4-Hydroxybutanoic acid (GHB)

Page 1

Reaxys

PubChem

eMolecules

Reactions (158)

Substances (19)

Structure

Citations (473)

Structure/Compound Data Chemical Name: 4-hydroxybutanoic acid Reaxys Registry Number: 1720582

CAS Registry Number: 591-81-1 Type of Substance: acyclic Molecular Formula: C4H8O3

Linear Structure Formula: HOCH2CH2CH2COOH Molecular Weight: 104.106

InChI Key: SJZRECIVHVDYJC-UHFFFAOYSA-N

1

N° of preparations All Preps | All Reactions 45 prep out of 91 reactions.

Available Data

N° of ref.

Identification Physical Data (18) Spectra (13) Bioactivity (83) Other Data (76)

320

Synthesize | Hide Details Find similar Chemical Names and Synonyms 4-hydroxybutanoic acid Identification Substance Label (9) Label

Reference

GHB

Ferrara; Tedeschi; Frison; Orlando; Mazzo; Zordan; Padrini; Palatini

European Journal of Clinical Pharmacology, 1996 , vol. 50, # 4 p. 305 - 310 Title/Abstract Full Text View citing articles Show Details

Banerjee, Pradeep K.; Olsen, Richard W.; Tillakaratne, Niranjala J. K.; Brailowsky, Simon; Tobin, Allan J.; Snead III, O. Carter

Journal of Pharmacology and Experimental Therapeutics, 1998 , vol. 287, # 2 p. 766 - 772 Title/Abstract Full Text View citing articles Show Details

Dimpfel; Dalhoff; Von Keutz

Antimicrobial Agents and Chemotherapy, 1996 , vol. 40, # 11 p. 2573 - 2576 Title/Abstract Full Text View citing articles Show Details

Snead III, O. Carter


Biochemical Pharmacology, 1996 , vol. 52, # 8 p. 1235 - 1243 Title/Abstract Full Text View citing articles Show Details

Nagy, Peter I.; TakaI cs-NovaI k, Krisztina; Ramek, Michael

Journal of Physical Chemistry B, 2001 , vol. 105, # 24 p. 5772 - 5781 Title/Abstract Full Text View citing articles Show Details

Mathivet, Pascal; Bernasconi, Raymond; De Barry, Jean; Marescaux, Christian; Bittiger, Helmut

European Journal of Pharmacology, 1997 , vol. 321, # 1 p. 67 - 75 Title/Abstract Full Text View citing articles Show Details

Follesa, Paolo; Mancuso, Luisa; Biggio, Francesca; Mostallino, Maria Cristina; Manca, Annalisa; Mascia, Maria Paola; Busonero, Fabio; Talani, Giuseppe; Sanna, Enrico; Biggio, Giovanni

Molecular Pharmacology, 2003 , vol. 63, # 4 p. 896 - 907 Title/Abstract Full Text View citing articles Show Details

Ferrara; Giorgetti; Zancaner; Orlando; Tagliabracci; Cavarzeran; Palatini

European Journal of Clinical Pharmacology, 1999 , vol. 54, # 11 p. 821 - 827 Title/Abstract Full Text View citing articles Show Details

Hicks, Alissa R.; Kapusta, Daniel R.; Varner, Kurt J.

Journal of Cardiovascular Pharmacology, 2004 , vol. 44, # 6 p. 631 - 638 Title/Abstract Full Text View citing articles Show Details

Schweitzer, Paul; Roberto, Marisa; Madamba, Samuel G.; Siggins, George Robert

Journal of Pharmacology and Experimental Therapeutics, 2004 , vol. 311, # 1 p. 172 - 179 Title/Abstract Full Text View citing articles Show Details

Dimitrijevic, Nikola; Dzitoyeva, Svetlana; Satta, Rosalba; Imbesi, Marta; Yildiz, Sevim; Manev, Hari

European Journal of Pharmacology, 2005 , vol. 519, # 3 p. 246 - 252 Title/Abstract Full Text View citing articles Show Details

Satta, Rosalba; Dimitrijevic, Nikola; Manev, Hari

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Bhattacharya, Indranil; Boje, Kathleen M. K.

Journal of Pharmacokinetics and Pharmacodynamics, 2006 , vol. 33, # 5 p. 657 - 681 Title/Abstract Full Text View citing articles Show Details

Wang, Qi; Lu, Ye; Morris, Marilyn E.

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Sevak, Rajkumar J.; Koek, Wouter; Daws, Lynette C.; Owens, William Anthony; Galli, Aurelio; France, Charles P.

European Journal of Pharmacology, 2008 , vol. 581, # 1-2 p. 105 - 112 Title/Abstract Full Text View citing articles Show Details

INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM); MAITRE, Michel; BOURGUIGNON, Jean-Jacques; SCHMITT, Martine; KLEIN, Christian; MENSAH-NYAGAN, Ayikoe, Guy; MATHIS, Chantal; CASSEL, Jean-Christophe

Patent: WO2013/24028 A1, 2013 ; Title/Abstract Full Text Show Details

Thiesen, Louise; Kehler, Jan; Clausen, Rasmus P.; Frolund, Bente; Bundgaard, Christoffer; Wellendorph, Petrine

Journal of Pharmacology and Experimental Therapeutics, 2015 , vol. 354, # 2 p. 166 - 174 Title/Abstract Full Text View citing articles Show Details

YALE UNIVERSITY; DIXIT, Vishwa, Deep

Patent: WO2016/123229 A1, 2016 ; Title/Abstract Full Text Show Details

4-HB

Samsung Electronics Co., Ltd.; Lee, Kyunghae; Lee, Mooho; Chwae, Jun; Park, Jinhwan; Lee, Jongmin; Cho, Kwangmyung; Park, Jaechan

Patent: US2015/259311 A1, 2015 ; Title/Abstract Full Text Show Details

Genomatica, Inc.; Burk, Mark J.; Burgard, Anthony P.; Osterhout, Robin E.; Sun, Jun

Patent: US9175297 B2, 2015 ; Title/Abstract Full Text Show Details

GHB, Negwer no. 283

Wang, Qi; Darling, Inger M.; Morris, Marilyn E.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 2 p. 751 - 761 Title/Abstract Full Text View citing articles Show Details

GBH

Banerjee; Snead III

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 273, # 3 p. 1534 - 1543 Title/Abstract Full Text View citing articles Show Details

Perez-Prior, M. Teresa; Manso, Jose A.; Del Pilar Garcia-Santos; Calle, Emilio; Casado, Julio

Journal of Organic Chemistry, 2005 , vol. 70, # 2 p. 420 - 426 Title/Abstract Full Text View citing articles Show Details

Tab. 1

Kesseler, Maria; Friedrich, Thomas; Hoeffken, Hans Wolfgang; Hauer, Bernhard

Advanced Synthesis and Catalysis, 2002 , vol. 344, # 10 p. 1103 - 1110 Title/Abstract Full Text View citing articles Show Details

educt to VI

El'chaninov; Stoyanov; Kagan

Russian Journal of Organic Chemistry, 2000 , vol. 36, # 11 p. 1683 - 1685 Title/Abstract Full Text View citing articles Show Details

4BHA

Kimura, Hiroshi; Iwama, Masanobu; Sasaki, Shintaro; Takeishi, Makoto

Chemistry Letters, 1999 , # 8 p. 737 - 738 Title/Abstract Full Text View citing articles Show Details

GHBA

Erhardt, Sophie; Andersson, Bengt; Nissbrandt, Hans; Engberg, Goeran


Naunyn-Schmiedeberg's Archives of Pharmacology, 1998 , vol. 357, # 6 p. 611 - 619 Title/Abstract Full Text View citing articles Show Details

GHB, Merck 4860

Howard, Sherrel G.; Feigenbaum, Jeffery J.

Biochemical Pharmacology, 1997 , vol. 53, # 1 p. 103 - 110 Title/Abstract Full Text View citing articles Show Details

Patent-Specific Data (3) Prophetic Compound

Related Markush Structure (RN)

28800548

Reference Samsung Electronics Co., Ltd.; Lee, Kyunghae; Lee, Mooho; Chwae, Jun; Park, Jinhwan; Lee, Jongmin; Cho, Kwangmyung; Park, Jaechan

Patent: US2015/259311 A1, 2015 ; Title/Abstract Full Text Show Details

24593161; 24593169

INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM); MAITRE, Michel; BOURGUIGNON, JeanJacques; SCHMITT, Martine; KLEIN, Christian; MENSAH-NYAGAN, Ayikoe, Guy; MATHIS, Chantal; CASSEL, Jean-Christophe Patent: WO2013/24028 A1, 2013 ; Title/Abstract Full Text Show Details

prophetic product

AVANTGARDE S.p.A.

Patent: EP631779 A1, 1995 ;

Title/Abstract Full Text Show Details

Related Structure (1) Related Structure

Reference

Das Gleichgewicht mit γ-Butyrolacton in verd. wss. Loesung bei 100grad liegt bei ca. 25prozent Saeure und ca. 75prozent Lacton.

Beilstein Handbook

Full Text Show Details

Derivative (4) Comment (Derivative) K+ -Salz: Leitfaehigkeit

Λ?

Reference in W.

Hoeiland; Vikingstad

Journal of the Chemical Society, Faraday Transactions 1: Physical Chemistry in Condensed Phases, 1975 , vol. 71, p. 2007,2009-2015 Full Text Show Details

Ag - Salz: aus Na-Salz, AgNO3

Wulff et al.

Chemische Berichte, 1971 , vol. 104, p. 1387,1392 Full Text Show Details

Na - Salz: aus γ-Butyrolakton, NaOH

Wulff et al.

Chemische Berichte, 1971 , vol. 104, p. 1387,1392 Full Text Show Details

disodium salt Further Data see Handbook (Preparation)

Reppe et al.

Justus Liebigs Annalen der Chemie, 1955 , vol. 596, p. 162,182 Full Text Show Details

I.G.Farbenind.

Patent: DE759483 , 1938 ; DRP/DRBP Org.Chem. Full Text Show Details

Physical Data Melting Point (3) Melting Point

Solvent (Melting Point)

Reference

34 °C

diethyl ether

Wiberg, Kenneth B.; Waldron, Roy F.

Journal of the American Chemical Society, 1991 , vol. 113, # 20 p. 7697 - 7705 Title/Abstract Full Text View citing articles Show Details

15 - 18 °C

diethyl ether

Stoll; Rouve

Helvetica Chimica Acta, 1935 , vol. 18, p. 1087,1124 Full Text View citing articles Show Details


Fittig; Chanlarow

Justus Liebigs Annalen der Chemie, 1884 , vol. 226, p. 331,332 Full Text View citing articles Show Details

Chromatographic Data (2) Chromatographic data

Location

Reference

GC (Gas chromatography)

Dong, Guohui; Ai, Zhihui; Zhang, Lizhi

RSC Advances, 2014 , vol. 4, # 11 p. 5553 - 5560 Title/Abstract Full Text View citing articles Show Details

Hao, Shuxian; Wei, Ya; Li, Laihao; Yang, Xianqing; Cen, Jianwei; Huang, Hui; Lin, Wanling; Yuan, Xiaomin

Food Chemistry, 2015 , vol. 173, p. 274 - 282 Title/Abstract Full Text View citing articles Show Details

Rahmani, Amir; Khataee, Alireza; Kaymak, Baris; Vahid, Behrouz; Fathinia, Mehrangiz; Dindarsafa, Mahsa

RSC Advances, 2016 , vol. 6, # 84 p. 81219 - 81230 Title/Abstract Full Text Show Details

GC (Gas chromatography)

supporting information

Wang, Xincheng; Song, Yanlei; Huang, Chongpin; Liang, Fengbing; Chen, Biaohua

Green Chemistry, 2014 , vol. 16, # 9 p. 4234 - 4240 Title/Abstract Full Text View citing articles Show Details

Crystal Property Description (1) Colour & Other Properties

Reference

hygroskopische Nadeln

Stoll; Rouve

Helvetica Chimica Acta, 1935 , vol. 18, p. 1087,1124 Full Text View citing articles Show Details

Dissociation Exponent (5) Dissociation Exponent (pK)

Dissociation Group

Temperature (Dissociation Exponent)

Solvent (Dissociation Exponent)

Method (Dissociation Exponent)

Type (Dissociation Exponent)

Comment (Dissociation Exponent)

4.46

O-H

25 °C

H2O

potentiometric

a1/apparent

solvent dependence

Nagy, Peter I.; TakaI cs-NovaI k, Krisztina; Ramek, Michael

Journal of Physical Chemistry B, 2001 , vol. 105, # 24 p. 5772 - 5781 Title/Abstract Full Text View citing articles Show Details

4.45

O-H

37 °C

H2O

potentiometric

a1/apparent

solvent dependence

Nagy, Peter I.; TakaI cs-NovaI k, Krisztina; Ramek, Michael

Journal of Physical Chemistry B, 2001 , vol. 105, # 24 p. 5772 - 5781 Title/Abstract Full Text View citing articles Show Details

(pk')pKa

Taylor; Conrad

Biochemistry, 1972 , vol. 11, p. 1383,1385 Full Text Show Details

4.72

25 °C

H2O ethanol

potentiometric

a1/apparent

Ratio of solvents: 9:1

Storm,D.R.; Koshland,D.E.

Journal of the American Chemical Society, 1972 , vol. 94, p. 5805 - 5814 Full Text View citing articles Show Details

4.71

25 °C

apparent

Henry

Zeitschrift fuer Physikalische Chemie, Stoechiometrie und Verwandtschaftslehre, 1892 , vol. 10, p. 113,116, 125, 126 Full Text Show Details

Reference

Electrical Data (1) Description (Electrical Data)

Reference

Electrical conductivity

Hoeiland; Vikingstad

Journal of the Chemical Society, Faraday Transactions 1: Physical Chemistry in Condensed Phases, 1975 , vol. 71, p. 2007,2009-2015 Full Text Show Details


Further Information (1) Description (Further Information)

Reference

Further information

Wulff et al.

Chemische Berichte, 1971 , vol. 104, p. 1387,1392 Full Text Show Details

Liquid Phase (1) Description (Liquid Phase)

Reference

Association in the liquid state

Yarim-Agaev, N. L.; Kalinichenko, V. P.

Russian Journal of Physical Chemistry, 1983 , vol. 57, # 1 p. 13 - 15 Zhurnal Fizicheskoi Khimii, 1983 , vol. 57, # 1 p. 23 - 27 Title/Abstract Full Text Show Details

Liquid/Liquid Systems (MCS) (1) Description (Liquid/Liquid Systems (MCS))

Solvent (Liquid/Liquid Systems (MCS))

Reference

Distribution between solvent 1 + 2

H2O

Long et al.

Journal of Physical Chemistry, 1951 , vol. 55, p. 823-828,829 Full Text Show Details

Liquid/Vapour Systems (MCS) (1) Description (Liquid/Vapour Systems (MCS))

Partner (Liquid/Vapour Systems (MCS))

Solvent (Liquid/Vapour Systems (MCS))

Partial pressures of the components

4-butanolide; S2

H2O

Reference Yarim-Agaev, N. L.; Kalinichenko, V. P.

Russian Journal of Physical Chemistry, 1983 , vol. 57, # 1 p. 13 - 15 Zhurnal Fizicheskoi Khimii, 1983 , vol. 57, # 1 p. 23 27 Title/Abstract Full Text Show Details

Partition octan-1-ol/water (MCS) (2) log POW

Temperature (Partition octan-1-ol/water (MCS))

Reference

-0.47

25 °C

Nagy, Peter I.; TakaI cs-NovaI k, Krisztina; Ramek, Michael

Journal of Physical Chemistry B, 2001 , vol. 105, # 24 p. 5772 - 5781 Title/Abstract Full Text View citing articles Show Details

-0.47

37 °C

Nagy, Peter I.; TakaI cs-NovaI k, Krisztina; Ramek, Michael

Journal of Physical Chemistry B, 2001 , vol. 105, # 24 p. 5772 - 5781 Title/Abstract Full Text View citing articles Show Details

Spectra NMR Spectroscopy (5) Description (NMR Spectroscopy)

Nucleus (NMR Spectroscopy)

Solvents (NMR Spectroscopy)

Temperature (NMR Spectroscopy)

Chemical shifts

1H

D2O various solvent(s)

Buikliskii, V. D.; Panyushkin, V. T.; Soldatenko, I. I.

J. Gen. Chem. USSR (Engl. Transl.), 1990 , vol. 60, # 11 p. 2413 - 2415,2158 - 2160 Title/Abstract Full Text Show Details

NMR with shift reagents

Buikliskii, V. D.; Panyushkin, V. T.; Soldatenko, I. I.

J. Gen. Chem. USSR (Engl. Transl.), 1990 , vol. 60, # 11 p. 2413 - 2415,2158 - 2160 Title/Abstract Full Text Show Details

Chemical shifts

1H

dimethylsulfoxide-d6

Dardoize; Goasdoue; Goadoue; Laborit; Topall

Tetrahedron, 1989 , vol. 45, # 24 p. 7783 - 7794 Title/Abstract Full Text View citing articles Show Details

Reference

Chemical shifts

13C

benzene-d6

Gouesnard, Jean-Paul

Bulletin de la Societe Chimique de France, 1989 , # 1 p. 88 94 Title/Abstract Full Text Show Details


Chemical shifts

1H

D2O

34.1 °C

Dillon, K. B.; Harrison, M. R.; Rossotti, F. J. C.

Journal of Magnetic Resonance (1969-1992), 1980 , vol. 39, # 3 p. 499 - 508 Title/Abstract Full Text View citing articles Show Details

IR Spectroscopy (1) Description (IR Spectroscopy)

Reference

IR

Dafforn,G.A.; Koshland,D.E.

Journal of the American Chemical Society, 1977 , vol. 99, p. 7246 - 7257 Full Text View citing articles Show Details

Mass Spectrometry (6)

Description (Mass Spectrometry)

Location

Reference

gas chromatography mass spectrometry (GCMS) spectrum

Dong, Guohui; Ai, Zhihui; Zhang, Lizhi

RSC Advances, 2014 , vol. 4, # 11 p. 5553 - 5560 Title/Abstract Full Text View citing articles Show Details

Rahmani, Amir; Khataee, Alireza; Kaymak, Baris; Vahid, Behrouz; Fathinia, Mehrangiz; Dindarsafa, Mahsa

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fragmentation pattern spectrum

Page/Page column 2

Genomatica, Inc.; Burk, Mark J.; Burgard, Anthony P.; Osterhout, Robin E.; Sun, Jun

Patent: US9175297 B2, 2015 ;

gas chromatography mass spectrometry (GCMS) fragmentation pattern spectrum

supporting information

Song, Ji-Won; Jeon, Eun-Yeong; Song, Da-Hyun; Jang, Hyun-Young; Bornscheuer, Uwe T.; Oh, DeokKun; Park, Jin-Byung

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GCMS (Gas chromatography mass spectrometry) EI (Electron impact) Spectrum

Li, Qingling; Zhang, Guo-Fang

Rapid Communications in Mass Spectrometry, 2012 , vol. 26, # 11 p. 1355 - 1362 Title/Abstract Full Text View citing articles Show Details

Tandem mass spectrometry ESI (Electrospray ionisation) Negative ion spectroscopy Spectrum

Rebollido-Fernandez, M. Maira; Castiñeiras, Daisy E.; Dolores Bõveda; Luz Couce; Cocho, José A.; Fraga, Jose M.

Rapid Communications in Mass Spectrometry, 2012 , vol. 26, # 18 p. 2131 - 2144 Title/Abstract Full Text View citing articles Show Details

HRMS (High resolution mass spectrometry) ESI (Electrospray ionisation) Negative chemical ionization Spectrum

Lammens, Tijs M.; Franssen, Maurice C. R.; Scott, Elinor L.; Sanders, Johan P. M.

