

Measurement Parameter

qualitative

Measurement Object

Regan; Galysh; Morris; Journal of medicinal chemistry; vol. 10; nb. 4; (1967); p. 649 - 652, View in Reaxys 731 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Details

Infiltration effective concentration of compound produced loss of response to painful stimuli in wheals of guinea pig at the time of peak action (5 min following intradermal injection)

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intradermal administration

Measurement Parameter

EC50

Unit

mg/mL

Qualitative value

Quantitative value

0.74

Measurement pX

2.56

Regan; Galysh; Morris; Journal of medicinal chemistry; vol. 10; nb. 4; (1967); p. 649 - 652, View in Reaxys 732 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Activity (surface) relative to lidocaine that abolishes corneal reflex in guinea pig, tested 5 min after injection of 2 or 3 drops

Biological Species/NCBI ID

guinea pig

Cells/Cell Lines

cornea cell

Substance RN

3917968View in Reaxys

Qualitative Results

RA not calculated

Measurement Parameter

qualitative

Measurement Object

Regan; Galysh; Morris; Journal of medicinal chemistry; vol. 10; nb. 4; (1967); p. 649 - 652, View in Reaxys 733 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Concentration of compound which causes a loss of response to painful stimuli in wheals of guinea pig, at the time of peak action (5min following intradermal injection)

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Measurement Parameter

EC50

Unit

µg/mL

328/467

2018-05-14 08:43:54

Qualitative value

Quantitative value

740

Measurement pX

2.56

Regan; Galysh; Morris; Journal of medicinal chemistry; vol. 10; nb. 4; (1967); p. 649 - 652, View in Reaxys 734 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Surface EC50 is the concentration of compound which abolishes corneal reflex in guinea pig 5 min after instillation of 2 or 3 drops

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Measurement Parameter

EC50

Unit

mg/mL

Qualitative value

Quantitative value

9.2

Measurement pX

1.47

Regan; Galysh; Morris; Journal of medicinal chemistry; vol. 10; nb. 4; (1967); p. 649 - 652, View in Reaxys 735 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was evaluated for the local anesthetic activity 60 min after injection of equieffective concentration of 0.5g/ml

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Measurement Parameter

Activity

Unit

Qualitative value

Quantitative value

A. M. ROE; R. A. BURTON; G. L. WILLEY; M. W. BAINES; A. C. RASMUSSEN; Journal of medicinal chemistry; vol. 11; nb. 4; (1968); p. 814 - 819, View in Reaxys 736 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Local anesthetic activity of the compound was determined in mice 10 min after injection of equieffective concentration of 0.5 g/100ml

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Unit

Measurement Object

Local anesthetic activity

Qualitative value

Quantitative value

A. M. ROE; R. A. BURTON; G. L. WILLEY; M. W. BAINES; A. C. RASMUSSEN; Journal of medicinal chemistry; vol. 11; nb. 4; (1968); p. 814 - 819, View in Reaxys 737 of 1220 Bioassay Category Bioassay Details

In Vitro (Efficacy) Threshold irritant concentration was determined and expressed as lidocaine ratio at a concentration of 55.4mM in mice

329/467

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Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Measurement Object

Lidocaine ratio

Quantitative value

Tsatsas; Sandris; Kontonassios; Zaroslinski; Browne; Possley; Journal of medicinal chemistry; vol. 10; nb. 2; (1967); p. 235 - 242, View in Reaxys 738 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Acute toxicity of the compound was estimated in male CF1 mice 7 days after i.v. administration

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Measurement Parameter

LD50

Unit

mg/mL

Qualitative value

Quantitative value

Regan; Galysh; Morris; Journal of medicinal chemistry; vol. 10; nb. 4; (1967); p. 649 - 652, View in Reaxys 739 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Local anaesthetic potency duration in rabbit corneal test at 0.25 ml of 2 solution/conjunctival sac

Biological Species/NCBI ID

Leporidae

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Unit

minute

Measurement Object

Potency duration

Qualitative value

Quantitative value

Campaigne; Bosin; Journal of medicinal chemistry; vol. 10; nb. 5; (1967); p. 945 - 946, View in Reaxys 740 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Relative toxicity is the ratio of lethal dose to that of lidocaine upon i.v. dose in mice

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Qualitative Results

Relative Toxicity not calculated

Measurement Parameter

qualitative

Measurement Object

Relative Toxicity

Regan; Galysh; Morris; Journal of medicinal chemistry; vol. 10; nb. 4; (1967); p. 649 - 652, View in Reaxys 741 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Surface EC50 that abolishes corneal reflex in guinea pig 5 min after instillation of 2 or 3 drops

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

330/467

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Qualitative Results

RA not calculated

Measurement Parameter

qualitative

Measurement Object

Regan; Galysh; Morris; Journal of medicinal chemistry; vol. 10; nb. 4; (1967); p. 649 - 652, View in Reaxys 742 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

The surface EC50 is the concentration of compound which abolishes corneal reflex in guinea pig, 5 min after instillation of 2 or 3 drops

Biological Species/NCBI ID

guinea pig

Cells/Cell Lines

cornea cell

Substance RN

3917968View in Reaxys

Measurement Parameter

EC50

Unit

µg/mL

Qualitative value

Quantitative value

9200

Measurement pX

1.47

Regan; Galysh; Morris; Journal of medicinal chemistry; vol. 10; nb. 4; (1967); p. 649 - 652, View in Reaxys 743 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Local anesthetic activity of the compound was determined in mice 60 min after injection of equieffective concentration of 0.5 g/100ml

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Unit

Measurement Object

Local anesthetic activity

Qualitative value

Quantitative value

A. M. ROE; R. A. BURTON; G. L. WILLEY; M. W. BAINES; A. C. RASMUSSEN; Journal of medicinal chemistry; vol. 11; nb. 4; (1968); p. 814 - 819, View in Reaxys 744 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

RA(infil)/RT ratio gives the safety margin of the compound anesthetic relative to lidocaine is unity

Substance RN

3917968View in Reaxys

Measurement Parameter

ratio

Quantitative value

Regan; Galysh; Morris; Journal of medicinal chemistry; vol. 10; nb. 4; (1967); p. 649 - 652, View in Reaxys 745 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Details

Duration of local anesthetic activity after intravenous administration of the compound measured as concentration

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Measurement Parameter

percentage

Unit

331/467

2018-05-14 08:43:54

Measurement Object

Duration

Qualitative value

Quantitative value

100

Tsatsas; Costakis; Zaroslinski; Browne; Possley; Journal of medicinal chemistry; vol. 12; nb. 5; (1969); p. 870 - 873, View in Reaxys 746 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested for local anaesthesia in the rabbit corneal test at 0.25 ml of 2 solution/ conjunctival sac

Biological Species/NCBI ID

Leporidae

Cells/Cell Lines

cornea cell

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Unit

minute

Measurement Object

Potency duration

Qualitative value

Quantitative value

Campaigne; Bosin; Journal of medicinal chemistry; vol. 10; nb. 5; (1967); p. 945 - 946, View in Reaxys 747 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Infiltration relative activity of guinea pig to that of relative toxicity in mouse upon i.v. administration; gives the safety margin of the compound anesthetic relative to lidocaine

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Measurement Parameter

ratio

Quantitative value

Regan; Galysh; Morris; Journal of medicinal chemistry; vol. 10; nb. 4; (1967); p. 649 - 652, View in Reaxys 748 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Details

Compound was evaluated for the local anesthetic activity 10 min after injection of equieffective concentration of 0.5g/ml

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Measurement Parameter

Activity

Unit

Qualitative value

Quantitative value

A. M. ROE; R. A. BURTON; G. L. WILLEY; M. W. BAINES; A. C. RASMUSSEN; Journal of medicinal chemistry; vol. 11; nb. 4; (1968); p. 814 - 819, View in Reaxys 749 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lethal dose of the compound in mouse upon i.p. administration

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

332/467

2018-05-14 08:43:54

Substance Route of Adm.

intraperitoneal administration

Qualitative Results

Measurement Parameter

LD50

Unit

mg/kg

Measurement Object

Lethal dose

Quantitative value

Onuaguluchi; Igbo; Archives Internationales de Pharmacodynamie et de Therapie; vol. 274; nb. 2; (1985); p. 253 - 266, View in Reaxys 750 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lethal dose of the compound in frog upon parenteral administration

Biological Species/NCBI ID

Anura

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Qualitative Results

159

Measurement Parameter

LD50

Unit

mg/kg

Measurement Object

Lethal dose

Quantitative value

159

Onuaguluchi; Igbo; Archives Internationales de Pharmacodynamie et de Therapie; vol. 289; nb. 2; (1987); p. 278 - 289, View in Reaxys 751 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lowest toxic dose of the compound in man after implantation

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

5.174

Measurement Parameter

TDLo

Unit

mg/kg

Measurement Object

Lowest toxic dose

Quantitative value

5.174

Sundaram; Canadian Medical Association Journal; vol. 137; nb. 3; (1987); p. 219 - 220, View in Reaxys 752 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lethal dose of the compound in rat upon s.c. administration

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Qualitative Results

570

Measurement Parameter

LD50

Unit

mg/kg

Quantitative value

570

Bioorganic & medicinal chemistry; vol. 2; (1970); p. 299, View in Reaxys 753 of 1220 Bioassay Category Bioassay Details

Toxicity/Safety Pharmacology Lethal dose of the compound in guinea pig upon i.v. administration

333/467

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Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Qualitative Results

24.5

Measurement Parameter

LD50

Unit

mg/kg

Measurement Object

Lethal dose

Quantitative value

24.5

NARANJO P; DE NARANJO EB; Arch Int Pharmacodyn Ther (1899-1996); vol. 113; nb. 3-4; (1958); p. 313 - 335, View in Reaxys 754 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lethal dose of the compound in mouse upon p.o. administration

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

oral administration

Qualitative Results

220

Measurement Parameter

LD50

Unit

mg/kg

Measurement Object

Lethal dose

Quantitative value

220

Bioorganic & medicinal chemistry; vol. 2; (1970); p. 299, View in Reaxys 755 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lethal dose of the compound in rabbit upon i.t. administration

Biological Species/NCBI ID

Leporidae

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intratracheal administration

Qualitative Results

Measurement Parameter

LD50

Unit

mg/kg

Measurement Object

Lethal dose

Quantitative value

Luduena; Bogado; Tullar; Archives internationales de pharmacodynamie et de thérapie; vol. 200; nb. 2; (1972); p. 359 - 369, View in Reaxys 756 of 1220 Substance Effect

Toxic

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lowest toxic dose of the compound in human upon p.o. administration

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

oral administration

Qualitative Results

1.6

Measurement Parameter

TDLo

334/467

2018-05-14 08:43:54

Unit

mg/kg

Measurement Object

Toxic dose

Quantitative value

1.6

Hess; Walson; Annals of Emergency Medicine; vol. 17; nb. 7; (1988); p. 725 - 727, View in Reaxys 757 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lethal dose of the compound in rat upon i.v. administration

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Qualitative Results

Measurement Parameter

LD50

Unit

mg/kg

Measurement Object

Lethal dose

Quantitative value

Bioorganic & medicinal chemistry; vol. 2; (1970); p. 299, View in Reaxys 758 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Details

Distribution half life of compound (monoethylglycinexylidide (MEGX)) in pregnant women (N=10) with gestational diabetes mellitus upon administration of 200 mg

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

59.77

Measurement Parameter

t1/2

Unit

minute

Measurement Object

Distribution half life

Quantitative value

59.77

Moises, Elaine Christine Dantas; Duarte, Luciana De Barros; Cavalli, Ricardo De Carvalho; Marques, Maria Paula; Lanchote, Vera Lucia; Duarte, Geraldo; Da Cunha, Sergio Pereira; European Journal of Clinical Pharmacology; vol. 64; nb. 12; (2008); p. 1189 - 1196, View in Reaxys 759 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Details

Percent of total dose reached systemic circulation of cats (N=8) upon transdermal application of 700 mg patch

Biological Species/NCBI ID

domestic cat

Substance RN

3917968View in Reaxys

Substance Route of Adm.

transdermal administration

Qualitative Results

56 +/- 29

Measurement Parameter

Absorption

Unit

Measurement Object

Percent of total dose reached systemic circulation

Quantitative value

Ko; Maxwell; Abbo; Weil; Journal of Veterinary Pharmacology and Therapeutics; vol. 31; nb. 4; (2008); p. 359 - 367, View in Reaxys 760 of 1220 Bioassay Category

Pharmacokinetic

335/467

2018-05-14 08:43:54

Bioassay Details

Skin concentrations of compound (contralateral thoracic skin without the patch) in cats (N=8) after transdermal application of 700 mg patch

Biological Species/NCBI ID

domestic cat

Substance RN

3917968View in Reaxys

Substance Route of Adm.

transdermal administration

Qualitative Results

2.2 +/- 0.6

Measurement Parameter

concentration (parameters)

Unit

µg/g

Quantitative value

2.2

Ko; Maxwell; Abbo; Weil; Journal of Veterinary Pharmacology and Therapeutics; vol. 31; nb. 4; (2008); p. 359 - 367, View in Reaxys 761 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Skin concentrations of compound (thoracic skin beneath the patch) in cats (N=8) after transdermal application of 700 mg patch

Biological Species/NCBI ID

domestic cat

Substance RN

3917968View in Reaxys

Qualitative Results

211 +/- 113

Measurement Parameter

concentration (parameters)

Unit

µg/g

Measurement Object

Skin concentrations of compound (thoracic skin beneath the patch) in cats (N=8) after transdermal application

Quantitative value

211

Ko; Maxwell; Abbo; Weil; Journal of Veterinary Pharmacology and Therapeutics; vol. 31; nb. 4; (2008); p. 359 - 367, View in Reaxys 762 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Bioavailability of compound in cats

Biological Species/NCBI ID

domestic cat

Substance RN

3917968View in Reaxys

Qualitative Results

6.3 +/- 2.7

Measurement Parameter

F (drug bioavailability)

Unit

Measurement Object

Bioavailability

Quantitative value

6.3

Ko; Maxwell; Abbo; Weil; Journal of Veterinary Pharmacology and Therapeutics; vol. 31; nb. 4; (2008); p. 359 - 367, View in Reaxys 763 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Time taken to reach maximum concentration of compound metabolite (monoethylglycinexylidide) in pregnant women (N=6) with gestational diabetes mellitus upon administration of 200 mg

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

193.14

Measurement Parameter

tmax

Unit

minute

336/467

2018-05-14 08:43:54

Measurement Object

Time taken to reach maximum concentration

Quantitative value

193.14

Pharmacokinetic

Bioassay Details

Maximum plasma concentration in pregnant women (N=10) upon administration of 200 mg of 2 compound

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

879.11

Measurement Parameter

Cmax

Unit

ng/mL

Measurement Object

Maximum plasma concentration

Quantitative value

879.11

Pharmacokinetic

Bioassay Details

Rate absorption of compound in cats (N=8) at 12-72 h after transdermal application of 700 mg patch

Biological Species/NCBI ID

domestic cat

Substance RN

3917968View in Reaxys

Qualitative Results

109 +/- 49

Measurement Parameter

qualitative

Measurement Object

Absorption rate

Ko; Maxwell; Abbo; Weil; Journal of Veterinary Pharmacology and Therapeutics; vol. 31; nb. 4; (2008); p. 359 - 367, View in Reaxys 766 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Area under time curve concentration in pregnant women (N=10) upon administration of 200 mg of 2 compound

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

256.01

Measurement Parameter

AUC (0-inf)

Unit

µg.min/mL

Measurement Object

Area under plasma concentration time curve

Quantitative value

256.01

Metabolism/Transport

Bioassay Details

Clearance of compound in pregnant women (N=10) upon administration of 200 mg

Biological Species/NCBI ID

human

337/467

2018-05-14 08:43:54

Substance RN

3917968View in Reaxys

Qualitative Results

10.61

Measurement Parameter

CL (drug clearance)

Unit

mL/min/kg

Measurement Object

Clearance

Quantitative value

10.61

Pharmacokinetic

Bioassay Details

Maximum concentration of compound metabolite (monoethylglycinexylidide) in pregnant women (N=10) upon administration of 200 mg

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

82.71

Measurement Parameter

Cmax

Unit

ng/mL

Measurement Object

Maximum concentration of compound metabolite (monoethylglycinexylidide)

Quantitative value

82.71

Metabolism/Transport

Bioassay Details

Volume of distribution of compound in pregnant women (N=10) upon administration of 200 mg

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

3.26

Measurement Parameter

Vd/F

Unit

L/kg

Measurement Object

Volume of distribution

Quantitative value

3.26

Metabolism/Transport

Bioassay Details

Distribution half life of compound (monoethylglycinexylidide (MEGX)) in pregnant women (N=10) upon administration of 200 mg

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

7.64

Measurement Parameter

t1/2

Unit

minute

Measurement Object

Distribution half life

Quantitative value

7.64

338/467

2018-05-14 08:43:54

Pharmacokinetic

Bioassay Details

Time taken to reach maximum concentration of compound metabolite (monoethylglycinexylidide) in pregnant women (N=10) upon administration of 200 mg

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

44.71

Measurement Parameter

tmax

Unit

minute

Measurement Object

Maximum concentration of compound

Quantitative value

44.71

Pharmacokinetic

Bioassay Details

Area under time curve concentration of compound metabolite (monoethylglycinexylidide) in pregnant women (N=10) upon administration of 200 mg

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

29.91

Measurement Parameter

AUC (0-inf)

Unit

µg.min/mL

Measurement Object

Area under time curve concentration

Quantitative value

29.91

Pharmacokinetic

Bioassay Details

Steady-state plasma concentration of compound metabolite (monoethylglycinexylidide) in cats (N=8) at 12-72 h after transdermal application of 700 mg patch

Biological Species/NCBI ID

domestic cat

Substance RN

3917968View in Reaxys

Substance Route of Adm.

transdermal administration

Qualitative Results

0.012 +/- 0.009

Measurement Parameter

Cmax

Unit

µg/mL

Measurement Object

Steady-state plasma concentration

Quantitative value

0.012

Ko; Maxwell; Abbo; Weil; Journal of Veterinary Pharmacology and Therapeutics; vol. 31; nb. 4; (2008); p. 359 - 367, View in Reaxys 774 of 1220 Bioassay Category Bioassay Details

Pharmacokinetic Maximum concentration of compound metabolite (monoethylglycinexylidide) in pregnant women (N=6) with gestational diabetes mellitus upon administration of 200 mg

339/467

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Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

141.38

Measurement Parameter

Cmax

Unit

ng/mL

Measurement Object

Maximum concentration

Quantitative value

141.38

Pharmacokinetic

Bioassay Details

Steady-state plasma concentration of compound in cats (N=8) at 12-72 h after transdermal application of 700 mg patch

Biological Species/NCBI ID

domestic cat

Substance RN

3917968View in Reaxys

Substance Route of Adm.

transdermal administration

Qualitative Results

0.083 +/- 0.032

Measurement Parameter

Cmax

Unit

µg/mL

Measurement Object

Steady-state plasma concentration

Quantitative value

0.083

Ko; Maxwell; Abbo; Weil; Journal of Veterinary Pharmacology and Therapeutics; vol. 31; nb. 4; (2008); p. 359 - 367, View in Reaxys 776 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Maximum plasma concentration in pregnant women with estational diabetes mellitus (N=6) upon administration of 200 mg of 2 compound

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

1145.58

Measurement Parameter

Cmax

Unit

ng/mL

Measurement Object

Maximum plasma concentration

Quantitative value

1145.58

Pharmacokinetic

Bioassay Details

Area under time curve concentration in pregnant women (N=6) with gestational diabetes mellitus upon administration of 200 mg of 2 compound

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

455.95

Measurement Parameter

AUC (0-inf)

340/467

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Unit

µg.min/mL

Measurement Object

Area under time curve concentration

Quantitative value

455.95

Metabolism/Transport

Bioassay Details

Clearance of compound in pregnant women (N=6) with gestational diabetes mellitus upon administration of 200 mg

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

5.64

Measurement Parameter

Cl/F

Unit

mL/min/kg

Measurement Object

Clearance

Quantitative value

5.64

Pharmacokinetic

Bioassay Details

Area under time curve concentration of compound metabolite (monoethylglycinexylidide) in pregnant women (N=6) with gestational diabetes mellitus upon administration of 200 mg

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

108.23

Measurement Parameter

AUC (0-inf)

Unit

µg.min/mL

Quantitative value

108.23

Inhibitor

Bioassay Category

Metabolism/Transport

Bioassay Details

Volume of distribution of compound in pregnant women (N=6) with gestational diabetes mellitus upon administration of 200 mg

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

2.19

Measurement Parameter

Vd/F

Unit

L/kg

Quantitative value

2.19

341/467

2018-05-14 08:43:54

781 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Time taken to reach maximum plasma concentration of compound in human at 0-24 h following dermal application in the form of patch

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Measurement Parameter

tmax

Unit

hour

Measurement Object

Time taken to reach maximum plasma concentration

Qualitative value

Quantitative value

11.6

Deviation

2.97

, View in Reaxys 782 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Absorption of compound in human following 12 h of dermal application in the form of patch

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

topical administration

Measurement Parameter

Absorption

Unit

Measurement Object

absorption

Qualitative value

Quantitative value

Deviation

1.6

, View in Reaxys 783 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Time taken to reach maximum plasma concentration of compound in patients with herpes zoster following dermal application in the form of patch

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Measurement Parameter

tmax

Unit

hour

Measurement Object

Time taken to reach maximum plasma concentration

Qualitative value

Quantitative value

13.3

Deviation

1.58

, View in Reaxys 784 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Maximum plasma concentration of compound in healthy volunteers following dermal administration in the form of patch

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

342/467

2018-05-14 08:43:54

Substance Route of Adm.

topical administration

Measurement Parameter

Cmax

Unit

ng/mL

Measurement Object

Maximum plasma concentration

Qualitative value

Quantitative value

127.8

Deviation

63.3

, View in Reaxys 785 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Maximum plasma concentration of compound in human at 49.5-72 h following dermal administration in the form of patch

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

topical administration

Measurement Parameter

qualitative

Measurement Object

Maximum plasma concentration

Qualitative value

Not Published

, View in Reaxys 786 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Absorption of compound in human following 36 h of dermal application in the form of patch

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

topical administration

Measurement Parameter

Absorption

Unit

Measurement Object

absorption

Qualitative value

Quantitative value

Deviation

1.2

, View in Reaxys 787 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Mean clearance of compound in human following intravenous administration

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Measurement Parameter

CL (drug clearance)

Unit

L/min

Measurement Object

Mean clearance

Qualitative value

Quantitative value

0.635

Deviation

0.175

343/467

2018-05-14 08:43:54

, View in Reaxys 788 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Absorption of compound in human

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Measurement Parameter

Absorption

Unit

Measurement Object

absorption

Qualitative value

Quantitative value

, View in Reaxys 789 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Absorption of compound in human following 36 h of dermal application in the form of patch

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

topical administration

Measurement Parameter

Absorption

Unit

µg

Measurement Object

absorption

Qualitative value

Quantitative value

188170

Deviation

72249.5

, View in Reaxys 790 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Time taken to reach maximum plasma concentration of compound in human following dermal application in the form of patch

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Measurement Parameter

tmax

Unit

hour

Measurement Object

Time taken to reach maximum plasma concentration

Qualitative value

Quantitative value

11.2

Deviation

1.78

, View in Reaxys 791 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Maximum plasma concentration of compound in patients with herpes zoster following dermal administration in the form of patch

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

topical administration

344/467

2018-05-14 08:43:54

Measurement Parameter

Cmax

Unit

ng/mL

Measurement Object

Maximum plasma concentration

Qualitative value

Quantitative value

82.5

Deviation

43.3

, View in Reaxys 792 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Time taken to reach maximum plasma concentration of compound in human at 49.5-72 h following dermal application in the form of patch

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Measurement Parameter

tmax

Unit

hour

Measurement Object

Time taken to reach maximum plasma concentration

Qualitative value

Quantitative value

Deviation

2.17

, View in Reaxys 793 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Terminal half life of compound in human following intravenous administration

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Measurement Parameter

t1/2 el

Unit

minute

Measurement Object

Terminal half life

Qualitative value

Quantitative value

106.9

Deviation

, View in Reaxys 794 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Time taken to reach maximum plasma concentration of compound in human at 25.5-48 h following dermal application in the form of patch

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Measurement Parameter

tmax

Unit

hour

Measurement Object

Time taken to reach maximum plasma concentration

Qualitative value

Quantitative value

35.2

345/467

2018-05-14 08:43:54

Deviation

2.65

, View in Reaxys 795 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Maximum plasma concentration of compound in human at 25.5-48 h following dermal administration in the form of patch

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

topical administration

Measurement Parameter

qualitative

Measurement Object

Maximum plasma concentration

Qualitative value

Not Published

, View in Reaxys 796 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Maximum plasma concentration of compound in human at 0-24 h following dermal administration in the form of patch