Green Chemistry, 2010 , vol. 12, # 8 p. 1430 - 1436 Title/Abstract Full Text View citing articles Show Details

Title/Abstract Full Text Show Details

UV/VIS Spectroscopy (1) Description (UV/VIS Spectroscopy)

Reference

UV/VIS

Dafforn,G.A.; Koshland,D.E.

Journal of the American Chemical Society, 1977 , vol. 99, p. 7246 - 7257 Full Text View citing articles Show Details

Bioactivity Pharmacological Data (79) 1 of 79

Comment (Pharmacological Data)

Bioactivities present

Reference

Beilstein Handbook

Full Text Show Details

AVANTGARDE S.p.A.

Patent: EP631779 A1, 1995 ;


Title/Abstract Full Text Show Details

Storm,D.R.; Koshland,D.E.

Journal of the American Chemical Society, 1972 , vol. 94, p. 5805 - 5814 Full Text View citing articles Show Details

Storm,D.R.; Koshland,D.E.

Journal of the American Chemical Society, 1972 , vol. 94, p. 5815 - 5825 Full Text View citing articles Show Details

Dafforn,G.A.; Koshland,D.E.

Journal of the American Chemical Society, 1977 , vol. 99, p. 7246 - 7257 Full Text View citing articles Show Details

Pfizer Inc.

Patent: US4814342 A1, 1989 ; Title/Abstract Full Text Show Details

Austin,A.T.; Howard,J.

Journal of the Chemical Society, 1961 , p. 3284 - 3289 Full Text View citing articles Show Details

Sankyo Company, Limited

Patent: US5624935 A1, 1997 ; Title/Abstract Full Text Show Details

Avantgarde S.p.A.

Patent: US5627212 A1, 1997 ; Title/Abstract Full Text Show Details

Wise, Alan; Brown, Andrew James

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ISIS Pharmaceuticals, Inc.

Patent: US6762281 B2, 2004 ; Title/Abstract Full Text Show Details

SLOWAVE, INC.

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Wright, Emma Jayne; Huckle, James William; Ali, Saad Aboul Majeed

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Bhattacharyya, Alakananda; Manila, Maynard D.

Patent: US2006/4212 A1, 2006 ; Title/Abstract Full Text Show Details

BAYLOR COLLEGE OF MEDICINE

Patent: US2006/18921 A1, 2006 ; Title/Abstract Full Text Show Details

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Stoll; Rouve

Helvetica Chimica Acta, 1935 , vol. 18, p. 1087,1124 Full Text View citing articles Show Details

Fittig; Chanlarow

Justus Liebigs Annalen der Chemie, 1884 , vol. 226, p. 331,332 Full Text View citing articles Show Details

Fichter; Herbrand

Chemische Berichte, 1896 , vol. 29, p. 1193 Full Text View citing articles Show Details

Bentley; Haworth; Perkin

Journal of the Chemical Society, 1896 , vol. 69, p. 175 Full Text View citing articles Show Details

2 of 79

Comment (Pharmacological Data)

Bioactivities present

Reference

Marvel; Birkhimer

Journal of the American Chemical Society, 1929 , vol. 51, p. 261 Full Text View citing articles Show Details

Perkin; Sprankling

Journal of the Chemical Society, 1899 , vol. 75, p. 17 Full Text View citing articles Show Details

Boorman; Linstead

Journal of the Chemical Society, 1933 , p. 577,580 Full Text View citing articles Show Details

Coffin; Long

Journal of the American Chemical Society, 1952 , vol. 74, p. 5767 Full Text View citing articles Show Details

Fittig; Roeder

Justus Liebigs Annalen der Chemie, 1885 , vol. 227, p. 19 Full Text Show Details

Michael


Chemische Berichte, 1901 , vol. 34, p. 4044 Full Text Show Details

Henry

Bulletin de la Societe Chimique de France, 1886 , vol. <2>45, p. 341 Chem. Zentralbl., 1898 , vol. 69, # II p. 273 Full Text Show Details

Paul

Comptes Rendus Hebdomadaires des Seances de l'Academie des Sciences, 1942 , vol. 215, p. 304 Full Text Show Details

Adkins; Krsek

Journal of the American Chemical Society, 1948 , vol. 70, p. 385 Journal of the American Chemical Society, 1949 , vol. 71, p. 3053,3054 Full Text Show Details

Willstaetter

Chemische Berichte, 1902 , vol. 35, p. 602 Full Text Show Details

Fruehling

Monatshefte fuer Chemie, 1882 , vol. 3, p. 697 Full Text Show Details

Hamonet

Bulletin de la Societe Chimique de France, 1905 , vol. <3>33, p. 530 Comptes Rendus Hebdomadaires des Seances de l'Academie des Sciences, 1904 , vol. 138, p. 1611 Full Text Show Details

Reppe et al.

Justus Liebigs Annalen der Chemie, 1955 , vol. 596, p. 162,182 Full Text Show Details

Saizew,A.

Justus Liebigs Annalen der Chemie, 1874 , vol. 171, p. 274 Full Text Show Details

Saizew,A.

Justus Liebigs Annalen der Chemie, 1874 , vol. 171, p. 261 Journal fuer Praktische Chemie (Leipzig), 1882 , vol. <2>25, p. 64 Full Text Show Details

Chanlarow

Justus Liebigs Annalen der Chemie, 1884 , vol. 226, p. 326 Full Text Show Details

Kailan

Zeitschrift fuer Physikalische Chemie, Stoechiometrie und Verwandtschaftslehre, 1920 , vol. 94, p. 119 Zeitschrift fuer Physikalische Chemie, Stoechiometrie und Verwandtschaftslehre, 1922 , vol. 101, p. 89 Full Text Show Details

Henry

Zeitschrift fuer Physikalische Chemie, Stoechiometrie und Verwandtschaftslehre, 1892 , vol. 10, p. 113,116, 125, 126 Full Text Show Details

I.G.Farbenind.

Patent: DE759483 , 1938 ; DRP/DRBP Org.Chem. Full Text Show Details

Long et al.

Journal of Physical Chemistry, 1951 , vol. 55, p. 823-828,829 Full Text Show Details

3 of 79

Comment (Pharmacological Data)

Bioactivities present

Reference

Paul; Tchelitcheff

Bulletin de la Societe Chimique de France, 1948 , p. 197,202 Full Text Show Details

Cherbuliez et al.

Helvetica Chimica Acta, 1958 , vol. 41, p. 1163,1167 Full Text Show Details

Kuhnle et al.

Journal of the Chemical Society, Chemical Communications, 1972 , p. 287 Full Text View citing articles Show Details

Wulff et al.

Chemische Berichte, 1971 , vol. 104, p. 1387,1392 Full Text Show Details

Taylor; Conrad

Biochemistry, 1972 , vol. 11, p. 1383,1385 Full Text Show Details

Baschkirow et al.

Neftekhimiya, 1970 , vol. 10, p. 569 Chem.Abstr., 1970 , vol. 73, # 109227 Full Text Show Details

Hoeiland; Vikingstad

Journal of the Chemical Society, Faraday Transactions 1: Physical Chemistry in Condensed Phases, 1975 , vol. 71, p. 2007,2009-2015 Full Text Show Details

Sawai

Bulletin of the Chemical Society of Japan, 1990 , vol. 63, # 3 p. 692 - 696 Title/Abstract Full Text View citing articles Show Details

Wiberg, Kenneth B.; Waldron, Roy F.

Journal of the American Chemical Society, 1991 , vol. 113, # 20 p. 7697 - 7705 Title/Abstract Full Text View citing articles Show Details

Kao, Lien-Chung; Sen, Ayusman

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Buikliskii, V. D.; Panyushkin, V. T.; Soldatenko, I. I.

J. Gen. Chem. USSR (Engl. Transl.), 1990 , vol. 60, # 11 p. 2413 - 2415,2158 - 2160 Title/Abstract Full Text Show Details

Dardoize; Goasdoue; Goadoue; Laborit; Topall

Tetrahedron, 1989 , vol. 45, # 24 p. 7783 - 7794 Title/Abstract Full Text View citing articles Show Details

Motnyak, L. A.; Burmakov, A. I.; Kunshenko, B. V.; Neizvestnaya, T. A.; Alekseeva, L. A.; Yagupol'skii, L. M.

Journal of Organic Chemistry USSR (English Translation), 1983 , vol. 19, # 4 p. 634 - 640 Zhurnal Organicheskoi Khimii, 1983 , vol. 19, # 4 p. 720 - 726 Title/Abstract Full Text Show Details

Gouesnard, Jean-Paul

Bulletin de la Societe Chimique de France, 1989 , # 1 p. 88 - 94 Title/Abstract Full Text Show Details

Bianco, A.; Passacantilli, P.; Righi, G.

Synthetic Communications, 1988 , vol. 18, # 15 p. 1765 - 1772 Title/Abstract Full Text Show Details

Low, G. K.-C.; Duffield, A. M.

Organic Mass Spectrometry, 1985 , vol. 20, # 10 p. 595 - 599 Title/Abstract Full Text Show Details

Bourguignon; Schoenfelder; Schmitt; Wermuth; Hechler; Charlier; Maitre

Journal of Medicinal Chemistry, 1988 , vol. 31, # 5 p. 893 - 897 Title/Abstract Full Text View citing articles Show Details

Thomas; Schontube

Pharmazie, 1993 , vol. 48, # 8 p. 623 - 624 Title/Abstract Full Text View citing articles Show Details

Yarim-Agaev, N. L.; Kalinichenko, V. P.

Russian Journal of Physical Chemistry, 1983 , vol. 57, # 1 p. 13 - 15 Zhurnal Fizicheskoi Khimii, 1983 , vol. 57, # 1 p. 23 - 27 Title/Abstract Full Text Show Details

Yorifuji, Takamitsu; Sugai, Ichiro; Matsumoto, Hideki; Tabuchi, Akira

Agricultural and Biological Chemistry, 1982 , vol. 46, # 5 p. 1361 - 1368 Title/Abstract Full Text Show Details

4 of 79

Comment (Pharmacological Data)

Bioactivities present

Reference

Dillon, K. B.; Harrison, M. R.; Rossotti, F. J. C.

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6 of 79

Comment (Pharmacological Data)

Bioactivities present

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Comment

Bioactivities present


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JANSSEN PHARMACEUTICA N.V.

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7 of 79

Comment (Pharmacological Data)

Bioactivities present

Reference

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Wellendorph, Petrine; Hog, Signe; Sabbatini, Paola; Pedersen, Martin H. F.; Martiny, Lars; Knudsen, Gitte M.; Frolund,


Bente; Clausen, Rasmus P.; Braeuner-Osborne, Hans

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Sun, Chengguo; Hu, Bingcheng; Liu, Zuliang

Heteroatom Chemistry, 2012 , vol. 23, # 3 p. 295 - 303 Title/Abstract Full Text View citing articles Show Details

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CONCERT PHARMACEUTICALS INC.; TUNG, Roger, D.; MORGAN, Adam; SILVERMAN, I., Robert

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Thompson, Andrew J.; Alqazzaz, Mona; Ulens, Chris; Lummis, Sarah C.R.

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Rebollido-Fernandez, M. Maira; Castiñeiras, Daisy E.; Dolores Bõveda; Luz Couce; Cocho, José A.; Fraga, Jose M.

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Wang, Qi; Morris, Marilyn E.

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Abanades, Sergio; Farre, Magi; Segura, Mireia; Pichini, Simona; Pastor, Antoni; Pacifici, Roberta; Pellegrini, Manuela; Torre, Rafael De La

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Molnar, Tuende; Fekete, Erzsebet Kutine; Kardos, Julianna; Palkovits, Miklos

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Fischer, Wiebke; Praetor, Katrin; Metzner, Linda; Neubert, Reinhard H.H.; Brandsch, Matthias

European Journal of Pharmaceutics and Biopharmaceutics, 2008 , vol. 70, # 2 p. 486 - 492 Title/Abstract Full Text View citing articles Show Details

Castelli, M. Paola

Mini-Reviews in Medicinal Chemistry, 2008 , vol. 8, # 12 p. 1188 - 1202 Title/Abstract Full Text View citing articles Show Details

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8 of 79

Comment (Pharmacological Data)

Bioactivities present

Reference

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INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM); MAITRE, Michel; BOURGUIGNON, JeanJacques; SCHMITT, Martine; KLEIN, Christian; MENSAH-NYAGAN, Ayikoe, Guy; MATHIS, Chantal; CASSEL, Jean-Christophe

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Song, Ji-Won; Jeon, Eun-Yeong; Song, Da-Hyun; Jang, Hyun-Young; Bornscheuer, Uwe T.; Oh, Deok-Kun; Park, Jin-Byung

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Bruguerolle; Mesdjian; Valli; Blanc; Andanson; Jadot; Bouyard

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Kelly, Vincent P.; Sherratt, Philip J.; Crouch, Dorothy H.; Hayes, John D.

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Wang, Mong-Heng; Wade, David; Chen, Laishun; White, Steven; Yang, Chung S.

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Cho; Song; Kim; Kang; Choi

European Journal of Biochemistry, 1993 , vol. 211, # 3 p. 757 - 762 Title/Abstract Full Text View citing articles Show Details

Malec; Modzelewski; Malawska; Gorczyca

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Comment (Pharmacological Data)

Bioactivities present

Reference

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Angewandte Chemie - International Edition, 2013 , vol. 52, # 39 p. 10231 - 10236 Angew. Chem., 2013 , vol. 125, # 39 p. 10421 - 10426,6 Title/Abstract Full Text View citing articles Show Details

Vogensen, Stine B.; Marek, Ales; Bay, Tina; Wellendorph, Petrine; Kehler, Jan; Bundgaard, Christoffer; Frolund, Bente; Pedersen, Martin H. F.; Clausen, Rasmus P.

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JOHNSON, Joseph

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Gekkan Yakuji. Pharmaceuticals Monthly.,1966, 8, 1073., 1966 , vol. 8, p. 1073 Full Text Show Details

Clarke's Analysis of Drugs and Poisons Full Text Show Details

Orphan Medical Inc., Xyrem¿ (Sodium oxybate) oral solution, Product leaflet Full Text Show Details

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Wang, Xincheng; Song, Yanlei; Huang, Chongpin; Liang, Fengbing; Chen, Biaohua


Green Chemistry, 2014 , vol. 16, # 9 p. 4234 - 4240 Title/Abstract Full Text View citing articles Show Details

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10 of 79

Comment (Pharmacological Data)

Bioactivities present

Reference

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Paritala, Hanumantharao; Suzuki, Yuta; Carroll, Kate S.

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Patent: WO2015/83129 A1, 2015 ; Title/Abstract Full Text Show Details

Thiesen, Louise; Kehler, Jan; Clausen, Rasmus P.; Frolund, Bente; Bundgaard, Christoffer; Wellendorph, Petrine

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Samsung Electronics Co., Ltd.; Lee, Kyunghae; Lee, Mooho; Chwae, Jun; Park, Jinhwan; Lee, Jongmin; Cho, Kwangmyung; Park, Jaechan

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Genomatica, Inc.; Burk, Mark J.; Burgard, Anthony P.; Osterhout, Robin E.; Sun, Jun

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Bévalot; Cartiser; Bottinelli; Guitton; Fanton

Forensic Science International, 2016 , vol. 259, p. 133 - 154 Title/Abstract Full Text View citing articles Show Details

Li, Xiyuan; Ding, Yuan; Liu, Yupeng; Zhang, Yao; Song, Jinqing; Wang, Qiao; Li, Mengqiu; Qin, Yaping; Huang, Shangzhi; Yang, Yanling

Gene, 2015 , vol. 574, # 1 p. 41 - 47 Title/Abstract Full Text Show Details

Sadones, Nele; Archer, John R. H; Ingels, Ann-Sofie M. E; Dargan, Paul I.; Wood, David M.; Wood, Michelle; Neels, Hugo; Lambert, Willy E.; Stove, Christophe P.

Drug testing and analysis, 2015 , vol. 7, # 4 p. 336 - 340 Title/Abstract Full Text Show Details

Evren, Cuneyt; Bozkurt, Muge

Dusunen Adam, 2015 , vol. 28, # 4 p. 283 - 300 Title/Abstract Full Text View citing articles Show Details

Yin, Renzhan; Zhang, Le; Liu, Ronghou; Mei, Yuanfei; Yu, Wenjuan

Fuel, 2016 , vol. 170, p. 1 - 8 Title/Abstract Full Text Show Details

Chadha, Renu; Bali, Alka; Bansal, Gulshan

Journal of Pharmaceutical and Biomedical Analysis, 2016 , vol. 121, p. 39 - 55 Title/Abstract Full Text View citing articles Show Details

Ma, Richard; Perera, Seán

British Journal of General Practice, 2016 , vol. 66, # 642 p. 4 - 5 Title/Abstract Full Text View citing articles Show Details

Mehling, Lena-Maria; Johansen, Sys Stybe; Wang, Xin; Doberentz, Elke; Madea, Burkhard; Hess, Cornelius

Forensic Science International, 2016 , vol. 259, p. e25 - e31 Title/Abstract Full Text View citing articles Show Details

Heikman, Pertti; Sundström, Mira; Pelander, Anna; Ojanperä, Ilkka

Human Psychopharmacology, 2016 , vol. 31, # 1 p. 44 - 52


Title/Abstract Full Text View citing articles Show Details

Franken, Linda G.; Andrews, Louise M.; Slooff, Valerie D.; De Wildt, Saskia N.; Koch, Birgit C. P.

Therapeutic Drug Monitoring, 2016 , vol. 38, # 1 p. 1 - 3 Title/Abstract Full Text View citing articles Show Details

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12 of 79

Comment (Pharmacological Data)

Bioactivities present

Reference

Lan, Renny S.; Smith, Christy A.; Hyman, Michael R.

Remediation, 2013 , vol. 23, # 4 p. 23 - 42 Title/Abstract Full Text View citing articles Show Details

Jiménez-Pérez; Sevilla; Pineda; Blázquez; Gonzalez-Rodriguez

Journal of Electroanalytical Chemistry, 2016 , vol. 766, p. 141 - 146 Title/Abstract Full Text View citing articles Show Details

Bonneau, Adeline; Boulanger, Renaud; Lebrun, Marc; Maraval, Isabelle; Gunata, Ziya

International Journal of Food Science and Technology, 2016 , vol. 51, # 3 p. 789 - 800 Title/Abstract Full Text View citing articles Show Details

Jiménez-Pérez; Sevilla; Pineda; Blázquez; Gonzalez-Rodriguez

Electrochimica Acta, 2016 , vol. 193, p. 154 - 159 Title/Abstract Full Text View citing articles Show Details

Tomlinson, Monica F.; Brown, Matthew; Hoaken, Peter N.S.