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

topical administration

Measurement Parameter

qualitative

Measurement Object

Maximum plasma concentration

Qualitative value

Not Published

, View in Reaxys 797 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Minimum plasma concentration of compound in human following dermal administration in the form of patch

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Measurement Parameter

Cmin

Unit

ng/mL

Measurement Object

Minimum plasma concentration

Qualitative value

Quantitative value

, View in Reaxys 798 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Absorption of compound in human following 12 h of dermal application in the form of patch

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

topical administration

Measurement Parameter

Absorption

Unit

µg

Measurement Object

absorption

346/467

2018-05-14 08:43:54

Qualitative value

Quantitative value

63772.9

Deviation

32468.9

, View in Reaxys 799 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Absorption (flux) of compound in human following 12 h of dermal application in the form of patch

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

topical administration

Qualitative Results

Absorption not calculated

Measurement Parameter

qualitative

Measurement Object

absorption

, View in Reaxys 800 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Area under plasma concentration curve of compound in human following intravenous infusion

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Measurement Parameter

qualitative

Measurement Object

Area under plasma concentration curve

Qualitative value

Not Published

, View in Reaxys 801 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Time taken to reach maximum plasma concentration of compound in patients with herpetic neuralgia following dermal application in the form of patch

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Measurement Parameter

tmax

Unit

hour

Measurement Object

Time taken to reach maximum plasma concentration

Qualitative value

Quantitative value

13.9

Deviation

5.54

, View in Reaxys 802 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Area under plasma concentration curve of compound in human 12 h following dermal application in the form of patch

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Measurement Parameter

qualitative

Measurement Object

Area under plasma concentration curve

347/467

2018-05-14 08:43:54

Qualitative value

Not Published

, View in Reaxys 803 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Absorption (flux) of compound in human following 36 h of dermal application in the form of patch

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

topical administration

Qualitative Results

Absorption not calculated

Measurement Parameter

qualitative

Measurement Object

absorption

, View in Reaxys 804 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Maximum plasma concentration of compound in human

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Measurement Parameter

Cmax

Unit

ng/mL

Qualitative value

Quantitative value

128

, View in Reaxys 805 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Area under plasma concentration curve of compound in human 36 h (3x12 h) following dermal application in the form of patch

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Measurement Parameter

qualitative

Measurement Object

Area under plasma concentration curve

Qualitative value

Not Published

, View in Reaxys 806 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Maximum plasma concentration of compound in patients with post herpetic neuralgia following dermal administration in the form of patch

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

topical administration

Measurement Parameter

Cmax

Unit

ng/mL

Measurement Object

Maximum plasma concentration

Qualitative value

Quantitative value

52.1

Deviation

30.6

348/467

2018-05-14 08:43:54

, View in Reaxys 807 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Maximum plasma concentration of compound in human following dermal administration in the form of patch

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

topical administration

Measurement Parameter

Cmax

Unit

ng/mL

Measurement Object

Maximum plasma concentration

Qualitative value

Quantitative value

277

, View in Reaxys 808 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Percent of mice to be fatal from chloroform induced cardiac arrhythmias at the dose of 70.58 mg/kg in 40 mice

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Unit

Qualitative value

Quantitative value

Graeff; Johnson; Saint Dennis; Martin; Journal of medicinal chemistry; vol. 14; nb. 1; (1971); p. 60 - 62, View in Reaxys 809 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Average heart rate of mice in chloroform induced cardiac arrhythmia condition upon compound administration at 70.58 mg/kg; n= 40

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Qualitative Results

Rate not calculated

Measurement Parameter

qualitative

Measurement Object

Rate

Graeff; Johnson; Saint Dennis; Martin; Journal of medicinal chemistry; vol. 14; nb. 1; (1971); p. 60 - 62, View in Reaxys 810 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Normalized duration of anesthetic activity of the compound (2.0 as base) was measured and compared with Lidocaine by rat sciatic nerve block method, at pH 6.4

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Qualitative Results

Normalized duration not calculated

Measurement Parameter

qualitative

Measurement Object

Normalized duration

McKenzie; Foye; Journal of medicinal chemistry; vol. 15; nb. 3; (1972); p. 291 - 295, View in Reaxys 811 of 1220 Bioassay Category

In Vitro (Efficacy)

349/467

2018-05-14 08:43:54

Bioassay Details

Compound was evaluated for its local irritation relative to lidocaine in rabbit; denotes weak irritation

Biological Species/NCBI ID

Leporidae

Substance RN

3917968View in Reaxys

Measurement Parameter

qualitative

Qualitative value

Not Published

Akerman; Lars; Nilsson; Sievertsson; Dahlbom; Journal of medicinal chemistry; vol. 14; nb. 8; (1971); p. 710 - 714, View in Reaxys 812 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested to determine duration of anesthetic activity of the compound (2.0 as base) by rat sciatic nerve block method, at pH 6.4

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

time

Unit

minute

Qualitative value

Quantitative value

169

McKenzie; Foye; Journal of medicinal chemistry; vol. 15; nb. 3; (1972); p. 291 - 295, View in Reaxys 813 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Percent of mice protected from chloroform induced cardiac arrhythmias at the dose of 70.58 mg/kg in 40 mice

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Unit

Qualitative value

Quantitative value

56.7

Graeff; Johnson; Saint Dennis; Martin; Journal of medicinal chemistry; vol. 14; nb. 1; (1971); p. 60 - 62, View in Reaxys 814 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Effect of the compound in sciatic nerve block evaluated in vitro in frog relative to lidocaine

Biological Species/NCBI ID

Anura

Substance RN

3917968View in Reaxys

Qualitative Results

Sciatic nerve block not calculated

Measurement Parameter

qualitative

Measurement Object

Sciatic nerve block

Akerman; Lars; Nilsson; Sievertsson; Dahlbom; Journal of medicinal chemistry; vol. 14; nb. 8; (1971); p. 710 - 714, View in Reaxys 815 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Ratio of per cent loss of corneal reflex of the compound to that of lidocaine

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

350/467

2018-05-14 08:43:54

Measurement Parameter

ratio

Quantitative value

Sharma; Mital; Banerjee; Journal of medicinal chemistry; vol. 14; nb. 1; (1971); p. 68 - 70, View in Reaxys 816 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Percent surface local anesthetic activity of the compound was evaluated in guinea pig

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Unit

Measurement Object

Percent surface local anesthetic activity

Qualitative value

Quantitative value

Casadio; Pala; Bruzzese; Turba; Marazzi-Uberti; Journal of medicinal chemistry; vol. 13; nb. 3; (1970); p. 418 - 421, View in Reaxys 817 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Percent of mice protected from chloroform induced cardiac arrhythmia upon compound administration at 70.58 mg/kg; n= 40

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

percentage

Unit

Measurement Object

protected animals

Qualitative value

Quantitative value

56.7

Graeff; Johnson; Saint Dennis; Martin; Journal of medicinal chemistry; vol. 14; nb. 1; (1971); p. 60 - 62, View in Reaxys 818 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Local anesthetic effect in sciatic nerve block by 2 of compound expressed as duration of hind limb paralysis in guinea pig

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Measurement Parameter

time

Unit

minute

Qualitative value

Quantitative value

Akerman; Lars; Nilsson; Sievertsson; Dahlbom; Journal of medicinal chemistry; vol. 14; nb. 8; (1971); p. 710 - 714, View in Reaxys 819 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested for duration of corneal anesthesia in rabbit (concentration of the base 2); 6-14

Biological Species/NCBI ID

Leporidae

Cells/Cell Lines

cornea cell

Substance RN

3917968View in Reaxys

351/467

2018-05-14 08:43:54

Measurement Parameter

time

Unit

minute

Qualitative value

Quantitative value

Abou-ouf; Youssef; Kader; Journal of medicinal chemistry; vol. 14; nb. 5; (1971); p. 443 - 445, View in Reaxys 820 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested for per cent loss of corneal reflex in guinea pigs

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Measurement Parameter

percentage

Unit

Measurement Object

ME50

Qualitative value

Quantitative value

0.05

Sharma; Mital; Banerjee; Journal of medicinal chemistry; vol. 14; nb. 1; (1971); p. 68 - 70, View in Reaxys 821 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Normalized index in comparison with irritation index of the lidocaine (2.0 as base) was measured by rabbit intradermal wheal method, at pH 7.0

Biological Species/NCBI ID

Leporidae

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Measurement Object

Irritation index

Quantitative value

McKenzie; Foye; Journal of medicinal chemistry; vol. 15; nb. 3; (1972); p. 291 - 295, View in Reaxys 822 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Local anesthetic effect for peridural anesthesia by 2 of compound expressed as duration of hind limb paralysis in guinea pig

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Measurement Parameter

time

Unit

minute

Qualitative value

Quantitative value

Akerman; Lars; Nilsson; Sievertsson; Dahlbom; Journal of medicinal chemistry; vol. 14; nb. 8; (1971); p. 710 - 714, View in Reaxys 823 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Toxicity of the compound was determined in mice (male albino) by iv administration

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Qualitative Results

352/467

2018-05-14 08:43:54

Measurement Parameter

Toxicity

Measurement Object

Toxicity

Quantitative value

Akerman; Lars; Nilsson; Sievertsson; Dahlbom; Journal of medicinal chemistry; vol. 14; nb. 8; (1971); p. 710 - 714, View in Reaxys 824 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Details

Local anesthetic activity of the compound was determined in mouse after subcutaneous administration at a dose of 10 mg/ml

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

subcutaneous administration

Measurement Parameter

Activity

Unit

Qualitative value

Quantitative value

100

Pala; Donetti; Mantegani; Bianchi; Journal of medicinal chemistry; vol. 14; nb. 9; (1971); p. 896 - 897, View in Reaxys 825 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested to determine duration of anesthetic activity of the compound (2.0 as base) by guinea pig intradermal wheal method, at pH 6.9

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Measurement Parameter

time

Unit

minute

Qualitative value

Quantitative value

McKenzie; Foye; Journal of medicinal chemistry; vol. 15; nb. 3; (1972); p. 291 - 295, View in Reaxys 826 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Details

Side effects liability was assessed in the rats 8 hr after the initial injection and was recorded during next 24 hours.

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Measurement Parameter

ED50

Unit

Qualitative value

Quantitative value

2.5

Hermans; Verhoeven; Janssen; Journal of medicinal chemistry; vol. 13; nb. 5; (1970); p. 835 - 838, View in Reaxys 827 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Effect of the compound on average heart rate in chloroform induced cardiac arrhythmias at the dose of 70.58 mg/kg in 40 mice

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

353/467

2018-05-14 08:43:54

Qualitative Results

Average heart rate not calculated

Measurement Parameter

qualitative

Measurement Object

Average heart rate

Graeff; Johnson; Saint Dennis; Martin; Journal of medicinal chemistry; vol. 14; nb. 1; (1971); p. 60 - 62, View in Reaxys 828 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Normalized duration of anesthetic activity of the compound (2.0 as base) was measured and compared with Lidocaine by guinea pig intradermal wheal method, at pH 6.9

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Qualitative Results

Normalized duration not calculated

Measurement Parameter

qualitative

Measurement Object

Normalized duration

McKenzie; Foye; Journal of medicinal chemistry; vol. 15; nb. 3; (1972); p. 291 - 295, View in Reaxys 829 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested for its ability to produce complete loss of blink reflex in guinea pigs

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Measurement Parameter

percentage

Unit

Measurement Object

Minimum effective concentration

Qualitative value

Quantitative value

0.07

Sharma; Mital; Banerjee; Journal of medicinal chemistry; vol. 14; nb. 1; (1971); p. 68 - 70, View in Reaxys 830 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested to determine onset of anesthetic activity of the compound (2.0 as base) by guinea pig intradermal wheal method, at pH 6.9

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Unit

minute

Measurement Object

Onset

Qualitative value

Quantitative value

McKenzie; Foye; Journal of medicinal chemistry; vol. 15; nb. 3; (1972); p. 291 - 295, View in Reaxys 831 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Details

Effect of the compound in sciatic nerve block evaluated in vivo in guinea pig/rat, 0.2ml injected at the hip relative to lidocaine

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Qualitative Results

Sciatic nerve block not calculated

354/467

2018-05-14 08:43:54

Measurement Parameter

qualitative

Measurement Object

Sciatic nerve block

Akerman; Lars; Nilsson; Sievertsson; Dahlbom; Journal of medicinal chemistry; vol. 14; nb. 8; (1971); p. 710 - 714, View in Reaxys 832 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Potency of the compound with reference to lidocaine at 0.2 concentration after 14.83 min was tested in guinea pig

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Quantitative value

Srivastava; Journal of medicinal chemistry; vol. 13; nb. 2; (1970); p. 304 - 305, View in Reaxys 833 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Percent surface local anesthetic activity of the compound was evaluated in guinea pig.

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Unit

Qualitative value

Quantitative value

Casadio; Pala; Bruzzese; Turba; Marazzi-Uberti; Journal of medicinal chemistry; vol. 13; nb. 3; (1970); p. 418 - 421, View in Reaxys 834 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

In vivo hepatic intrinsic clearance of the compound in rat upon intravenous administration

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Qualitative Results

591

Measurement Parameter

CLint

Unit

mL/min/kg

Quantitative value

591

Hermans; Verhoeven; Janssen; Journal of medicinal chemistry; vol. 13; nb. 5; (1970); p. 835 - 838, View in Reaxys 835 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Tested for concentration in saline that block the sciatic nerve of frog for 2 hr

Biological Species/NCBI ID

Anura

Substance RN

3917968View in Reaxys

Measurement Parameter

concentration (parameters)

Unit

Qualitative value

Quantitative value

0.5

Stubbins; Journal of medicinal chemistry; vol. 13; nb. 3; (1970); p. 558 - 559, View in Reaxys

355/467

2018-05-14 08:43:54

836 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Irritancy was assessed by measuring the swelling of the hindpaw after local injection in rats;(+) = Present

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Measurement Object

Irritancy

Qualitative value

Hermans; Verhoeven; Janssen; Journal of medicinal chemistry; vol. 13; nb. 5; (1970); p. 835 - 838, View in Reaxys 837 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Percent surface anaesthesia on the guinea pig cornea, at 0.2 concentration after 14.83 min

Biological Species/NCBI ID

guinea pig

Cells/Cell Lines

cornea cell

Substance RN

3917968View in Reaxys

Measurement Parameter

percentage

Unit

Measurement Object

Anesthetic activity

Qualitative value

Quantitative value

100

Srivastava; Journal of medicinal chemistry; vol. 13; nb. 2; (1970); p. 304 - 305, View in Reaxys 838 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Details

Local anesthetic activity of the compound was evaluated in mouse at a concentration of 10mg/ml administered subcutaneously

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

subcutaneous administration

Measurement Parameter

Activity

Unit

Qualitative value

Quantitative value

100

Pala; Donetti; Mantegani; Bianchi; Journal of medicinal chemistry; vol. 14; nb. 9; (1971); p. 896 - 897, View in Reaxys 839 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Tested for concentration in saline that abolish pain sensation for about 24 hr in the guinea pig intradermal wheal test

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Measurement Parameter

concentration (parameters)

Unit

Qualitative value

Quantitative value

0.5

Stubbins; Journal of medicinal chemistry; vol. 13; nb. 3; (1970); p. 558 - 559, View in Reaxys

356/467

2018-05-14 08:43:54

840 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Tested for the concentration in saline produces corneal anaesthesia in rabbits lasting for hours

Biological Species/NCBI ID

Leporidae

Cells/Cell Lines

cornea cell

Substance RN

3917968View in Reaxys

Measurement Parameter

concentration (parameters)

Unit

Qualitative value

Quantitative value

0.5

Stubbins; Journal of medicinal chemistry; vol. 13; nb. 3; (1970); p. 558 - 559, View in Reaxys 841 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Tested for the concentration that reverse the blockade by procaine in rat at 1 concentration; 0.02-0.03

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

concentration (parameters)

Unit

Qualitative value

Quantitative value

0.02

Stubbins; Journal of medicinal chemistry; vol. 13; nb. 3; (1970); p. 558 - 559, View in Reaxys 842 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Local anesthetic effect in sciatic nerve block by 2 of compound in presence of 1:200000 of epinephrine expressed as duration of hind limb paralysis in guinea pig

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Measurement Parameter

time

Unit

minute

Measurement Object

Hind limb paralysis

Qualitative value

Quantitative value

108

Concomitants: Compound name

Epinephrine

Concomitants: Compound role

COM

Akerman; Lars; Nilsson; Sievertsson; Dahlbom; Journal of medicinal chemistry; vol. 14; nb. 8; (1971); p. 710 - 714, View in Reaxys 843 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Plasma clearance of the compound in rat upon intravenous administration

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Qualitative Results

357/467

2018-05-14 08:43:54

Measurement Parameter

CL (drug clearance)

Unit

mL/min/kg

Measurement Object

Plasma clearance

Quantitative value

Hermans; Verhoeven; Janssen; Journal of medicinal chemistry; vol. 13; nb. 5; (1970); p. 835 - 838, View in Reaxys 844 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Tested for the concentration that block the indirectly elicited twitch of the rat phrenic nerve diaphragm preparation; 0.02-0.03

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

concentration (parameters)

Unit

Qualitative value

Quantitative value

0.02

Stubbins; Journal of medicinal chemistry; vol. 13; nb. 3; (1970); p. 558 - 559, View in Reaxys 845 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Tested for the concentration that block contractions of rat stomach fundus strip smooth muscles for 4 hr

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

concentration (parameters)

Unit

µg/mL

Qualitative value

Quantitative value

100

Stubbins; Journal of medicinal chemistry; vol. 13; nb. 3; (1970); p. 558 - 559, View in Reaxys 846 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Effect of the compound tested for Corneal anesthesia in rabbit,2.0.25ml applied for 0.5min relative to lidocaine

Biological Species/NCBI ID

Leporidae

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Measurement Object

Corneal anaesthesia

Quantitative value

Akerman; Lars; Nilsson; Sievertsson; Dahlbom; Journal of medicinal chemistry; vol. 14; nb. 8; (1971); p. 710 - 714, View in Reaxys 847 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested to determine onset of anesthetic activity of the compound (2.0 as base) by rat sciatic nerve block method, at pH 6.4

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Unit

minute

358/467

2018-05-14 08:43:54

Measurement Object

Onset

Qualitative value

Quantitative value

McKenzie; Foye; Journal of medicinal chemistry; vol. 15; nb. 3; (1972); p. 291 - 295, View in Reaxys 848 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Tested for the concentration that block contractions of guinea pig ileum smooth muscles for 4 hr

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Measurement Parameter

concentration (parameters)

Unit

µg/mL

Qualitative value

Quantitative value

100

Stubbins; Journal of medicinal chemistry; vol. 13; nb. 3; (1970); p. 558 - 559, View in Reaxys 849 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Tested for the concentration that block contractions of rabbit aortic strip smooth muscles for 4 hr

Biological Species/NCBI ID

Leporidae

Substance RN

3917968View in Reaxys

Measurement Parameter

concentration (parameters)

Unit

µg/mL

Qualitative value

Quantitative value

100

Stubbins; Journal of medicinal chemistry; vol. 13; nb. 3; (1970); p. 558 - 559, View in Reaxys 850 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Percent fatal activity was measured in mice upon compound administration at 70.58 mg/kg; n= 40

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Unit

Measurement Object

Percent fatal activity was measured in mice

Qualitative value

Quantitative value

Graeff; Johnson; Saint Dennis; Martin; Journal of medicinal chemistry; vol. 14; nb. 1; (1971); p. 60 - 62, View in Reaxys 851 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Toxicity was measured in mice upon compound administration at 70.58 mg/kg; n= 40

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

Toxicity

Unit

Measurement Object

Toxicity

Qualitative value

359/467

2018-05-14 08:43:54

Quantitative value

86.7

Graeff; Johnson; Saint Dennis; Martin; Journal of medicinal chemistry; vol. 14; nb. 1; (1971); p. 60 - 62, View in Reaxys 852 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Tested for concentration in saline that block axonal conduction of squid nerves for many hours even after repeated washing

Cells/Cell Lines

nerve cell

Substance RN

3917968View in Reaxys

Measurement Parameter

concentration (parameters)

Unit

Qualitative value

Quantitative value

0.5

Stubbins; Journal of medicinal chemistry; vol. 13; nb. 3; (1970); p. 558 - 559, View in Reaxys 853 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Local anesthetic effect if or peridural anesthesia by 2 of compound in presence of 1:200000 of epinephrine expressed as duration of hind limb paralysis in guinea pig

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Measurement Parameter

time

Unit

minute

Measurement Object

Hind limb paralysis

Qualitative value

Quantitative value

Akerman; Lars; Nilsson; Sievertsson; Dahlbom; Journal of medicinal chemistry; vol. 14; nb. 8; (1971); p. 710 - 714, View in Reaxys 854 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Anesthetic activity was assessed by measuring the rapidity of response to a noxious stimulus applied to the hind 5 cm of the tail.

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

ED50

Unit

Measurement Object

Rapidity of response to a noxious stimulus applied to the hind 5 cm of the tail

Qualitative value

Quantitative value

Hermans; Verhoeven; Janssen; Journal of medicinal chemistry; vol. 13; nb. 5; (1970); p. 835 - 838, View in Reaxys 855 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Intradermal anaesthesia (block anaesthesia) in guinea pig, at 0.2 concentration after 44.10 min was tested in guinea pig

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Measurement Parameter

percentage

Unit

Measurement Object

Anesthetic activity

360/467

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Qualitative value

Quantitative value

98.33

Srivastava; Journal of medicinal chemistry; vol. 13; nb. 2; (1970); p. 304 - 305, View in Reaxys 856 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

LD50 of the compund was determined in mice (male albino) by sc administration

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

subcutaneous administration

Qualitative Results

265

Measurement Parameter

LD50

Unit

mg/kg

Quantitative value

265

Akerman; Lars; Nilsson; Sievertsson; Dahlbom; Journal of medicinal chemistry; vol. 14; nb. 8; (1971); p. 710 - 714, View in Reaxys 857 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lethal dose of the compound in rabbit upon intravenous administration

Biological Species/NCBI ID

Leporidae

Substance RN

3917968View in Reaxys

Qualitative Results

25.6

Measurement Parameter

LD50

Unit

mg/kg

Quantitative value

25.6

Drugs Jap.; vol. 6; (1982); p. 879, View in Reaxys 858 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lowest toxic dose of the compound in man upon i.v. administration

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Qualitative Results

Measurement Parameter

TDLo

Unit

mg/kg

Measurement Object

Lowest toxic dose

Quantitative value

Hilleman; Mohiuddin; Destache; Drug Intelligence and Clinical Pharmacy; vol. 19; nb. 9; (1985); p. 669 - 673, View in Reaxys 859 of 1220 Substance Effect

Toxic

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lowest toxic dose of the compound in human upon p.o. administration

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

oral administration

361/467

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Qualitative Results

1632

Measurement Parameter

TDLo

Unit

mg/kg

Measurement Object

Toxic dose

Quantitative value

1632

Mofenson; Caraccio; Miller; Greensher; Clinical Pediatrics; vol. 22; nb. 3; (1983); p. 190 - 192, View in Reaxys 860 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lethal dose of the compound in mouse upon i.m. administration

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intramuscular administration

Qualitative Results

117

Measurement Parameter

LD50

Unit

mg/kg

Measurement Object

Lethal dose

Quantitative value

117

Drug development research; vol. 21; (1990); p. 277, View in Reaxys 861 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lowest toxic dose of the compound in man upon i.v. administration

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Qualitative Results

7.143

Measurement Parameter

TDLo

Unit

mg/kg

Measurement Object

Lowest toxic dose

Quantitative value

7.143

Marriott; Bieza; Chest; vol. 61; nb. 7; (1972); p. 682 - 683, View in Reaxys 862 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

A score1 for a direct tail withdrawal between 6 and 10 sec.

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

score

Measurement Object

Score

Quantitative value

Van Bever; Knaeps; Willems; Hermans; Janssen; Journal of medicinal chemistry; vol. 16; nb. 4; (1973); p. 394 - 397, View in Reaxys 863 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Duration of dose administered for local anaesthesia

Biological Species/NCBI ID

Rattus norvegicus

362/467

2018-05-14 08:43:54

Substance RN

3917968View in Reaxys

Measurement Parameter

time

Unit

minute

Qualitative value

Quantitative value

Van Bever; Knaeps; Willems; Hermans; Janssen; Journal of medicinal chemistry; vol. 16; nb. 4; (1973); p. 394 - 397, View in Reaxys 864 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Duration of dose administered for local anaesthesia

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

time

Unit

minute

Qualitative value

Quantitative value

Van Bever; Knaeps; Willems; Hermans; Janssen; Journal of medicinal chemistry; vol. 16; nb. 4; (1973); p. 394 - 397, View in Reaxys 865 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Duration of dose administered for local anaesthesia

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

time

Unit

minute

Qualitative value

Quantitative value

Van Bever; Knaeps; Willems; Hermans; Janssen; Journal of medicinal chemistry; vol. 16; nb. 4; (1973); p. 394 - 397, View in Reaxys 866 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Duration of dose administered for local anaesthesia

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

time

Unit

minute

Qualitative value

Quantitative value

Van Bever; Knaeps; Willems; Hermans; Janssen; Journal of medicinal chemistry; vol. 16; nb. 4; (1973); p. 394 - 397, View in Reaxys 867 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested in vitro for local anesthetic activity against sciatic nerve of frog.(relative values, lidocaine=1)

Biological Species/NCBI ID

Anura

Substance RN

3917968View in Reaxys

363/467

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Qualitative Results

Rate of block not calculated

Measurement Parameter

qualitative

Measurement Object

Rate of block

Kronberg; Leard; Takman; Journal of medicinal chemistry; vol. 16; nb. 6; (1973); p. 739 - 743, View in Reaxys 868 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Details

Prevention of chloroform-induced ventricular fibrillation in the mouse upon p.o. administration

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

oral administration

Measurement Parameter

ED50

Unit

µM/kg

Qualitative value

Quantitative value

495

Banitt; Coyne; Schmid; Mendel; Journal of Medicinal Chemistry; vol. 18; nb. 11; (1975); p. 1130 - 1134, View in Reaxys 869 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Concentration required to produce nerve blockage at duration of 90 minutes in cat was determined

Biological Species/NCBI ID

domestic cat

Substance RN

3917968View in Reaxys

Measurement Parameter

MEC

Unit

Qualitative value

Quantitative value

Rastogi; Anand; Gupta; Sharma; Journal of Medicinal Chemistry; vol. 16; nb. 7; (1973); p. 797 - 804, View in Reaxys 870 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Duration of dose administered for local anaesthesia in rats

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

time

Unit

minute

Qualitative value

Quantitative value

Van Bever; Knaeps; Willems; Hermans; Janssen; Journal of medicinal chemistry; vol. 16; nb. 4; (1973); p. 394 - 397, View in Reaxys 871 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Number of animals with positive response at the dose of 20mg/ml for local anaesthesia out of 15 animals

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Measurement Object

Anesthetic activity

Quantitative value

364/467

2018-05-14 08:43:54

Van Bever; Knaeps; Willems; Hermans; Janssen; Journal of medicinal chemistry; vol. 16; nb. 4; (1973); p. 394 - 397, View in Reaxys 872 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

A score 3 (subsurgical analgesia) for a slow reaction time exceeding 10 sec.

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

score

Measurement Object

Score

Quantitative value

Van Bever; Knaeps; Willems; Hermans; Janssen; Journal of medicinal chemistry; vol. 16; nb. 4; (1973); p. 394 - 397, View in Reaxys 873 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

A score 3 (subsurgical analgesia) for a slow reaction time exceeding 10 sec.

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

score

Measurement Object

Score

Quantitative value

Van Bever; Knaeps; Willems; Hermans; Janssen; Journal of medicinal chemistry; vol. 16; nb. 4; (1973); p. 394 - 397, View in Reaxys 874 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Acute toxicity was determined in mouse by ip administration

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Qualitative Results

105

Measurement Parameter

TD (toxic dose)

Unit

mg/kg

Measurement Object

Acute toxicity

Quantitative value

105

Kronberg; Leard; Takman; Journal of medicinal chemistry; vol. 16; nb. 6; (1973); p. 739 - 743, View in Reaxys 875 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Number of animals with positive response at the dose of 5.0mg/ml for local anaesthesia out of 10 animals

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Measurement Object

Anesthetic activity

Quantitative value

Van Bever; Knaeps; Willems; Hermans; Janssen; Journal of medicinal chemistry; vol. 16; nb. 4; (1973); p. 394 - 397, View in Reaxys 876 of 1220 Bioassay Category

In Vitro (Efficacy)

365/467

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Bioassay Details

Number of animals with positive response at the dose of 1.25mg/ml for local anaesthesia out of 10 animals

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Measurement Object

Anesthetic activity

Quantitative value

Van Bever; Knaeps; Willems; Hermans; Janssen; Journal of medicinal chemistry; vol. 16; nb. 4; (1973); p. 394 - 397, View in Reaxys 877 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Details

Compound was tested for intradermal irritation in rabbit at 2 dose after intradermal administration; no irritation to very slight irritation

Biological Species/NCBI ID

Leporidae

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intradermal administration

Measurement Parameter

Activity

Measurement Object

Intradermal irritation in rabbit

Quantitative value

Kronberg; Leard; Takman; Journal of medicinal chemistry; vol. 16; nb. 6; (1973); p. 739 - 743, View in Reaxys 878 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested in vivo for local anesthetic activity against sciatic nerve of rat latency time for nerve block was reported

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

Latency

Unit

minute

Qualitative value

Quantitative value

Kronberg; Leard; Takman; Journal of medicinal chemistry; vol. 16; nb. 6; (1973); p. 739 - 743, View in Reaxys 879 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested in vivo for local anesthesia against sciatic nerve of rat and duration for nerve block was reported at frequency of 0.5.

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

time

Unit

minute

Qualitative value

Quantitative value

Kronberg; Leard; Takman; Journal of medicinal chemistry; vol. 16; nb. 6; (1973); p. 739 - 743, View in Reaxys 880 of 1220 Bioassay Category Bioassay Details

In Vitro (Efficacy) Compound was tested in vivo for local anesthesia against sciatic nerve of rat and duration for nerve block was reported at frequency of 1.0.

366/467

2018-05-14 08:43:54

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

time

Unit

minute

Qualitative value

Quantitative value

Kronberg; Leard; Takman; Journal of medicinal chemistry; vol. 16; nb. 6; (1973); p. 739 - 743, View in Reaxys 881 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Number of animals with positive response at the dose of 2.5mg/ml for local anaesthesia out of 10 animals

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Measurement Object

Anesthetic activity

Quantitative value

Van Bever; Knaeps; Willems; Hermans; Janssen; Journal of medicinal chemistry; vol. 16; nb. 4; (1973); p. 394 - 397, View in Reaxys 882 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Number of animals with positive response at the dose of 10.0mg/ml for local anaesthesia out of 10 animals

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Measurement Object

Anesthetic activity

Quantitative value

Van Bever; Knaeps; Willems; Hermans; Janssen; Journal of medicinal chemistry; vol. 16; nb. 4; (1973); p. 394 - 397, View in Reaxys 883 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested in vivo for local anesthesia against sciatic nerve of rat and duration for nerve block was reported at frequency of 2.0.

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

time

Unit

minute

Qualitative value

Quantitative value

115

Kronberg; Leard; Takman; Journal of medicinal chemistry; vol. 16; nb. 6; (1973); p. 739 - 743, View in Reaxys 884 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Acute toxicity was determined in mouse by iv administration

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

367/467

2018-05-14 08:43:54

Qualitative Results

19.5

Measurement Parameter

TD (toxic dose)

Unit

mg/kg

Measurement Object

Acute toxicity

Quantitative value

19.5

Kronberg; Leard; Takman; Journal of medicinal chemistry; vol. 16; nb. 6; (1973); p. 739 - 743, View in Reaxys 885 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Details

Compound was tested for intradermal irritation in rabbit at 4 dose after intradermal administration; very slight irritation to moderate irritation

Biological Species/NCBI ID

Leporidae

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intradermal administration

Measurement Parameter

Activity

Measurement Object

Intradermal irritation in rabbit

Qualitative value

Kronberg; Leard; Takman; Journal of medicinal chemistry; vol. 16; nb. 6; (1973); p. 739 - 743, View in Reaxys 886 of 1220 Bioassay Category

In Vivo (Animal models)

Bioassay Details

A single iv injection of 0.4 ml of the test solution given the seizures recorded during the next 24h

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Qualitative Results

Seizure not calculated

Measurement Parameter

qualitative

Measurement Object

Seizure

Van Bever; Knaeps; Willems; Hermans; Janssen; Journal of medicinal chemistry; vol. 16; nb. 4; (1973); p. 394 - 397, View in Reaxys 887 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Concentration required to produce infiltration anesthetic activity in guinea pig at duration of 15 minutes

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Measurement Parameter

MEC

Unit

Qualitative value

Quantitative value

0.5

Rastogi; Anand; Gupta; Sharma; Journal of Medicinal Chemistry; vol. 16; nb. 7; (1973); p. 797 - 804, View in Reaxys 888 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Spinal anesthetic activity was determined in dogs at duration of 150 minutes

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Measurement Parameter

MEC

368/467

2018-05-14 08:43:54

Unit

Qualitative value

Quantitative value

Rastogi; Anand; Gupta; Sharma; Journal of Medicinal Chemistry; vol. 16; nb. 7; (1973); p. 797 - 804, View in Reaxys 889 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Irritating concentration required to produce surface anesthetic activity in rabbit at therapeutic ratio 2

Biological Species/NCBI ID

Leporidae

Substance RN

3917968View in Reaxys

Measurement Parameter

MIC

Unit

Qualitative value

Quantitative value

Rastogi; Anand; Gupta; Sharma; Journal of Medicinal Chemistry; vol. 16; nb. 7; (1973); p. 797 - 804, View in Reaxys 890 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

A score 4 (surgical analgesia) for no reaction

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

score

Measurement Object

Score

Quantitative value

Van Bever; Knaeps; Willems; Hermans; Janssen; Journal of medicinal chemistry; vol. 16; nb. 4; (1973); p. 394 - 397, View in Reaxys 891 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

A score 4 (surgical analgesia) for no reaction

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

score

Measurement Object

Score

Quantitative value

Van Bever; Knaeps; Willems; Hermans; Janssen; Journal of medicinal chemistry; vol. 16; nb. 4; (1973); p. 394 - 397, View in Reaxys 892 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

A score 4 (surgical analgesia) for no reaction

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

score

Measurement Object

Score

Quantitative value

Van Bever; Knaeps; Willems; Hermans; Janssen; Journal of medicinal chemistry; vol. 16; nb. 4; (1973); p. 394 - 397, View in Reaxys 893 of 1220 Bioassay Category

In Vitro (Efficacy)

369/467

2018-05-14 08:43:54

Bioassay Details

Irritating concentration required to produce infiltration anesthetic activity in guinea pig at therapeutic ratio 4

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Measurement Parameter

MIC

Unit

Qualitative value

Quantitative value

Rastogi; Anand; Gupta; Sharma; Journal of Medicinal Chemistry; vol. 16; nb. 7; (1973); p. 797 - 804, View in Reaxys 894 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

A score 2 for a slow tail withdrawal between 6 and 10 sec.

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

score

Measurement Object

Score

Quantitative value

Van Bever; Knaeps; Willems; Hermans; Janssen; Journal of medicinal chemistry; vol. 16; nb. 4; (1973); p. 394 - 397, View in Reaxys 895 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

A score 2 for a slow tail withdrawal between 6 and 10 sec.

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

score

Measurement Object

Score

Quantitative value

Van Bever; Knaeps; Willems; Hermans; Janssen; Journal of medicinal chemistry; vol. 16; nb. 4; (1973); p. 394 - 397, View in Reaxys 896 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

A score 2 for a slow tail withdrawal between 6 and 10 sec.

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

score

Measurement Object

Score

Quantitative value

Van Bever; Knaeps; Willems; Hermans; Janssen; Journal of medicinal chemistry; vol. 16; nb. 4; (1973); p. 394 - 397, View in Reaxys 897 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Number of animals with positive response at the dose of 0.63mg/ml for local anaesthesia out of 10 animals

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

370/467

2018-05-14 08:43:54

Measurement Parameter

Activity

Measurement Object

Anesthetic activity

Quantitative value

Van Bever; Knaeps; Willems; Hermans; Janssen; Journal of medicinal chemistry; vol. 16; nb. 4; (1973); p. 394 - 397, View in Reaxys 898 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Concentration required to produce surface anesthetic activity in rabbit at duration of 15 minutes

Biological Species/NCBI ID

Leporidae

Substance RN

3917968View in Reaxys

Measurement Parameter

MEC

Unit

Qualitative value

Quantitative value

Rastogi; Anand; Gupta; Sharma; Journal of Medicinal Chemistry; vol. 16; nb. 7; (1973); p. 797 - 804, View in Reaxys 899 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Urinary recovery of metabolites and unchanged compound in healthy volunteers

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

>98

Measurement Parameter

percentage of dose excreted in urine

Unit

Quantitative value

Media Release: Noven Pharmaceuticals, 1998; (1998), View in Reaxys 900 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Cmax following application of 46.1mg in 2 cm2 of DentiPatch¿ in healthy volunteers

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

0.476

Measurement Parameter

tmax

Unit

hour

Measurement Object

Cmax

Quantitative value

0.476

Media Release: Noven Pharmaceuticals, 1998; (1998), View in Reaxys 901 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Details

Elimination half life following 1.55 mg patch in healthy volunteers

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

1.7

Measurement Parameter

t1/2 el

Unit

hour

371/467

2018-05-14 08:43:54

Quantitative value

1.7

Media Release: Noven Pharmaceuticals, 1998; (1998), View in Reaxys 902 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Elimination half life following 4.79 mg IV dose in healthy volunteers

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Qualitative Results

1.866

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

1.866

Media Release: Noven Pharmaceuticals, 1998; (1998), View in Reaxys 903 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Plasma levels during 15 min of application of DentiPatch¿ to healthy volunteers

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

<0.1

Measurement Parameter

concentration (parameters)

Unit

µg/mL

Measurement Object

Cmax

Quantitative value

0.1

Media Release: Noven Pharmaceuticals, 1998; (1998), View in Reaxys 904 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Protein unbound lidocaine in serum and plasma of healthy volunteers

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Measurement Parameter

fu (unbound fraction)

Unit

Qualitative value

Quantitative value

Media Release: Noven Pharmaceuticals, 1998; (1998), View in Reaxys 905 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Cmax following application of 46.1mg in 2 cm2 of DentiPatch¿ in healthy volunteers

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

0.0165

Measurement Parameter

Cmax

Unit

µg/mL

Measurement Object

Cmax

Quantitative value

0.0165

372/467

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Media Release: Noven Pharmaceuticals, 1998; (1998), View in Reaxys 906 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lowest toxic dose of the compound in child upon i.v. administration

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Qualitative Results

Measurement Parameter

TDLo

Unit

mg/kg

Measurement Object

Lowest toxic dose

Quantitative value

Edgren; Tilelli; Gehrz; Journal of Toxicology - Clinical Toxicology; vol. 24; nb. 1; (1986); p. 51 - 58, View in Reaxys 907 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lowest lethal dose of the compound in dog upon i.v. administration

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Qualitative Results

65.7

Measurement Parameter

LDLo

Unit

mg/kg

Measurement Object

Lowest lethal dose

Quantitative value

65.7

Journal de pharmacologie; vol. 2; (1971); p. 240, View in Reaxys 908 of 1220 Substance Effect

Toxic

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lowest toxic dose of the compound in human upon i.v. administration

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Qualitative Results

Measurement Parameter

TDLo

Unit

mg/kg

Measurement Object

Toxic dose

Quantitative value

Jonville; Barbier; Blond; Boscq; Autret; Breteau; Journal of Toxicology - Clinical Toxicology; vol. 28; nb. 1; (1990); p. 101 106, View in Reaxys 909 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lethal dose of the compound in mouse upon i.v. administration

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

373/467

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Substance Route of Adm.

intravenous administration

Qualitative Results

Measurement Parameter

LD50

Unit

mg/kg

Quantitative value

COLLINS; LARGE; The Journal of pharmacy and pharmacology; vol. 14 (Suppl); (1962); p. 48T-58T, View in Reaxys 910 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lethal dose of the compound in rat upon i.p. administration

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intraperitoneal administration

Qualitative Results

122

Measurement Parameter

LD50

Unit

mg/kg

Quantitative value

122

KRANTZ Jr.; LU; O'MALLEY; The Journal of pharmacology and experimental therapeutics; vol. 111; nb. 2; (1954); p. 224 228, View in Reaxys 911 of 1220 Target Name

7-Methoxycoumarin-O-Demethylase [human]

Target Synonyms

7-methoxycoumarin-o-demethylase

Target, Subunit, Species

7-Methoxycoumarin-O-Demethylase [human]

Target Mutant/Chimera Details

7-Methoxycoumarin-O-Demethylase [human]:Wild

Target Species (Bioactivity)

human

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Competitive inhibition of the compound against Methoxyresorufin O-demethylase in human liver cytochrome P-450 1A2

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Measurement Parameter

Ki (inhibition constant)

Unit

Qualitative value

Quantitative value

1540000

Measurement pX

2.81

912 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Peak plasma concentration (Cmax) of lidocaine following a 60 g application to 400 cm2 of intact skin for 3 hours

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

topical administration

Qualitative Results

0.12

374/467

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Measurement Parameter

Cmax

Unit

µg/mL

Measurement Object

Cmax

Quantitative value

0.12

Astrazeneca Pharmaceuticals Lp, Emla, (Lidocaine 2.5% And Prilocaine 2.5%) Anesthetic Disc, Cream, Product Leaflet, View in Reaxys 913 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Details

Formation rate of MEGX by hepatic microsomes from phenobarbital-treated rats after incubation with 10 uM lidocaine for 10 min at 37degreeC in 0.1M potassium phosphate buffer, pH 7.4 and NADPH (0.4 mM)

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Qualitative Results

5.14+/-0.49

Measurement Parameter

qualitative

Measurement Object

Formation rate of metabolite

Concomitants: Compound name

Lidocaine (10 uM); NADPH (0.4 mM)

Concomitants: Compound role

COM; COM

Nakamoto, Tatsuo; Oda, Yutaka; Imaoka, Susumu; Funae, Yoshihiko; Fujimori, Mitsugu; Drug Metabolism and Disposition; vol. 25; nb. 3; (1997); p. 296 - 300, View in Reaxys 914 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Details

Percent protein binding of the compound in rat serum

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Qualitative Results

0.38

Measurement Parameter

plasma protein binding

Unit

Measurement Object

Plasma binding

Quantitative value

0.38

Shibata, Yoshihiro; Takahashi, Hiroyuki; Ishii, Yasuyuki; Drug Metabolism and Disposition; vol. 28; nb. 12; (2000); p. 1518 - 1523, View in Reaxys 915 of 1220 Target Name

Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p08684

Target PDB ID

1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human

Bioassay Category

Metabolism/Transport

375/467

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Bioassay Details

Maximum velocity for CYP3A4 catalyzed MEGX formation in human liver microsomes

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

33.9

Measurement Parameter

qualitative

Measurement Object

Vmax2

Huang, Weili; Lin, Yvonne S.; McConn II, Donavon J.; Calamia, Justina C.; Totah, Rheem A.; Isoherranen, Nina; Glodowski, Mary; Thummel, Kenneth E.; Drug Metabolism and Disposition; vol. 32; nb. 12; (2004); p. 1434 - 1445, View in Reaxys 916 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Fetal/maternal ratio for lidocaine at delivery in pregnant women following administration of perineal analgesia with 20 ml 2 lidocaine

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Measurement Parameter

ratio

Quantitative value

0.46

Cavalli, Ricardo De Carvalho; Lanchote, Vera Lucia; Duarte, Geraldo; Dantas, Elaine Christine Moises; De Prado, Maria Fernanda Massoni; De Duarte, Luciana Barros; Da Cunha, Sergio Pereira; European Journal of Clinical Pharmacology; vol. 60; nb. 8; (2004); p. 569 - 574, View in Reaxys 917 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Details

Elimination half life in pregnant women following administration of perineal analgesia with 20 ml 2 lidocaine

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

Metabolism/Transport

Bioassay Details

Formation rate of 3-OH LID by hepatic microsomes from phenobarbital-treated rats after incubation with 100 uM lidocaine for 10 min at 37degreeC in 0.1M potassium phosphate buffer, pH 7.4 and NADPH (0.4 mM)

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Qualitative Results

0.56+/-0.04

Measurement Parameter

qualitative

Measurement Object

Formation rate of metabolite

Concomitants: Compound name

Lidocaine (100 uM); NADPH (0.4 mM)

Concomitants: Compound role

COM; COM

376/467

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Nakamoto, Tatsuo; Oda, Yutaka; Imaoka, Susumu; Funae, Yoshihiko; Fujimori, Mitsugu; Drug Metabolism and Disposition; vol. 25; nb. 3; (1997); p. 296 - 300, View in Reaxys 919 of 1220 Target Name

Cytochrome P450 3A1 [Rattus norvegicus]

Target Synonyms

cyp3a-1; cyp3a1; cypiiia1; cytochrome p450 3a1; cytochrome p450-pcn1

Target Uniprot ID

p04800

Target, Subunit, Species

Cytochrome P450 3A1 [Rattus norvegicus]

Target Mutant/Chimera Details

Cytochrome P450 3A1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Bioassay Category

Metabolism/Transport

Bioassay Details

Compound N-De-ethylation by rat recombinant CYP3A1 enzyme was determined

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Qualitative Results

0.081 +/- 0.004

Measurement Parameter

qualitative

Measurement Object

ENZYME ACTIVITY

Matsubara; Kim; Miyata; Shimada; Nagata, Kiyoshi; Yamazoe; Journal of Pharmacology and Experimental Therapeutics; vol. 309; nb. 3; (2004); p. 1282 - 1290, View in Reaxys 920 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Local anesthetic activity of the compound was tested in vivo by mouse tail anesthesia

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

IC50

Unit

Qualitative value

Quantitative value

0.01

Measurement pX

G Caliendo; G Greco; P Grieco; G Mattace Raso; R Meli; E Novellino; E Perissutti; V Santagada; European journal of medicinal chemistry; vol. 31; nb. 2; (1996); p. 99 - 104, View in Reaxys 921 of 1220 Target Name

Acetylcholine receptor subunit alpha-like 1 [human];+Nicotinic acetylcholine receptor (Delta 1) [human];+Nicotinic acetylcholine receptor (Gamma 1) [human];+Acetylcholine receptor subunit beta-like 1 [human]

Target Synonyms

acetylcholine receptor subunit alpha-like 1 + nicotinic acetylcholine receptor (delta 1) + nicotinic acetylcholine receptor (gamma 1) + acetylcholine receptor subunit beta-like 1

Target, Subunit, Species

Acetylcholine receptor subunit alpha-like 1 [human]; Acetylcholine receptor subunit beta-like 1 [human]; Nicotinic acetylcholine receptor (Delta 1) [human]; Nicotinic acetylcholine receptor (Gamma 1) [human]

Target Mutant/Chimera Details

Acetylcholine receptor subunit alpha-like 1 [human]:Wild + Nicotinic acetylcholine receptor (Delta 1) [human]:Wild + Nicotinic acetylcholine receptor (Gamma 1) [human]:Wild + Acetylcholine receptor subunit beta-like 1 [human]:Wild

Target Species (Bioactivity)

human

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

377/467

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Bioassay Details

Half-maximal inhibition of Nicotinic acetylcholine receptor alpha3beta4 activity in SH-SY5Y cells using 86Rb efflux assays

Biological Species/NCBI ID

human

Cells/Cell Lines

SH-SY5Y cell line

Substance RN

3917968View in Reaxys

Measurement Parameter

IC50

Unit

Qualitative value

Quantitative value

63000

Measurement pX

4.2

922 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Oral bioavailability of the compound in rat

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

oral administration

Qualitative Results

Measurement Parameter

F (drug bioavailability)

Unit

Measurement Object

Bioavailability

Quantitative value

Shibata, Yoshihiro; Takahashi, Hiroyuki; Ishii, Yasuyuki; Drug Metabolism and Disposition; vol. 28; nb. 12; (2000); p. 1518 - 1523, View in Reaxys 923 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Details

Formation rate of MEGX by hepatic microsomes from phenobarbital-treated rats after incubation with 100 uM lidocaine for 10 min at 37degreeC in 0.1M potassium phosphate buffer, pH 7.4 and NADPH (0.4 mM)

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Qualitative Results

13.47+/-1.62

Measurement Parameter

qualitative

Measurement Object

Formation rate of metabolite

Concomitants: Compound name

Lidocaine (100 uM); NADPH (0.4 mM)

Concomitants: Compound role

COM; COM

Nakamoto, Tatsuo; Oda, Yutaka; Imaoka, Susumu; Funae, Yoshihiko; Fujimori, Mitsugu; Drug Metabolism and Disposition; vol. 25; nb. 3; (1997); p. 296 - 300, View in Reaxys 924 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Time to reach peak plasma concentration of MEGX in pregnant women following administration of perineal analgesia with 20 ml 2 lidocaine

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

1.5

378/467

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Measurement Parameter

tmax

Unit

hour

Quantitative value

1.5

Metabolism/Transport

Bioassay Details

Elimination half life was determined from pig skeletal muscle

Biological Species/NCBI ID

pig

Substance RN

3917968View in Reaxys

Qualitative Results

0.8+/-0.15

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

0.8

Feldman; Hartvig; Wiklund; Doucette; Antoni; Gee; Ulin; Langstrom; Biopharmaceutics and drug disposition; vol. 18; nb. 2; (1997); p. 151 - 164, View in Reaxys 926 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Local anesthetic activity of the compound was tested in vivo by corneal anesthesia in rabbit; expressed as of the anesthetic activity of lidocaine = 100