Aggression and Violent Behavior, 2016 , vol. 27, p. 9 - 29 Title/Abstract Full Text View citing articles Show Details

Prieto, Auxiliadora; Escapa, Isabel F.; Martínez, Virginia; Dinjaski, Nina; Herencias, Cristina; de la Peña, Fernando; Tarazona, Natalia; Revelles, Olga

Environmental Microbiology, 2016 , vol. 18, # 2 p. 341 - 357 Title/Abstract Full Text View citing articles Show Details

Caputo, Fabio; Vignoli, Teo; Tarli, Claudia; Domenicali, Marco; Zoli, Giorgio; Bernardi, Mauro; Addolorato, Giovanni

International Journal of Environmental Research and Public Health, 2016 , vol. 13, # 3 art. no. 290 Title/Abstract Full Text View citing articles Show Details

Busardò, Francesco Paolo; Bertol, Elisabetta; Mannocchi, Giulio; Tittarelli, Roberta; Pantano, Flaminia; Vaiano, Fabio; Baglio, Giovanni; Kyriakou, Chrystalla; Marinelli, Enrico

Forensic Science International, 2016 , vol. 265, p. 172 - 181 Title/Abstract Full Text View citing articles Show Details

Wang, Chao; Tang, Desong; Gao, Yong-Gui; Zhang, Lian-Hui

Journal of Bacteriology, 2016 , vol. 198, # 6 p. 930 - 940 Title/Abstract Full Text View citing articles Show Details

Gao, Yuefang; Wang, Haitao; Guo, Junhong; Peng, Pai; Zhai, Meizhi; She, Diao

Polymer Degradation and Stability, 2016 , vol. 126, p. 179 - 187 Title/Abstract Full Text View citing articles Show Details

Margalho, Cláudia; Castanheira, Alice; Real, Francisco Corte; Gallardo, Eugenia; López-Rivadulla, Manuel

Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences, 2016 , vol. 1020, p. 14 - 23 Title/Abstract Full Text View citing articles Show Details

Kim, Pyoungchung; Weaver, Samuel; Labbé, Nicole

Journal of Analytical and Applied Pyrolysis, 2016 , vol. 118, p. 325 - 334 Title/Abstract Full Text View citing articles Show Details

Qu, Guangfei; He, Weiwei; Cai, Yingying; Huang, Xi; Ning, Ping

Carbohydrate Polymers, 2016 , vol. 148, p. 390 - 396 Title/Abstract Full Text View citing articles Show Details

Rhodes, Scott D.; Mccoy, Thomas P.; Tanner, Amanda E.; Stowers, Jason; Bachmann, Laura H.; Nguyen, Annie L.; Ross, Michael W.

Clinical Infectious Diseases, 2016 , vol. 62, # 11 p. 1450 - 1453 Title/Abstract Full Text View citing articles Show Details

Lang, Julien; Gonzalez-Mula, Almudena; Taconnat, Ludivine; Clement, Gilles; Faure, Denis

New Phytologist, 2016 , vol. 210, # 3 p. 974 - 983 Title/Abstract Full Text View citing articles Show Details

Ryoo, Hyeon-Ju; Choo, Esther K.

Western Journal of Emergency Medicine, 2016 , vol. 17, # 3 p. 295 - 301 Title/Abstract Full Text View citing articles Show Details

Ishiwari, Keita; Sircar, Ratna

NeuroReport, 2016 , vol. 27, # 9 p. 627 - 631 Title/Abstract Full Text View citing articles Show Details

Patassini, Stefano; Begley, Paul; Xu, Jingshu; Church, Stephanie J.; Reid, Suzanne J.; Kim, Eric H.; Curtis, Maurice A.; Dragunow, Mike; Waldvogel, Henry J.; Snell, Russell G.; Unwin, Richard D.; Faull, Richard L.M.; Cooper, Garth J.S.

Biochimica et Biophysica Acta - Molecular Basis of Disease, 2016 , vol. 1862, # 9 p. 1650 - 1662 Title/Abstract Full Text View citing articles Show Details

Cai, Wenfei; Liu, Ronghou

Fuel, 2016 , vol. 182, p. 677 - 686 Title/Abstract Full Text Show Details

Çavdar, Safiye; Özgür, Merve; Kirazli, Özlem; Karahüseyinoğlu, Serçin; Onat, Filiz

Journal of Chemical Neuroanatomy, 2016 , vol. 77, p. 93 - 99 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

Bioactivities present

Reference

Castro, André L.; Tarelho, Sónia; Dias, Mário; Reis, Flávio; Teixeira, Helena M.

International Journal of Legal Medicine, 2016 , vol. 130, # 4 p. 959 - 965 Title/Abstract Full Text View citing articles Show Details

Mekonnen, Dereje Worku; Ludewig, Frank

Plant Molecular Biology, 2016 , vol. 91, # 4-5 p. 429 - 440 Title/Abstract Full Text View citing articles Show Details

Malaspina; Roullet; Pearl; Ainslie; Vogel; Gibson


Neurochemistry International, 2016 , vol. 99, p. 72 - 84 Title/Abstract Full Text View citing articles Show Details

Sinclair, Julia M. A.; Chambers, Sophia E.; Shiles, Celia J.; Baldwin, David S.

Drug Safety, 2016 , vol. 39, # 7 p. 627 - 645 Title/Abstract Full Text View citing articles Show Details

Lang, Julien; Faure, Denis

Plant Signaling and Behavior, 2016 , vol. 11, # 5 art. no. E1178440, p. 3 Title/Abstract Full Text View citing articles Show Details

Kamo, Miyu; Tojo, Motoaki; Yamazaki, Yusuke; Itabashi, Takeshi; Takeda, Hisashi; Wakana, Daigo; Hosoe, Tomoo

Journal of Antibiotics, 2016 , vol. 69, # 6 p. 451 - 455 Title/Abstract Full Text View citing articles Show Details

Picinelli Lobo, Anna; Antón-Díaz, María José; Mangas Alonso, Juan José; Suárez Valles, Belén

Food Chemistry, 2016 , vol. 213, p. 505 - 513 Title/Abstract Full Text View citing articles Show Details

Zeiger, William A.; Sun, Lisa R.; Bosemani, Thangamadhan; Pearl, Phillip L.; Stafstrom, Carl E.

Pediatric Neurology, 2016 , vol. 58, p. 113 - 115 Title/Abstract Full Text View citing articles Show Details

Jambunathan, Pooja; Zhang, Kechun

Journal of Industrial Microbiology and Biotechnology, 2016 , vol. 43, # 8 p. 1037 - 1058 Title/Abstract Full Text View citing articles Show Details

Tan, Lei; Lu, Shaoyou; Fang, Zhanqiang; Cheng, Wen; Tsang, Eric Pokeung

Applied Catalysis B: Environmental, 2017 , vol. 200, p. 200 - 210 Title/Abstract Full Text View citing articles Show Details

Tan, Lei; Lu, Shaoyou; Fang, Zhanqiang; Cheng, Wen; Tsang, Eric Pokeung

Applied Catalysis B: Environmental, 2017 , vol. 200, p. 200 - 210 Title/Abstract Full Text Show Details

Baumel; Rousseau-Gueutin; Sapienza-Bianchi; Gareil; Duong; Rousseau; Coriton; Amirouche; Sciandrello; Duarte; Caçador; Castillo; Ainouche

Biological Invasions, 2016 , vol. 18, # 8 p. 2123 - 2135 Title/Abstract Full Text View citing articles Show Details

Klimek, Beata; Sitarz, Anna; Choczyński, Maciej; Niklińska, Maria

Water, Air, and Soil Pollution, 2016 , vol. 227, # 8 art. no. 265 Title/Abstract Full Text View citing articles Show Details

Klimek, Beata; Sitarz, Anna; Choczyński, Maciej; Niklińska, Maria

Water, Air, and Soil Pollution, 2016 , vol. 227, # 8 Title/Abstract Full Text Show Details

Wang, Kevin Y.; Barker, Peter B.; Lin, Doris D. M.

Child's Nervous System, 2016 , vol. 32, # 7 p. 1305 - 1309 Title/Abstract Full Text View citing articles Show Details

Jiang, Guozhan; Hill, David J.; Kowalczuk, Marek; Johnston, Brian; Adamus, Grazyna; Irorere, Victor; Radecka, Iza

International Journal of Molecular Sciences, 2016 , vol. 17, # 7 art. no. 1157 Title/Abstract Full Text View citing articles Show Details

Horvath, Gabriella-Ana; Hukin, Juliette; Stockler-Ipsiroglu, Sylvia G.; Aroichane, Maryam

Neuropediatrics, 2016 , vol. 47, # 4 p. 263 - 267 Title/Abstract Full Text View citing articles Show Details

Zhu, Shusheng; Vivanco, Jorge M.; Manter, Daniel K.

Applied Soil Ecology, 2016 , vol. 107, p. 324 - 333 Title/Abstract Full Text View citing articles Show Details

Soyka, Michael; Mutschler, Jochen

Progress in Neuro-Psychopharmacology and Biological Psychiatry, 2016 , vol. 70, p. 148 - 161 Title/Abstract Full Text View citing articles Show Details

Giannoukos, Stamatios; Brkić, Boris; Taylor, Stephen; Marshall, Alan; Verbeck, Guido F.

Chemical Reviews, 2016 , vol. 116, # 14 p. 8146 - 8172 Title/Abstract Full Text View citing articles Show Details

13 of 79

Comment (Pharmacological Data)

Bioactivities present

Reference

Xu, Huajun; Zheng, Xiaojiao; Qian, Yingjun; Guan, Jian; Yi, Hongliang; Zou, Jianyin; Wang, Yuyu; Meng, Lili; Zhao, Aihua; Yin, Shankai; Jia, Wei

Scientific Reports, 2016 , vol. 6, art. no. 30958 Title/Abstract Full Text View citing articles Show Details

Kamal, Rama M.; Dijkstra, Boukje A.G.; Loonen, Anton J.; De Jong, Cornelis A.J.

Journal of Addiction Medicine, 2016 , vol. 10, # 4 p. 229 - 235 Title/Abstract Full Text View citing articles Show Details

Cader Mhd Haniffa, Mhd Abd; Ching, Yern Chee; Abdullah, Luqman Chuah; Poh, Sin Chew; Chuah, Cheng Hock

Polymers, 2016 , vol. 8, # 7 art. no. 246 Title/Abstract Full Text View citing articles Show Details

Gogou, Maria; Spilioti, Martha; Tramma, Despoina; Papadopoulou-Alataki, Efimia; Evangeliou, Athanasios

Indian Journal of Pediatrics, 2016 , vol. 83, # 9 p. 1036 - 1037 Title/Abstract Full Text View citing articles Show Details

Możejko-Ciesielska, Justyna; Kiewisz, Robert

Microbiological Research, 2016 , vol. 192, p. 271 - 282 Title/Abstract Full Text View citing articles Show Details

YALE UNIVERSITY; DIXIT, Vishwa, Deep

Patent: WO2016/123229 A1, 2016 ; Title/Abstract Full Text Show Details

Vourc'h, Mickael; Feuillet, Fanny; Mahe, Pierre-Joachim; Sebille, Véronique; Asehnoune, Karim; Lasocki, Sigismond; Gergaud, Soizic; Gaillard, Thomas; Lascarrou, Jean-Baptiste; Vinatier, Isabelle; Martin-Lefevre, Laurent; Yehia, Aihem; Colin, Gwenhael; Lebert, Christine; Fiancette, Maud; Henry-Lagarrigue, Matthieu; Lacherad, Jean-Claude; Jaber, Samir; Jong, Audrey De; Chanques, Gerald; Roquilly, Antoine; Cinotti, Raphaël; Dit Latte, Dominique Demeure; Reignier, Jean; Garret, Charlotte; Bretonniere, Céric; Brule, Noëlle; Nicolet, Laurent; Zambon, Olivier; Mimoz, Olivier; Moriconi, Mikael; Gacoin, Arnaud; Tadie, Jean-Marc; Tulzo, Yves Le; Lescot, Thomas; Morin, Paul; Jonas, Maud; Thibaut, Freddy; Ferrandiere, Martine


Trials, 2016 , vol. 17, # 1 art. no. 415 Title/Abstract Full Text View citing articles Show Details

Sharpless, Brian A.

Neuropsychiatric Disease and Treatment, 2016 , vol. 12, p. 1761 - 1767 Title/Abstract Full Text View citing articles Show Details

INVISTA North America S.á.r.l.; Botes, Adriana Leonora; Conradie, Alex Van Eck

Patent: US2016/222420 A1, 2016 ; Title/Abstract Full Text Show Details

Beauregard, Yannick; Ramsay, Juliana; Ramsay, Bruce

Journal of Polymers and the Environment, 2016 , vol. 24, # 3 p. 281 - 285 Title/Abstract Full Text Show Details

Scotcher, Daniel; Jones, Christopher; Posada, Maria; Galetin, Aleksandra; Rostami-Hodjegan, Amin

AAPS Journal, 2016 , vol. 18, # 5 p. 1082 - 1094 Title/Abstract Full Text Show Details

Zhou, Molin; Ndeurumio, Kessy H.; Zhao, Lei; Hu, Zhuoyan

Journal of Agricultural and Food Chemistry, 2016 , vol. 64, # 33 p. 6443 - 6450 Title/Abstract Full Text Show Details

Rochford, Kevin; Chen, Feng; Waguespack, Yan; Figliozzi, Robert W.; Kharel, Madan K.; Zhang, Qiaojuan; Martin-Caraballo, Miguel; Hsia, S. Victor

PLoS ONE, 2016 , vol. 11, # 8 art. no. E0161119 Title/Abstract Full Text Show Details

Rahmani, Amir; Khataee, Alireza; Kaymak, Baris; Vahid, Behrouz; Fathinia, Mehrangiz; Dindarsafa, Mahsa

RSC Advances, 2016 , vol. 6, # 84 p. 81219 - 81230 Title/Abstract Full Text Show Details

Oliver, Neal J; Rabinovitch-Deere, Christine A; Carroll, Austin L; Nozzi, Nicole E; Case, Anna E; Atsumi, Shota

Current Opinion in Chemical Biology, 2016 , vol. 35, p. 43 - 50 Title/Abstract Full Text Show Details

Hu, Jingwen; Xia, Runpu; Yang, Hua; Lu, Xiuping

Polymer Composites, 2016 , vol. 37, # 10 p. 3113 - 3121 Title/Abstract Full Text Show Details

Miller; Bellini; Vizza; Hasenöhrl; Tilley

Catalysis Science and Technology, 2016 , vol. 6, # 18 p. 6870 - 6878 Title/Abstract Full Text Show Details

Mowry, James B.; Spyker, Daniel A.; Cantilena, Louis R.; McMillan, Naya; Ford, Marsha

Clinical Toxicology, 2014 , vol. 52, # 10 p. 1032 - 1283 Title/Abstract Full Text Show Details

Lin, Yongming; Deng, Haojun; Du, Kun; Li, Jian; Lin, Han; Chen, Can; Fisher, Loretta; Wu, Chengzhen; Hong, Tao; Zhang, Guangshuai

Soil and Tillage Research, 2017 , vol. 165, p. 315 - 324 Title/Abstract Full Text Show Details

Liu, Kegang; Jiang, Xiaohua; Hunziker, Patrick

Nanoscale, 2016 , vol. 8, # 36 p. 16091 - 16156 Title/Abstract Full Text Show Details

14 of 79

Comment (Pharmacological Data)

Bioactivities present

Reference

Jimenez-Jimenez, Felix Javier; Garcia-Martin, Elena; Alonso-Navarro, Hortensia; Martinez, Carmen; Zurdo, Martin; TurpinFenoll, Laura; Millan-Pascual, Jorge; Adeva-Bartolome, Teresa; Cubo, Esther; Navacerrada, Francisco; Rojo-Sebastian, Ana; Rubio, Lluisa; Ortega-Cubero, Sara; Pastor, Pau; Calleja, Marisol; Plaza-Nieto, Jose Francisco; Pilo-De-La-Fuente, Belen; Arroyo-Solera, Margarita; Garcia-Albea, Esteban; Agundez, Jose A.G.

Medicine (United States), 2015 , vol. 94, # 47 p. e2125 - e2125 Title/Abstract Full Text Show Details

Choi, Sol; Kim, Hyun Uk; Kim, Tae Yong; Lee, Sang Yup

Metabolic Engineering, 2016 , vol. 38, p. 264 - 273 Title/Abstract Full Text Show Details

Villumsen, Inge S.; Wellendorph, Petrine; Smart, Trevor G.

BMC Neuroscience, 2015 , vol. 16, # 1 art. no. 8 Title/Abstract Full Text Show Details

Meyer, Markus R.

Archives of Toxicology, 2016 , vol. 90, # 10 p. 2421 - 2444 Title/Abstract Full Text Show Details Telving, Rasmus; Hasselstrøm, Jørgen Bo; Andreasen, Mette Findal

Forensic Science International, 2016 , vol. 266, p. 453 - 461 Title/Abstract Full Text Show Details

Kyriakou, Chrystalla; Marchei, Emilia; Scaravelli, Giulia; García-Algar, Oscar; Supervía, August; Graziano, Silvia

Journal of Pharmaceutical and Biomedical Analysis, 2016 , vol. 128, p. 53 - 60 Title/Abstract Full Text Show Details

Gopi; Swetha; Chandra Shekar; Soni, Keshav Chand; Krishna; Ramakrishna; Saini, Bijendra

Ozone: Science and Engineering, 2016 , vol. 38, # 6 p. 482 - 493 Title/Abstract Full Text Show Details

Ramírez-Bahena, Martha Helena; Flores-Félix, José David; Chahboune, Rajaa; Toro, Marcia; Velázquez, Encarna; Peix, Alvaro

Systematic and Applied Microbiology, 2016 , vol. 39, # 6 p. 378 - 383 Title/Abstract Full Text Show Details

Jansen; Vogel; Salomons; Pearl; Roullet; Gibson

Journal of Inherited Metabolic Disease, 2016 , vol. 39, # 6 p. 795 - 800 Title/Abstract Full Text Show Details

Mok, Pei-Shze; Ch’ng, Diana Hooi-Ean; Ong, Soo-Peng; Numata, Keiji; Sudesh, Kumar

AMB Express, 2016 , vol. 6, # 1 art. no. 97 Title/Abstract Full Text Show Details

Fijałkowski, Łukasz; Sałat, Kinga; Podkowa, Adrian; Zaręba, Paula; Nowaczyk, Alicja

European Journal of Pharmaceutical Sciences, 2017 , vol. 96, p. 362 - 372 Title/Abstract Full Text Show Details


Brand, Bodo; Scheinhardt, Markus O.; Friedrich, Juliane; Zimmer, Daisy; Reinsch, Norbert; Ponsuksili, Siriluck; Schwerin, Manfred; Ziegler, Andreas

BMC Genetics, 2016 , vol. 17, # 1 art. no. 135 Title/Abstract Full Text Show Details

Vogel, Alexander L.; Schneider, Johannes; Müller-Tautges, Christina; Klimach, Thomas; Hoffmann, Thorsten

Environmental Science and Technology, 2016 , vol. 50, # 20 p. 10814 - 10822 Title/Abstract Full Text Show Details

Wiergowski, Marek; Anand, Jacek Sein; Karnecki, Karol; Sołtyszewski, Ireneusz; Jankowski, Zbigniew

Romanian Journal of Legal Medicine, 2016 , vol. 24, # 3 p. 219 - 225 Title/Abstract Full Text Show Details

Hentati, Olfa; Oliveira, Vanessa; Sena, Clara; Bouji, Mohamed Seddik Mahmoud; Wali, Ahmed; Ksibi, Mohamed

Ecotoxicology, 2016 , vol. 25, # 8 p. 1500 - 1513 Title/Abstract Full Text Show Details

Miller; Bellini; Vizza; Hasenöhrl; Tilley

Catalysis Science and Technology, 2016 , vol. 6, # 18 p. 6870 - 6878 Title/Abstract Full Text Show Details

Vogel, Alexander L.; Schneider, Johannes; Müller-Tautges, Christina; Klimach, Thomas; Hoffmann, Thorsten

Environmental Science and Technology, 2016 , vol. 50, # 20 p. 10814 - 10822 Title/Abstract Full Text Show Details

Claassens, Nico J.; Sousa, Diana Z.; Dos Santos, Vitor A. P. Martins; De Vos, Willem M.; Van Der Oost, John

Nature Reviews Microbiology, 2016 , vol. 14, # 11 p. 692 - 706 Title/Abstract Full Text Show Details

Ng, Lee-Mei; Sudesh, Kumar

Journal of Bioscience and Bioengineering, 2016 , vol. 122, # 5 p. 550 - 557 Title/Abstract Full Text Show Details

Mercolini, Laura; Protti, Michele

Journal of Pharmaceutical and Biomedical Analysis, 2016 , vol. 130, p. 202 - 219 Title/Abstract Full Text Show Details

15 of 79

Comment (Pharmacological Data)

Bioactivities present

Reference

Guo, Tianyang; Fang, Pingping; Jiang, Juanjuan; Zhang, Feng; Yong, Wei; Liu, Jiahui; Dong, Yiyang

Journal of Chromatography A, 2016 , vol. 1471, p. 27 - 33 Title/Abstract Full Text Show Details

Asadullin, Azat R.; Galeeva, Elena Kh.; Achmetova, Elvina A.; Nikolaev, Ivan V.

International Journal of Environmental and Science Education, 2016 , vol. 11, # 14 art. no. IJESE..001, p. 6697 - 6703 Title/Abstract Full Text Show Details

Jurnak, Frances

Nutrition and Metabolic Insights, 2016 , vol. 8, p. 57 - 77 Title/Abstract Full Text Show Details

Vogel; Ainslie; Jansen; Salomons; Gibson

Biochimica et Biophysica Acta - Molecular Basis of Disease, 2017 , vol. 1863, # 1 p. 33 - 42 Title/Abstract Full Text Show Details

Zhao, Lijuan; Huang, Yuxiong; Hannah-Bick, Cameron; Fulton, Aaron N.; Keller, Arturo A.

NanoImpact, 2016 , vol. 3-4, p. 58 - 66 Title/Abstract Full Text Show Details

Sadones, Nele; Van Bever, Elien; Archer, John R.H.; Wood, David M.; Dargan, Paul I.; Van Bortel, Luc; Lambert, Willy E.; Stove, Christophe P.

Journal of Chromatography A, 2016 , vol. 1465, p. 175 - 183 Title/Abstract Full Text Show Details

Loder, Andrew J.; Han, Yejun; Hawkins, Aaron B.; Lian, Hong; Lipscomb, Gina L.; Schut, Gerrit J.; Keller, Matthew W.; Adams, Michael W.W.; Kelly, Robert M.

Metabolic Engineering, 2016 , vol. 38, p. 446 - 463 Title/Abstract Full Text Show Details

Jamey, Carole; Kintz, Pascal; Martrille, Laurent; Raul, Jean-Sébastien

Journal of Analytical Toxicology, 2016 , vol. 40, # 7 art. no. BKW058, p. 546 - 552 Title/Abstract Full Text Show Details

Skidmore, Chloe R.; Kaufman, Erin A.; Crowell, Sheila E.

Child and Adolescent Psychiatric Clinics of North America, 2016 , vol. 25, # 4 p. 735 - 753 Title/Abstract Full Text Show Details

Vercruysse, Jop; Poupaert, Andries; Vanholme, Ruben; Bastien, Catherine; Vanholme, Bartel; Boerjan, Wout; Prins, Wolter; Ronsse, Frederik

Journal of Analytical and Applied Pyrolysis, 2016 , vol. 122, p. 377 - 386 Title/Abstract Full Text Show Details

Beauchamp, Gillian A.; Hendrickson, Robert G.; Hatten, Benjamin W.

Journal of Emergency Medicine, 2016 , vol. 51, # 4 p. 382 - 11,388 Title/Abstract Full Text Show Details

Vercruysse, Jop; Poupaert, Andries; Vanholme, Ruben; Bastien, Catherine; Vanholme, Bartel; Boerjan, Wout; Prins, Wolter; Ronsse, Frederik

Journal of Analytical and Applied Pyrolysis, 2016 , vol. 122, p. 377 - 386 Title/Abstract Full Text Show Details

Akiyama, Tomoyuki; Osaka, Hitoshi; Shimbo, Hiroko; Kuhara, Tomiko; Shibata, Takashi; Kobayashi, Katsuhiro; Kurosawa, Kenji; Yoshinaga, Harumi

Brain and Development, 2016 , vol. 38, # 9 p. 871 - 874 Title/Abstract Full Text Show Details

Horino, Asako; Kawawaki, Hisashi; Fukuoka, Masataka; Tsuji, Hitomi; Hattori, Yuka; Inoue, Takeshi; Nukui, Megumi; Kuki, Ichiro; Okazaki, Shin; Tomiwa, Kiyotaka; Hirose, Shinichi

Brain and Development, 2016 , vol. 38, # 9 p. 866 - 870 Title/Abstract Full Text Show Details

Pinzari, Flavia; Ceci, Andrea; Abu-Samra, Nadir; Canfora, Loredana; Maggi, Oriana; Persiani, Annamaria

Research in Microbiology, 2016 , vol. 167, # 9-10 p. 710 - 722 Title/Abstract Full Text Show Details

Downing, Martin J.; Houang, Steven T.; Scheinmann, Roberta; Yoon, Irene S.; Chiasson, Mary Ann; Hirshfield, Sabina

Sleep Health, 2016 , vol. 2, # 4 p. 322 - 329


Title/Abstract Full Text Show Details

Ainslie, Garrett R.; Gibson, K. Michael; Vogel, Kara R.

Pharmacology Research and Perspectives, 2016 , vol. 4, # 6 art. no. E00265 Title/Abstract Full Text Show Details

Jesse; Bråthen; Ferrara; Keindl; Ben-Menachem; Tanasescu; Brodtkorb; Hillbom; Leone; Ludolph

Acta Neurologica Scandinavica, 2017 , vol. 135, # 1 p. 4 - 16 Title/Abstract Full Text Show Details

Seo, Chan; Park, Meejung; Choi, Boyeon; Lee, Sooyeun; Paik, Man-Jeong

Metabolomics, 2016 , vol. 12, # 12 art. no. 190 Title/Abstract Full Text Show Details

Syafiq, Ishak Muhammad; Huong, Kai-Hee; Shantini; Vigneswari; Aziz, Nursolehah Abd; Amirul, Al-Ashraf Abdullah; Bhubalan, Kesaven

Enzyme and Microbial Technology, 2017 , vol. 98, p. 1 - 8 Title/Abstract Full Text Show Details

16 of 79

17 of 79

Comment (Pharmacological Data)

Bioactivities present

Reference

Cho, Sang Hyun; Lee, Hyo Jung; Jeon, Che Ok

International Journal of Systematic and Evolutionary Microbiology, 2016 , vol. 66, # 11 art. no. 001438, p. 4839 - 4843 Title/Abstract Full Text Show Details

Hines, Elizabeth

Clinical Pediatric Emergency Medicine, 2016 , vol. 17, # 4 p. 296 - 301 Title/Abstract Full Text Show Details

Chen, Guo-Qiang; Jiang, Xiao-Ran; Guo, Yingying

Synthetic and Systems Biotechnology, 2016 , vol. 1, # 4 p. 236 - 242 Title/Abstract Full Text Show Details

Holloway, Ian W.; Dougherty, Ryan; Gildner, Jennifer; Beougher, Sean C.; Pulsipher, Craig; Montoya, Jorge A.; Plant, Aaron; Leibowitz, Arleen

Journal of Acquired Immune Deficiency Syndromes, 2017 , vol. 74, # 1 p. 15 - 20 Title/Abstract Full Text Show Details

Monteverde; Gómez-Consarnau; Suffridge; Sañudo-Wilhelmy

Geobiology, 2017 , vol. 15, # 1 p. 3 - 18 Title/Abstract Full Text Show Details

Okino, Tetsuya; Ushirogawa, Hiroshi; Matoba, Kumiko; Nishimatsu, Shin-ichiro; Saito, Mineki

Parasitology International, 2017 , vol. 66, # 2 p. 116 - 118 Title/Abstract Full Text Show Details

Hearne, Evelyn; Grund, Jean-Paul Cornelius; Van Hout, Marie Claire; McVeigh, Jim

Harm Reduction Journal, 2016 , vol. 13, # 1 art. no. 14 Title/Abstract Full Text Show Details

Kubáň, Pavel; Hauser, Peter C.

Electrophoresis, 2017 , vol. 38, # 1 p. 95 - 114 Title/Abstract Full Text Show Details

Mehling, Lena-Maria; Piper, Thomas; Dib, Josef; Pedersen, Daniel Sejer; Madea, Burkhard; Hess, Cornelius; Thevis, Mario

Forensic Toxicology, 2017 , vol. 35, # 1 p. 77 - 85 Title/Abstract Full Text Show Details

Reisner, Sari L; Poteat, Tonia; Keatley, JoAnne; Cabral, Mauro; Mothopeng, Tampose; Dunham, Emilia; Holland, Claire E; Max, Ryan; Baral, Stefan D

The Lancet, 2016 , vol. 388, # 10042 p. 412 - 436 Title/Abstract Full Text Show Details

Wiergowski, Marek; Anand, Jacek Sein; Karnecki, Karol; Sołtyszewski, Ireneusz; Jankowski, Zbigniew

Romanian Journal of Legal Medicine, 2016 , vol. 24, # 4 p. 318 - 324 Title/Abstract Full Text Show Details

Kamaly, Nazila; Yameen, Basit; Wu, Jun; Farokhzad, Omid C.

Chemical Reviews, 2016 , vol. 116, # 4 p. 2602 - 2663 Title/Abstract Full Text Show Details

Beck, Matthias H.; Poehlein, Anja; Bengelsdorf, Frank R.; Schiel-Bengelsdorf, Bettina; Daniel, Rolf; Dürre, Peter

Genome Announcements, 2015 , vol. 3, # 5 art. no. E01112-15 Title/Abstract Full Text Show Details

Croce, Annamaria; Battistel, Ezio; Chiaberge, Stefano; Spera, Silvia; De Angelis, Francesco; Reale, Samantha

ChemSusChem, 2017 , vol. 10, # 1 p. 171 - 181 Title/Abstract Full Text Show Details

Neikrug, Ariel B.; Crawford, Megan R.; Ong, Jason C.

Behavioral Sleep Medicine, 2017 , vol. 15, # 2 p. 158 - 171 Title/Abstract Full Text Show Details

Giulivi, Cecilia; Napoli, Eleonora; Tassone, Flora; Halmai, Julian; Hagerman, Randi

Biochemical Journal, 2016 , vol. 473, # 21 p. 3871 - 3888 Title/Abstract Full Text Show Details

Jiménez-Pérez; Sevilla; Pineda; Blázquez; Gonzalez-Rodriguez

International Journal of Electrochemical Science, 2016 , vol. 11, # 12 p. 10473 - 10487 Title/Abstract Full Text Show Details

Ray, Subhasree; Kalia, Vipin Chandra

Indian Journal of Microbiology, 2017 , vol. 57, # 1 p. 39 - 47 Title/Abstract Full Text Show Details

Gonçalves, Davi Martinelli; Kolstee, Johann; Ryan, Dermot; Race, Kane

Contemporary Drug Problems, 2016 , vol. 43, # 4 p. 314 - 330 Title/Abstract Full Text Show Details

Busardò, Francesco Paolo; Kyriakou, Chrystalla; Marchei, Emilia; Pacifici, Roberta; Pedersen, Daniel Sejer; Pichini, Simona

Journal of Pharmaceutical and Biomedical Analysis, 2017 , vol. 137, p. 123 - 131 Title/Abstract Full Text Show Details

Comment (Pharmacological Data)

physiological behaviour discussed


Reference

LABORATORIO FARMACEUTICO C.T. S.R.L.; CACCIAGLIA, Roberto; CLERICI, Francesca; CALDERONE, Vincenzo; CHERICONI, Silvio; MEINI, Milo; MONCINI, Marco

Patent: WO2015/83129 A1, 2015 ; Title/Abstract Full Text Show Details

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Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Thiesen, Louise; Kehler, Jan; Clausen, Rasmus P.; Frolund, Bente; Bundgaard, Christoffer; Wellendorph, Petrine

Journal of Pharmacology and Experimental Therapeutics, 2015 , vol. 354, # 2 p. 166 - 174 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Morse, Bridget L.; Morris, Marilyn E.

Journal of Pharmacology and Experimental Therapeutics, 2013 , vol. 346, # 3 p. 504 - 513 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Vogensen, Stine B.; Marek, Ales; Bay, Tina; Wellendorph, Petrine; Kehler, Jan; Bundgaard, Christoffer; Frolund, Bente; Pedersen, Martin H. F.; Clausen, Rasmus P.

Journal of Medicinal Chemistry, 2013 , vol. 56, # 20 p. 8201 - 8205 Title/Abstract Full Text View citing articles Show Details

Show next 20

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Hide facts

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM); MAITRE, Michel; BOURGUIGNON, JeanJacques; SCHMITT, Martine; KLEIN, Christian; MENSAH-NYAGAN, Ayikoe, Guy; MATHIS, Chantal; CASSEL, Jean-Christophe

Patent: WO2013/24028 A1, 2013 ; Title/Abstract Full Text Show Details

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Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

rat

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

used as sodium salt; 200 mg/kg dose in sterile water for injection

Method (Pharmacological Data)

Example 6.- In vivo pharmacokinetic studies.The pharmacokinetics of exemplary compounds was determined by comparison with 4hydroxybutyric acid by dosing the compounds in rats according to the following study design and sampling procedure.Study Design:DosingTreatme Animal Solutio DosingTest Dosing Dose Sampling Time nt s n Volume VehicleCompound Route mg/kg Points Group N= Cone. mL/kgmg/m Lhydroxybuta Predose, 5, 15, 306 noic acid, PO 4 200 40 5 SWFI min,sodium salt1 , 2, 4, and 6 hoursSWFI: Sterile water for injectionSampling procedure:6.1 SamplingThe results of the in vivo studies are disclosed in the following table (Table 2): Table 2a 2 hr for IV and 4 hr for POb calculated up to 2hr for IV and 4 hr for POAs shown in Table 2, the pharmcokinetics of IV-b, sodium salt was considerably increased relative to 4-hydroxybutyric acid, sodium salt . This is particularly clear from a comparison of the relative values of AUC0-.infin.and of t1/2for the two compounds.

Results

Tmax (h) = 0.5; Cmax (ug/ml) = 150; Cmin (ug/ml) = 2 after 4 h; AUC0-infinity (hr*ug/ml) = 170; t1/2 = 0.61 up to 4 h

Location

Page/Page column 50-52

Reference

CONCERT PHARMACEUTICALS INC.; TUNG, Roger, D.; MORGAN, Adam; SILVERMAN, I., Robert

Patent: WO2012/112492 A1, 2012 ; Title/Abstract Full Text Show Details

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Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

rat


Route of Application

intravenous

Kind of Dosing (Pharmacological Data)

used as sodium salt; 200 mg/kg dose in sterile water for injection

Method (Pharmacological Data)

Example 6.- In vivo pharmacokinetic studies.The pharmacokinetics of exemplary compounds was determined by comparison with 4hydroxybutyric acid by dosing the compounds in rats according to the following study design and sampling procedure.Study Design:DosingTreatme Animal Solutio DosingTest Dosing Dose Sampling Time nt s n Volume VehicleCompound Route mg/kg Points Group N= Cone. mL/kgmg/m Lhydroxybuta Predose, 5, 15, 306 noic acid, PO 4 200 40 5 SWFI min,sodium salt1 , 2, 4, and 6 hoursSWFI: Sterile water for injectionSampling procedure:6.1 SamplingThe results of the in vivo studies are disclosed in the following table (Table 2): Table 2a 2 hr for IV and 4 hr for POb calculated up to 2hr for IV and 4 hr for POAs shown in Table 2, the pharmcokinetics of IV-b, sodium salt was considerably increased relative to 4-hydroxybutyric acid, sodium salt . This is particularly clear from a comparison of the relative values of AUC0-.infin.and of t1/2for the two compounds.

Results

Cmin (ug/ml) = 8 after 2 h; AUC0-infinity (hr*ug/ml) = 427; CL (ml/min/kg) = 8; Vz (l/kg) = 0.2; t1/2 = 0.26 up to 2 h

Location

Page/Page column 50-52

Reference

CONCERT PHARMACEUTICALS INC.; TUNG, Roger, D.; MORGAN, Adam; SILVERMAN, I., Robert

Patent: WO2012/112492 A1, 2012 ; Title/Abstract Full Text Show Details

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Effect (Pharmacological Data)

receptor; stimulation of

Species or TestSystem (Pharmacological Data)

oocyte of Xenopus laevis; genetically modified/infected with: pGEMHE-Erwinia ligand-gated ion channel-human α7 nACh receptor signal sequence

Sex

female

Concentration (Pharmacological Data)

100 mmol/l

Further Details (Pharmacological Data)

stage V - VI oocyte used; two-electrode voltage-clamp; Rmax: maximal current relative to 10 mM GABA (γ-aminobutyric acid); response rate related to: Erwinia ligand-gated ion channel

Type (Pharmacological Data)

response rate

Value of Type (Pharmacological Data)

8,2 percent of Rmax

Reference

Thompson, Andrew J.; Alqazzaz, Mona; Ulens, Chris; Lummis, Sarah C.R.

Neuropharmacology, 2012 , vol. 63, # 4 p. 761 - 767 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transporter mediated L-[3H]proline uptake into cells; inhibition of

Species or TestSystem (Pharmacological Data)

Caco-2 cells; genetically modified/infected with: human PAT1

Further Details (Pharmacological Data)

PAT1: proton-coupled amino acid transporter 1; radioligand: L-[3H]proline, 10 nM; inhibition constant (Ki); Ki related to: human PAT1

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

65 nmol/l

Reference

Thondorf, Iris; Voigt, Valerie; Schaefer, Sarah; Gebauer, Sabine; Zebisch, Katja; Laug, Linda; Brandsch, Matthias

Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 21 p. 6409 - 6418 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transporter mediated L-[3H]proline uptake into cells; inhibition of

Species or TestSystem

Caco-2 cells; genetically modified/infected with: human PAT1


(Pharmacological Data)

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Further Details (Pharmacological Data)

PAT1: proton-coupled amino acid transporter 1; radioligand: L-[3H]proline, 10 nM

Results

molecular target: human PAT1

Reference

Thondorf, Iris; Voigt, Valerie; Schaefer, Sarah; Gebauer, Sabine; Zebisch, Katja; Laug, Linda; Brandsch, Matthias

Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 21 p. 6409 - 6418 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

inward current; effect on

Species or TestSystem (Pharmacological Data)

oocyte of Xenopus laevis; genetically modified/infected with: RDL subunit cDNA subcloned into pRmHa3-RDL into oocyte expression vector pGEMHE

Concentration (Pharmacological Data)

<= 10 mmol/l

Further Details (Pharmacological Data)

RDL: resistance to dieldrin

Results

no effect (related to RDL receptor)

Reference

McGonigle, Ian; Lummis, Sarah C. R.