Biological Species/NCBI ID

Leporidae

Cells/Cell Lines

cornea cell

Substance RN

3917968View in Reaxys

Unit

Qualitative value

Quantitative value

100

Metabolism/Transport

Bioassay Details

Formation rate of 3-OH LID by hepatic microsomes from phenobarbital-untreated rats after incubation with 100 uM lidocaine for 10 min at 37degreeC in 0.1M potassium phosphate buffer, pH 7.4 and NADPH (0.4 mM)

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Qualitative Results

0.59+/-0.06

Measurement Parameter

qualitative

Measurement Object

Formation rate of metabolite

Concomitants: Compound name

Lidocaine (100 uM); NADPH (0.4 mM)

Concomitants: Compound role

COM; COM

Nakamoto, Tatsuo; Oda, Yutaka; Imaoka, Susumu; Funae, Yoshihiko; Fujimori, Mitsugu; Drug Metabolism and Disposition; vol. 25; nb. 3; (1997); p. 296 - 300, View in Reaxys 928 of 1220 Bioassay Category

Metabolism/Transport

379/467

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Bioassay Details

Formation rate of 3-OH LID by hepatic microsomes from phenobarbital-treated rats after incubation with 10 uM lidocaine for 10 min at 37degreeC in 0.1M potassium phosphate buffer, pH 7.4 and NADPH (0.4 mM)

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Qualitative Results

0.58+/-0.03

Measurement Parameter

qualitative

Measurement Object

Formation rate of metabolite

Concomitants: Compound name

Lidocaine (10 uM); NADPH (0.4 mM)

Concomitants: Compound role

COM; COM

Nakamoto, Tatsuo; Oda, Yutaka; Imaoka, Susumu; Funae, Yoshihiko; Fujimori, Mitsugu; Drug Metabolism and Disposition; vol. 25; nb. 3; (1997); p. 296 - 300, View in Reaxys 929 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

In vivo anesthetic activity of the compound tested in mouse tail

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

IC50

Unit

Qualitative value

Quantitative value

0.01

Measurement pX

G Caliendo; R Di Carlo; G Greco; P Grieco; R Meli; E Novellino; E Perissutti; V Santagada; European journal of medicinal chemistry; vol. 30; nb. 7-8; (1995); p. 603 - 608, View in Reaxys 930 of 1220 Substance Action on Target

Inhibitor

Bioassay Category

In Vivo (Animal models)

Bioassay Details

Inhibition of nicotine-induced antinociception in tail-flick test after s.c. administration in mice

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

subcutaneous administration

Measurement Parameter

% Inhibition

Unit

Measurement Object

Inhibition of nicotine-induced antinociception

Qualitative value

Quantitative value

Damaj; Slemmer; Carroll; Martin; Journal of Pharmacology and Experimental Therapeutics; vol. 289; nb. 3; (1999); p. 1229 1236, View in Reaxys 931 of 1220 Target Name Target Synonyms

Cytochrome P450 3A18 [Rattus norvegicus] cyp3a18; cypiiia18; cytochrome p450 3a18; cytochrome p450(6)beta-2

Target Uniprot ID

q64581

Target, Subunit, Species

Cytochrome P450 3A18 [Rattus norvegicus]

380/467

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Target Mutant/Chimera Details

Cytochrome P450 3A18 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Bioassay Category

Metabolism/Transport

Bioassay Details

Compound N-De-ethylation by rat recombinant CYP3A18 enzyme was determined

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Qualitative Results

0.067 +/- 0.006

Measurement Parameter

qualitative

Measurement Object

ENZYME ACTIVITY

Matsubara; Kim; Miyata; Shimada; Nagata, Kiyoshi; Yamazoe; Journal of Pharmacology and Experimental Therapeutics; vol. 309; nb. 3; (2004); p. 1282 - 1290, View in Reaxys 932 of 1220 Target Name

Cytochrome P450 1A2 [human]

Target Synonyms

cholesterol 25-hydroxylase; cyp1a2; cypia2; cytochrome p(3)450; cytochrome p450 1a2; cytochrome p450 4; cytochrome p450-p3

Target Uniprot ID

p05177

Target PDB ID

2hi4

Target, Subunit, Species

Cytochrome P450 1A2 [human]

Target Mutant/Chimera Details

Cytochrome P450 1A2 [human]:Wild

Target Species (Bioactivity)

human

Substance Action on Target

Inhibitor

Bioassay Category

Metabolism/Transport

Bioassay Details

Inhibitioory potency against cytochrome P-450 1A2 (CYP1A2) activity (Methoxyresorufin O-demethylase) in human liver microsomes

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

7 +/- 4

Measurement Parameter

% Inhibition

Unit

Quantitative value

933 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

In vivo anesthetic activity of the compound tested in rabbit cornea

Biological Species/NCBI ID

Leporidae

Cells/Cell Lines

cornea cell

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Unit

Qualitative value

Quantitative value

100

381/467

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Metabolism/Transport

Bioassay Details

Elimination half life was determined from pig lung

Biological Species/NCBI ID

pig

Substance RN

3917968View in Reaxys

Qualitative Results

1.08+/-0.083

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

1.08

Feldman; Hartvig; Wiklund; Doucette; Antoni; Gee; Ulin; Langstrom; Biopharmaceutics and drug disposition; vol. 18; nb. 2; (1997); p. 151 - 164, View in Reaxys 935 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Details

Distribution half life in pregnant women following administration of perineal analgesia with 20 ml 2 lidocaine

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

0.4

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

0.4

Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p08684

Target PDB ID

1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human

Bioassay Category

Metabolism/Transport

Bioassay Details

Maximum velocity for CYP3A4 catalyzed MEGX formation in human liver microsomes

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

3.99

Measurement Parameter

qualitative

Measurement Object

Vmax

382/467

2018-05-14 08:43:54

Metabolism/Transport

Bioassay Details

Formation rate of MEGX by hepatic microsomes from phenobarbital-untreated rats after incubation with 10 uM lidocaine for 10 min at 37degreeC in 0.1M potassium phosphate buffer, pH 7.4 and NADPH (0.4 mM)

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Qualitative Results

1.02+/-0.07

Measurement Parameter

qualitative

Measurement Object

Formation rate of metabolite

Concomitants: Compound name

Lidocaine (10 uM); NADPH (0.4 mM)

Concomitants: Compound role

COM; COM

Nakamoto, Tatsuo; Oda, Yutaka; Imaoka, Susumu; Funae, Yoshihiko; Fujimori, Mitsugu; Drug Metabolism and Disposition; vol. 25; nb. 3; (1997); p. 296 - 300, View in Reaxys 938 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Surface anesthetic activity of the compound was determined in vivo by corneal anesthesia in rabbit

Biological Species/NCBI ID

Leporidae

Cells/Cell Lines

cornea cell

Substance RN

3917968View in Reaxys

Qualitative Results

log AUC not calculated

Measurement Parameter

qualitative

Measurement Object

log AUC

Metabolism/Transport

Bioassay Details

Clearance in pregnant women following administration of perineal analgesia with 20 ml 2 lidocaine

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

12.2

Measurement Parameter

CL (drug clearance)

Unit

mL/min/kg

Quantitative value

12.2

Metabolism/Transport

Bioassay Details

Maximum velocity for CYP3A5 catalyzed MEGX formation in human liver microsomes

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

1.51

383/467

2018-05-14 08:43:54

Measurement Parameter

qualitative

Measurement Object

Vmax

Metabolism/Transport

Bioassay Details

Elimination half life was determined from pig blood

Biological Species/NCBI ID

pig

Substance RN

3917968View in Reaxys

Qualitative Results

1.33+/-0.26

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

1.33

Feldman; Hartvig; Wiklund; Doucette; Antoni; Gee; Ulin; Langstrom; Biopharmaceutics and drug disposition; vol. 18; nb. 2; (1997); p. 151 - 164, View in Reaxys 942 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Peak plasma concentration (Cmax) of lidocaine following a 60 g application to 400 cm2 of intact skin for 24 hours

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

topical administration

Qualitative Results

0.28

Measurement Parameter

Cmax

Unit

µg/mL

Measurement Object

Cmax

Quantitative value

0.28

Astrazeneca Pharmaceuticals Lp, Emla, (Lidocaine 2.5% And Prilocaine 2.5%) Anesthetic Disc, Cream, Product Leaflet, View in Reaxys 943 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Tmax of lidocaine following a 60 g application to 400 cm2 of intact skin for 24 hours

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

10.0000

Measurement Parameter

tmax

Unit

hour

Quantitative value

Astrazeneca Pharmaceuticals Lp, Emla, (Lidocaine 2.5% And Prilocaine 2.5%) Anesthetic Disc, Cream, Product Leaflet, View in Reaxys 944 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Time to reach peak plasma concentration in pregnant women following administration of perineal analgesia with 20 ml 2 lidocaine

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

384/467

2018-05-14 08:43:54

Qualitative Results

0.25

Measurement Parameter

tmax

Unit

hour

Quantitative value

0.25

In Vitro (Efficacy)

Bioassay Details

Michaelis-Menten constant for metabolism of the compound in rat hepatocytes

Biological Species/NCBI ID

Rattus norvegicus

Cells/Cell Lines

liver cell

Substance RN

3917968View in Reaxys

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Measurement Object

Michaelis Menten constant

Qualitative value

Quantitative value

1.7

Measurement pX

5.77

Shibata, Yoshihiro; Takahashi, Hiroyuki; Ishii, Yasuyuki; Drug Metabolism and Disposition; vol. 28; nb. 12; (2000); p. 1518 - 1523, View in Reaxys 946 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Details

Formation rate of MEGX by hepatic microsomes from phenobarbital-untreated rats after incubation with 100 uM lidocaine for 10 min at 37degreeC in 0.1M potassium phosphate buffer, pH 7.4 and NADPH (0.4 mM)

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Qualitative Results

2.98+/-0.39

Measurement Parameter

qualitative

Measurement Object

Formation rate of metabolite

Concomitants: Compound name

Lidocaine (100 uM); NADPH (0.4 mM)

Concomitants: Compound role

COM; COM

Nakamoto, Tatsuo; Oda, Yutaka; Imaoka, Susumu; Funae, Yoshihiko; Fujimori, Mitsugu; Drug Metabolism and Disposition; vol. 25; nb. 3; (1997); p. 296 - 300, View in Reaxys 947 of 1220 Target Name

Target Synonyms

acetylcholine receptor subunit alpha-like 1 + nicotinic acetylcholine receptor (delta 1) + nicotinic acetylcholine receptor (gamma 1) + acetylcholine receptor subunit beta-like 1

Target, Subunit, Species

Target Mutant/Chimera Details

385/467

2018-05-14 08:43:54

Target Species (Bioactivity)

human

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Half-maximal inhibition of Nicotinic acetylcholine receptor alpha4beta4 activity in SH-SY5Y cells using 86Rb efflux assays

Biological Species/NCBI ID

human

Cells/Cell Lines

SH-SY5Y cell line

Substance RN

3917968View in Reaxys

Measurement Parameter

IC50

Unit

Qualitative value

Quantitative value

250000

Measurement pX

3.6

948 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Details

Formation rate of 3-OH LID by hepatic microsomes from phenobarbital-untreated rats after incubation with 10 uM lidocaine for 10 min at 37degreeC in 0.1M potassium phosphate buffer, pH 7.4 and NADPH (0.4 mM)

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Qualitative Results

0.64+/-0.07

Measurement Parameter

qualitative

Measurement Object

Formation rate of metabolite

Concomitants: Compound name

Lidocaine (10 uM); NADPH (0.4 mM)

Concomitants: Compound role

COM; COM

Nakamoto, Tatsuo; Oda, Yutaka; Imaoka, Susumu; Funae, Yoshihiko; Fujimori, Mitsugu; Drug Metabolism and Disposition; vol. 25; nb. 3; (1997); p. 296 - 300, View in Reaxys 949 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Area under concentration time curve in pregnant women following administration of perineal analgesia with 20 ml 2 lidocaine

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

7.67

Measurement Parameter

AUC (0-inf)

Unit

µg.h/mL

Quantitative value

7.67

In Vitro (Efficacy) Mean peak uptake of lidocaine from pig myocardium n=4 at 0.48+/-0.26 min

386/467

2018-05-14 08:43:54

Biological Species/NCBI ID

pig

Cells/Cell Lines

cardiac muscle cell

Substance RN

3917968View in Reaxys

Measurement Parameter

Uptake

Quantitative value

5.95

Feldman; Hartvig; Wiklund; Doucette; Antoni; Gee; Ulin; Langstrom; Biopharmaceutics and drug disposition; vol. 18; nb. 2; (1997); p. 151 - 164, View in Reaxys 951 of 1220 Target Name

Target Synonyms

acetylcholine receptor subunit alpha-like 1 + nicotinic acetylcholine receptor (delta 1) + nicotinic acetylcholine receptor (gamma 1) + acetylcholine receptor subunit beta-like 1

Target, Subunit, Species

Target Mutant/Chimera Details

Target Species (Bioactivity)

human

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Half-maximal inhbition of Nicotinic acetylcholine receptor alpha1 activity in TE671/RD cells using 86Rb efflux assays

Biological Species/NCBI ID

human

Cells/Cell Lines

TE 671 cell line

Substance RN

3917968View in Reaxys

Measurement Parameter

IC50

Unit

Qualitative value

Quantitative value

52000

Measurement pX

4.28

952 of 1220 Target Name

Cytochrome P450 3A2 [Rattus norvegicus]

Target Synonyms

cyp3a-2; cyp3a11; cyp3a2; cypiiia2; cytochrome p450 3a2; cytochrome p450-pcn2; cytochrome p450/6-beta-a; testosterone 6-beta-hydroxylase

Target Uniprot ID

p05183

Target, Subunit, Species

Cytochrome P450 3A2 [Rattus norvegicus]

Target Mutant/Chimera Details

Cytochrome P450 3A2 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Bioassay Category

Metabolism/Transport

Bioassay Details

Compound N-De-ethylation by rat recombinant CYP3A2 enzyme was determined

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

387/467

2018-05-14 08:43:54

Qualitative Results

0.174 +/- 0.006

Measurement Parameter

qualitative

Measurement Object

ENZYME ACTIVITY

Matsubara; Kim; Miyata; Shimada; Nagata, Kiyoshi; Yamazoe; Journal of Pharmacology and Experimental Therapeutics; vol. 309; nb. 3; (2004); p. 1282 - 1290, View in Reaxys 953 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Details

Clearance in pregnant women following administration of perineal analgesia with 20 ml 2 lidocaine

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

3.1

Measurement Parameter

Vd (volume of distribution)

Unit

L/kg

Quantitative value

3.1

In Vitro (Efficacy)

Bioassay Details

Infiltration anesthetic activity of the compound was determined in vivo by mouse tail anesthesia

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

pIC50

Quantitative value

1.8

Measurement pX

1.8

In Vitro (Efficacy)

Bioassay Details

In vivo duration of local anesthetic activity in rat sciatic nerve block (each rat received 0.2mL of 2 anesthetic solution )

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

time

Unit

minute

Qualitative value

Quantitative value

110

Metabolism/Transport

Bioassay Details

Compound N-De-ethylation by rat recombinant CYP3A62 enzyme was determined

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Qualitative Results

0.054 +/- 0.012

Measurement Parameter

qualitative

388/467

2018-05-14 08:43:54

Measurement Object

ENZYME ACTIVITY

Matsubara; Kim; Miyata; Shimada; Nagata, Kiyoshi; Yamazoe; Journal of Pharmacology and Experimental Therapeutics; vol. 309; nb. 3; (2004); p. 1282 - 1290, View in Reaxys 957 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Details

Blood to plasma concentration ratio of the compound in rat

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Qualitative Results

1.27

Measurement Parameter

ratio

Measurement Object

Cmax

Quantitative value

1.27

Shibata, Yoshihiro; Takahashi, Hiroyuki; Ishii, Yasuyuki; Drug Metabolism and Disposition; vol. 28; nb. 12; (2000); p. 1518 - 1523, View in Reaxys 958 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Area under concentration time curve of MEGX in pregnant women following administration of perineal analgesia with 20 ml 2 lidocaine

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

1.37

Measurement Parameter

AUC (0-inf)

Unit

µg.h/mL

Quantitative value

1.37

Metabolism/Transport

Bioassay Details

Steady-state volume of distribution (mean 1.5, ±0.3 SD, n=13) after intravenous administration

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

1.1 - 2.1

Measurement Parameter

Vd (volume of distribution)

Unit

L/kg

Quantitative value

1.6

Astrazeneca Pharmaceuticals Lp, Emla, (Lidocaine 2.5% And Prilocaine 2.5%) Anesthetic Disc, Cream, Product Leaflet, View in Reaxys 960 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Mean peak uptake of lidocaine from pig lung n=4 at 0.35+/-0.01 min

Biological Species/NCBI ID

pig

Organs/Tissues

lung

Substance RN

3917968View in Reaxys

Measurement Parameter

Uptake

Quantitative value

4.2

389/467

2018-05-14 08:43:54

Feldman; Hartvig; Wiklund; Doucette; Antoni; Gee; Ulin; Langstrom; Biopharmaceutics and drug disposition; vol. 18; nb. 2; (1997); p. 151 - 164, View in Reaxys 961 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Details

Bound to plasma proteins, primarily alpha-1-acid glycoprotein.

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

~70

Measurement Parameter

Protein binding (%)

Unit

Quantitative value

Astrazeneca Pharmaceuticals Lp, Emla, (Lidocaine 2.5% And Prilocaine 2.5%) Anesthetic Disc, Cream, Product Leaflet, View in Reaxys 962 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Details

The systemic clearance

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

10 - 20

Measurement Parameter

CL (drug clearance)

Unit

mL/min/kg

Quantitative value

Astrazeneca Pharmaceuticals Lp, Emla, (Lidocaine 2.5% And Prilocaine 2.5%) Anesthetic Disc, Cream, Product Leaflet, View in Reaxys 963 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Toxic concentration that decreases in cardiac output, total peripheral resistance and mean arterial pressure.

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

Measurement Parameter

Unit

µg/mL

Measurement Object

Toxic concentration

Quantitative value

Measurement pX

4.73

Astrazeneca Pharmaceuticals Lp, Emla, (Lidocaine 2.5% And Prilocaine 2.5%) Anesthetic Disc, Cream, Product Leaflet, View in Reaxys 964 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Details

Half life of MEGX in pregnant women following administration of perineal analgesia with 20 ml 2 lidocaine

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

Measurement Parameter

t1/2 el

390/467

2018-05-14 08:43:54

Unit

hour

Quantitative value

Pharmacokinetic

Bioassay Details

Percent of an absorbed dose of lidocaine can be recovered in the urine as metabolites or parent drug.

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

> 98

Measurement Parameter

percentage of dose excreted in urine

Unit

Quantitative value

Astrazeneca Pharmaceuticals Lp, Emla, (Lidocaine 2.5% And Prilocaine 2.5%) Anesthetic Disc, Cream, Product Leaflet, View in Reaxys 966 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Details

Plasma elimination half of lidocaine life following IV administration

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

~1.08 - 2.5

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

1.79

Astrazeneca Pharmaceuticals Lp, Emla, (Lidocaine 2.5% And Prilocaine 2.5%) Anesthetic Disc, Cream, Product Leaflet, View in Reaxys 967 of 1220 Target Name

Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p08684

Target PDB ID

1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human

Bioassay Category

Metabolism/Transport

Bioassay Details

Michaelis-Menton constant for CYP3A4 catalyzed MEGX formation in human liver microsomes

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

5927

Measurement Parameter

Km (Michaelis constant)

391/467

2018-05-14 08:43:54

Unit

µM

Quantitative value

5927

Measurement pX

2.23

Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p08684

Target PDB ID

1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human

Bioassay Category

Metabolism/Transport

Bioassay Details

Michaelis-Menton constant for CYP3A4 catalyzed MEGX formation in human liver microsomes

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

78.9

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Quantitative value

78.9

Measurement pX

4.1

Pharmacokinetic

Bioassay Details

Peak plasma concentration in pregnant women following administration of perineal analgesia with 20 ml 2 lidocaine

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

3.22

Measurement Parameter

Cmax

Unit

µg/mL

Measurement Object

Peak plasma concentration

Quantitative value

3.22

In Vitro (Efficacy) Mean peak uptake of lidocaine from pig skeletal muscle n=4 at 1.5+/-1.4 min

392/467

2018-05-14 08:43:54

Biological Species/NCBI ID

pig

Substance RN

3917968View in Reaxys

Measurement Parameter

Uptake

Quantitative value

3.3

Feldman; Hartvig; Wiklund; Doucette; Antoni; Gee; Ulin; Langstrom; Biopharmaceutics and drug disposition; vol. 18; nb. 2; (1997); p. 151 - 164, View in Reaxys 971 of 1220 Bioassay Category

Metabolism/Transport

Bioassay Details

Michaelis-Menton constant for CYP3A5 catalyzed MEGX formation in human liver microsomes

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

1217

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Quantitative value

1217

Measurement pX

2.91

Metabolism/Transport

Bioassay Details

Michaelis-Menton constant for CYP3A5 catalyzed MEGX formation in human liver microsomes

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

21.8

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Quantitative value

21.8

Measurement pX

4.66

Target Synonyms

acetylcholine receptor subunit alpha-like 1 + nicotinic acetylcholine receptor (delta 1) + nicotinic acetylcholine receptor (gamma 1) + acetylcholine receptor subunit beta-like 1

Target, Subunit, Species

Target Mutant/Chimera Details

Target Species (Bioactivity)

human

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

393/467

2018-05-14 08:43:54

Bioassay Details

Half-maximal inhibition of Nicotinic acetylcholine receptor alpha4beta2 activity in SH-SY5Y cells using 86Rb efflux assays

Biological Species/NCBI ID

human

Cells/Cell Lines

SH-SY5Y cell line

Substance RN

3917968View in Reaxys

Measurement Parameter

IC50

Unit

Qualitative value

Quantitative value

190000

Measurement pX

3.72

974 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Acute toxicity in male mouse after ip administration

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Qualitative Results

110

Measurement Parameter

LD50

Unit

mg/kg

Measurement Object

Acute toxicity

Quantitative value

110

Pharmacokinetic

Bioassay Details

Tmax of lidocaine following a 60 g application to 400 cm2 of intact skin for 3 hours

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

4.0000

Measurement Parameter

tmax

Unit

hour

Quantitative value

Astrazeneca Pharmaceuticals Lp, Emla, (Lidocaine 2.5% And Prilocaine 2.5%) Anesthetic Disc, Cream, Product Leaflet, View in Reaxys 976 of 1220 Bioassay Category

Pharmacokinetic

Bioassay Details

Peak plasma concentration of MEGX in pregnant women following administration of perineal analgesia with 20 ml 2 lidocaine

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

0.229

Measurement Parameter

Cmax

Unit

µg/mL

Measurement Object

Peak plasma concentration

Quantitative value

0.229

394/467

2018-05-14 08:43:54

Metabolism/Transport

Bioassay Details

Elimination half life was determined from pig myocardium

Biological Species/NCBI ID

pig

Substance RN

3917968View in Reaxys

Qualitative Results

0.93+/-0.3

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

0.93

Feldman; Hartvig; Wiklund; Doucette; Antoni; Gee; Ulin; Langstrom; Biopharmaceutics and drug disposition; vol. 18; nb. 2; (1997); p. 151 - 164, View in Reaxys 978 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Ratio of LD50 to that of IC50 in mouse

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Qualitative Results

5.1000000000

Measurement Parameter

therapeutic index

Measurement Object

Therapeutic index

Quantitative value

5.1

Metabolism/Transport

Bioassay Details

Maximum velocity for CYP3A5 catalyzed MEGX formation in human liver microsomes

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

20.6

Measurement Parameter

qualitative

Measurement Object

Vmax2

Cytochrome P450 3A9 [Rattus norvegicus]

Target Synonyms

3ah15; cyp3a13; cyp3a9; cypiiia9; cytochrome p450 3a9; cytochrome p450 olfactive 3; cytochrome p450-olf3

Target Uniprot ID

p51538

Target, Subunit, Species

Cytochrome P450 3A9 [Rattus norvegicus]

Target Mutant/Chimera Details

Cytochrome P450 3A9 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Bioassay Category

Metabolism/Transport

Bioassay Details

Compound N-De-ethylation by rat recombinant CYP3A9 enzyme was determined

395/467

2018-05-14 08:43:54

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Qualitative Results

0.178 +/- 0.007

Measurement Parameter

qualitative

Measurement Object

ENZYME ACTIVITY

Matsubara; Kim; Miyata; Shimada; Nagata, Kiyoshi; Yamazoe; Journal of Pharmacology and Experimental Therapeutics; vol. 309; nb. 3; (2004); p. 1282 - 1290, View in Reaxys 981 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Effect of the compound on change in mean arterial blood pressure in dogs

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Qualitative Results

MABP not calculated

Measurement Parameter

qualitative

Measurement Object

MABP

McMaster; Byrnes; Feldman; Takman; Tenthorey; Journal of Medicinal Chemistry; vol. 22; nb. 10; (1979); p. 1177 - 1182, View in Reaxys 982 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Compound was tested for its toxicity by measuring the percent mice exhibiting ataxia

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Qualitative Results

100

Measurement Parameter

Toxicity

Unit

Measurement Object

Toxicity

Quantitative value

100

McMaster; Byrnes; Feldman; Takman; Tenthorey; Journal of Medicinal Chemistry; vol. 22; nb. 10; (1979); p. 1177 - 1182, View in Reaxys 983 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested for antiarrhythmic activity in coronary artery ligated dogs before drug administration

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Qualitative Results

Vent. rate not calculated

Measurement Parameter

qualitative

Measurement Object

Vent. rate

McMaster; Byrnes; Feldman; Takman; Tenthorey; Journal of Medicinal Chemistry; vol. 22; nb. 10; (1979); p. 1177 - 1182, View in Reaxys 984 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Effective Dose for protection against CNS toxicity in mice

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

396/467

2018-05-14 08:43:54

Measurement Parameter

ED50

Unit

mM/kg

Measurement Object

Toxicity

Qualitative value

Quantitative value

0.26

McMaster; Byrnes; Feldman; Takman; Tenthorey; Journal of Medicinal Chemistry; vol. 22; nb. 10; (1979); p. 1177 - 1182, View in Reaxys 985 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Percent of mice protected against chloroform induced ventricular fibrillation

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

percentage

Unit

Measurement Object

Protection rate

Qualitative value

Quantitative value

100

McMaster; Byrnes; Feldman; Takman; Tenthorey; Journal of Medicinal Chemistry; vol. 22; nb. 10; (1979); p. 1177 - 1182, View in Reaxys 986 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Compound was tested for its toxicity by measuring the percent mice exhibiting death

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

Toxicity

Unit

Measurement Object

Toxicity

Quantitative value

McMaster; Byrnes; Feldman; Takman; Tenthorey; Journal of Medicinal Chemistry; vol. 22; nb. 10; (1979); p. 1177 - 1182, View in Reaxys 987 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested for antiarrhythmic activity in coronary artery ligated dogs after drug administration

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Measurement Parameter

percentage

Unit

Measurement Object

Vent.ectopic

Qualitative value

Quantitative value

McMaster; Byrnes; Feldman; Takman; Tenthorey; Journal of Medicinal Chemistry; vol. 22; nb. 10; (1979); p. 1177 - 1182, View in Reaxys 988 of 1220 Bioassay Category Bioassay Details

In Vitro (Efficacy) Potency of the compound relative to that of Compound 1 was calculated on molar basis in mice

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Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Quantitative value

McMaster; Byrnes; Feldman; Takman; Tenthorey; Journal of Medicinal Chemistry; vol. 22; nb. 10; (1979); p. 1177 - 1182, View in Reaxys 989 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Change in ECG interval was measured approximately 2 min after the beginning of reperfusion at a compound concentration of 100 uM in rat heart

Biological Species/NCBI ID

Rattus norvegicus

Organs/Tissues

heart

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Unit

Measurement Object

Change in ECG interval

Qualitative value

Quantitative value

Deviation

Koufaki, Maria; Calogeropoulou, Theodora; Rekka, Eleni; Chryselis, Michael; Papazafiri, Panagiota; Gaitanaki, Catherine; Makriyannis, Alexandros; Bioorganic and Medicinal Chemistry; vol. 11; nb. 23; (2003); p. 5209 - 5219, View in Reaxys 990 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested for antiarrhythmic activity in coronary artery ligated dogs before drug administration

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Measurement Parameter

percentage

Unit

Measurement Object

Vent.ectopic

Qualitative value

Quantitative value

McMaster; Byrnes; Feldman; Takman; Tenthorey; Journal of Medicinal Chemistry; vol. 22; nb. 10; (1979); p. 1177 - 1182, View in Reaxys 991 of 1220 Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Compound was tested for its toxicity by measuring the percent mice exhibiting convulsions

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Qualitative Results

100

Measurement Parameter

Toxicity

Unit

Measurement Object

Toxicity

Quantitative value

100

398/467

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McMaster; Byrnes; Feldman; Takman; Tenthorey; Journal of Medicinal Chemistry; vol. 22; nb. 10; (1979); p. 1177 - 1182, View in Reaxys 992 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Anti-arrhythmic activity was determined as percent of total heart beats during exactly the same period (10 min) for each treatment in the first 15 min of reperfusion in rat heart at a compound concentration of 30 uM

Biological Species/NCBI ID

Rattus norvegicus

Organs/Tissues

heart

Substance RN

3917968View in Reaxys

Qualitative Results

Premature beats not calculated

Measurement Parameter

qualitative

Measurement Object

Premature beats

In Vitro (Efficacy)

Bioassay Details

Effect of the compound on reduction of ventricular ectopic activity to 5 or less for 5 consecutive min

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Unit

mM/kg

Measurement Object

Reduction of ventricular ectopic activity

Qualitative value

Quantitative value

0.21

McMaster; Byrnes; Feldman; Takman; Tenthorey; Journal of Medicinal Chemistry; vol. 22; nb. 10; (1979); p. 1177 - 1182, View in Reaxys 994 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested for antiarrhythmic activity in coronary artery ligated dogs after drug administration

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Qualitative Results

Vent. rate not calculated

Measurement Parameter

qualitative

Measurement Object

Vent. rate

McMaster; Byrnes; Feldman; Takman; Tenthorey; Journal of Medicinal Chemistry; vol. 22; nb. 10; (1979); p. 1177 - 1182, View in Reaxys 995 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Biological Species/NCBI ID

Rattus norvegicus

Organs/Tissues

heart

Substance RN

3917968View in Reaxys

Qualitative Results

Premature beats not calculated

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Measurement Parameter

qualitative

Measurement Object

Premature beats

Toxicity/Safety Pharmacology

Bioassay Details

Dose required to cause CNS toxicity in dogs

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Qualitative Results

270

Measurement Parameter

Toxicity

Unit

µM/kg

Measurement Object

CNS toxicity

Quantitative value

270

McMaster; Byrnes; Feldman; Takman; Tenthorey; Journal of Medicinal Chemistry; vol. 22; nb. 10; (1979); p. 1177 - 1182, View in Reaxys 997 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Change in ECG interval was measured approximately 2 min after the beginning of reperfusion at a compound concentration of 30 uM in rat heart

Biological Species/NCBI ID

Rattus norvegicus

Organs/Tissues

heart

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Unit

Measurement Object

Change in ECG interval

Qualitative value

Quantitative value

Deviation

In Vitro (Efficacy)

Bioassay Details

Effective dose for prevent seizures from maximum electroshock (MES)

Substance RN

3917968View in Reaxys

Measurement Parameter

ED50

Unit

mg/kg

Qualitative value

Quantitative value

Anger; Madge; Mulla; Riddall; Journal of Medicinal Chemistry; vol. 44; nb. 2; (2001); p. 115 - 137, View in Reaxys 999 of 1220 Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Inhibitory concentration against veratridine-induced guanidine flux (vs ion flux)

Substance RN

3917968View in Reaxys

Measurement Parameter

IC50

Unit

µM

Qualitative value

400/467

2018-05-14 08:43:54

Quantitative value

Measurement pX

4.01

Anger; Madge; Mulla; Riddall; Journal of Medicinal Chemistry; vol. 44; nb. 2; (2001); p. 115 - 137, View in Reaxys 1000 of 1220

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Toxic dose in rotarod assay

Substance RN

3917968View in Reaxys

Measurement Parameter

TD50

Unit

mg/kg

Measurement Object

Toxic dosse

Qualitative value

Quantitative value

Anger; Madge; Mulla; Riddall; Journal of Medicinal Chemistry; vol. 44; nb. 2; (2001); p. 115 - 137, View in Reaxys 1001 of 1220

Target Name

Sodium channel protein type 9 subunit alpha;+Sodium channel subunit beta-1

Target Synonyms

sodium channel protein type 9 subunit alpha + scn1b; sodium channel subunit beta-1

Target, Subunit, Species

Sodium channel protein type 9 subunit alpha; Sodium channel subunit beta-1

Target Mutant/Chimera Details

Sodium channel protein type 9 subunit alpha:Wild + Sodium channel subunit beta-1:Wild

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Inhibition of [3H]BTX binding at site 2 of the sodium channel

Substance RN

3917968View in Reaxys

Measurement Parameter

Ki (inhibition constant)

Unit

Qualitative value

Quantitative value

265000

Measurement pX

3.58

Concomitants: Compound name

[3H]BIX

Concomitants: Compound role

RAD

Anger; Madge; Mulla; Riddall; Journal of Medicinal Chemistry; vol. 44; nb. 2; (2001); p. 115 - 137, View in Reaxys 1002 of 1220

Target Name

Sodium channel protein type 9 subunit alpha;+Sodium channel subunit beta-1

Target Synonyms

sodium channel protein type 9 subunit alpha + scn1b; sodium channel subunit beta-1

Target, Subunit, Species

Sodium channel protein type 9 subunit alpha; Sodium channel subunit beta-1

Target Mutant/Chimera Details

Sodium channel protein type 9 subunit alpha:Wild + Sodium channel subunit beta-1:Wild

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Inhibition of [3H]BTX binding at site 2 of the sodium channel

Substance RN

3917968View in Reaxys

Measurement Parameter

IC50

Unit

Qualitative value

401/467

2018-05-14 08:43:54

Quantitative value

113000

Measurement pX

3.95

Concomitants: Compound name

[3H]BIX

Concomitants: Compound role

RAD

Anger; Madge; Mulla; Riddall; Journal of Medicinal Chemistry; vol. 44; nb. 2; (2001); p. 115 - 137, View in Reaxys 1003 of 1220

1004 of 1220

Target Name

Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p08684

Target PDB ID

1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human

Bioassay Category

Metabolism/Transport

Bioassay Details

Maximum velocity for metabolic N-dealkylation reaction mediated by human cytochromeP450 3A4 (CYP3A4)

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

2.40

Measurement Parameter

qualitative

Measurement Object

log Vmax

Target Name

Sodium channel protein type 9 subunit alpha [guinea pig];+Sodium channel subunit beta-1 [guinea pig]

Target Synonyms

sodium channel protein type 9 subunit alpha + sodium channel subunit beta-1

Target, Subunit, Species

Sodium channel protein type 9 subunit alpha [guinea pig]; Sodium channel subunit beta-1 [guinea pig]

Target Mutant/Chimera Details

Sodium channel protein type 9 subunit alpha [guinea pig]:Wild + Sodium channel subunit beta-1 [guinea pig]:Wild

Target Species (Bioactivity)

guinea pig

Substance Action on Target

Radioligand (/ligand)

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested for binding of [3H]BTX-A 20alpha-benzoate to sodium channels in guinea pig cortical synaptoneurosomes

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Measurement Parameter

pIC50

Quantitative value

3.62

Measurement pX

3.62

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Concomitants: Compound name

[3H]Batrachotoxin A 20-alpha-benzoate

Concomitants: Compound role

RAD

S. P. GUPTA; Chemical reviews; vol. 91; nb. 6; (1991); p. 1109 - 1119, View in Reaxys 1005 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Concentration of the drug required to produce 1 hour anaesthesia

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Unit

Qualitative value

Quantitative value

1.05

S. P. GUPTA; Chemical reviews; vol. 91; nb. 6; (1991); p. 1109 - 1119, View in Reaxys 1006 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Minimum concentration required to completely block the excitability

Substance RN

3917968View in Reaxys

Qualitative Results

log MBC not calculated

Measurement Parameter

qualitative

Measurement Object

log MBC

S. P. GUPTA; Chemical reviews; vol. 91; nb. 6; (1991); p. 1109 - 1119, View in Reaxys 1007 of 1220

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested for inhibition of BTX-elicited phosphoinositide break down

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Measurement Parameter

pIC50

Measurement Object

BTX-elicited phosphoinositide break down

Quantitative value

3.96

Measurement pX

3.96

S. P. GUPTA; Chemical reviews; vol. 91; nb. 6; (1991); p. 1109 - 1119, View in Reaxys 1008 of 1220

Target Name

cytochrome-c oxidase

Target Synonyms

cytochrome c oxidase; cytochrome-c oxidase; cytochrome-c oxidase activity; nadh cytochrome c oxidase

Target, Subunit, Species

cytochrome-c oxidase

Target Mutant/Chimera Details

cytochrome-c oxidase:Wild

Substance Action on Target

Radioligand (/ligand)

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Binding affinity of the compound against cytochrome C oxidase

Substance RN

3917968View in Reaxys

Qualitative Results

1/Ki not calculated

Measurement Parameter

qualitative

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Measurement Object

1/Ki

S. P. GUPTA; Chemical reviews; vol. 91; nb. 6; (1991); p. 1109 - 1119, View in Reaxys 1009 of 1220

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested for inhibition of BTX-elicited sodium flux

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Measurement Parameter

pIC50

Measurement Object

BTX-elicited sodium flux

Quantitative value

3.85

Measurement pX

3.85

S. P. GUPTA; Chemical reviews; vol. 91; nb. 6; (1991); p. 1109 - 1119, View in Reaxys 1010 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Anesthetic activity of infiltration was determined

Substance RN

3917968View in Reaxys

Qualitative Results

AAI not calculated

Measurement Parameter

qualitative

Measurement Object

AAI

S. P. GUPTA; Chemical reviews; vol. 91; nb. 6; (1991); p. 1109 - 1119, View in Reaxys 1011 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Effect of the compound to treat intestine, rectal and vaginal diseases in human

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

Not tested

Patent; ASTRA AKTIEBOLAG; WO1999/12521; (1999); (A1), View in Reaxys 1012 of 1220

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lethal dose of the compound in mouse upon s.c. administration

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

subcutaneous administration

Qualitative Results

163

Measurement Parameter

LD50

Unit

mg/kg

Measurement Object

Lethal dose

Quantitative value

163

AVANT; WEATHERBY; Proceedings of the Society for Experimental Biology and Medicine. Society for Experimental Biology and Medicine (New York, N.Y.); vol. 103; (1960); p. 353 - 356, View in Reaxys 1013 of 1220

Bioassay Category

Pharmacokinetic

Bioassay Details

Increased in neonate

Biological Species/NCBI ID

human

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Substance RN

3917968View in Reaxys

Qualitative Results

2±1

Measurement Parameter

Excretion

Unit

Quantitative value

Goodman & Gilman's The Pharmacological Basis of Therapeutics, 10th ed., 2001; (2001), View in Reaxys 1014 of 1220

Bioassay Category

Metabolism/Transport

Bioassay Details

Decreased in neonate.Increased in case of myocardial infarction,cardiopulmonary bypass surgery,uremia and in aged. Unchanged in case of nephrotic syndrome,smoking and in children

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

70 ± 5

Measurement Parameter

Protein binding (%)

Unit

Quantitative value

Goodman & Gilman's The Pharmacological Basis of Therapeutics, 10th ed., 2001; (2001), View in Reaxys 1015 of 1220

Bioassay Category

Metabolism/Transport

Bioassay Details

Increased in case of cirrhosis,myocardial infarction(half life increased when infusion longer than 24hours,probably related to increased plasma binding),neonate and obese.Unchanged in case of uremia,cardiopulmonary bypass surgery and congestive heart failure(short term,nochange;long term,marked increase)

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

1.8 ± 0.4

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

1.8

Goodman & Gilman's The Pharmacological Basis of Therapeutics, 10th ed., 2001; (2001), View in Reaxys 1016 of 1220

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Toxic concentration to cause occasional toxicity

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

Measurement Parameter

Unit

µg/mL

Measurement Object

Toxic concentration

Quantitative value

Measurement pX

4.43

Goodman & Gilman's The Pharmacological Basis of Therapeutics, 10th ed., 2001; (2001), View in Reaxys 1017 of 1220

Bioassay Category

Metabolism/Transport

Bioassay Details

Decreased in case of congestive heart failure,cirrhosis,cardiopulmonary bypass surgery(decrease (~40)on day 3 after surgery; return toward normal on day 7)and in obese. Increased in case of smoking. Unchanged in case of uremia,acute viral hepatitis(during acute phase,blood clearance was

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13 ± 4ml/min/Kg,which increased to 20 ± 4ml/min/Kg after recovery) and in neonate and aged (Decreased CL with increasing age noted in patients with MI)CYP3A substrate Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

9.2 ± 2.4*

Measurement Parameter

CL (drug clearance)

Unit

mL/min/kg

Quantitative value

9.2

Goodman & Gilman's The Pharmacological Basis of Therapeutics, 10th ed., 2001; (2001), View in Reaxys 1018 of 1220

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Toxic concentration to cause frequent toxicity

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

>10

Measurement Parameter

Unit

µg/mL

Measurement Object

Toxic concentration

Quantitative value

Measurement pX

4.43

Goodman & Gilman's The Pharmacological Basis of Therapeutics, 10th ed., 2001; (2001), View in Reaxys 1019 of 1220

Bioassay Category

Pharmacokinetic

Bioassay Details

Increased in case of cirrhosis and in agedcommercial preparations are for parenteral administration

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

35 ± 11*

Measurement Parameter

F (drug bioavailability)

Unit

Quantitative value

Goodman & Gilman's The Pharmacological Basis of Therapeutics, 10th ed., 2001; (2001), View in Reaxys 1020 of 1220

Bioassay Category

Metabolism/Transport

Bioassay Details

Decreased in case of congestive heart failure,cardiopulmonary bypass surgery(decrease (~40)on day 3 after surgery; return toward normal on day 7).Increased in case of cirrhosis,neonate.Unchanged in case of uremia,aged and obese

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

1.1 ± 0.4

Measurement Parameter

Vd (volume of distribution)

Unit

L/kg

Quantitative value

1.1

Goodman & Gilman's The Pharmacological Basis of Therapeutics, 10th ed., 2001; (2001), View in Reaxys 1021 of 1220

Bioassay Category

Pharmacokinetic

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Bioassay Details

Peak concentration. Therapeutic range of blood concentrations for control of ventricular arrhythmias. Levels of 6-10 and >10 µg/ml cause occasional and frequent toxicity, respectively

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

2-5

Measurement Parameter

Cmax

Unit

µg/mL

Measurement Object

Cmax

Quantitative value

3.5

Goodman & Gilman's The Pharmacological Basis of Therapeutics, 10th ed., 2001; (2001), View in Reaxys 1022 of 1220

Bioassay Category

Metabolism/Transport

Bioassay Details

Intrinsic clearance of compound in the form of monoethylglycinexylidide in human upon oral administration; Value expressed as mL/min/g liver

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

oral administration

Measurement Parameter

CLint

Unit

mL/min/g

Measurement Object

Intrinsic clearance

Qualitative value

Quantitative value

3.53

Iwatsubo, Takafumi; Hirota, Noriko; Ooie, Tsuyoshi; Suzuki, Hiroshi; Shimada, Noriaki; Chiba, Kan; Ishizaki, Takashi; Green, Carol E.; Tyson, Charles A.; Sugiyama, Yuichi; Pharmacology and Therapeutics; vol. 73; nb. 2; (1997); p. 147 - 171, View in Reaxys 1023 of 1220

Bioassay Category

Metabolism/Transport

Bioassay Details

Michaelis-Menten constant (high affinity component) for formation of monoethylglycinexylidide in human liver microsomes upon incubation with compound (20-5000 uM) for 60 min

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Measurement Object

Michaelis-menten constant

Qualitative value

Quantitative value

1623

Measurement pX

2.79

Bioassay Category

Metabolism/Transport

Bioassay Details

Michaelis-Menten constant (low affinity component) for formation of monoethylglycinexylidide in human liver microsomes upon incubation with compound (20-5000 uM) for 60 min

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

407/467

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Measurement Parameter

Km (Michaelis constant)

Unit

µM

Measurement Object

Michaelis-menten constant

Qualitative value

Quantitative value

52.9

Measurement pX

4.28

Bioassay Category

Metabolism/Transport

Bioassay Details

Fraction of compound unbound in human blood upon oral administration

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

oral administration

Measurement Parameter

protein binding

Measurement Object

Fraction of compound unbound

Quantitative value

0.296

Bioassay Category

Pharmacokinetic

Bioassay Details

Fraction of compound absorbed in human intestine upon oral administration

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

oral administration

Measurement Parameter

Absorption

Measurement Object

Fraction of compound absorbed

Quantitative value

0.84

Bioassay Category

Metabolism/Transport

Bioassay Details

In vitro hepatic clearance of the compound

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Measurement Parameter

CLH

Unit

mL/min

Measurement Object

Hepatic clearance

Qualitative value

Quantitative value

758

408/467

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1028 of 1220

Bioassay Category

Metabolism/Transport

Bioassay Details

In vivo hepatic clearance of the compound

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Measurement Parameter

CLH

Unit

mL/min

Measurement Object

Clearance

Qualitative value

Quantitative value

875

Bioassay Category

Metabolism/Transport

Bioassay Details

In vitro intrinsic clearance of compound (20-5000 uM) in the form of monoethylglycinexylidide measured in human liver microsomes upon incubation for 60 min; Value expressed as mL/min/g liver

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Measurement Parameter

CLint

Unit

mL/min/g

Measurement Object

Intrinsic clearance

Qualitative value

Quantitative value

2.4

Bioassay Category

Metabolism/Transport

Bioassay Details

In vitro intrinsic clearance of the compound metabolized by CYP3A4

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Measurement Parameter

CLint

Unit

mL/min

Measurement Object

Intrinsic clearance

Qualitative value

Quantitative value

6970

Bioassay Category

Metabolism/Transport

Bioassay Details

Hepatic clearance of compound in human upon oral administration

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

oral administration

409/467

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Measurement Parameter

CL (drug clearance)

Unit

mL/min

Measurement Object

Half Life

Qualitative value

Quantitative value

1298

Bioassay Category

Metabolism/Transport

Bioassay Details

Urinary excretion of monoethylglycinexylidide (metabolite) in human upon oral administration of compound

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

oral administration

Measurement Parameter

percentage of dose excreted in urine

Unit

Measurement Object

Urinary excretion

Qualitative value

Quantitative value

3.7

Bioassay Category

Metabolism/Transport

Bioassay Details

Renal clearance of compound in human upon oral administration

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

oral administration

Measurement Parameter

CLR

Unit

mL/min

Qualitative value

Quantitative value

129

Bioassay Category

Metabolism/Transport

Bioassay Details

Total clearance of compound in human upon oral administration

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

oral administration

Measurement Parameter

CL (drug clearance)

Unit

mL/min

Measurement Object

Total clearance

Qualitative value

410/467

2018-05-14 08:43:54

Quantitative value

4603

Bioassay Category

Metabolism/Transport

Bioassay Details

Urinary excretion of metabolites (other than monoethylglycinexylidide) in human upon oral administration of compound

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

oral administration

Measurement Parameter

percentage of dose excreted in urine

Unit

Measurement Object

Urinary excretion

Qualitative value

Quantitative value

76.2

Bioassay Category

Metabolism/Transport

Bioassay Details

Maximal rate of metabolism (high affinity component) of compound (20-5000 uM) measured for formation of monoethylglycinexylidide in human liver microsomes upon incubation for 60 min; Value expressed as nmol/min/mg protein

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

Vmax1 not calculated

Measurement Parameter

qualitative

Measurement Object

Vmax1

Bioassay Category

Metabolism/Transport

Bioassay Details

In vivo total clearance of the compound

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Measurement Parameter

CL (drug clearance)

Unit

mL/min

Measurement Object

Total clearance

Qualitative value

Quantitative value

1094

Bioassay Category

Metabolism/Transport

Bioassay Details

Maximal rate of metabolism (low affinity component) of compound (20-5000 uM) measured for formation of monoethylglycinexylidide in human liver microsomes upon incubation for 60 min; Value expressed as nmol/min/mg protein

411/467

2018-05-14 08:43:54

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Qualitative Results

Vmax2 not calculated

Measurement Parameter

qualitative

Measurement Object

Vmax2

Bioassay Category

Metabolism/Transport

Bioassay Details

Blood to plasma concentration ratio of compound in human upon oral administration

Biological Species/NCBI ID

human

Substance RN

3917968View in Reaxys

Substance Route of Adm.

oral administration

Measurement Parameter

blood/plasma ratio

Measurement Object

Blood to plasma concentration ratio

Quantitative value

0.839

Bioassay Category

In Vivo (Animal models)

Bioassay Details

Compound was tested for its anticonvulsant activity in the subcutaneous pentylenetetrazole seizure threshold(Sc Met)test after i.p administration in mice