Biochemistry, 2010 , vol. 49, # 13 p. 2897 - 2902 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

[125I]BnOPh-GHB Binding; inhibition of

Species or TestSystem (Pharmacological Data)

cerebral cortical membranes of Sprague-Dawley rat

Sex

male

Further Details (Pharmacological Data)

GHB: γ-hydroxybutyric acid; inhibition constant (Ki); Ki related to: GHB binding site

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

4.4 μmol/l

Location

supporting information

Reference

Wellendorph, Petrine; Hog, Signe; Sabbatini, Paola; Pedersen, Martin H. F.; Martiny, Lars; Knudsen, Gitte M.; Frolund, Bente; Clausen, Rasmus P.; Braeuner-Osborne, Hans

Journal of Pharmacology and Experimental Therapeutics, 2010 , vol. 335, # 2 p. 458 - 464 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

[125I]BnOPh-GHB Binding; inhibition of

Species or TestSystem (Pharmacological Data)

cerebral cortical membranes of Sprague-Dawley rat

Sex

male

Further Details (Pharmacological Data)

GHB: γ-hydroxybutyric acid

Results

molecular target: rat GHB binding site

Location

supporting information

Reference

Wellendorph, Petrine; Hog, Signe; Sabbatini, Paola; Pedersen, Martin H. F.; Martiny, Lars; Knudsen, Gitte M.; Frolund, Bente; Clausen, Rasmus P.; Braeuner-Osborne, Hans

Journal of Pharmacology and Experimental Therapeutics, 2010 , vol. 335, # 2 p. 458 - 464


Title/Abstract Full Text View citing articles Show Details

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Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

Ca. 100 - 800 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in sterile 0.9percent saline

Method (Pharmacological Data)

rats rendered diabetic by a single injection of streptozotocin; potency of title comp. to decrease lever pressing maintained by food, before and after streptozotocin treatment assessed

Further Details (Pharmacological Data)

vehicle control

Results

title comp. dose-dependently decreased responding before and after streptozotocin injection, but it was less potent after streptozotocin; diagram

Reference

Sevak, Rajkumar J.; Koek, Wouter; Daws, Lynette C.; Owens, William Anthony; Galli, Aurelio; France, Charles P.

European Journal of Pharmacology, 2008 , vol. 581, # 1-2 p. 105 - 112 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transport

Species or TestSystem (Pharmacological Data)

Human kidney HK-2 cells

Concentration (Pharmacological Data)

1 - 60 mmol/l

Method (Pharmacological Data)

cells treated with title comp.; time depen. study measured by incub. at room temperature for 0.5 to 120 min with varying pH from 5 to 7.4; sodium dependence measured; lysed; radioactivity measured by liquid scintillation counting

Further Details (Pharmacological Data)

further study: effect of salicylate, CHC, pCMB, DIDS, probenecid, rifampicin, TEA, phloretin, L-lactate, D-Lactate, bytyrate on title comp. uptake detd.

Results

title comp. uptake was pH dependent, uptake rate signif. increased with decreasing pH; at pH 7.5 title comp. uptake was reduced in absence of sodium, at pH 6 uptake was not affected by presence, absence of sodium; CHC inhibited title comp. uptake; fig.

Reference

Wang, Qi; Lu, Ye; Morris, Marilyn E.

Pharmaceutical Research, 2007 , vol. 24, # 6 p. 1067 - 1078 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Human kidney HK-2 cells

Concentration (Pharmacological Data)

1 - 60 mmol/l

Method (Pharmacological Data)

cells treated with title comp.; time depen. study measured by incub. at room temperature for 0.5 to 120 min with varying pH from 5 to 7.4; sodium dependence measured; lysed; radioactivity measured by liquid scintillation counting

Further Details (Pharmacological Data)

further study: effect of salicylate, CHC, pCMB, DIDS, probenecid, rifampicin, TEA, phloretin, L-lactate, D-Lactate, bytyrate on title comp. uptake detd.


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Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

0.28 mmol/l

Results

title comp. showed Km of 2.07 mM, Vmax of 27.6 nmol/mg.min, diff. clearance of 0.54 μl/mg.min, resp.; title comp. uptake inhibited by butyrate, D-lactate, L-lactate, phloretin, pCMB, salicylate, DIDS; rifampicin, TEA had no effect; fig.; table.

Reference

Wang, Qi; Lu, Ye; Morris, Marilyn E.

Pharmaceutical Research, 2007 , vol. 24, # 6 p. 1067 - 1078 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transport

Species or TestSystem (Pharmacological Data)

Human kidney HK-2 cells

Concentration (Pharmacological Data)

1 - 60 mmol/l

Method (Pharmacological Data)

cells loaded in polycarbonate transwell inserts; title comp. loaded in apical and basal chamber; incubated at diff. pH levels at room temperature with or without CHC; samples collected; permeability measured

Results

at pH 6 and 7.5 cellular accumulation of title comp. was higher in basal chamber and comparitively lesser in apical region; fig.

Reference

Wang, Qi; Lu, Ye; Morris, Marilyn E.

Pharmaceutical Research, 2007 , vol. 24, # 6 p. 1067 - 1078 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

mutagenic

Species or TestSystem (Pharmacological Data)

Salmonella typhimurium TA98

Concentration (Pharmacological Data)

100 - 10000 μg/plate

Method (Pharmacological Data)

histidine auxotroph strain, title comp. in presence/absence of S9 mix added to molten selective top agar at 45 deg C; vortexed mixture overlaid onto surface of minimal bottom agar; plates incubated (48 h, 37 deg C); number of revertants/plate determ.

Further Details (Pharmacological Data)

liver S9 homogenate from male Sprague-Dawley rats or Syrian golden hamsters injected with Aroclor 1254 at 500 mg/kg body wt; control: H2O; positive response: at least doubling in mean number of revertants/plate together with dose-related increase

Comment (Pharmacological Data)

No effect

Reference

Seifried; Clarke; Junghans; San

Chemical Research in Toxicology, 2006 , vol. 19, # 5 p. 627 - 644 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

mutagenic

Species or TestSystem (Pharmacological Data)

Salmonella typhimurium TA100

Concentration (Pharmacological Data)

100 - 10000 μg/plate

Method (Pharmacological Data)

histidine auxotroph strain, title comp. in presence/absence of S9 mix added to molten selective top agar at 45 deg C; vortexed mixture overlaid onto surface of minimal bottom agar; plates incubated (48 h, 37 deg C); number of revertants/plate determ.

Further Details (Pharmacological Data)

liver S9 homogenate from male Sprague-Dawley rats or Syrian golden hamsters injected with Aroclor 1254 at 500 mg/kg body wt; control: H2O; positive response: at least doubling in mean number of revertants/plate together with dose-related increase


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Comment (Pharmacological Data)

No effect

Reference

Seifried; Clarke; Junghans; San

Chemical Research in Toxicology, 2006 , vol. 19, # 5 p. 627 - 644 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

mutagenic

Species or TestSystem (Pharmacological Data)

Salmonella typhimurium TA102

Concentration (Pharmacological Data)

100 - 10000 μg/plate

Method (Pharmacological Data)

histidine auxotroph strain, title comp. in presence/absence of S9 mix added to molten selective top agar at 45 deg C; vortexed mixture overlaid onto surface of minimal bottom agar; plates incubated (48 h, 37 deg C); number of revertants/plate determ.

Further Details (Pharmacological Data)

liver S9 homogenate from male Sprague-Dawley rats or Syrian golden hamsters injected with Aroclor 1254 at 500 mg/kg body wt; control: H2O; positive response: at least doubling in mean number of revertants/plate together with dose-related increase

Comment (Pharmacological Data)

No effect

Reference

Seifried; Clarke; Junghans; San

Chemical Research in Toxicology, 2006 , vol. 19, # 5 p. 627 - 644 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

mutagenic

Species or TestSystem (Pharmacological Data)

Salmonella typhimurium TA1535

Concentration (Pharmacological Data)

100 - 10000 μg/plate

Method (Pharmacological Data)

histidine auxotroph strain, title comp. in presence/absence of S9 mix added to molten selective top agar at 45 deg C; vortexed mixture overlaid onto surface of minimal bottom agar; plates incubated (48 h, 37 deg C); number of revertants/plate determ.

Further Details (Pharmacological Data)

liver S9 homogenate from male Sprague-Dawley rats or Syrian golden hamsters injected with Aroclor 1254 at 500 mg/kg body wt; control: H2O; positive response: at least doubling in mean number of revertants/plate together with dose-related increase

Comment (Pharmacological Data)

No effect

Reference

Seifried; Clarke; Junghans; San

Chemical Research in Toxicology, 2006 , vol. 19, # 5 p. 627 - 644 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

mutagenic

Species or TestSystem (Pharmacological Data)

Salmonella typhimurium TA1537

Concentration (Pharmacological Data)

100 - 10000 μg/plate

Method (Pharmacological Data)

histidine auxotroph strain, title comp. in presence/absence of S9 mix added to molten selective top agar at 45 deg C; vortexed mixture overlaid onto surface of minimal bottom agar; plates incubated (48 h, 37 deg C); number of revertants/plate determ.

Further Details (Pharmacological Data)

liver S9 homogenate from male Sprague-Dawley rats or Syrian golden hamsters injected with Aroclor 1254 at 500 mg/kg body wt; control: H2O; positive response: at least doubling in mean number of revertants/plate together with dose-related increase


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Comment (Pharmacological Data)

No effect

Reference

Seifried; Clarke; Junghans; San

Chemical Research in Toxicology, 2006 , vol. 19, # 5 p. 627 - 644 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

hypnogenic

Species or TestSystem (Pharmacological Data)

Sprague Dawley rat

Sex

male

Route of Application

intravenous

Concentration (Pharmacological Data)

165 mg/kg

Method (Pharmacological Data)

title comp. administered to rats, immediately followed by saline (n=4) or salicylic acid (SA, 175 mg/kg; n=4); loss in righting reflex (LRR), return of righting reflex (RRR) measured; SHE duration calculated

Further Details (Pharmacological Data)

SHE: sedative/hypnotic effect (absolute difference between LRR and RRR)

Results

title comp. alone caused pronounced SHE; title comp. SHE was abolished by SA

Reference

Bhattacharya, Indranil; Boje, Kathleen M. K.

Journal of Pharmacokinetics and Pharmacodynamics, 2006 , vol. 33, # 5 p. 657 - 681 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transport

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat kidney cortex BBM vesicles

Concentration (Pharmacological Data)

<= 50 mmol/l

Kind of Dosing (Pharmacological Data)

<3H>-labeled title comp. used

Method (Pharmacological Data)

vesicles added to uptake medium (various pH values) containing <3H>title comp. in 1:10 dilution; stopped; presoaked overnight in buffer containing unlabeled title comp.; radioactivity counted by liquid scintillation spectroscopy

Further Details (Pharmacological Data)

ref.: L-lactate; BBM: brush border membrane; further study with arachidonic acid (AA), D- and L-lactate, pyruvate, 1,4-butanediol (BTD), β-hydroxybutyrate (BHB), α-cyano-4-hydroxycinnamate (CHC)

Results

title comp. uptake decreased with increase in pH; Km: 8.0 mmol/l and Vmax: 838 pmol/mg/s; uptake of title comp. was signif. decreased in presence of CHC, AA, D- and L-lactate, pyruvate; BTD and BHB had no effect on title comp. uptake; diagram

Reference

Wang, Qi; Darling, Inger M.; Morris, Marilyn E.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 2 p. 751 - 761 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transport

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat kidney cortex BLM vesicles

Concentration (Pharmacological Data)

<= 50 mmol/l

Kind of Dosing (Pharmacological

<3H>-labeled title comp. used


Data)

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Method (Pharmacological Data)

vesicles added to uptake medium (various pH values) containing <3H>title comp. in 1:10 dilution; stopped; presoaked overnight in buffer containing unlabeled title comp.; radioactivity counted by liquid scintillation spectroscopy

Further Details (Pharmacological Data)

ref.: L-lactate; BLM: basolateral membrane; further study with arachidonic acid (AA), D- and L-lactate, pyruvate, 1,4-butanediol (BTD), βhydroxybutyrate (BHB), α-cyano-4-hydroxycinnamate (CHC), phloretin

Results

title comp. uptake decreased with increase in pH; Km: 10.5 mmol/l, Vmax: 806 pmol/mg/s; uptake of title comp. signif. decreased in presence of CHC, AA, D- and L-lactate, pyruvate and phloretin; BTD and BHB had no effect on title comp. uptake; diagram

Reference

Wang, Qi; Darling, Inger M.; Morris, Marilyn E.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 2 p. 751 - 761 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transport

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat kidney cortex BBM vesicles

Concentration (Pharmacological Data)

<= 50 mmol/l

Kind of Dosing (Pharmacological Data)

<3H>-labeled title comp. used

Method (Pharmacological Data)

vesicles added to uptake medium (with sodium/potassium/bicarbonate gradient) containing <3H>title comp. in 1:10 dilution; stopped; presoaked overnight in buffer containing unlabeled title comp.; radioactivity counted by liquid scintillation spectroscopy

Further Details (Pharmacological Data)

ref.: L-lactate; BBM: brush border membrane; further study with arachidonic acid (AA), D- and L-lactate, pyruvate, 1,4-butanediol (BTD), β-hydroxybutyrate (BHB), α-cyano-4-hydroxycinnamate (CHC)

Results

title comp. uptake displayed overshoot phenomenon; did not demonstrate saturation; uptake of title comp. inhibited in presence of AA, Dlactate, pyruvate but not by L-lactate, BTD, CHC, BHB; potassium/bicarbonate had no effect on uptake; diagram

Reference

Wang, Qi; Darling, Inger M.; Morris, Marilyn E.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 2 p. 751 - 761 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transport

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat kidney cortex BLM vesicles

Concentration (Pharmacological Data)

<= 50 mmol/l

Kind of Dosing (Pharmacological Data)

<3H>-labeled title comp. used

Method (Pharmacological Data)

vesicles added to uptake medium (with sodium/potassium/bicarbonate gradient) containing <3H>title comp. in 1:10 dilution; stopped; presoaked overnight in buffer containing unlabeled title comp.; radioactivity counted by liquid scintillation spectroscopy

Further Details (Pharmacological Data)

ref.: L-lactate; BLM: basolateral membrane

Results

title comp. uptake observed; sodium/potassium/bicarbonate did not enhance uptake of title comp.; diagram

Reference

Wang, Qi; Darling, Inger M.; Morris, Marilyn E.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 2 p. 751 - 761 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transport

Species or TestSystem (Pharmacological Data)

MDA-MB231 cells expressing rat MCT1 gene


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Concentration (Pharmacological Data)

0.1 - 30 mmol/l

Kind of Dosing (Pharmacological Data)

<3H>title comp. used

Method (Pharmacological Data)

cells were added with uptake buffer (varying pH: 5.5-8.0); <3H>title comp. added; incubated at 0.5-60 min; stopped; radioactivity determined by liquid scintillation spectroscopy

Further Details (Pharmacological Data)

control: mock cells; ref.: L-lactate; further study with tetraethylammonium, D-lactate, α-cyano-4-hydroxycinnamate, phloretin, probenecid and salicylic acid; MCT: monocarboxylate transporter

Results

title comp. uptake in cells exhibited passive diffusion with no saturation observed at higher concentrations; Km: 4.6 mmol/l; uptake was signif. inhibited by D-lactate, α-CHC, phloretin, probenecid, salicylic acid but not tetraethylammonium; diagram

Reference

Wang, Qi; Darling, Inger M.; Morris, Marilyn E.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 2 p. 751 - 761 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transport

Species or TestSystem (Pharmacological Data)

MDA-MB231 cells expressing rat MCT1 gene

Concentration (Pharmacological Data)

0.1 - 30 mmol/l

Kind of Dosing (Pharmacological Data)

<3H>title comp. used

Method (Pharmacological Data)

cells were added with uptake buffer (sodium gradient); <3H>title comp. added; incubated at 0.5-60 min; stopped; radioactivity determined by liquid scintillation spectroscopy

Further Details (Pharmacological Data)

control: mock cells; MCT: monocarboxylate transporter

Results

title comp. uptake observed; sodium gradient did not enhance uptake of title comp.; diagram

Reference

Wang, Qi; Darling, Inger M.; Morris, Marilyn E.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 2 p. 751 - 761 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

patient with ARG; effect on

Species or TestSystem (Pharmacological Data)

human

Method (Pharmacological Data)

Example 56A patient with ARG was treated with the Class IV agent Zolpidem 10 mg, The Class III agent alprazolam 2 mg, the Class V agent gabapentin 200 mg, and the Class II agent sodium salt of gamma-hydroxyl butyrate 5.25 grams prior to sleep. The patient was treated chronically on a nightly basis. Sometimes, according to the patient's judgement, 3.75 grams of the sodium salt of gamma-hydroxyl butyric acid was consumed upon awakening, which usually was about six hours after the first dose of medications. The second dose of GHB usually did not induce sleep. The patient experienced markedly more restful sleep, markedly decreased fatigue, and increased motivation on this regimen.; Example 63In another example a patient with ARG was given the Class I agent 660 ml red wine 13.5percent alcohol by volume, the Class III agent alprazolam 3 mg, the Class V agent gabapentin 300 mg, and the Class IV agent 10 mg Zolpidem. Five hours later, the patient was awoken and given the Class II agent the sodium salt of gamma- hydroxyl butyric acid 3 grams. The patient slept an additional three hours and had dramatic decrease in fatigue.

Results

The patient experienced markedly more restful sleep, markedly decreased fatigue, and increased motivation on this regimen; The patient slept an additional three hours and had dramatic decrease in fatigue

Location

Page/Page column 80; 84

Reference

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

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Effect (Pharmacological Data)

hypertensive


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Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intravenous

Concentration (Pharmacological Data)

180 - 1000 mg/kg

Method (Pharmacological Data)

conscious rats with implanted radio telemetry probe; injection of title comp.; MAP and heart rate were continuously monitored

Further Details (Pharmacological Data)

MAP: mean arterial pressure; further studies using GABAb receptor antagonist CGP 35348 or antagonist of receptors for title comp. NCS382; saline control

Results

title comp. dose-dependently increased MAP and heart rate; hypertension and tachycardia elicited by title comp. GABAb receptor activation; increase in heart rate at large title comp. doses via title comp. receptors

Reference

Hicks, Alissa R.; Kapusta, Daniel R.; Varner, Kurt J.

Journal of Cardiovascular Pharmacology, 2004 , vol. 44, # 6 p. 631 - 638 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

sympathomimetic

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intravenous

Concentration (Pharmacological Data)

560 mg/kg

Method (Pharmacological Data)

conscious rats with implanted bipolar electrodes placed on branch of renal sympathetic nerve; injection of title comp.; renal sympathetic nerve activity (RSNA) was recorded

Further Details (Pharmacological Data)

MAP: mean arterial pressure; further studies using GABAb receptor antagonist CGP 35348; saline control

Results

title comp. increased RSNA via GABAb receptors (figure)

Reference

Hicks, Alissa R.; Kapusta, Daniel R.; Varner, Kurt J.

Journal of Cardiovascular Pharmacology, 2004 , vol. 44, # 6 p. 631 - 638 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

ion current; effect on

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat hippocampal neurons

Sex

male

Concentration (Pharmacological Data)

0.1 - 10 mmol/l

Method (Pharmacological Data)

CA1 hippocampal pyramidal neurons continuously superfused with gassed artificial cerebrospinal fluid (aCSF) at 31 deg C, title comp. added to aCSF; GIRK currents and hyperpolarization-activated H-current (Ih) recorded with voltage clamp

Further Details (Pharmacological Data)

reference γ-aminobutyric acid (GABA)A receptor agonist baclofen; role of GABAA, γ-hydroxybutyrate (GHB) receptor and G protein-coupled inwardly rectifying K(+) (GIRK) conductance examined using selective antagonists and Ba(2+), resp.