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

subcutaneous administration

Measurement Parameter

ED50

Unit

mg/kg

Qualitative value

Quantitative value

F Lepage; F Tombret; G Cuvier; A Marivain; JM Gillardin; European journal of medicinal chemistry; vol. 27; (1992); p. 581 - 593, View in Reaxys 1041 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Details

Compound was tested for its anticonvulsant activity in the maximal electroshock seizure (MES) test after i.p administration in mice

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intraperitoneal administration

Measurement Parameter

ED50

Unit

mg/kg

Measurement Object

Anticonvulsant activity

Qualitative value

Quantitative value

14.4

412/467

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F Lepage; F Tombret; G Cuvier; A Marivain; JM Gillardin; European journal of medicinal chemistry; vol. 27; (1992); p. 581 - 593, View in Reaxys 1042 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Protective effect of compound on ouabain induced arrhythmia was determined in 15 anaesthetized dogs upon i.v. administration of 2mg/kg dose

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Qualitative Results

Protective effect not calculated

Measurement Parameter

qualitative

Measurement Object

Protective effect

Zoltan ZUBOVICS; Lajos TOLDY; Andras VARRO; Gyorgy RABLOCZKY; Maria KURTHY; Peter DVORTSAK; Gyorgy JERKOVICH; Eva TOMORI; European journal of medicinal chemistry; vol. 21; nb. 5; (1986); p. 370 - 378, View in Reaxys 1043 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Details

Ability of the compound to prolong the onset of aconitine induced arrhythmias was evaluated (i.p) in mice

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intraperitoneal administration

Measurement Parameter

ED50

Unit

mg/kg

Measurement Object

Prolong the onset of aconitine induced arrhythmias

Qualitative value

Quantitative value

Bioassay Category

In Vivo (Animal models)

Bioassay Details

Protection index (PI=TD50/ED50) against maximal electroshock seizure in mouse upon i.p administration

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intraperitoneal administration

Measurement Parameter

number

Measurement Object

Quantitative value

4.5

F Lepage; F Tombret; G Cuvier; A Marivain; JM Gillardin; European journal of medicinal chemistry; vol. 27; (1992); p. 581 - 593, View in Reaxys 1045 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Protection index (PI=TD50/ED50) against maximal electroshock seizure in rat upon oral administration

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

413/467

2018-05-14 08:43:54

Substance Route of Adm.

oral administration

Measurement Parameter

number

Measurement Object

Qualitative value

Quantitative value

1.13

F Lepage; F Tombret; G Cuvier; A Marivain; JM Gillardin; European journal of medicinal chemistry; vol. 27; (1992); p. 581 - 593, View in Reaxys 1046 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Protection index (PI=TD50/ED50) against maximal electroshock seizure in rat upon oral administration

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

oral administration

Measurement Parameter

number

Measurement Object

Quantitative value

9.1

F Lepage; F Tombret; G Cuvier; A Marivain; JM Gillardin; European journal of medicinal chemistry; vol. 27; (1992); p. 581 - 593, View in Reaxys 1047 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Protective effect of compound on ouabain induced arrhythmia was determined in 15 anaesthetized dogs upon i.v. administration of 8mg/kg dose

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Qualitative Results

Protective effect not calculated

Measurement Parameter

qualitative

Measurement Object

Protective effect

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Effect of compound (2mg/kg) in Bacl2 induced arrhythmia was determined in conscious rabbits upon i.v administration; value expressed as protective effect/number of animals ; 2/10

Biological Species/NCBI ID

Leporidae

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Qualitative Results

Protective effect not calculated

Measurement Parameter

qualitative

Measurement Object

Protective effect

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Local anaesthetic activity of the compound was determined in vitro by measuring 50 block time in sciatic nerve of the frog at a concentration of 2.5mM

414/467

2018-05-14 08:43:54

Biological Species/NCBI ID

Anura

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Unit

minute

Measurement Object

Block time

Qualitative value

Quantitative value

A Geronikaki; G Theophilidis; European journal of medicinal chemistry; vol. 27; (1992); p. 709 - 716, View in Reaxys 1050 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Details

Effect of the compound on onset of aconitine induced severe ventricular arrhythmias was determined in mice upon i.p. administration of 40mg/kg dose

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intraperitoneal administration

Measurement Parameter

Activity

Unit

second

Qualitative value

Quantitative value

144.5

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Latent period was determined in toad after injecting the compound

Biological Species/NCBI ID

Anura

Substance RN

3917968View in Reaxys

Measurement Parameter

Latency

Unit

minute

Measurement Object

Latent period was determined in toad

Qualitative value

Quantitative value

37.2

Li, Wen; You, Qidong; Bioorganic and Medicinal Chemistry Letters; vol. 17; nb. 13; (2007); p. 3733 - 3735, View in Reaxys 1052 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Details

Compound was tested for its anticonvulsant activity in the maximal electroshock seizure(MES) test after oral administration in rats

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

oral administration

Measurement Parameter

ED50

Unit

mg/kg

Qualitative value

Quantitative value

31.2

415/467

2018-05-14 08:43:54

F Lepage; F Tombret; G Cuvier; A Marivain; JM Gillardin; European journal of medicinal chemistry; vol. 27; (1992); p. 581 - 593, View in Reaxys 1053 of 1220

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Toxic dose against mouse upon i.p. adminsitration

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Qualitative Results

65.1

Measurement Parameter

TD50

Unit

mg/kg

Measurement Object

Toxic dose

Quantitative value

65.1

F Lepage; F Tombret; G Cuvier; A Marivain; JM Gillardin; European journal of medicinal chemistry; vol. 27; (1992); p. 581 - 593, View in Reaxys 1054 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Details

Protective effect of compound on ouabain induced arrhythmia was determined in 10 anaesthetized dogs upon i.v. administration of 0.5mg/kg dose

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Qualitative Results

Protective effect not calculated

Measurement Parameter

qualitative

Measurement Object

Protective effect

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Protective effect of compound on ouabain induced arrhythmia was determined in 15 anaesthetized dogs upon i.v. administration of 4mg/kg dose

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Qualitative Results

Protective effect not calculated

Measurement Parameter

qualitative

Measurement Object

Protective effect

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Protection index (PI=TD50/ED50) against subcutaneous metrazol seizure threshold in mouse upon i.p administration

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intraperitoneal administration

Measurement Parameter

number

416/467

2018-05-14 08:43:54

Measurement Object

Qualitative value

Quantitative value

0.1

F Lepage; F Tombret; G Cuvier; A Marivain; JM Gillardin; European journal of medicinal chemistry; vol. 27; (1992); p. 581 - 593, View in Reaxys 1057 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Details

Effect of the compound on onset of aconitine induced severe ventricular arrhythmias was determined in mice upon p.o. administration of 100mg/kg dose

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

oral administration

Measurement Parameter

Activity

Unit

second

Qualitative value

Quantitative value

119.5

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Toxic dose against rat upon oral adminsitration

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Qualitative Results

283.4

Measurement Parameter

TD50

Unit

mg/kg

Measurement Object

Toxic dose

Quantitative value

283.4

F Lepage; F Tombret; G Cuvier; A Marivain; JM Gillardin; European journal of medicinal chemistry; vol. 27; (1992); p. 581 - 593, View in Reaxys 1059 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Protective effect of compound on ouabain induced arrhythmia was determined in 15 anaesthetized dogs upon i.v. administration of 1mg/kg dose

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Qualitative Results

Protective effect not calculated

Measurement Parameter

qualitative

Measurement Object

Protective effect

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Effect of the compound on the recovery of the action potential was determined in sciatic nerve of the frog at a concentration of 2.5mM; Value ranges from 20-25min

417/467

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Biological Species/NCBI ID

Anura

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Unit

minute

Measurement Object

Recovery time

Qualitative value

Quantitative value

A Geronikaki; G Theophilidis; European journal of medicinal chemistry; vol. 27; (1992); p. 709 - 716, View in Reaxys 1061 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Details

Compound was tested for its anticonvulsant activity in the subcutaneous pentylenetetrazole seizure threshold(Sc Met)test after oral administration in rats

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

oral administration

Measurement Parameter

ED50

Unit

mg/kg

Qualitative value

Quantitative value

250

F Lepage; F Tombret; G Cuvier; A Marivain; JM Gillardin; European journal of medicinal chemistry; vol. 27; (1992); p. 581 - 593, View in Reaxys 1062 of 1220

Substance Action on Target

Blocker

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

In vitro effective dose of the compound required for sciatic nerve block in toad

Biological Species/NCBI ID

Anura

Substance RN

3917968View in Reaxys

Measurement Parameter

ED50

Unit

Qualitative value

Quantitative value

0.019

Li, Wen; You, Qidong; Bioorganic and Medicinal Chemistry Letters; vol. 17; nb. 13; (2007); p. 3733 - 3735, View in Reaxys 1063 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Effect of compound in ouabain induced arrhythmia in anaesthetized dogs

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Measurement Parameter

ED50

Unit

mg/kg

Measurement Object

ouabain induced arrhythmia

Qualitative value

Quantitative value

418/467

2018-05-14 08:43:54

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

In vivo infiltration anesthetic activity of the compound was determined on mouse tail

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

pIC50

Quantitative value

1.8

Measurement pX

1.8

G Caliendo; G Greco; P Grieco; G Mattace Raso; R Meli; E Novellino; E Perissutti; V Santagada; European journal of medicinal chemistry; vol. 31; (1996); p. 99 - 104, View in Reaxys 1065 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Infiltration anesthesia was expressed as log 1/IC50 in mouse

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

pIC50

Measurement Object

Infiltration anesthesia expressed as log 1/IC50

Quantitative value

1.8

Measurement pX

1.8

G Caliendo; R Di Carlo; G Greco; P Grieco; R Meli; E Novellino; E Perissutti; V Santagada; European journal of medicinal chemistry; vol. 30; (1995); p. 603 - 608, View in Reaxys 1066 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

In vivo duration of local anaesthetic activity in rat sciatic nerve block (rat received 0.2mL of 2 anaesthetic solution)

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

time

Unit

minute

Qualitative value

Quantitative value

117

Giuseppe Caliendo; Ferdinando Fiorino; Paolo Grieco; Elisa Perissutti; Vincenzo Santagada; Rosaria Meli; Giuseppina Mattace Raso; Angelina Zanesco; Gilberto De Nucci; European journal of medicinal chemistry; vol. 34; nb. 12; (1999); p. 1043 - 1051, View in Reaxys 1067 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

In vivo duration of local anaesthetic activity in rat sciatic nerve block (rat received 0.2mL of 2 anaesthetic solution)

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

time

Unit

minute

Qualitative value

Quantitative value

117

419/467

2018-05-14 08:43:54

Deviation

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Antiarrhythmic activity of mice measured as number of mice protected against CaCl2 induced arrhythmia/total number of animals tested at a concentration of 30mg/kg(i.p); 4/5

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intraperitoneal administration

Measurement Parameter

Activity

Measurement Object

Antiarrhythmic activity

Quantitative value

Ludmila Leite; Daina Jansone; Maris Veveris; Helena Cirule; Yuris Popelis; Gagik Melikyan; Anna Avetisyan; Edmunds Lukevics; European journal of medicinal chemistry; vol. 34; nb. 10; (1999); p. 859 - 865, View in Reaxys 1069 of 1220

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lethality of compound on CaCl2 induced arrhythmia in rat at a dose of 0.3mg/kg (i.v.) was determined expressed as survival rate

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Measurement Parameter

Survival activity

Unit

Qualitative value

Quantitative value

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

In vivo anaesthetic activity of the compound was tested in rabbit cornea

Biological Species/NCBI ID

Leporidae

Cells/Cell Lines

cornea cell

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Measurement Object

Anaesthetic activity

Quantitative value

100

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Surface anesthetic activity was expressed as the logarithm of percentage of the area under the curve with respect tolidocane in rabbit cornea

Biological Species/NCBI ID

Leporidae

Cells/Cell Lines

cornea cell

Substance RN

3917968View in Reaxys

420/467

2018-05-14 08:43:54

Measurement Parameter

qualitative

Measurement Object

Anesthetic activity

Qualitative value

Not Published

G Caliendo; R Di Carlo; G Greco; P Grieco; R Meli; E Novellino; E Perissutti; V Santagada; European journal of medicinal chemistry; vol. 30; (1995); p. 603 - 608, View in Reaxys 1072 of 1220

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lethality of compound on CaCl2 induced arrhythmia in rat at a dose of 3.0mg/kg (i.v.) was determined expressed as survival rate

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Measurement Parameter

Survival activity

Unit

Qualitative value

Quantitative value

Bioassay Category

In Vivo (Animal models)

Bioassay Details

In vivo anesthetic activity determined 15 min after sc administration of compound in mice tail

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

subcutaneous administration

Measurement Parameter

IC50

Unit

Qualitative value

Quantitative value

0.016

Deviation

0.0043

Measurement pX

1.8

G Caliendo; R Di Carlo; G Greco; P Grieco; R Meli; E Novellino; E Perissutti; V Santagada; European journal of medicinal chemistry; vol. 30; (1995); p. 603 - 608, View in Reaxys 1074 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Details

Antiarrhythmic activity of mice measured as number of mice protected against CaCl2 induced arrhythmia/total number of animals tested at a concentration of 15mg/kg(i.p); 2/5

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intraperitoneal administration

Measurement Parameter

Activity

Measurement Object

Antiarrhythmic activity

Quantitative value

Bioassay Category

In Vitro (Efficacy)

421/467

2018-05-14 08:43:54

Bioassay Details

In vivo local surface anesthetic activity evaluated by determining the number of stimuli to the cornea every 3 min in rabbit cornea

Biological Species/NCBI ID

Leporidae

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Unit

Measurement Object

Local surface anesthetic activity

Qualitative value

Quantitative value

100

G Caliendo; R Di Carlo; G Greco; P Grieco; R Meli; E Novellino; E Perissutti; V Santagada; European journal of medicinal chemistry; vol. 30; (1995); p. 603 - 608, View in Reaxys 1076 of 1220

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Therapeutic index of LD50 to that of IC50

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Qualitative Results

8.2300000000

Measurement Parameter

therapeutic index

Measurement Object

Therapeutic index

Quantitative value

8.23

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Chronotropic activity of the compound was tested in rat right atria; n=6

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Qualitative Results

Maximal response not calculated

Measurement Parameter

qualitative

Measurement Object

Maximal response

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lethality of compound on CaCl2 induced arrhythmia in rat at a dose of 1.0mg/kg (i.v.) was determined expressed as survival rate

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Measurement Parameter

Survival activity

Unit

Qualitative value

Quantitative value

422/467

2018-05-14 08:43:54

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Arrhythmia-score of the compound on CaCl2 -induced arrhythmia in rat at a dose of 1.0mg/kg (i.v.)

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Measurement Parameter

number

Measurement Object

Arrhythmia score

Quantitative value

2.1

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Blood-brain permeability of the compound in CNS was determined; ' +' denotes the capability to penetrate blood-brain barrier

Substance RN

3917968View in Reaxys

Measurement Parameter

qualitative

Measurement Object

Blood-brain permeability in CNS

Qualitative value

Not Published

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Therapeutic index of the compound as acute toxicity over anaesthetic activity in mouse

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

therapeutic index

Unit

mg/kg

Qualitative value

Quantitative value

8.23

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Chronotropic activity of the compound was tested in rat right atria

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Qualitative Results

Maximum response not calculated

Measurement Parameter

qualitative

Measurement Object

Maximum response

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

In vivo anaesthetic activity of the compound was tested in rabbit cornea

423/467

2018-05-14 08:43:54

Biological Species/NCBI ID

Leporidae

Substance RN

3917968View in Reaxys

Measurement Parameter

percentage

Unit

Measurement Object

Anaesthetic activity

Qualitative value

Quantitative value

100

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Inhibitory activity of the compound tested in mouse

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

IC50

Unit

Qualitative value

Quantitative value

0.0068

Measurement pX

2.17

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

In vivo local anesthetic activity of the compound was determined on mouse tail

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

IC50

Unit

Qualitative value

Quantitative value

0.01

Deviation

0.0043

Measurement pX

G Caliendo; G Greco; P Grieco; G Mattace Raso; R Meli; E Novellino; E Perissutti; V Santagada; European journal of medicinal chemistry; vol. 31; (1996); p. 99 - 104, View in Reaxys 1086 of 1220

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Therepeutic indices of the compound in mouse determined as Ratio of LD50 to that of IC50

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

therapeutic index

Measurement Object

Quantitative value

5.1

424/467

2018-05-14 08:43:54

G Caliendo; G Greco; P Grieco; G Mattace Raso; R Meli; E Novellino; E Perissutti; V Santagada; European journal of medicinal chemistry; vol. 31; (1996); p. 99 - 104, View in Reaxys 1087 of 1220

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Acute toxicity of the compound was measured in male mouse after ip administration

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intraperitoneal administration

Measurement Parameter

LD50

Unit

mg/kg

Qualitative value

Quantitative value

110

G Caliendo; G Greco; P Grieco; G Mattace Raso; R Meli; E Novellino; E Perissutti; V Santagada; European journal of medicinal chemistry; vol. 31; (1996); p. 99 - 104, View in Reaxys 1088 of 1220

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Acute toxicity of the compound tested in mouse after ip administration

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intraperitoneal administration

Qualitative Results

56000.0000

Measurement Parameter

LD50

Unit

µM

Quantitative value

56000

Measurement pX

1.25

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Acute toxicity of the compound tested in mouse after ip administration

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intraperitoneal administration

Measurement Parameter

LD50

Unit

Qualitative value

Quantitative value

0.05

Deviation

0.0039

Measurement pX

1.3

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

In vivo local anesthetic activity of the compound was determined on rabbit cornea

425/467

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Biological Species/NCBI ID

Leporidae

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Unit

Measurement Object

Local anesthetic activity

Qualitative value

Quantitative value

100

G Caliendo; G Greco; P Grieco; G Mattace Raso; R Meli; E Novellino; E Perissutti; V Santagada; European journal of medicinal chemistry; vol. 31; (1996); p. 99 - 104, View in Reaxys 1091 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

In vivo duration of local anesthetic activity in rat sciatic nerve block

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

time

Unit

minute

Measurement Object

Duration of local anesthetic activity

Qualitative value

Quantitative value

110

G Caliendo; G Greco; P Grieco; G Mattace Raso; R Meli; E Novellino; E Perissutti; V Santagada; European journal of medicinal chemistry; vol. 31; (1996); p. 99 - 104, View in Reaxys 1092 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Details

Arrhythmia-score of the compound on CaCl2 -induced arrhythmia in rat at a dose of 0.3mg/kg (i.v.)

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Measurement Parameter

number

Measurement Object

Arrhythmia score

Quantitative value

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

In vivo anaesthetic activity of the compound was tested in mouse tail

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

IC50

Unit

Measurement Object

Anaesthetic activity

Qualitative value

Quantitative value

0.0068

Measurement pX

2.17

426/467

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Bioassay Category

In Vitro (Efficacy)

Bioassay Details

In vivo anaesthetic activity of the compound was tested in mouse tail

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

IC50

Unit

Measurement Object

Anaesthetic activity

Qualitative value

Quantitative value

0.0068

Deviation

0.0039

Measurement pX

2.17

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

In vivo surface anesthetic activity of the compound was determined on rabbit corne

Biological Species/NCBI ID

Leporidae

Substance RN

3917968View in Reaxys

Qualitative Results

log AUC not calculated

Measurement Parameter

qualitative

Measurement Object

log AUC

G Caliendo; G Greco; P Grieco; G Mattace Raso; R Meli; E Novellino; E Perissutti; V Santagada; European journal of medicinal chemistry; vol. 31; (1996); p. 99 - 104, View in Reaxys 1096 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Arrhythmia-score of the compound on CaCl2 -induced arrhythmia in rat at a dose of 3.0mg/kg (i.v.)

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Measurement Parameter

number

Measurement Object

Arrhythmia score

Quantitative value

1.8

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

In vivo duration of local anaesthetic activity in rat sciatic nerve block (rat received 0.2mL of 1 anaesthetic solution)

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

time

Unit

minute

427/467

2018-05-14 08:43:54

Qualitative value

Quantitative value

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

In vivo duration of local anaesthetic activity in rat sciatic nerve block (rat received 0.2mL of 1 anaesthetic solution)

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

time

Unit

minute

Qualitative value

Quantitative value

Deviation

10.7

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

In vitro inhibitory activity against Plasmodium falciparum W2 strain infected in red blood cells (5 ul) upon incubation with compound dissolved in DMSO at 37 degree C for 72 hrs in 5% CO2, 5% O2 and 90% N2 using SYBR Green viability assay with DMSO as negative control

Biological Species/NCBI ID

Plasmodium falciparum W2

Cells/Cell Lines

erythrocyte

Substance RN

3917968View in Reaxys

Qualitative Results

Inconclusive active and P value <0.05 in both replicates in two independent screens of each parasite line

Measurement Parameter

pIC50

Quantitative value

-5

Yuan, Jing; Johnson, Ronald L.; Huang, Ruili; Wichterman, Jennifer; Jiang, Hongying; Hayton, Karen; Fidock, David A.; Wellems, Thomas E.; Inglese, James; Austin, Christopher P.; Su, Xin-Zhuan; Nature Chemical Biology; vol. 5; nb. 10; (2009); p. 765 - 771, View in Reaxys 1100 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested for surface anaesthetic effect on rabbit cornea

Biological Species/NCBI ID

Leporidae

Cells/Cell Lines

cornea cell

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Quantitative value

A. F. Harms; H. M. Tersteege; W. TH. Nauta; Journal of medicinal chemistry; vol. 4; nb. 3; (1961); p. 575 - 577, View in Reaxys 1101 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested for conduction anaesthetic effect on rat tail

428/467

2018-05-14 08:43:54

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Quantitative value

A. F. Harms; H. M. Tersteege; W. TH. Nauta; Journal of medicinal chemistry; vol. 4; nb. 3; (1961); p. 575 - 577, View in Reaxys 1102 of 1220

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Concentration that cause toxicity was determined upon intraperitoneal administration of compound in mice

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intramuscular administration

Measurement Parameter

LD50

Unit

mg/kg

Qualitative value

Quantitative value

140

Werner R. Boehme; Mary Lee Graeme; William G. Scharpf; Estelle Siegmund; Edgar Schipper; Martin Tobkes; Journal of medicinal chemistry; vol. 4; nb. 1; (1961); p. 183 - 205, View in Reaxys 1103 of 1220

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Concentration that cause toxicity was determined upon intraperitoneal administration of compound in mice

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intramuscular administration

Measurement Parameter

LD50

Unit

mg/kg

Qualitative value

Quantitative value

175

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Irritating effect of the compound

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Measurement Object

Irritating effect

Quantitative value

A. F. Harms; H. M. Tersteege; W. TH. Nauta; Journal of medicinal chemistry; vol. 4; nb. 3; (1961); p. 575 - 577, View in Reaxys 1105 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Local anaesthetic activity with respect to parent compound compared to standard as 1 was determined

Biological Species/NCBI ID

Leporidae

Substance RN

3917968View in Reaxys

429/467

2018-05-14 08:43:54

Measurement Parameter

Activity

Quantitative value

1.8

HARMS; NAUTA; Journal of medicinal and pharmaceutical chemistry; vol. 2; (1960); p. 57 - 77, View in Reaxys 1106 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Approximate anaesthetic concentration was determined by infiltration technique in dogs

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Measurement Parameter

percentage

Unit

Measurement Object

AD50

Qualitative value

Quantitative value

0.1

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested for infiltration anaesthetic effect on guinea pig back

Biological Species/NCBI ID

guinea pig

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Quantitative value

A. F. Harms; H. M. Tersteege; W. TH. Nauta; Journal of medicinal chemistry; vol. 4; nb. 3; (1961); p. 575 - 577, View in Reaxys 1108 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Approximate anaesthetic concentration was determined by infiltration technique in dogs; Range is 0.1-0.25

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Measurement Parameter

percentage

Unit

Measurement Object

AD50

Qualitative value

Quantitative value

0.25

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Antiarrhythmic activity was determined by measuring the reduction in duration of methacholineinduced auricular arrhythmia in dogs at a dose of 5 mg/kg

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Measurement Parameter

percentage

Unit

Measurement Object

Reduction activity

430/467

2018-05-14 08:43:54

Qualitative value

Quantitative value

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Irritant ratio of the compound (Threshold irritant concentration/~ AD50)

Substance RN

3917968View in Reaxys

Measurement Parameter

Activity

Measurement Object

Irritant ratio

Quantitative value

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Antiarrhythmic effect in conscious coronary artery ligated dog after 5 min intravenous administration of 10 mg/kg dose

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Measurement Parameter

percentage

Unit

Measurement Object

Normal beats

Qualitative value

Quantitative value

Deviation

Hoefle; Blouin; Fleming; Hastings; Hinkley; Mertz; Steffe; Stratton; Werbel; Journal of Medicinal Chemistry; vol. 34; nb. 1; (1991); p. 7 - 12, View in Reaxys 1112 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Percent of normal beats 20 min after a dose of 5 mg/kg of the compound given intravenously over a 5-min period in coronary ligated dogs.