Results

at 0.1-1 mmol/l title comp. did not affect postsynaptic properties; at 10 mmol/l inwardly rectifying K(+) current induced with concomitant decrease of Ih (graph, diagram); title comp. activate only GABAA and not GHB receptors to augment GIRK current

Reference

Schweitzer, Paul; Roberto, Marisa; Madamba, Samuel G.; Siggins, George Robert


Journal of Pharmacology and Experimental Therapeutics, 2004 , vol. 311, # 1 p. 172 - 179 Title/Abstract Full Text View citing articles Show Details

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Effect (Pharmacological Data)

ethanol withdrawal; effect on

Species or TestSystem (Pharmacological Data)

rat cerebellar neurons

Concentration (Pharmacological Data)

0.01 - 100 mmol/l

Kind of Dosing (Pharmacological Data)

dissolved in medium

Method (Pharmacological Data)

neurons enriched in granule cells from cerebella of 8-day-old rats exposed to EtOH for 5 days in basal EM, then medium replaced with EtOH-free, title comp.-containing EM for 3 h; mRNA of GABAA receptor subunits measured by RNase protection assay

Further Details (Pharmacological Data)

EM: Eagle's medium; examined GABAA receptor subunits: α1, α6, γ2L and γ2S, α4

Results

title comp. conc.-dependently reduced, at 100 mmol/l completely prevented the EtOH withdrawal induced increase of α4 expression; changes of α1 and γ2 subunit expression unaffected (diagram)

Reference

Follesa, Paolo; Mancuso, Luisa; Biggio, Francesca; Mostallino, Maria Cristina; Manca, Annalisa; Mascia, Maria Paola; Busonero, Fabio; Talani, Giuseppe; Sanna, Enrico; Biggio, Giovanni

Molecular Pharmacology, 2003 , vol. 63, # 4 p. 896 - 907 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

ethanol withdrawal; effect on

Species or TestSystem (Pharmacological Data)

rat cerebellar neurons

Concentration (Pharmacological Data)

0.01 - 100 mmol/l

Kind of Dosing (Pharmacological Data)

dissolved in medium

Method (Pharmacological Data)

neurons enriched in granule cells from cerebella of 8-day-old rats exposed to EtOH for 5 days in basal EM, then medium replaced with EtOH-free, title comp.-containing EM for 6 h; cellular metabolic activity measured with the resazurin (TOX-8) system

Further Details (Pharmacological Data)

EM: Eagle's medium

Results

title comp. conc.-dependently reduced, at 100 mmol/l completely prevented EtOH withdrawal induced impairment of cellular metabolism (diagram)

Reference

Follesa, Paolo; Mancuso, Luisa; Biggio, Francesca; Mostallino, Maria Cristina; Manca, Annalisa; Mascia, Maria Paola; Busonero, Fabio; Talani, Giuseppe; Sanna, Enrico; Biggio, Giovanni

Molecular Pharmacology, 2003 , vol. 63, # 4 p. 896 - 907 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor regulation

Species or TestSystem (Pharmacological Data)

human GABAA receptor α1β2γ2L subunit expressing XLO

Concentration (Pharmacological Data)

0.01 - 100 mmol/l

Kind of Dosing (Pharmacological Data)

dissolved in H2O, diluted in modified Barth's solution

Method

oocytes exposed to title comp. +/- 1 μmol/l diazepam (D) for 1 min, then 6-10 μmol/l GABA added for 30 s; GABA-induced Cl(-) currents


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(Pharmacological Data)

recorded by whole-cell patch-clamp

Further Details (Pharmacological Data)

XLO: Xenopus laevis oocyte; GABA: γ-aminobutyric acid; effect on GABA-induced current and enhancement of GABA-induced currents by D studied

Comment (Pharmacological Data)

No effect

Reference

Follesa, Paolo; Mancuso, Luisa; Biggio, Francesca; Mostallino, Maria Cristina; Manca, Annalisa; Mascia, Maria Paola; Busonero, Fabio; Talani, Giuseppe; Sanna, Enrico; Biggio, Giovanni

Molecular Pharmacology, 2003 , vol. 63, # 4 p. 896 - 907 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transport

Endpoint of Effect (Pharmacological Data)

inhibition of 14C-lactic acid permeability

Species or TestSystem (Pharmacological Data)

Caco-2 cells

Concentration (Pharmacological Data)

10 mmol/l

Kind of Dosing (Pharmacological Data)

title comp. and 14C-lactic acid (1 μM) were dissolved in Hank's balanced salt soln.; NaHCO3: 25 mM, on the basolateral side

Method (Pharmacological Data)

14C-lactic acid was applied to the apical side of cell monolayer in presence of title comp. for 60 min at 37 deg C, apical pH 7.4; basolateral pH 7.4 with adding NaHCO3; permeability was estimated by measuring of radioactivity on the basolateral side

Further Details (Pharmacological Data)

effect of title comp. on 14C-lactic acid permeation through the cell monolayer

Results

moderate inhibtion of 14C-lactic acid permeability: to 72.8 percent of the control value

Reference

Ogihara, Takuo; Tamai, Ikumi; Tsuji, Akira

Journal of Pharmaceutical Sciences, 1999 , vol. 88, # 11 p. 1217 - 1221 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

human

Sex

male and female

Route of Application

peroral

Concentration (Pharmacological Data)

12.5 - 25 mg/kg

Kind of Dosing (Pharmacological Data)

given with syrup in a solution of 10 ml volume

Method (Pharmacological Data)

title comp. given to 12 healthy volunteers (aged 22 - 36 years) in crossover study; psychomotor performance measured using the tests CFF, CTT, RCT, CRT and VVT up to 180 min

Further Details (Pharmacological Data)

CFF: critical flicker fusion; CTT: critical tracking task; RCT: response competition test; CRT: choice reaction time; VVT: visual vigilance task; placebo control

Comment (Pharmacological Data)

No effect

Reference

Ferrara; Giorgetti; Zancaner; Orlando; Tagliabracci; Cavarzeran; Palatini

European Journal of Clinical Pharmacology, 1999 , vol. 54, # 11 p. 821 - 827 Title/Abstract Full Text View citing articles Show Details


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Effect (Pharmacological Data)

tranquilizing

Species or TestSystem (Pharmacological Data)

human

Sex

male and female

Route of Application

peroral

Concentration (Pharmacological Data)

12.5 - 25 mg/kg

Kind of Dosing (Pharmacological Data)

given with syrup in a solution of 10 ml volume

Method (Pharmacological Data)

title comp. given to 12 healthy volunteers (aged 22 - 36 years) in crossover study; mood (alertness, calmness, contentedness) assessed using visual analogue scales before and 120 min after title comp.

Further Details (Pharmacological Data)

placebo control

Results

title comp. increased calmness at 12.5 mg/kg and decreased contentedness at 12.5 and 25 mg/kg

Reference

Ferrara; Giorgetti; Zancaner; Orlando; Tagliabracci; Cavarzeran; Palatini

European Journal of Clinical Pharmacology, 1999 , vol. 54, # 11 p. 821 - 827 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

toxicity

Species or TestSystem (Pharmacological Data)

human

Sex

male and female

Route of Application

peroral

Concentration (Pharmacological Data)

12.5 - 25 mg/kg

Kind of Dosing (Pharmacological Data)

given with syrup in a solution of 10 ml volume

Method (Pharmacological Data)

title comp. given to 12 healthy volunteers (aged 22 - 36 years) in crossover study; side-effects recorded for 120 min

Further Details (Pharmacological Data)

placebo control

Results

title comp. at 12.5 and 25 mg/kg caused within 20 min subjective symptoms of dizziness or a sense of dullness in 50 and 66 percent, resp., disappearing within 30 - 60 min

Reference

Ferrara; Giorgetti; Zancaner; Orlando; Tagliabracci; Cavarzeran; Palatini

European Journal of Clinical Pharmacology, 1999 , vol. 54, # 11 p. 821 - 827 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

EEG activity

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rats

Sex

male

Route of Application

intraperitoneal

Concentration

100 mg/kg


(Pharmacological Data)

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Exposure Period (Pharmacological Data)

0 - 3 h

Method (Pharmacological Data)

adult rats (200-300 g) implanted with monopolar EEG recording electrodes (frontopatietal cortex); title compd. administering, EEG monitoring

Further Details (Pharmacological Data)

GHB - γ-hydroxybutyric acid

Results

GHB-induced bilaterally synchronous spike-wave discharges shown

Reference

Banerjee, Pradeep K.; Olsen, Richard W.; Tillakaratne, Niranjala J. K.; Brailowsky, Simon; Tobin, Allan J.; Snead III, O. Carter

Journal of Pharmacology and Experimental Therapeutics, 1998 , vol. 287, # 2 p. 766 - 772 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neuroregulatoric

Species or TestSystem (Pharmacological Data)

BKL:SD rat

Sex

male

Route of Application

intravenous

Concentration (Pharmacological Data)

12.5 - 1600 mg/kg

Method (Pharmacological Data)

microelectrode lowered into zona compacta-SN; title comp. injected, and extracellular recordings from DA neurons performed

Further Details (Pharmacological Data)

further investigation with GABAB-receptor antagonist (SCH 50911) or NCS-382 (specific antagonist of title comp. binding sites); reference comp.: baclofen (1 - 32 mg/kg); SN: substantia nigra; DA: dopamine

Results

title comp. dose-dependently decreased firing rate of nigral DA neurons, regularized firing pattern and reduced percentage of burst firing; this effect mediated by GABAB receptors

Reference

Erhardt, Sophie; Andersson, Bengt; Nissbrandt, Hans; Engberg, Goeran

Naunyn-Schmiedeberg's Archives of Pharmacology, 1998 , vol. 357, # 6 p. 611 - 619 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

inhibition of activity of NADP-malic enzyme from Bradyrhizobium japonicum A1017

Reference

Chen; Okabe; Osano; Tajima

Bioscience, Biotechnology and Biochemistry, 1997 , vol. 61, # 2 p. 384 - 386 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

releasing hormones

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rats

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

500 mg/kg

Method (Pharmacological Data)

striatal dopamine release monitored for 2 h by microdialysis in awake and urethane-anesthetized (1.5 g/kg) rats (250-300 g); dialysate analyzed by HPLC

Results

title comp. significantly inhibited striatal dopamine release in conscious animals; anesthetic pretreatment abolished inhibitory effect of title comp.; in urethane-anesthetized animals i.p. output same in basal and saline control but not in s.c. route


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Reference

Howard, Sherrel G.; Feigenbaum, Jeffery J.

Biochemical Pharmacology, 1997 , vol. 53, # 1 p. 103 - 110 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

Wistar rat cerebral cortex membranes

Sex

male

Concentration (Pharmacological Data)

Ca. 1E-06 - 0.01 mol/l

Method (Pharmacological Data)

GABAB receptor competition binding assay; membranes were incubated with unlabeled title comp. in presence of <3H>GABA and isoguvacine (GABAA agonist) in Tris-HCl buffer at pH 7.40; samples filtered and radioactivity determined

Further Details (Pharmacological Data)

non-specific binding determined in the presence 100 μmol/l R-(-)-baclofen; reference comp.: R-(-)-baclofen, selective GABAB receptor agonist; GABA: γ-aminobutyric acid

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

93 μmol/l

Results

title comp. inhibited <3H>GABA binding to GABAB receptor in dose-dependent manner with Ki = 79 μmol/l

Reference

Mathivet, Pascal; Bernasconi, Raymond; De Barry, Jean; Marescaux, Christian; Bittiger, Helmut

European Journal of Pharmacology, 1997 , vol. 321, # 1 p. 67 - 75 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

Wistar rat cerebellar membranes

Sex

male

Method (Pharmacological Data)

GABAB receptor competition binding assay; membranes were incubated with unlabeled title comp. in presence of <3H>GABA and isoguvacine (GABAA agonist) in Tris-HCl buffer at pH 7.40; samples filtered and radioactivity determined

Further Details (Pharmacological Data)

non-specific binding determined in the presence 100 μmol/l R-(-)-baclofen; reference comp.: R-(-)-baclofen, selective GABAB receptor agonist; GABA: γ-aminobutyric acid

Results

title comp. inhibited <3H>GABA binding to GABAB receptor

Reference

Mathivet, Pascal; Bernasconi, Raymond; De Barry, Jean; Marescaux, Christian; Bittiger, Helmut

European Journal of Pharmacology, 1997 , vol. 321, # 1 p. 67 - 75 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

Wistar rat hippocampal membranes

Sex

male

Method (Pharmacological Data)

GABAB receptor competition binding assay; membranes were incubated with unlabeled title comp. in presence of <3H>GABA and isoguvacine (GABAA agonist) in Tris-HCl buffer at pH 7.40; samples filtered and radioactivity determined

Further Details (Pharmacological Data)

non-specific binding determined in the presence 100 μmol/l R-(-)-baclofen; reference comp.: R-(-)-baclofen, selective GABAB receptor agonist; GABA: γ-aminobutyric acid

Results

title comp. inhibited <3H>GABA binding to GABAB receptor

Reference

Mathivet, Pascal; Bernasconi, Raymond; De Barry, Jean; Marescaux, Christian; Bittiger, Helmut


European Journal of Pharmacology, 1997 , vol. 321, # 1 p. 67 - 75 Title/Abstract Full Text View citing articles Show Details

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Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

Wistar rat cerebral cortex membranes

Sex

male

Concentration (Pharmacological Data)

Ca. 1E-06 - 0.01 mol/l

Method (Pharmacological Data)

GABAB receptor competition binding assay; membranes were incubated with unlabeled title comp. and <3H>CGP 27492 in Krebs-Henseleit buffer for 40 min at 20 deg C; samples filtered and radioactivity determined

Further Details (Pharmacological Data)

non-specific binding determined with 10 μmol/l R-(-)-baclofen; reference comp.: R-(-)-baclofen, selective GABAB receptor agonist; GABA: γ-aminobutyric acid; further investigation with title comp. dehydrogenase inhibitors valproate and ethosuximide

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

93 μmol/l

Results

title comp. inhibited <3H>CGP 27492 binding to GABAB receptor in dose-dependent manner with Ki = 80 μmol/l; title comp. was not reconverted to GABA

Reference

Mathivet, Pascal; Bernasconi, Raymond; De Barry, Jean; Marescaux, Christian; Bittiger, Helmut

European Journal of Pharmacology, 1997 , vol. 321, # 1 p. 67 - 75 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

Wistar rat cerebral cortex membranes

Sex

male

Concentration (Pharmacological Data)

Ca. 1E-06 - 0.01 mol/l

Method (Pharmacological Data)

GABAB receptor competition binding assay; membranes were incubated with unlabeled title comp. in presence of <3H>CGP 54626 in Krebs-Henseleit buffer at pH 7.40; samples filtered and radioactivity determined

Further Details (Pharmacological Data)

non-specific binding determined with 10 μmol/l unlabeled CGP 54626; reference comp.: R-(-)-baclofen, selective GABAB receptor agonist; GABA: γ-aminobutyric acid; further investigation with 5'-guanyl-imidodiphosphate (Gpp(NH)p)

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

5.5 mmol/l

Results

title comp. inhibited <3H>CGP 54626 binding to GABAB receptor in dose-dependent manner with Ki = 3.3 mmol/l; effect was modulated by guanine nucleotide binding proteins (IC50 in presence of 300 μmol/l Gpp(NH)p 38 mmol/l)

Reference

Mathivet, Pascal; Bernasconi, Raymond; De Barry, Jean; Marescaux, Christian; Bittiger, Helmut

European Journal of Pharmacology, 1997 , vol. 321, # 1 p. 67 - 75 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

Wistar rat hippocampal membranes


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Sex

male

Method (Pharmacological Data)

GABAB receptor competition binding assay; membranes were incubated with unlabeled title comp. in presence of <3H>CGP 54626 in Krebs-Henseleit buffer at pH 7.40; samples filtered and radioactivity determined

Further Details (Pharmacological Data)

non-specific binding determined with 10 μmol/l unlabeled CGP 54626; GABA: γ-aminobutyric acid; further investigation with 5'-guanylimidodiphosphate (Gpp(NH)p)

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

3.9 mmol/l

Results

title comp. inhibited <3H>CGP 54626 binding to GABAB receptor in dose-dependent manner with Ki = 2.3 mmol/l; effect was modulated by guanine nucleotide binding proteins (IC50 in presence of 300 μmol/l Gpp(NH)p 28 mmol/l)

Reference

Mathivet, Pascal; Bernasconi, Raymond; De Barry, Jean; Marescaux, Christian; Bittiger, Helmut

European Journal of Pharmacology, 1997 , vol. 321, # 1 p. 67 - 75 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

Wistar rat cerebellar membranes

Sex

male

Concentration (Pharmacological Data)

Ca. 1E-05 - 0.1 mol/l

Method (Pharmacological Data)

GABAB receptor competition binding assay; membranes were incubated with unlabeled title comp. in presence of <3H>CGP 54626 in Krebs-Henseleit buffer at pH 7.40; samples filtered and radioactivity determined

Further Details (Pharmacological Data)

non-specific binding determined with 10 μmol/l unlabeled CGP 54626; GABA: γ-aminobutyric acid; further investigation with 5'-guanylimidodiphosphate (Gpp(NH)p)

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

5.9 mmol/l

Results

title comp. inhibited <3H>CGP 54626 binding to GABAB receptor in dose-dependent manner with Ki = 3.5 mmol/l; effect was modulated by guanine nucleotide binding proteins (IC50 in presence of 300 μmol/l Gpp(NH)p 18 mmol/l)

Reference

Mathivet, Pascal; Bernasconi, Raymond; De Barry, Jean; Marescaux, Christian; Bittiger, Helmut

European Journal of Pharmacology, 1997 , vol. 321, # 1 p. 67 - 75 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

human

Sex

male

Route of Application

peroral

Concentration (Pharmacological Data)

25 mg/kg

Method (Pharmacological Data)

16 cirrhotic patients (8 without ascites and 8 with ascites), lidocain and antipyrin administered; blood samples taken and urine collected, vital signs monitored, liver metabolic function evaluated

Further Details (Pharmacological Data)

effect of moderate or severe liver dysfunction on the pharmacokinetics


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Results

apparent oral clearance reduced from 9.1 to 4.5 in nonascitic and to 4.1 ml*min-1*kg1- in ascitic patients; terminal half-life was significantly longer om nonascitic patients;Cmax increased only in nonascitic patients relative to healthy patients

Reference

Ferrara; Tedeschi; Frison; Orlando; Mazzo; Zordan; Padrini; Palatini

European Journal of Clinical Pharmacology, 1996 , vol. 50, # 4 p. 305 - 310 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

antagonist

Species or TestSystem (Pharmacological Data)

rat hippocampus

Sex

male

Concentration (Pharmacological Data)

2.5 μmol/l

Method (Pharmacological Data)

effect of title comp. on 2 μmol/l C-, L-, or O-induced electically evoked population spike amplitude of pyramidal cell (PSA) measured by conventional electrophysiological methods on brain slices superfused with chilled artificial cerebrospinal fluid

Further Details (Pharmacological Data)

C=ciprofloxacin; L=lomefloxacin; O=ofloxacin

Results

prevented increases in PSA induced by C, L or O

Reference

Dimpfel; Dalhoff; Von Keutz

Antimicrobial Agents and Chemotherapy, 1996 , vol. 40, # 11 p. 2573 - 2576 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

brain tissue from Sprague-Dawley rat

Sex

male

Concentration (Pharmacological Data)

5 mmol/l

Kind of Dosing (Pharmacological Data)

title comp. used as ammonium salt

Method (Pharmacological Data)

in vitro; brain tissue was isol. from rats; tissue sections thawed at 20 degC for 1 h, preincub. in 100 mmol/l phosphate buffer (pH 6.0) for 30 min and dried, then incub. in the same buffer with 25 nmol/l 3H-label. title comp. for 30 min (all at 4 degC)

Further Details (Pharmacological Data)

binding of title comp. to GABAB in rat brain; non-specific binding was determined by autoradiography in the presence of 5 mmol/l Na(+)free title comp. and 25 nmol/l 3H-labeled title comp. (spec. act. 44.5 Ci/mmol)

Results

high density of binding in the CA1 region of hippocampus, septum, and superficial (I-III) laminae of frontal, parietal, and temporal cortex; colocalization with GABAB binding only in laminae of cortex and in ventrobasal thalamus, (figure)

Reference

Snead III, O. Carter

Biochemical Pharmacology, 1996 , vol. 52, # 8 p. 1235 - 1243 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor blocking agent

Species or TestSystem (Pharmacological Data)

brain tissue from Sprague-Dawley rat

Sex

male

Concentration (Pharmacological Data)

250 - 1000 μmol/l

Method (Pharmacological

in vitro; brain tissue was isolat. from rats; tissue sections were preincub. in Tris-HCl (pH 7.4) contain. 190 mmol/l sucrose and 2.5 mmol/l CaCl2 for 40 min at 20 degC and dried, then incub. in buffer contain. 50 nmol/l <3H>GABA for 20 min at 4 degC


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Further Details (Pharmacological Data)

effect of title comp. on <3H>GABAB binding in rat brain; mixture contain. 100 μmol/l isoguvacin; binding was determined by autoradiography

Comment (Pharmacological Data)

No effect

Reference

Snead III, O. Carter

Biochemical Pharmacology, 1996 , vol. 52, # 8 p. 1235 - 1243 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

GABA release

Species or TestSystem (Pharmacological Data)

Sprague Dawley rats

Sex

male

Concentration (Pharmacological Data)

250 - 1500 μmol/l

Method (Pharmacological Data)

rats (200-300 g) anesthetized, EEG recording electrodes implanted (frontoparietal cortex), cannulated (ventrobasal nucleus of thalamus); 7 days postsurgery, title compd. perfusion, perfusate anal. (HPLC, electrochem. detection)

Further Details (Pharmacological Data)

GABA - γ-aminobutyric acid; dialysis protocol: 2 h stabilization, dialysate sampling from 3 h (every 15 min), title compd. perfusion (2 μl/min) 60 min at 4th hour of dialysis

Results

dose- and time-dependent decrease of basal extracellular levels of GABA evaluated (diagram); no significant effect 2.5-3 h after perfusion

Reference

Banerjee; Snead III

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 273, # 3 p. 1534 - 1543 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

K(1+)-evoked GABA release

Species or TestSystem (Pharmacological Data)

Sprague Dawley rats

Sex

male

Concentration (Pharmacological Data)

250 - 1500 μmol/l

Method (Pharmacological Data)

rats (200-300 g) anesthetized, EEG recording electrodes implanted (frontoparietal cortex), cannulated (ventrobasal nucleus of thalamus); 7 days postsurgery, title compd. and KCl perfusion, perfusate anal. (HPLC, electrochem. detection)

Further Details (Pharmacological Data)

GABA - γ-aminobutyric acid; dialysis protocol: 2 h stabilization, dialysate sampling from 3 h (every 15 min), title compd. perfusion (2 μl/min) 60 min, KCl (30 mM) last 20 min at 4th hour period of dialysis

Results

significant dose-dependent decrease of basal extracellular levels of GABA evaluated (table); title compd.-induced spike-wave discharges (EEG recordings) given (diagram)

Reference

Banerjee; Snead III

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 273, # 3 p. 1534 - 1543 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

K(1+)-evoked glutamate release

Species or TestSystem (Pharmacological Data)

Sprague Dawley rats

Sex

male

Concentration (Pharmacological Data)

250 - 1500 μmol/l


75 of 79

76 of 79

77 of 79

Method (Pharmacological Data)

rats (200-300 g) anesthetized, EEG recording electrodes implanted (frontoparietal cortex), cannulated (ventrobasal nucleus of thalamus); 7 days postsurgery, title compd. and KCl perfusion, perfusate anal. (HPLC, electrochem. detection)

Further Details (Pharmacological Data)

dialysis protocol: 2 h stabilization, dialysate sampling from 3 h (every 15 min), title compd. perfusion (2 μl/min) 60 min starting, KCl (30 mM) last 20 min at 4th hour period of dialysis

Results

significant dose-dependent decrease of basal extracellular levels of glutamate evaluated (table); title compd.-induced spike-wave discharges (EEG recordings) given (diagram)

Reference

Banerjee; Snead III

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 273, # 3 p. 1534 - 1543 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

Accumulation

Species or TestSystem (Pharmacological Data)

rat glial cells

Concentration (Pharmacological Data)

20 mmol/l

Kind of Dosing (Pharmacological Data)

sodium salt

Method (Pharmacological Data)

in vitro; primary cultures established from newborn rat hemispheres; cultured in DMEM for 48 h and then incubated with <3H>labeled taurine in Krebs-Ringer phosphate buffer for 10 min; pH 7.4; 37 deg C; title comp. added to culture or incubation medium

Further Details (Pharmacological Data)

taurine uptake determined in primary and secondary cultures

Results

increased taurine uptake to 112 percent of control when added to culture medium or to incubation medium

Reference

Petegnief, Valerie; Lleu, Pierre-Louis; Gupta, Ramesh C.; Bourguignon, Jean-Jacques; Rebel, Gerard

Biochemical Pharmacology, 1995 , vol. 49, # 3 p. 399 - 410 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

drug dependence

Species or TestSystem (Pharmacological Data)

Wistar rats

Sex

male

Route of Application

peroral

Concentration (Pharmacological Data)

1 percent w/v

Method (Pharmacological Data)

rats (4 months old, 400-500 g) were forced to drink 1 percent aqueous solution of the title compound for 14 consecutive days; then for 20 consecutive weeks rats were given free choice of title compound solution and tap water

Further Details (Pharmacological Data)

the criterion of preference of title compound defined as a daily intake of title compound solution greater than 50 percent of total fluid intake

Results

virtually equal number of title compound preference days (10.15) and water preference days (9.85) recorded, however large individual variability observed (data in figures)

Reference

Colombo; Agabio; Balaklievskaia; Diaz; Lobina; Reali; Gessa

European Journal of Pharmacology, 1995 , vol. 285, # 1 p. 103 - 107 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

determination of plasmalevel after bolusinjection of 50 mg/kg, followed by infusion of 15 mg/kg*h

Reference

Thomas; Schontube

Pharmazie, 1993 , vol. 48, # 8 p. 623 - 624 Title/Abstract Full Text View citing articles Show Details


78 of 79

79 of 79

Comment (Pharmacological Data)

percent inhibition at 10 mkM of binding to GHB receptor in crude membranes from rat brain = 55, at 1 mkM = 35; IC50 = 6.6 mkM

Reference

Bourguignon; Schoenfelder; Schmitt; Wermuth; Hechler; Charlier; Maitre

Journal of Medicinal Chemistry, 1988 , vol. 31, # 5 p. 893 - 897 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

competitve inhibition of the activity of 3-guanidinopropionate amidinohydrolase from Pseudomonas aeruginosa PAO 1, Ki = 6.9 mM; weak inhibition of the activity of 4-guanidinobutyrate amidinohydrolase from Pseudomonas sp. ATCC 14676 at 5.0 mM

Reference

Yorifuji, Takamitsu; Sugai, Ichiro; Matsumoto, Hideki; Tabuchi, Akira

Agricultural and Biological Chemistry, 1982 , vol. 46, # 5 p. 1361 - 1368 Title/Abstract Full Text Show Details

Ecotoxicology (4) 1 of 4

2 of 4

3 of 4

Effect (Ecotoxicology)

behavioral symtoms

Species or TestSystem (Ecotoxicology)

Drosophila melanogaster, fruitfly

Sex

male

Concentration (Ecotoxicology)

10 - 40 nmol

Kind of Dosing (Ecotoxicology)

title comp. dissolved in Ringer solution (pH 7.6-7.8), 0.2 μl injected per fly

Method (Ecotoxicology)

wild-type Canton-S or cheapdate mutant 5 to 7-day-old flies anaesthetized by CO2; injected with title comp. intra-abdominally; periods of locomotor activity (movements/min) and immobility counted during 30 min using Drosophila activity monitoring System

Further Details (Ecotoxicology)

cheapdate mutant: ethanol-sensitive; reference comp.: ethanol; control: vehicle; further investigation with GABAB receptor antagonist CGP54626, GABAB RNA interference, γ-hydroxybutyric acid receptor antagonist NCS-382; GABA: γ-aminobutyric acid

Results

title comp. prolonged immobility immediately after injection (not significant); locomotor activity was lower vs. ethanol and interrupted by periods of immobility; cheapdate flies were more sensitive; presence and activation of GABAB receptor required

Reference

Dimitrijevic, Nikola; Dzitoyeva, Svetlana; Satta, Rosalba; Imbesi, Marta; Yildiz, Sevim; Manev, Hari

European Journal of Pharmacology, 2005 , vol. 519, # 3 p. 246 - 252 Title/Abstract Full Text View citing articles Show Details

Effect (Ecotoxicology)

behavioral symtoms

Species or TestSystem (Ecotoxicology)

Drosophila melanogaster, fruitfly wild type Canton-S

Sex

male

Concentration (Ecotoxicology)

40 nmol

Kind of Dosing (Ecotoxicology)

title comp. dissolved in Ringer solution (pH 7.6-7.8), 0.2 μl injected per fly

Method (Ecotoxicology)

5 to 7-day-old flies were injected with title comp. intra-abdominally; 4 h later ethanol injected (200 nmol); periods of locomotor activity (movements/min) and immobility counted during 30 min using Drosophila activity monitoring System for 30 minutes

Further Details (Ecotoxicology)

further investigation: the order of injections was changed vice versa; effects of repeated administration of title comp. also analysed

Results

pretreatment with ethanol attenuated the behavioural effects of title comp.; pretreatment with the title comp. did not alter the response to ethanol injection; repeated administration of title comp. reduced title comp. effects (figures)

Reference

Dimitrijevic, Nikola; Dzitoyeva, Svetlana; Satta, Rosalba; Imbesi, Marta; Yildiz, Sevim; Manev, Hari

European Journal of Pharmacology, 2005 , vol. 519, # 3 p. 246 - 252 Title/Abstract Full Text View citing articles Show Details

Effect (Ecotoxicology)

biotransformation

Species or TestSystem (Ecotoxicology)

Drosophila melanogaster, fruitfly

Sex

male

Concentration (Ecotoxicology)

40 nmol

Kind of Dosing

title comp. dissolved in Ringer solution (pH 7.6-7.8), 0.2 μl injected per fly


(Ecotoxicology)

4 of 4

Method (Ecotoxicology)

wild-type Canton-S or cheapdate mutant 5 to 7-day-old flies anaesthetized by CO2; injected with title comp. intra-abdominally; 15-240 min later homogenized; title comp. elimination rate measured using GC/MS assay

Further Details (Ecotoxicology)

GC/MS assay: gas chromatography/mass spectrometry; effects of elimination of title comp. after repeated administration 4 h apart tested on wild-type flies

Results

title comp. conc. decreased time-dependently (figure); no difference in title comp. elimination in mutant and wild-type strains of flies observed; the previous exposure to the title comp. did not alter title comp. elimination

Reference

Dimitrijevic, Nikola; Dzitoyeva, Svetlana; Satta, Rosalba; Imbesi, Marta; Yildiz, Sevim; Manev, Hari

European Journal of Pharmacology, 2005 , vol. 519, # 3 p. 246 - 252 Title/Abstract Full Text View citing articles Show Details

Effect (Ecotoxicology)

bacteria; examination of

Endpoint of Effect (Ecotoxicology)

CFU

Species or TestSystem (Ecotoxicology)

soil microcosm

Method (Ecotoxicology)

substrate utilization assay using Biolog(TM) EcoPlates; soil suspension (150 μl) containing 1E4 CFU was added to wells and incub. at 28 deg C in the presence of title comp. as carbon sourse; CFU measured at 590 nm ca. every 12 h for 140 h

Further Details (Ecotoxicology)

colony-forming unit (CFU); 3 soil samples were collected on May 1997 from an operational sewage farm in Nottinghamshire where sludge was injected into the soil from 1975 year and 2 soil sample - nearby grassland sites where no sludge was applied

Results

slow growth not reaching OD 2.5 before 40 h in all soil samples tested

Reference

Lawlor, Kirsten; Knight, Bruce P.; Barbosa-Jefferson, Vera L.; Lane, Peter W.; Lilley, Andrew K.; Paton, Graeme I.; McGrath, Steve P.; O'Flaherty, Sile M.; Hirsch, Penny R.

FEMS Microbiology Ecology, 2000 , vol. 33, # 2 p. 129 - 137 Title/Abstract Full Text View citing articles Show Details

Other Data Concentration in the Environment (2) 1 of 2

2 of 2

Media (Concentration in the Environment)

air

Location

Great Smoky Mountain National Park, Tennessee, USA

Contamination Concentration

0 - 364.7 pg/l

Method, Remarks (Concentration in the Environment)

in fine organic aerosol; nighttime samples collected from July 15 to August 25, 1995; rural area; sampling time: 10-12 h; water extraction; GC-MS analysis

Reference

Yu, Liya E.; Shulman, Michelle L.; Kopperud, Royal; Hildemann, Lynn M.

Environmental Science and Technology, 2005 , vol. 39, # 3 p. 707 - 715 Title/Abstract Full Text View citing articles Show Details

Media (Concentration in the Environment)

air

Location

Great Smoky Mountain National Park, Tennessee, USA

Contamination Concentration

0 - 178.4 pg/l

Method, Remarks (Concentration in the Environment)

in fine organic aerosol; daytime samples collected from July 15 to August 25, 1995; rural area; sampling time: 10-12 h; diurnal trend of title comp. conc. presented (histogram); water extraction; GC-MS analysis

Reference

Yu, Liya E.; Shulman, Michelle L.; Kopperud, Royal; Hildemann, Lynn M.

Environmental Science and Technology, 2005 , vol. 39, # 3 p. 707 - 715 Title/Abstract Full Text View citing articles Show Details

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Reference

Alzheimer's disease

Page/Page column title page; 70-74

YALE UNIVERSITY; DIXIT, Vishwa, Deep

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Familial Cold Autoinflammatory syndrome

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YALE UNIVERSITY; DIXIT, Vishwa, Deep


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LRP3 inflammasome inhibitor

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LRP3 inflammasome-related disease or disorder

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Macular degeneration

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Muckle-Wells Syndrome

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Pharmaceuticals

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YALE UNIVERSITY; DIXIT, Vishwa, Deep

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acute lung injury

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YALE UNIVERSITY; DIXIT, Vishwa, Deep

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age-related bone loss

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age-related functional decline

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arthritis

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atherosclerosis

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diabetic nephropathy

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glomerulonephritis

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multiple sclerosis

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type-2 diabetes

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YALE UNIVERSITY; DIXIT, Vishwa, Deep

Patent: WO2016/123229 A1, 2016 ;

Page/Page column 8-9

Massachusetts Institute of Technology

Patent: US2007/36855 A1, 2007 ;

Monomer for polymeric formulation for delivery of agents

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

binding gamma-aminobutyric acid (GABA) receptor or augmenting the actions of GABA and its cogeners

Sleeping disorders

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Insomnia

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Drug abuse

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Alcohol and opiate withdrawal

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Reduced level of growth hormone

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Anxiety

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Analgesia

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Acquired resistance to GABAnergic agents(ARG)

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Effects in certain neurological disorders

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ;


Title/Abstract Full Text Show Details

Parkinson's disease

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Depression

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Obesity

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Certain endocrine disturbances

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Tissue protection following hypoxia/anoxia such as in stroke or myocardial infarction

Increased level of intracranial pressure

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Hyperactivity

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Attention deficit hyperactivity disorder

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Decreased concentration

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Mania

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Hypomania

JOHNSON, Joseph

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Bipolar disorder

JOHNSON, Joseph

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Cyclothymia

JOHNSON, Joseph

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Sleepiness during waking hours

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Narcolepsy major

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details


Narcolepsy minor

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Restless legs syndrome

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Periodic limb movement disorder

JOHNSON, Joseph

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Subclinical restless legs syndrome

JOHNSON, Joseph

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Subclinical periodic limb movement disorder

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Obstructive sleep apnea

JOHNSON, Joseph

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Symptoms associated with acquired resistance to GABAminergic agents

JOHNSON, Joseph

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Fatigue(the feeling of tiredness)

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Unrestful sleep

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Difficulty dealing with stress

JOHNSON, Joseph

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Arthralgias (joint pain)

JOHNSON, Joseph

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Myalgias (muscle aching)

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Tense muscles

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Difficulty concentrating(brain fog)

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Impaired memory

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Sleepiness

JOHNSON, Joseph


Patent: WO2006/124609 A2, 2006 ;

Title/Abstract Full Text Show Details

Tender trigger points

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Periodic limb movement disorder of sleep

JOHNSON, Joseph

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Interstitial cystitis

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Irritable bowel syndrome

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Rheumatoid arthritis

JOHNSON, Joseph

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Lupus erythematosus

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Multiple sclerosis

JOHNSON, Joseph

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Treating ARG or related conditions

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

illicit/illegal drug

BAYLOR COLLEGE OF MEDICINE

Patent: US2006/18921 A1, 2006 ; Title/Abstract Full Text Show Details

angiogenic material

Wright, Emma Jayne; Huckle, James William; Ali, Saad Aboul Majeed

Patent: US2004/265282 A1, 2004 ; Title/Abstract Full Text Show Details

fixation devices for tissue repair

Wright, Emma Jayne; Huckle, James William; Ali, Saad Aboul Majeed

Patent: US2004/265282 A1, 2004 ; Title/Abstract Full Text Show Details

Reaxys Registry Number: 10424053

Type of Substance: acyclic Molecular Formula: C4H8O3

Linear Structure Formula: C3(13)CH8O3

Molecular Weight: 105.095

InChI Key: SJZRECIVHVDYJC-VQEHIDDOSA-N

2

1 prep out of 2 reactions.

1


Synthesize Find similar Reaxys Registry Number: 10424054

Type of Substance: acyclic Molecular Formula: C4H8O3

Linear Structure Formula: C3(13)CH8O3

1 prep out of 2 reactions.

1

Reaxys Registry Number: 10424055

Type of Substance: acyclic Molecular Formula: C4H8O3

Linear Structure Formula: C3(13)CH8O3

1 prep out of 2 reactions.

1

Reaxys Registry Number: 10424056

Type of Substance: acyclic Molecular Formula: C4H8O3

Linear Structure Formula: C3(13)CH8O3

1 prep out of 2 reactions.

1

Reaxys Registry Number: 9844738

Type of Substance: acyclic Molecular Formula: C4H8O3

Linear Structure Formula: C4H7DO3

Molecular Weight: 105.098

InChI Key: SJZRECIVHVDYJC-YUYPMLDFSA-N

1 prep out of 2 reactions.

1

Molecular Weight: 105.095

InChI Key: SJZRECIVHVDYJC-OUBTZVSYSA-N

3

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Molecular Weight: 105.095

InChI Key: SJZRECIVHVDYJC-AZXPZELESA-N

4

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Molecular Weight: 105.095

InChI Key: SJZRECIVHVDYJC-LBPDFUHNSA-N

5

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6

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7

Reaxys Registry Number: 9844739

Type of Substance: acyclic Molecular Formula: C4H8O3

Linear Structure Formula: C4H7DO3

Molecular Weight: 105.098

InChI Key: SJZRECIVHVDYJC-KLFDDBSISA-N

1 prep out of 2 reactions.

1

Reaxys Registry Number: 11163279

Molecular Formula: C4H8O3

Linear Structure Formula: C4H6O3(2)H2

1 prep out of 2 reactions.

Identification

2

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Molecular Weight: 106.09

InChI Key: SJZRECIVHVDYJC-DICFDUPASA-N

8

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Identification Patent-Specific Data (1) Prophetic Compound

Location in Patent

Reference

prophetic product

Paragraph 68

CONCERT PHARMACEUTICALS, INC.; TUNG, Roger D.; SILVERMAN, I. Robert

Patent: WO2014/31840 A1, 2014 ; Title/Abstract Full Text Show Details

Reaxys Registry Number: 10426836

Type of Substance: acyclic Molecular Formula: C4H8O3

Linear Structure Formula: (13)C4H8O3

1 prep out of 2 reactions.

1

Chemical Name: Lithium γ-hydroxybutyrate

1 prep out of 3 reactions.