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Measurement Parameter

percentage

Unit

Measurement Object

Normal beats

Qualitative value

Quantitative value

Hoefle; Blouin; Fleming; Hastings; Hinkley; Mertz; Steffe; Stratton; Werbel; Journal of Medicinal Chemistry; vol. 34; nb. 1; (1991); p. 7 - 12, View in Reaxys 1113 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Antiarrhythmic effect in conscious coronary artery ligated dog after 20 min intravenous administration of 5 mg/kg dose

Biological Species/NCBI ID

dog

431/467

2018-05-14 08:43:54

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Measurement Parameter

percentage

Unit

Measurement Object

Normal beats

Qualitative value

Quantitative value

Deviation

Hoefle; Blouin; Fleming; Hastings; Hinkley; Mertz; Steffe; Stratton; Werbel; Journal of Medicinal Chemistry; vol. 34; nb. 1; (1991); p. 7 - 12, View in Reaxys 1114 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Antiarrhythmic effect in conscious coronary artery ligated dog after 1 h intravenous administration of 5 mg/kg dose

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Measurement Parameter

percentage

Unit

Measurement Object

Normal beats

Qualitative value

Quantitative value

Deviation

Hoefle; Blouin; Fleming; Hastings; Hinkley; Mertz; Steffe; Stratton; Werbel; Journal of Medicinal Chemistry; vol. 34; nb. 1; (1991); p. 7 - 12, View in Reaxys 1115 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Percent of normal beats at the end of the dose.(5 mg/kg of the compound was given intravenously over a 5-min period in coronary ligated dogs.)

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Measurement Parameter

percentage

Unit

Measurement Object

Normal beats

Qualitative value

Quantitative value

Hoefle; Blouin; Fleming; Hastings; Hinkley; Mertz; Steffe; Stratton; Werbel; Journal of Medicinal Chemistry; vol. 34; nb. 1; (1991); p. 7 - 12, View in Reaxys 1116 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Activity rating calculated as effect due to test compound / effect due ideal drug x 100.5 mg/kg of compound given intravenously.

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

432/467

2018-05-14 08:43:54

Measurement Parameter

Activity

Quantitative value

Hoefle; Blouin; Fleming; Hastings; Hinkley; Mertz; Steffe; Stratton; Werbel; Journal of Medicinal Chemistry; vol. 34; nb. 1; (1991); p. 7 - 12, View in Reaxys 1117 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Details

Percent of normal beats 1 h after a dose of 5 mg/kg of the compound given intravenously over a 5min period in coronary ligated dogs.

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Measurement Parameter

percentage

Unit

Measurement Object

Normal beats

Qualitative value

Quantitative value

Hoefle; Blouin; Fleming; Hastings; Hinkley; Mertz; Steffe; Stratton; Werbel; Journal of Medicinal Chemistry; vol. 34; nb. 1; (1991); p. 7 - 12, View in Reaxys 1118 of 1220

Bioassay Category

In Vivo (Animal models)

Bioassay Details

Activity rating was determined by the effect of the compound / effect of ideal drug x 100 after intravenous administration of 5 mg/kg in dogs

Biological Species/NCBI ID

dog

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intravenous administration

Measurement Parameter

Activity

Quantitative value

Hoefle; Blouin; Fleming; Hastings; Hinkley; Mertz; Steffe; Stratton; Werbel; Journal of Medicinal Chemistry; vol. 34; nb. 1; (1991); p. 7 - 12, View in Reaxys 1119 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Antiarrhythmic activity determined by number of cats with occlusive arrhythmia including ventricular fibrilation out of 7 at 10 mg/kg dosage; Control is 5 out of 22

Biological Species/NCBI ID

domestic cat

Substance RN

3917968View in Reaxys

Qualitative Results

No. of cats not calculated

Measurement Parameter

qualitative

Measurement Object

No. of cats

L. N. Sernov; S. Ya. Skachilova; D. S. Blinov; V. V. Druzhinina; Ya. V. Kostin; E. V. Shilova; Pharm Chem J; vol. 39; nb. 7; (2005); p. 350 - 353, View in Reaxys 1120 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Antiarrhythmic activity determined by number of cats with reperfusive arrhythmia including ventricular fibrilation out of 6 at 10 mg/kg dosage; Control is 5 out of 17

Biological Species/NCBI ID

domestic cat

Substance RN

3917968View in Reaxys

Qualitative Results

No. of cats not calculated

433/467

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Measurement Parameter

qualitative

Measurement Object

No. of cats

L. N. Sernov; S. Ya. Skachilova; D. S. Blinov; V. V. Druzhinina; Ya. V. Kostin; E. V. Shilova; Pharm Chem J; vol. 39; nb. 7; (2005); p. 350 - 353, View in Reaxys 1121 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Antiarrhythmic activity determined by number of cats with reperfusive arrhythmia out of 6 at 10 mg/kg dosage ;Control is 17 out of 17

Biological Species/NCBI ID

domestic cat

Substance RN

3917968View in Reaxys

Qualitative Results

No. of cats not calculated

Measurement Parameter

qualitative

Measurement Object

No. of cats

L. N. Sernov; S. Ya. Skachilova; D. S. Blinov; V. V. Druzhinina; Ya. V. Kostin; E. V. Shilova; Pharm Chem J; vol. 39; nb. 7; (2005); p. 350 - 353, View in Reaxys 1122 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Antifibrillatory activity determined by number of calcium chloride arrhythmic mice with ventricular fibrilation out of 10 at 5 mg/kg dosage;Control is 7 out of 8

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Qualitative Results

No. of mice not calculated

Measurement Parameter

qualitative

Measurement Object

No. of mice

L. N. Sernov; S. Ya. Skachilova; D. S. Blinov; V. V. Druzhinina; Ya. V. Kostin; E. V. Shilova; Pharm Chem J; vol. 39; nb. 7; (2005); p. 350 - 353, View in Reaxys 1123 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Antifibrillatory activity determined by number of calcium chloride arrhythmic mice lost out of 10 at 5 mg/kg dosage

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Qualitative Results

No. of mice not calculated

Measurement Parameter

qualitative

Measurement Object

No. of mice

L. N. Sernov; S. Ya. Skachilova; D. S. Blinov; V. V. Druzhinina; Ya. V. Kostin; E. V. Shilova; Pharm Chem J; vol. 39; nb. 7; (2005); p. 350 - 353, View in Reaxys 1124 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Antiarrhythmic activity determined by number of cats with occlusive arrhythmia out of 7 at 10 mg/kg dosage to ;Control is 17 out of 22

Biological Species/NCBI ID

domestic cat

Substance RN

3917968View in Reaxys

Qualitative Results

No. of cats not calculated

Measurement Parameter

qualitative

Measurement Object

No. of cats

L. N. Sernov; S. Ya. Skachilova; D. S. Blinov; V. V. Druzhinina; Ya. V. Kostin; E. V. Shilova; Pharm Chem J; vol. 39; nb. 7; (2005); p. 350 - 353, View in Reaxys

434/467

2018-05-14 08:43:54

1125 of 1220

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Acute toxicity in mice after intraperitoneal administration of compound

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Substance Route of Adm.

intraperitoneal administration

Measurement Parameter

LD50

Unit

mg/kg

Measurement Object

Acute toxicity

Qualitative value

Quantitative value

203

Deviation

L. N. Sernov; S. Ya. Skachilova; D. S. Blinov; V. V. Druzhinina; Ya. V. Kostin; E. V. Shilova; Pharm Chem J; vol. 39; nb. 7; (2005); p. 350 - 353, View in Reaxys 1126 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Local anaesthetic activity of the compound was tested in mice at concentration of 1 percent

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

percentage

Unit

Measurement Object

response rate

Qualitative value

Quantitative value

100

SHAH; KETCHAM; Journal of medicinal chemistry; vol. 7; (1964); p. 614 - 619, View in Reaxys 1127 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Local anaesthetic activity of the compound was tested in mice at concentration of 0.01percent

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

percentage

Unit

Measurement Object

response rate

Qualitative value

Quantitative value

SHAH; KETCHAM; Journal of medicinal chemistry; vol. 7; (1964); p. 614 - 619, View in Reaxys 1128 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Antifibrillatory activity determined by number of calcium chloride arrhythmic mice with ventricular fibrilation out of 10 at 10 mg/kg dosage;Control is 7 out of 8

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Qualitative Results

No. of mice not calculated

Measurement Parameter

qualitative

Measurement Object

No. of mice

435/467

2018-05-14 08:43:54

L. N. Sernov; S. Ya. Skachilova; D. S. Blinov; V. V. Druzhinina; Ya. V. Kostin; E. V. Shilova; Pharm Chem J; vol. 39; nb. 7; (2005); p. 350 - 353, View in Reaxys 1129 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Antifibrillatory activity determined by number of calcium chloride arrhythmic mice lost out of 10 at 10 mg/kg dosage

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Qualitative Results

No. of mice not calculated

Measurement Parameter

qualitative

Measurement Object

No. of mice

L. N. Sernov; S. Ya. Skachilova; D. S. Blinov; V. V. Druzhinina; Ya. V. Kostin; E. V. Shilova; Pharm Chem J; vol. 39; nb. 7; (2005); p. 350 - 353, View in Reaxys 1130 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Local anaesthetic activity of the compound was tested in mice at concentration of 0.05 percent

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

percentage

Unit

Measurement Object

response rate

Qualitative value

Quantitative value

SHAH; KETCHAM; Journal of medicinal chemistry; vol. 7; (1964); p. 614 - 619, View in Reaxys 1131 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Local anaesthetic activity of the compound was tested in mice at concentration of 0.25percent

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

percentage

Unit

Measurement Object

response rate

Qualitative value

Quantitative value

SHAH; KETCHAM; Journal of medicinal chemistry; vol. 7; (1964); p. 614 - 619, View in Reaxys 1132 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Local anaesthetic activity of the compound was tested in mice at concentration of 0.50percent

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

percentage

Unit

Measurement Object

response rate

Qualitative value

Quantitative value

436/467

2018-05-14 08:43:54

SHAH; KETCHAM; Journal of medicinal chemistry; vol. 7; (1964); p. 614 - 619, View in Reaxys 1133 of 1220

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Local anaesthetic activity of the compound was tested in mice at concentration of 0.10percent

Biological Species/NCBI ID

Mus musculus

Substance RN

3917968View in Reaxys

Measurement Parameter

percentage

Unit

Measurement Object

response rate

Qualitative value

Quantitative value

SHAH; KETCHAM; Journal of medicinal chemistry; vol. 7; (1964); p. 614 - 619, View in Reaxys 1134 of 1220

1135 of 1220

Target Name

Carboxylesterase 1 [human]

Target Synonyms

carboxylesterase 1

Target, Subunit, Species

Carboxylesterase 1 [human]

Target Mutant/Chimera Details

Carboxylesterase 1 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine table 1; page 1224; page 1226; page 1227

Substance Dose

0.200000 mM

Measurement Parameter

CLint

Unit

mL/min/mg protein

Quantitative value

0.66

Deviation

0.0300000

Metabolite RN

636332

Metabolite name

2.6 Xylidine page 1224; page 1225; page 1226; page 1227; table 2

Target Name

Carboxylesterase 1 [human]

Target Synonyms

carboxylesterase 1

Target, Subunit, Species

Carboxylesterase 1 [human]

Target Mutant/Chimera Details

Carboxylesterase 1 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Enzymology substrate

437/467

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1136 of 1220

1137 of 1220

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine table 1; page 1224; page 1226; page 1227

Substance Dose

0.200000 mM

Measurement Parameter

Vmax

Unit

nmol/min/mg protein

Quantitative value

0.62

Deviation

0.0100000

Metabolite RN

636332

Metabolite name

2.6 Xylidine page 1224; page 1225; page 1226; page 1227; table 2

Target Name

Carboxylesterase 1 [human]

Target Synonyms

carboxylesterase 1

Target, Subunit, Species

Carboxylesterase 1 [human]

Target Mutant/Chimera Details

Carboxylesterase 1 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine table 1; page 1224; page 1226; page 1227

Substance Dose

0.200000 mM

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Quantitative value

0.96

Deviation

0.0600000

Measurement pX

6.02

Metabolite RN

636332

Metabolite name

2.6 Xylidine page 1224; page 1225; page 1226; page 1227; table 2

Target Name

Carboxylesterase 1 [human]

Target Synonyms

carboxylesterase 1

Target, Subunit, Species

Carboxylesterase 1 [human]

Target Mutant/Chimera Details

Carboxylesterase 1 [human]:Wild

Target Species (Bioactivity)

human

Bioassay Category

In Vitro (Efficacy)

438/467

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1138 of 1220

1139 of 1220

Bioassay Name

Enzymology substrate

Cells/Cell Lines

Sf21 cell line

Cell Fraction

Homogenate

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine table 1; page 1224; page 1226; page 1227

Substance Dose

0.100000 mM

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Quantitative value

0.35

Deviation

0.0600000

Measurement pX

6.46

Metabolite RN

636332; 741981

Metabolite name

2.6 Xylidine page 1224; page 1225; page 1226; page 1227; table 2; o-Toluidine page 1224; page 1225; page 1226; page 1227; table 2

Target Name

Carboxylesterase 1 [human]

Target Synonyms

carboxylesterase 1

Target, Subunit, Species

Carboxylesterase 1 [human]

Target Mutant/Chimera Details

Carboxylesterase 1 [human]:Wild

Target Species (Bioactivity)

human

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Enzymology substrate

Cells/Cell Lines

Sf21 cell line

Cell Fraction

Homogenate

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine table 1; page 1224; page 1226; page 1227

Substance Dose

0.100000 mM

Measurement Parameter

Vmax

Unit

nmol/min/mg protein

Quantitative value

0.14

Deviation

Metabolite RN

636332; 741981

Metabolite name

2.6 Xylidine page 1224; page 1225; page 1226; page 1227; table 2; o-Toluidine page 1224; page 1225; page 1226; page 1227; table 2

Target Name

Carboxylesterase 1 [human]

Target Synonyms

carboxylesterase 1

Target, Subunit, Species

Carboxylesterase 1 [human]

Target Mutant/Chimera Details

Carboxylesterase 1 [human]:Wild

Target Species (Bioactivity)

human

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Enzymology substrate

Cells/Cell Lines

Sf21 cell line

439/467

2018-05-14 08:43:54

1140 of 1220

Cell Fraction

Homogenate

Substance RN

3917968View in Reaxys

Substance Name

Lidocaine table 1; page 1224; page 1226; page 1227

Substance Dose

0.100000 mM

Measurement Parameter

CLint

Unit

mL/min/mg protein

Quantitative value

0.4

Deviation

0.0200000

Metabolite RN

636332; 741981

Metabolite name

2.6 Xylidine page 1224; page 1225; page 1226; page 1227; table 2; o-Toluidine page 1224; page 1225; page 1226; page 1227; table 2

Substance Effect

Skin permeable

Bioassay Category

Metabolism/Transport

Biological Species/NCBI ID

pig breed

Organs/Tissues

ear skin

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Measurement Parameter

amount

Unit

μmol/cm2

Quantitative value

0.092

Horita, Daisuke; Todo, Hiroaki; Sugibayashi, Kenji; Chemical and Pharmaceutical Bulletin; vol. 62; nb. 6; (2014); p. 578 585, View in Reaxys 1141 of 1220

Substance Effect

Skin permeable

Bioassay Category

Metabolism/Transport

Biological Species/NCBI ID

pig breed

Organs/Tissues

ear skin

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Measurement Parameter

amount

Unit

μmol/cm2

Quantitative value

0.205

Horita, Daisuke; Todo, Hiroaki; Sugibayashi, Kenji; Chemical and Pharmaceutical Bulletin; vol. 62; nb. 6; (2014); p. 578 585, View in Reaxys 1142 of 1220

Substance Effect

Skin permeable

Bioassay Category

Metabolism/Transport

Biological Species/NCBI ID

pig breed

Organs/Tissues

ear skin

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Measurement Parameter

amount

Unit

μmol/cm2

Quantitative value

0.156

440/467

2018-05-14 08:43:54

Horita, Daisuke; Todo, Hiroaki; Sugibayashi, Kenji; Chemical and Pharmaceutical Bulletin; vol. 62; nb. 6; (2014); p. 578 585, View in Reaxys 1143 of 1220

Substance Effect

Skin permeable

Bioassay Category

Metabolism/Transport

Biological Species/NCBI ID

pig breed

Organs/Tissues

ear skin

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Measurement Parameter

amount

Unit

μmol/cm2

Quantitative value

0.147

Horita, Daisuke; Todo, Hiroaki; Sugibayashi, Kenji; Chemical and Pharmaceutical Bulletin; vol. 62; nb. 6; (2014); p. 578 585, View in Reaxys 1144 of 1220

Substance Effect

Skin permeable

Bioassay Category

Metabolism/Transport

Biological Species/NCBI ID

pig breed

Organs/Tissues

ear skin

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Measurement Parameter

amount

Unit

μmol/cm2

Quantitative value

0.24

Horita, Daisuke; Todo, Hiroaki; Sugibayashi, Kenji; Chemical and Pharmaceutical Bulletin; vol. 62; nb. 6; (2014); p. 578 585, View in Reaxys 1145 of 1220

Substance Effect

Skin permeable

Bioassay Category

Metabolism/Transport

Biological Species/NCBI ID

pig breed

Organs/Tissues

ear skin

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Measurement Parameter

amount

Unit

μmol/cm2

Quantitative value

0.203

Horita, Daisuke; Todo, Hiroaki; Sugibayashi, Kenji; Chemical and Pharmaceutical Bulletin; vol. 62; nb. 6; (2014); p. 578 585, View in Reaxys 1146 of 1220

Substance Effect

Skin permeable

Bioassay Category

Metabolism/Transport

Biological Species/NCBI ID

pig breed

Organs/Tissues

ear skin

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Measurement Parameter

% increase

441/467

2018-05-14 08:43:54

Measurement Object

Permeability coefficient

Qualitative value

Active

Horita, Daisuke; Todo, Hiroaki; Sugibayashi, Kenji; Chemical and Pharmaceutical Bulletin; vol. 62; nb. 6; (2014); p. 578 585, View in Reaxys 1147 of 1220

Substance Effect

Skin permeable

Bioassay Category

Metabolism/Transport

Biological Species/NCBI ID

pig breed

Organs/Tissues

ear skin

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Measurement Parameter

% Inhibition

Measurement Object

Permeability coefficient

Qualitative value

Active

Horita, Daisuke; Todo, Hiroaki; Sugibayashi, Kenji; Chemical and Pharmaceutical Bulletin; vol. 62; nb. 6; (2014); p. 578 585, View in Reaxys 1148 of 1220

Substance Effect

Skin permeable

Bioassay Category

Metabolism/Transport

Biological Species/NCBI ID

pig breed

Organs/Tissues

ear skin

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Measurement Parameter

% increase

Measurement Object

reciprocal of electrical skin resistance

Qualitative value

Active

Horita, Daisuke; Todo, Hiroaki; Sugibayashi, Kenji; Chemical and Pharmaceutical Bulletin; vol. 62; nb. 6; (2014); p. 578 585, View in Reaxys 1149 of 1220

Substance Effect

Skin permeable

Bioassay Category

Metabolism/Transport

Biological Species/NCBI ID

pig breed

Organs/Tissues

ear skin

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Measurement Parameter

% Decrease

Measurement Object

reciprocal of electrical skin resistance

Qualitative value

Active

Horita, Daisuke; Todo, Hiroaki; Sugibayashi, Kenji; Chemical and Pharmaceutical Bulletin; vol. 62; nb. 6; (2014); p. 578 585, View in Reaxys 1150 of 1220

Substance Effect

Local Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

white mouse

Substance RN

3917968View in Reaxys

Substance Name

ω-diethylamino-2,6-dimethylacetanilide hydrochloride

442/467

2018-05-14 08:43:54

Substance Route of Adm.

subcutaneous administration

Measurement Parameter

time

Unit

second

Measurement Object

Mean response time

Quantitative value

25.33

Zalaru, Christina; Dumitrascu, Florea; Draghici, Constantin; Iovu, Mircea; Marinescu, Maria; Tarcomnicu, Isabela; Nitulescu, George Mihai; Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry; vol. 53; nb. 6; (2014); p. 733 - 739, View in Reaxys 1151 of 1220

Substance Effect

Local Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

white mouse

Substance RN

3917968View in Reaxys

Substance Name

ω-diethylamino-2,6-dimethylacetanilide hydrochloride

Substance Route of Adm.

subcutaneous administration

Measurement Parameter

percentage

Unit

Measurement Object

Duration of anesthesia

Quantitative value

100

Substance Effect

Antiarrhytmic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

white mouse

Substance RN

3917968View in Reaxys

Substance Name

ω-diethylamino-2,6-dimethylacetanilide hydrochloride

Substance Dose

50 mg/kg

Substance Route of Adm.

oral administration

Measurement Parameter

percentage

Unit

Measurement Object

Protection vs arrhytmia

Quantitative value

100

Concomitants: Compound RN

1731042

Concomitants: Compound name

chloroform

Concomitants: Compound role

IND

Substance Effect

Antiarrhytmic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

white mouse

443/467

2018-05-14 08:43:54

Substance RN

3917968View in Reaxys

Substance Name

ω-diethylamino-2,6-dimethylacetanilide hydrochloride

Substance Dose

50 mg/kg

Substance Route of Adm.

oral administration

Measurement Parameter

time

Unit

second

Measurement Object

onset of fibrillation

Quantitative value

32.8

Concomitants: Compound RN

1731042

Concomitants: Compound name

chloroform

Concomitants: Compound role

IND

Substance Effect

Antiarrhytmic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

white mouse

Substance RN

3917968View in Reaxys

Substance Name

ω-diethylamino-2,6-dimethylacetanilide hydrochloride

Substance Dose

50 mg/kg

Substance Route of Adm.

oral administration

Measurement Parameter

percentage

Unit

Measurement Object

Latency

Quantitative value

54.66

Concomitants: Compound RN

1731042

Concomitants: Compound name

chloroform

Concomitants: Compound role

IND

Bioassay Category

In Vitro (Efficacy)

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

spinal cord dorsal horn

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

2 mM

Measurement Parameter

% Inhibition

Qualitative value

Active

444/467

2018-05-14 08:43:54

Statistical sgnificance (Qualitative)

Measurement pX

2.7

Concomitants: Compound RN

2816484

Concomitants: Compound name

capsaicin

Concomitants: Compound role

IND

Zhang, Lianxi; Tanabe, Kumiko; Yanagidate, Fumi; Kawasaki, Yasuhiko; Chen, Guihua; Dohi, Shuji; Iida, Hiroki; European Journal of Pharmacology; vol. 734; nb. 1; (2014); p. 132 - 136, View in Reaxys 1156 of 1220

Bioassay Category

In Vitro (Efficacy)

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

spinal cord dorsal horn

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

2 mM

Measurement Parameter

% Inhibition

Qualitative value

Not active

Statistical sgnificance (Qualitative)

Measurement pX

Bioassay Category

In Vitro (Efficacy)

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

spinal cord dorsal horn

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

2 mM

Measurement Parameter

% Inhibition

Qualitative value

Active

Statistical sgnificance (Qualitative)

Measurement pX

2.7

Concomitants: Compound RN

1724431

Concomitants: Compound name

N-methyl-D-aspartic acid

Concomitants: Compound role

IND

Bioassay Category

In Vitro (Efficacy)

Biological Species/NCBI ID

Sprague Dawley rat

445/467

2018-05-14 08:43:54

Organs/Tissues

spinal cord dorsal horn

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

2 mM

Measurement Parameter

% Inhibition

Qualitative value

Active

Statistical sgnificance (Qualitative)

Measurement pX

2.7

Concomitants: Compound RN

3546627

Concomitants: Compound role

IND

Bioassay Category

In Vitro (Efficacy)

Biological Species/NCBI ID

Sprague Dawley rat

Organs/Tissues

spinal cord dorsal horn

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

2 mM

Measurement Parameter

% Inhibition

Qualitative value

Active

Statistical sgnificance (Qualitative)

Measurement pX

2.7

Target Name

UDP-glucuronosyltransferase 1-8

Target Synonyms

a3; gnt1; udp-glucuronosyltransferase 1-8; udp-glucuronosyltransferase 1-h; udp-glucuronosyltransferase 1a8; udpgt 1-8; ugt-1h; ugt1; ugt1*8; ugt1-08; ugt1.8; ugt1a8; ugt1h

Target, Subunit, Species

UDP-glucuronosyltransferase 1-8

Target Mutant/Chimera Details

UDP-glucuronosyltransferase 1-8:Wild

Target Transfection

Transfected

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

20 μM

Measurement Parameter

% Inhibition

Unit

Quantitative value

Measurement pX

446/467

2018-05-14 08:43:54

Concomitants: Compound RN

4890356; 78881

Concomitants: Compound role

SUB; COM

Oda, Shingo; Fujiwara, Ryoichi; Kutsuno, Yuki; Fukami, Tatsuki; Itoh, Tomoo; Yokoi, Tsuyoshi; Nakajima, Miki; Drug Metabolism and Disposition; vol. 43; nb. 6; (2015); p. 812 - 818, View in Reaxys 1161 of 1220

Target Name

UDP-glucuronosyltransferase 1-8

Target Synonyms

a3; gnt1; udp-glucuronosyltransferase 1-8; udp-glucuronosyltransferase 1-h; udp-glucuronosyltransferase 1a8; udpgt 1-8; ugt-1h; ugt1; ugt1*8; ugt1-08; ugt1.8; ugt1a8; ugt1h

Target, Subunit, Species

UDP-glucuronosyltransferase 1-8

Target Mutant/Chimera Details

UDP-glucuronosyltransferase 1-8:Wild

Target Transfection

Transfected

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

20 μM

Measurement Parameter

% Inhibition

Unit

Quantitative value

Measurement pX

Concomitants: Compound RN

4890356; 78881

Concomitants: Compound role

SUB; COM

Target Name

UDP-glucuronosyltransferase 1-8

Target Synonyms

a3; gnt1; udp-glucuronosyltransferase 1-8; udp-glucuronosyltransferase 1-h; udp-glucuronosyltransferase 1a8; udpgt 1-8; ugt-1h; ugt1; ugt1*8; ugt1-08; ugt1.8; ugt1a8; ugt1h

Target, Subunit, Species

UDP-glucuronosyltransferase 1-8

Target Mutant/Chimera Details

UDP-glucuronosyltransferase 1-8:Wild

Target Transfection

Transfected

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

20 μM

Measurement Parameter

% Inhibition

Unit

Quantitative value

Measurement pX

Concomitants: Compound RN

4890356; 78881

447/467

2018-05-14 08:43:54

Concomitants: Compound role

SUB; COM

Bioassay Category

Metabolism/Transport

Biological Species/NCBI ID

human

Population State

normal function

Organs/Tissues

nose mucosa

Cells/Cell Lines

airway epithelium cell

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

10 mM

Measurement Parameter

Papp (A-B)

Unit

cm/s

Quantitative value

6.08E-05

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

28954247

Concomitants: Compound name

lysophosphatidylcholine; tetracaine hydrochloride; mixture of

Concomitants: Compound role

COM

Patent; Loewi LLC; Mulvahill, Mark; US2015/359738; (2015); (A1) English, View in Reaxys 1164 of 1220

Bioassay Category

Metabolism/Transport

Biological Species/NCBI ID

human

Population State

normal function

Organs/Tissues

nose mucosa

Cells/Cell Lines

airway epithelium cell

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

10 mM

Measurement Parameter

Papp (A-B)

Unit

cm/s

Quantitative value

8.6E-06

Patent; Loewi LLC; Mulvahill, Mark; US2015/359738; (2015); (A1) English, View in Reaxys 1165 of 1220

Bioassay Category

Metabolism/Transport

Biological Species/NCBI ID

human

Population State

normal function

Organs/Tissues

nose mucosa

Cells/Cell Lines

airway epithelium cell

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

448/467

2018-05-14 08:43:54

Substance Dose

10 mM

Measurement Parameter

Papp (A-B)

Unit

cm/s

Quantitative value

2.89E-05

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

3572742

Concomitants: Compound name

sodium caprate

Concomitants: Compound role

COM

Patent; Loewi LLC; Mulvahill, Mark; US2015/359738; (2015); (A1) English, View in Reaxys 1166 of 1220

Bioassay Category

Metabolism/Transport

Biological Species/NCBI ID

human

Population State

normal function

Organs/Tissues

nose mucosa

Cells/Cell Lines

airway epithelium cell

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

10 mM

Measurement Parameter

Papp (A-B)

Unit

cm/s

Quantitative value

9.63E-05

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

3643164

Concomitants: Compound name

sodium deoxycholate

Concomitants: Compound role

COM

Patent; Loewi LLC; Mulvahill, Mark; US2015/359738; (2015); (A1) English, View in Reaxys 1167 of 1220

Bioassay Category

Metabolism/Transport

Biological Species/NCBI ID

human

Population State

normal function

Organs/Tissues

nose mucosa

Cells/Cell Lines

airway epithelium cell

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

10 mM

Measurement Parameter

Papp (A-B)

Unit

cm/s

Quantitative value

7.19E-05

449/467

2018-05-14 08:43:54

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

28954248

Concomitants: Compound name

polyoxyethylene lauryl ether; tetracaine hydrochloride; mixture of

Concomitants: Compound role

COM

Patent; Loewi LLC; Mulvahill, Mark; US2015/359738; (2015); (A1) English, View in Reaxys 1168 of 1220

Substance Effect

Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

8.33 μmol/kg

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

time

Unit

min

Measurement Object

complete block time for proprioception

Quantitative value

8.6

Tzeng, Jann-Inn; Wang, Jieh-Neng; Wang, Jhi-Joung; Chen, Yu-Wen; Hung, Ching-Hsia; Neuroscience Letters; vol. 618; (2016); p. 94 - 98, View in Reaxys 1169 of 1220

Substance Effect

Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

8.33 μmol/kg

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

time

Unit

min

Measurement Object

Recovery time for proprioception

Quantitative value

32.3

Tzeng, Jann-Inn; Wang, Jieh-Neng; Wang, Jhi-Joung; Chen, Yu-Wen; Hung, Ching-Hsia; Neuroscience Letters; vol. 618; (2016); p. 94 - 98, View in Reaxys 1170 of 1220

Substance Effect

Analgesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

450/467

2018-05-14 08:43:54

Substance Dose

8.33 μmol/kg

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

% Maximal possible effect (MPE)

Unit

Measurement Object

nociception

Quantitative value

100

Tzeng, Jann-Inn; Wang, Jieh-Neng; Wang, Jhi-Joung; Chen, Yu-Wen; Hung, Ching-Hsia; Neuroscience Letters; vol. 618; (2016); p. 94 - 98, View in Reaxys 1171 of 1220

Substance Effect

Analgesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

8.33 μmol/kg

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

time

Unit

min

Measurement Object

complete block time for nociception

Quantitative value

10.9

Tzeng, Jann-Inn; Wang, Jieh-Neng; Wang, Jhi-Joung; Chen, Yu-Wen; Hung, Ching-Hsia; Neuroscience Letters; vol. 618; (2016); p. 94 - 98, View in Reaxys 1172 of 1220

Substance Effect

Analgesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

8.33 μmol/kg

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

time

Unit

min

Measurement Object

Recovery time for nociception

Quantitative value

36.3

Tzeng, Jann-Inn; Wang, Jieh-Neng; Wang, Jhi-Joung; Chen, Yu-Wen; Hung, Ching-Hsia; Neuroscience Letters; vol. 618; (2016); p. 94 - 98, View in Reaxys 1173 of 1220

Substance Effect

Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

451/467

2018-05-14 08:43:54

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1.52-8.33 μmol/kg

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

ED50

Unit

μmol/kg

Measurement Object

Motor function

Quantitative value

3.8

Tzeng, Jann-Inn; Wang, Jieh-Neng; Wang, Jhi-Joung; Chen, Yu-Wen; Hung, Ching-Hsia; Neuroscience Letters; vol. 618; (2016); p. 94 - 98, View in Reaxys 1174 of 1220

Substance Effect

Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1.52-8.33 μmol/kg

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

ED50

Unit

μmol/kg

Measurement Object

proprioception

Quantitative value

3.1

Tzeng, Jann-Inn; Wang, Jieh-Neng; Wang, Jhi-Joung; Chen, Yu-Wen; Hung, Ching-Hsia; Neuroscience Letters; vol. 618; (2016); p. 94 - 98, View in Reaxys 1175 of 1220

Substance Effect

Analgesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1.52-8.33 μmol/kg

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

ED50

Unit

μmol/kg

Quantitative value

Tzeng, Jann-Inn; Wang, Jieh-Neng; Wang, Jhi-Joung; Chen, Yu-Wen; Hung, Ching-Hsia; Neuroscience Letters; vol. 618; (2016); p. 94 - 98, View in Reaxys 1176 of 1220

Substance Effect

Anaesthesic

Bioassay Category

In Vivo (Animal models)

452/467

2018-05-14 08:43:54

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

8.33 μmol/kg

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

% Maximal possible effect (MPE)

Unit

Measurement Object

Motor function

Quantitative value

100

Tzeng, Jann-Inn; Wang, Jieh-Neng; Wang, Jhi-Joung; Chen, Yu-Wen; Hung, Ching-Hsia; Neuroscience Letters; vol. 618; (2016); p. 94 - 98, View in Reaxys 1177 of 1220

Substance Effect

Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

8.33 μmol/kg

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

time

Unit

min

Measurement Object

complete block time for motor function

Quantitative value

6.9

Tzeng, Jann-Inn; Wang, Jieh-Neng; Wang, Jhi-Joung; Chen, Yu-Wen; Hung, Ching-Hsia; Neuroscience Letters; vol. 618; (2016); p. 94 - 98, View in Reaxys 1178 of 1220

Substance Effect

Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

8.33 μmol/kg

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

time

Unit

min

Measurement Object

Recovery time for motor function

Quantitative value

29.5

Tzeng, Jann-Inn; Wang, Jieh-Neng; Wang, Jhi-Joung; Chen, Yu-Wen; Hung, Ching-Hsia; Neuroscience Letters; vol. 618; (2016); p. 94 - 98, View in Reaxys

453/467

2018-05-14 08:43:54

1179 of 1220

Substance Effect

Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

8.33 μmol/kg

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

% Maximal possible effect (MPE)

Unit

Measurement Object

proprioception

Quantitative value

100

Tzeng, Jann-Inn; Wang, Jieh-Neng; Wang, Jhi-Joung; Chen, Yu-Wen; Hung, Ching-Hsia; Neuroscience Letters; vol. 618; (2016); p. 94 - 98, View in Reaxys 1180 of 1220

Substance Effect

Antiinflammatory

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Route of Adm.

intraperitoneal administration

Measurement Parameter

ID50

Unit

mg/kg

Quantitative value

26.8

Statistical sgnificance (Qualitative)

Patent; Grünenthal GmbH; CHRISTOPH, Thomas; INGHELBRECHT, Sabine, Karine, Katrien; EMBRECHTS, Roger, Carolus, Augusta; REINHOLD, Ulrich; SCHILLER, Marc; WULSTEN, Eva; SCHIENE, Klaus; BLOMS-FUNKE, Petra; FEIL, Ulrich; (31 pag.); EP2680833; (2016); (B1) English, View in Reaxys 1181 of 1220

Substance Effect

Antiinflammatory

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Route of Adm.

intraperitoneal administration

Measurement Parameter

ID50

Unit

mg/kg

Quantitative value

32.4

Statistical sgnificance (Qualitative)

454/467

2018-05-14 08:43:54

1182 of 1220

Substance Effect

Local Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

2.5 μmol

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

time

Unit

min

Measurement Object

Recovery time from motor activity

Quantitative value

Chen, Yu-Wen; Tzeng, Jann-Inn; Chen, Yu-Chung; Hung, Ching-Hsia; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 742; (2014); p. 125 - 130, View in Reaxys 1183 of 1220

Substance Effect

Local Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

2.5 μmol

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

time

Unit

min

Measurement Object

Recovery time from proprioception

Quantitative value

Chen, Yu-Wen; Tzeng, Jann-Inn; Chen, Yu-Chung; Hung, Ching-Hsia; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 742; (2014); p. 125 - 130, View in Reaxys 1184 of 1220

Substance Effect

Local Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

2.5 μmol

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

time

Unit

min

Measurement Object

Recovery time from nociception

Quantitative value

455/467

2018-05-14 08:43:54

Chen, Yu-Wen; Tzeng, Jann-Inn; Chen, Yu-Chung; Hung, Ching-Hsia; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 742; (2014); p. 125 - 130, View in Reaxys 1185 of 1220

Substance Effect

Local Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

2.5 μmol

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

% Maximal possible effect

Unit

Measurement Object

Motor activity

Quantitative value

100

Chen, Yu-Wen; Tzeng, Jann-Inn; Chen, Yu-Chung; Hung, Ching-Hsia; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 742; (2014); p. 125 - 130, View in Reaxys 1186 of 1220

Substance Effect

Local Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

2.5 μmol

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

% Maximal possible effect

Unit

Measurement Object

proprioception

Quantitative value

100

Chen, Yu-Wen; Tzeng, Jann-Inn; Chen, Yu-Chung; Hung, Ching-Hsia; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 742; (2014); p. 125 - 130, View in Reaxys 1187 of 1220

Substance Effect

Local Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

2.5 μmol

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

% Maximal possible effect

Unit

456/467

2018-05-14 08:43:54

Measurement Object

nociception

Quantitative value

100

Chen, Yu-Wen; Tzeng, Jann-Inn; Chen, Yu-Chung; Hung, Ching-Hsia; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 742; (2014); p. 125 - 130, View in Reaxys 1188 of 1220

Substance Effect

Local Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

0.50 - 2.50 μmol

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

ED50

Unit

μmol

Measurement Object

Motor activity

Quantitative value

1.23

Statistical sgnificance (Qualitative)

Chen, Yu-Wen; Tzeng, Jann-Inn; Chen, Yu-Chung; Hung, Ching-Hsia; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 742; (2014); p. 125 - 130, View in Reaxys 1189 of 1220

Substance Effect

Local Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1.18 μmol

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

% increase

Measurement Object

Possible effect of motor activity

Qualitative value

Active

Chen, Yu-Wen; Tzeng, Jann-Inn; Chen, Yu-Chung; Hung, Ching-Hsia; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 742; (2014); p. 125 - 130, View in Reaxys 1190 of 1220

Substance Effect

Local Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1.18 μmol

Substance Route of Adm.

intrathecal administration

457/467

2018-05-14 08:43:54

Substance Dosing Regimen

Single

Measurement Parameter

% increase

Measurement Object

Possible effect of Proprioception

Qualitative value

Active

Chen, Yu-Wen; Tzeng, Jann-Inn; Chen, Yu-Chung; Hung, Ching-Hsia; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 742; (2014); p. 125 - 130, View in Reaxys 1191 of 1220

Substance Effect

Local Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1.18 μmol

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

% increase

Measurement Object

Possible effect of Nociception

Qualitative value

Active

Chen, Yu-Wen; Tzeng, Jann-Inn; Chen, Yu-Chung; Hung, Ching-Hsia; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 742; (2014); p. 125 - 130, View in Reaxys 1192 of 1220

Substance Effect

Local Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

0.50 - 2.50 μmol

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

ED50

Unit

μmol

Measurement Object

nociception

Quantitative value

1.1

Statistical sgnificance (Qualitative)

Chen, Yu-Wen; Tzeng, Jann-Inn; Chen, Yu-Chung; Hung, Ching-Hsia; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 742; (2014); p. 125 - 130, View in Reaxys 1193 of 1220

Substance Effect

Local Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

458/467

2018-05-14 08:43:54

Substance Dose

0.50 - 2.50 μmol

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

ED50

Unit

μmol

Measurement Object

proprioception

Quantitative value

1.2

Statistical sgnificance (Qualitative)

Chen, Yu-Wen; Tzeng, Jann-Inn; Chen, Yu-Chung; Hung, Ching-Hsia; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 742; (2014); p. 125 - 130, View in Reaxys 1194 of 1220

Substance Effect

Local Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

0.50 - 2.50 μmol

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

ED25

Unit

μmol

Quantitative value

0.77

Statistical sgnificance (Qualitative)

Chen, Yu-Wen; Tzeng, Jann-Inn; Chen, Yu-Chung; Hung, Ching-Hsia; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 742; (2014); p. 125 - 130, View in Reaxys 1195 of 1220

Substance Effect

Local Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

0.50 - 2.50 μmol

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

ED75

Unit

μmol

Quantitative value

0.32

Statistical sgnificance (Qualitative)

Chen, Yu-Wen; Tzeng, Jann-Inn; Chen, Yu-Chung; Hung, Ching-Hsia; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 742; (2014); p. 125 - 130, View in Reaxys

459/467

2018-05-14 08:43:54

1196 of 1220

Substance Effect

Local Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

0.50 - 2.50 μmol

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

ED50

Unit

μmol

Quantitative value

1.18

Statistical sgnificance (Qualitative)

Chen, Yu-Wen; Tzeng, Jann-Inn; Chen, Yu-Chung; Hung, Ching-Hsia; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 742; (2014); p. 125 - 130, View in Reaxys 1197 of 1220

Substance Effect

Local Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

2.5 μmol

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

time

Unit

min

Measurement Object

duration of complete blockade for nociception

Quantitative value

Chen, Yu-Wen; Tzeng, Jann-Inn; Chen, Yu-Chung; Hung, Ching-Hsia; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 742; (2014); p. 125 - 130, View in Reaxys 1198 of 1220

Substance Effect

Local Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

2.5 μmol

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

time

Unit

min

Measurement Object

duration of complete blockade for proprioception

460/467

2018-05-14 08:43:54

Quantitative value

Chen, Yu-Wen; Tzeng, Jann-Inn; Chen, Yu-Chung; Hung, Ching-Hsia; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 742; (2014); p. 125 - 130, View in Reaxys 1199 of 1220

Substance Effect

Local Anaesthesic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

2.5 μmol

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

time

Unit

min

Measurement Object

duration of complete blockade for motor nerve

Quantitative value

Chen, Yu-Wen; Tzeng, Jann-Inn; Chen, Yu-Chung; Hung, Ching-Hsia; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 742; (2014); p. 125 - 130, View in Reaxys 1200 of 1220

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

12.5 μmol

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

time

Unit

min

Measurement Object

To remain on the rotarod

Quantitative value

111.5

Chen, Yu-Wen; Tzeng, Jann-Inn; Chen, Yu-Chung; Hung, Ching-Hsia; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 742; (2014); p. 125 - 130, View in Reaxys 1201 of 1220

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

2.50 μmol

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

time

Unit

min

Measurement Object

To remain on the rotarod

461/467

2018-05-14 08:43:54

Quantitative value

Chen, Yu-Wen; Tzeng, Jann-Inn; Chen, Yu-Chung; Hung, Ching-Hsia; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 742; (2014); p. 125 - 130, View in Reaxys 1202 of 1220

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

12.5 μmol

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

time

Unit

min

Measurement Object

To remain on the rotarod

Quantitative value

111.6

Chen, Yu-Wen; Tzeng, Jann-Inn; Chen, Yu-Chung; Hung, Ching-Hsia; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 742; (2014); p. 125 - 130, View in Reaxys 1203 of 1220

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

2.50 μmol

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

time

Unit

min

Measurement Object

To remain on the rotarod

Quantitative value

117.1

Chen, Yu-Wen; Tzeng, Jann-Inn; Chen, Yu-Chung; Hung, Ching-Hsia; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 742; (2014); p. 125 - 130, View in Reaxys 1204 of 1220

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

2.50 μmol

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

time

Unit

min

Measurement Object

To remain on the rotarod

Quantitative value

97.7

462/467

2018-05-14 08:43:54

Chen, Yu-Wen; Tzeng, Jann-Inn; Chen, Yu-Chung; Hung, Ching-Hsia; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 742; (2014); p. 125 - 130, View in Reaxys 1205 of 1220

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

12.5 μmol

Substance Route of Adm.

intrathecal administration

Substance Dosing Regimen

Single

Measurement Parameter

time

Unit

min

Measurement Object

To remain on the rotarod

Quantitative value

123.5

Chen, Yu-Wen; Tzeng, Jann-Inn; Chen, Yu-Chung; Hung, Ching-Hsia; Wang, Jhi-Joung; European Journal of Pharmacology; vol. 742; (2014); p. 125 - 130, View in Reaxys 1206 of 1220

Bioassay Category

Pharmacokinetic

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocainium chloride

Substance Route of Adm.

transdermal administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-4 h)

Unit

μM/h

Quantitative value

602

Bioassay Category

Pharmacokinetic

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocainium chloride

Substance Route of Adm.

transdermal administration

Substance Dosing Regimen

Single

Measurement Parameter

concentration (parameters)

Qualitative value

Not determined/not detected

Bioassay Category

Pharmacokinetic

Biological Species/NCBI ID

Sprague Dawley rat

463/467

2018-05-14 08:43:54

Substance RN

3917968View in Reaxys

Substance Name

lidocainium chloride

Substance Route of Adm.

transdermal administration

Substance Dosing Regimen

Single

Measurement Parameter

concentration (parameters)

Unit

Quantitative value

2.65

Bioassay Category

Pharmacokinetic

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocainium chloride

Substance Route of Adm.

transdermal administration

Substance Dosing Regimen

Single

Measurement Parameter

concentration (parameters)

Qualitative value

Not determined/not detected

Bioassay Category

Pharmacokinetic

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocainium chloride

Substance Route of Adm.

transdermal administration

Substance Dosing Regimen

Single

Measurement Parameter

concentration (parameters)

Unit

Quantitative value

16.5

Bioassay Category

Pharmacokinetic

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocainium chloride

Substance Route of Adm.

transdermal administration

Substance Dosing Regimen

Single

Measurement Parameter

concentration (parameters)

Qualitative value

Not determined/not detected

464/467

2018-05-14 08:43:54

Bioassay Category

Pharmacokinetic

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocainium chloride

Substance Route of Adm.

transdermal administration

Substance Dosing Regimen

Single

Measurement Parameter

concentration (parameters)

Unit

Quantitative value

159.6

Bioassay Category

Pharmacokinetic

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocainium chloride

Substance Route of Adm.

transdermal administration

Substance Dosing Regimen

Single

Measurement Parameter

concentration (parameters)

Unit

Quantitative value

12.8

Bioassay Category

Pharmacokinetic

Biological Species/NCBI ID

Sprague Dawley rat

Substance RN

3917968View in Reaxys

Substance Name

lidocainium chloride

Substance Route of Adm.

transdermal administration

Substance Dosing Regimen

Single

Measurement Parameter

concentration (parameters)

Unit

Quantitative value

348.5

Substance Effect

Antiinflammatory

Bioassay Category

In Vitro (Efficacy)

465/467

2018-05-14 08:43:54

Biological Species/NCBI ID

human

Population State

endometriosis

Cells/Cell Lines

endometrium cell

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/ml

Measurement Parameter

concentration (parameters)

Unit

pg/ml

Quantitative value

Patent; ISIFER AB; Edelstam, Greta; (4 pag.); US9849102; (2017); (B2) English, View in Reaxys 1216 of 1220

Substance Effect

Antiinflammatory

Bioassay Category

In Vitro (Efficacy)

Biological Species/NCBI ID

human

Population State

endometriosis

Cells/Cell Lines

endometrium cell

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/ml

Measurement Parameter

concentration (parameters)

Unit

pg/ml

Quantitative value

122

Patent; ISIFER AB; Edelstam, Greta; (4 pag.); US9849102; (2017); (B2) English, View in Reaxys 1217 of 1220

Substance Effect

Antiinflammatory

Bioassay Category

In Vitro (Efficacy)

Biological Species/NCBI ID

human

Population State

endometriosis

Cells/Cell Lines

endometrium cell

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/ml

Measurement Parameter

concentration (parameters)

Unit

pg/ml

Quantitative value

9.4

Patent; ISIFER AB; Edelstam, Greta; (4 pag.); US9849102; (2017); (B2) English, View in Reaxys 1218 of 1220

Substance Effect

Antiinflammatory

Bioassay Category

In Vitro (Efficacy)

Biological Species/NCBI ID

human

Population State

endometriosis

Cells/Cell Lines

endometrium cell

Substance RN

3917968View in Reaxys

466/467

2018-05-14 08:43:54

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/ml

Measurement Parameter

concentration (parameters)

Unit

pg/ml

Quantitative value

Patent; ISIFER AB; Edelstam, Greta; (4 pag.); US9849102; (2017); (B2) English, View in Reaxys 1219 of 1220

Substance Effect

Antiinflammatory

Bioassay Category

In Vitro (Efficacy)

Biological Species/NCBI ID

human

Population State

endometriosis

Cells/Cell Lines

endometrium cell

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/ml

Measurement Parameter

concentration (parameters)

Unit

pg/ml

Qualitative value

Quantitative value

Patent; ISIFER AB; Edelstam, Greta; (4 pag.); US9849102; (2017); (B2) English, View in Reaxys 1220 of 1220

Substance Effect

Antiinflammatory

Bioassay Category

In Vitro (Efficacy)

Biological Species/NCBI ID

human

Population State

endometriosis

Cells/Cell Lines

endometrium cell

Substance RN

3917968View in Reaxys

Substance Name

lidocaine hydrochloride

Substance Dose

1 mg/ml

Measurement Parameter

concentration (parameters)

Unit

pg/ml

Qualitative value

Quantitative value

Patent; ISIFER AB; Edelstam, Greta; (4 pag.); US9849102; (2017); (B2) English, View in Reaxys

467/467

2018-05-14 08:43:54