Identification Physical Data (1) Bioactivity (4) Other Data (2)

6

Molecular Weight: 108.062

InChI Key: SJZRECIVHVDYJC-JCDJMFQYSA-N

9

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Reaxys Registry Number: 5635275

CAS Registry Number: 63255-29-8 Type of Substance: acyclic


Molecular Formula: C4H7O3*Li Linear Structure Formula: C4H7O3(1-)*Li(1+)

Molecular Weight: 110.039

InChI Key: HQXIDRLGWYBFQL-UHFFFAOYSA-M

10

Synthesize | Hide Details Find similar Chemical Names and Synonyms Lithium γ-hydroxybutyrate, 4-hydroxybutanoyloxylithium, lithium hydroxybutyrate, lithium 4-hydroxybutanoate, lithium 4-hydroxybutyrate Identification Substance Label (1) Label

Reference

I

Lyubimov, B. I.; Yavorskii, A. N.

Pharmaceutical Chemistry Journal, 1983 , vol. 17, # 5 p. 378 - 380 Khimiko-Farmatsevticheskii Zhurnal, 1983 , vol. 17, # 5 p. 629 - 631 Title/Abstract Full Text View citing articles Show Details

Physical Data Crystal Property Description (1)

Colour & Other Properties

Reference Long, Daniel D.; Church, Timothy J.; Jacobsen, John R.; Jiang, Lan; Saito, Daisuke Roland; Stergiades, Ioanna; Van Dyke, Priscilla M.; Dalziel, Sean; Preza, Leticia Maria

Patent: US2007/219278 A1, 2007 ;

white

Title/Abstract Full Text Show Details

Bioactivity Pharmacological Data (4) 1 of 4

Comment (Pharmacological Data)

Bioactivities present

Reference

Wright, Emma Jayne; Huckle, James William; Ali, Saad Aboul Majeed

Patent: US2004/265282 A1, 2004 ; Title/Abstract Full Text Show Details

Long, Daniel D.; Church, Timothy J.; Jacobsen, John R.; Jiang, Lan; Saito, Daisuke Roland; Stergiades, Ioanna; Van Dyke, Priscilla M.; Dalziel, Sean; Preza, Leticia Maria

Patent: US2007/219278 A1, 2007 ; Title/Abstract Full Text Show Details

Lyubimov, B. I.; Yavorskii, A. N.

Pharmaceutical Chemistry Journal, 1983 , vol. 17, # 5 p. 378 - 380 Khimiko-Farmatsevticheskii Zhurnal, 1983 , vol. 17, # 5 p. 629 - 631 Title/Abstract Full Text View citing articles Show Details

Saratikov; Zamoshchina

Arzneimittel-Forschung/Drug Research, 1986 , vol. 36, # 10 p. 1448 - 1451 Title/Abstract Full Text View citing articles Show Details

ACTELION PHARMACEUTICALS LTD; GUDE, Markus; HUBSCHWERLEN, Christian; PANCHAUD, Philippe

Patent: WO2012/131588 A1, 2012 ; Title/Abstract Full Text Show Details

QUANTICEL PHARMACEUTICALS, INC; NIE, Zhe; STAFFORD, Jeffrey, Alan; VEAL, James, Marvin; WALLACE, Michael, Brennan

Patent: WO2014/89364 A1, 2014 ;


Title/Abstract Full Text Show Details

2 of 4

3 of 4

4 of 4

Comment (Pharmacological Data)

suppression of excitability of non-specific activating systems of the midbrain and posterior hypothalamus: 8-14percent; improvement of excitability of the hippocampus and amygdala: 10percent (rabbits, 10 mg/kg i.v., 1 h)

Reference

Saratikov; Zamoshchina

Arzneimittel-Forschung/Drug Research, 1986 , vol. 36, # 10 p. 1448 - 1451 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

acute toxicity: LD 50: 1265 mg/kg, intraperitoneal, mice

Reference

Lyubimov, B. I.; Yavorskii, A. N.

Pharmaceutical Chemistry Journal, 1983 , vol. 17, # 5 p. 378 - 380 Khimiko-Farmatsevticheskii Zhurnal, 1983 , vol. 17, # 5 p. 629 - 631 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

increased the duration of thiopental sodium anesthesia: 2.6-fold: dose: 50 mg/kg, 4.3-fold: dose: 100 mg/kg; ED 50: 72 mg/kg; reduced the spontaneous locomotor activity: 2-fold: dose 50 mg/kg, 3-fold: 100 mg/kg; ED 50: 200 mg/kg, mice

Reference

Lyubimov, B. I.; Yavorskii, A. N.

Pharmaceutical Chemistry Journal, 1983 , vol. 17, # 5 p. 378 - 380 Khimiko-Farmatsevticheskii Zhurnal, 1983 , vol. 17, # 5 p. 629 - 631 Title/Abstract Full Text View citing articles Show Details

Other Data Use (2) Use Pattern

Reference

angiogenic material

Wright, Emma Jayne; Huckle, James William; Ali, Saad Aboul Majeed

Patent: US2004/265282 A1, 2004 ; Title/Abstract Full Text Show Details

fixation devices for tissue repair

Wright, Emma Jayne; Huckle, James William; Ali, Saad Aboul Majeed

Patent: US2004/265282 A1, 2004 ; Title/Abstract Full Text Show Details

Chemical Name: ammonium oxybate

no reactions.

Other Data (3)

Reaxys Registry Number: 29378703

Molecular Formula: C4H8O3*H3N Linear Structure Formula: C4H8O3*H3N Molecular Weight: 121.136

InChI Key: AUYNCXRTGCQCAZ-UHFFFAOYSA-N

11

Synthesize | Hide Details Find similar Chemical Names and Synonyms ammonium oxybate, ammonium gamma-hydroxybutyrate Other Data Use (3) Use Pattern

Location

Reference

Pharmaceuticals

Page/Page column 34

Jazz Pharmaceuticals, Inc.; Cook, Harry; Hamilton, Martha; Danielson, Douglas; Goderstad, Colette; Reardan, Dayton T.

Patent: US2016/58862 A1, 2016 ; Title/Abstract Full Text Show Details

1


active agent

Page/Page column 34

Jazz Pharmaceuticals, Inc.; Cook, Harry; Hamilton, Martha; Danielson, Douglas; Goderstad, Colette; Reardan, Dayton T.

Patent: US2016/58862 A1, 2016 ; Title/Abstract Full Text Show Details

pharmaceutical composition, chemically stable and resistant to microbial growth

Page/Page column 34

Jazz Pharmaceuticals, Inc.; Cook, Harry; Hamilton, Martha; Danielson, Douglas; Goderstad, Colette; Reardan, Dayton T.

Patent: US2016/58862 A1, 2016 ; Title/Abstract Full Text Show Details

Chemical Name: sodium 4-hydroxybutanoate Reaxys Registry Number: 3709170

CAS Registry Number: 502-85-2 Type of Substance: acyclic Molecular Formula: C4H7O3*Na Linear Structure Formula: Na(1+)*O2CCH2CH2CH2OH(1-) =

2 prep out of 37 reactions.

Identification Physical Data (12) Spectra (21) Bioactivity (76) Other Data (237)

158

NaO2CCH2CH2CH2OH Molecular Weight: 126.088

InChI Key: XYGBKMMCQDZQOZ-UHFFFAOYSA-M

12

Synthesize | Hide Details Find similar Chemical Names and Synonyms sodium 4-hydroxybutanoate, 4-hydroxybutyric acid sodium salt, Xyrem® sodium oxysorbate, sodium gamma-hydroxybutyrate, sodium 4hydroxybutyrate, sodium hydroxybutyrate, sodium oxybate Identification Substance Label (12) Label

Reference

SO

Pross, Nathalie; Patat, Alain; Vivet, Philippe; Bidaut, Michelle; Fauchoux, Nicolas

British Journal of Clinical Pharmacology, 2015 , vol. 80, # 3 p. 480 - 492 Title/Abstract Full Text View citing articles Show Details

5

Lemoine, Hugues; Marković, Dean; Deguin, Brigitte

Journal of Organic Chemistry, 2014 , vol. 79, # 10 p. 4358 - 4366 Title/Abstract Full Text View citing articles Show Details

032

INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM); MAITRE, Michel; BOURGUIGNON, Jean-Jacques; SCHMITT, Martine; KLEIN, Christian; MENSAH-NYAGAN, Ayikoe, Guy; MATHIS, Chantal; CASSEL, Jean-Christophe

Patent: WO2013/24028 A1, 2013 ; Title/Abstract Full Text Show Details

3

Rival, Nicolas; Hazelard, Damien; Hanquet, Gilles; Kreuzer, Thomas; Bensoussan, Charlelie; Reymond, Sébastien; Cossy, Janine; Colobert, Françoise

Organic and Biomolecular Chemistry, 2012 , vol. 10, # 47 p. 9418 - 9428 Title/Abstract Full Text View citing articles Show Details

Renton; Shen; Eckert; Lee; Gala; Chen; Pramanik; Schumacher

Organic Process Research and Development, 2002 , vol. 6, # 1 p. 36 - 41 Title/Abstract Full Text View citing articles Show Details

Lee, Gary M.; Eckert, Jefrey; Gala, Dinesh; Schwartz, Martin; Renton, Paul; Pergamen, Edward; Whttington, Michael; Schumacher, Doris; Heimark, Larry; Shipkova, Petia

Organic Process Research and Development, 2001 , vol. 5, # 6 p. 622 - 629 Title/Abstract Full Text View citing articles Show Details

GHB

Van Sassenbroeck; De Paepe; Belpaire; Rosseel; Martens; Boon; Buylaert

Journal of Pharmacy and Pharmacology, 2001 , vol. 53, # 12 p. 1687 - 1696 Title/Abstract Full Text View citing articles Show Details

Carter, Lawrence P.; Flores, Lauren R.; Wu, Huifang; Chen, Weibin; Unzeitig, Andrew W.; Coop, Andy; France, Charles P.

Journal of Pharmacology and Experimental Therapeutics, 2003 , vol. 305, # 2 p. 668 - 674 Title/Abstract Full Text View citing articles Show Details

Borgen, Lowell A.; Okerholm, Richard; Morrison, Dennis; Lai, Allen

Journal of Clinical Pharmacology, 2003 , vol. 43, # 1 p. 59 - 65 Title/Abstract Full Text View citing articles Show Details


Borgen, Lowell A.; Okerholm, Richard A.; Lai, Allen; Scharf, Martin B.

Journal of Clinical Pharmacology, 2004 , vol. 44, # 3 p. 253 - 257 Title/Abstract Full Text View citing articles Show Details

Ottani, Alessandra; Vergoni, Anna Valeria; Saltini, Sabrina; Mioni, Chiara; Giuliani, Daniela; Bartiromo, Marta; Zaffe, Davide; Botticelli, Annibale R.; Ferrari, Anna; Bertolini, Alfio; Genedani, Susanna

European Journal of Pharmacology, 2004 , vol. 485, # 1-3 p. 183 - 191 Title/Abstract Full Text View citing articles Show Details

Carter; Unzeitig; Wu; Chen; Coop; Koek; France, Charles P.

Journal of Pharmacology and Experimental Therapeutics, 2004 , vol. 309, # 2 p. 540 - 547 Title/Abstract Full Text View citing articles Show Details

Morris, Marilyn E.; Hu, Ke; Wang, Qi

Journal of Pharmacology and Experimental Therapeutics, 2005 , vol. 313, # 3 p. 1194 - 1202 Title/Abstract Full Text View citing articles Show Details

Bhattacharya, Indranil; Boje, Kathleen M. K.

Journal of Pharmacology and Experimental Therapeutics, 2004 , vol. 311, # 1 p. 92 - 98 Title/Abstract Full Text View citing articles Show Details

Carter, Lawrence P.; Wu, Huifang; Chen, Weibin; Cruz, Christopher M.; Lamb; Koek, Wouter; Coop, Andy; France, Charles P.

Journal of Pharmacology and Experimental Therapeutics, 2004 , vol. 308, # 1 p. 182 - 188 Title/Abstract Full Text View citing articles Show Details

Sevak, Rajkumar J.; Koek, Wouter; Galli, Aurelio; France, Charles P.

Journal of Pharmacology and Experimental Therapeutics, 2007 , vol. 320, # 3 p. 1216 - 1223 Title/Abstract Full Text View citing articles Show Details

Kapadia, Roopa; Boehlke, Mark; Maher, Timothy J.

Life Sciences, 2007 , vol. 80, # 11 p. 1046 - 1050 Title/Abstract Full Text View citing articles Show Details

Raybon, Joseph J.; Boje, Kathleen M. K.

Journal of Pharmacology and Experimental Therapeutics, 2007 , vol. 320, # 3 p. 1252 - 1260 Title/Abstract Full Text View citing articles Show Details

20

Tang, Tony P.; Ellman, Jonathan A.

Journal of Organic Chemistry, 2002 , vol. 67, # 22 p. 7819 - 7832 Title/Abstract Full Text View citing articles Show Details

8

Simkovic, Ivan; Alfoeldi, Juraj; Matulova, Maria

Carbohydrate Research, 1986 , vol. 152, p. 137 - 142 Title/Abstract Full Text View citing articles Show Details

Renton; Gala; Lee

Tetrahedron Letters, 2001 , vol. 42, # 41 p. 7141 - 7143 Title/Abstract Full Text View citing articles Show Details

educt 2 to 1

Antopolsky, Maxim; Azhayev, Alex

Helvetica Chimica Acta, 1999 , vol. 82, # 12 p. 2130 - 2140 Title/Abstract Full Text View citing articles Show Details

4HB

Gatley, S. John; Ding, Yu-Shin; Volkow, Nora D.; Chen, Ruoyan; Sugano, Yuichi; Fowler, Joanna S.

European Journal of Pharmacology, 1995 , vol. 281, # 2 p. 141 - 149 Title/Abstract Full Text View citing articles Show Details

HO(CH2)3COONa, Scheme 3

Dardoize; Goasdoue; Goadoue; Laborit; Topall

Tetrahedron, 1989 , vol. 45, # 24 p. 7783 - 7794 Title/Abstract Full Text View citing articles Show Details

10 n=4

Goto; Okamoto; Okutani; Imada

Chemical and Pharmaceutical Bulletin, 1985 , vol. 33, # 10 p. 4422 - 4431 Title/Abstract Full Text View citing articles Show Details

12

Kricheldorf,H.R.; Kaschig,J.

Justus Liebigs Annalen der Chemie, 1976 , p. 882 - 890 Full Text View citing articles Show Details

Patent-Specific Data (6)

Related Markush Structure (RN)

Location in Patent

Page/Page column

PTM Biolabs, Inc.; Zhao, Yingming; Xie, Zhongyu

Patent: US2015/51093 A1, 2015 ;

INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM); MAITRE, Michel; BOURGUIGNON, JeanJacques; SCHMITT, Martine; KLEIN, Christian; MENSAH-NYAGAN, Ayikoe, Guy; MATHIS, Chantal; CASSEL, Jean-Christophe

Patent: WO2013/24028 A1, 2013 ;

24593161; 24593169

Reference

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

19823527

NORAC, INC.

Patent: WO2009/129350 A2, 2009 ;


Title/Abstract Full Text Show Details

11333568

THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK

Patent: WO2006/53186 A2, 2006 ;

Title/Abstract Full Text Show Details

11339658

ORPHAN MEDICAL, INC.

Patent: WO2006/29155 A2, 2006 ;

Title/Abstract Full Text Show Details

Claim

Laboratorio Farmaceutico C.T. S.r.l.

Patent: US4983632 A1, 1991 ; Title/Abstract Full Text Show Details

Eli Lilly and Company

Patent: US6040442 A1, 2000 ; Title/Abstract Full Text Show Details

COOK, HARRY N.; HAMILTON, MARTHA; DANIELSON, DOUG; GODERSTAD, COLETTE; REARDAN, DAYTON

Patent: US2002/77334 A1, 2002 ; Title/Abstract Full Text Show Details

Physical Data Crystal Phase (1) Description (Crystal Phase)

Reference

Association in the solid state

Morssli, M.; Cassanas, G.; Bardet, L.; Pauvert, B.; Terol, A.

Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy, 1991 , vol. 47, # 5 p. 529 - 541 Title/Abstract Full Text View citing articles Show Details

Crystal Property Description (5) Colour & Other Properties

Location

Reference

white

Lemoine, Hugues; Marković, Dean; Deguin, Brigitte

Journal of Organic Chemistry, 2014 , vol. 79, # 10 p. 4358 - 4366 Title/Abstract Full Text View citing articles Show Details

white

Paragraph 00341

ONYX THERAPEUTICS, INC.; MCMINN, Dustin; JOHNSON, Henry; MOEBIUS, David, C.

Patent: WO2014/152127 A1, 2014 ; Title/Abstract Full Text Show Details

white

supporting information

Smeenk, Linde E. J.; Dailly, Nicolas; Hiemstra, Henk; Van Maarseveen, Jan H.; Timmerman, Peter

Organic Letters, 2012 , vol. 14, # 5 p. 1194 - 1197 Title/Abstract Full Text View citing articles Show Details

white

supporting information

Rival, Nicolas; Hazelard, Damien; Hanquet, Gilles; Kreuzer, Thomas; Bensoussan, Charlelie; Reymond, Sébastien; Cossy, Janine; Colobert, Françoise

Organic and Biomolecular Chemistry, 2012 , vol. 10, # 47 p. 9418 - 9428 Title/Abstract Full Text View citing articles Show Details

white

THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK

Patent: WO2006/53186 A2, 2006 ; Title/Abstract Full Text Show Details

Partition octan-1-ol/water (MCS) (1) log POW

Location

Reference

-0.6

supporting information

Stratton, Christopher F.; Newman, David J.; Tan, Derek S.

Bioorganic and Medicinal Chemistry Letters, 2015 , vol. 25, # 21 p. 4802 - 4807 Title/Abstract Full Text View citing articles Show Details

Solubility (MCS) (5) Solubility

Saturation

Temperature

Solvent (Solubility

Location

Reference


(Solubility (MCS)) 1000 g·l-1

in solution

65 °C

(MCS)) water

Paragraph 0277

Jazz Pharmaceuticals, Inc.; Cook, Harry; Hamilton, Martha; Danielson, Douglas; Goderstad, Colette; Reardan, Dayton T.

Patent: US2016/58862 A1, 2016 ; Title/Abstract Full Text Show Details

450 g·l-1

in solution

25 °C

water

Paragraph 0277

Jazz Pharmaceuticals, Inc.; Cook, Harry; Hamilton, Martha; Danielson, Douglas; Goderstad, Colette; Reardan, Dayton T.

Patent: US2016/58862 A1, 2016 ; Title/Abstract Full Text Show Details

500 g·l-1

in solution

25 °C

water

Paragraph 0277

Jazz Pharmaceuticals, Inc.; Cook, Harry; Hamilton, Martha; Danielson, Douglas; Goderstad, Colette; Reardan, Dayton T.

Patent: US2016/58862 A1, 2016 ; Title/Abstract Full Text Show Details

600 g·l-1

in solution

25 °C

water

Paragraph 0277

Jazz Pharmaceuticals, Inc.; Cook, Harry; Hamilton, Martha; Danielson, Douglas; Goderstad, Colette; Reardan, Dayton T.

Patent: US2016/58862 A1, 2016 ; Title/Abstract Full Text Show Details

750 g·l-1

in solution

25 °C

water

Paragraph 0277

Jazz Pharmaceuticals, Inc.; Cook, Harry; Hamilton, Martha; Danielson, Douglas; Goderstad, Colette; Reardan, Dayton T.

Patent: US2016/58862 A1, 2016 ; Title/Abstract Full Text Show Details

Spectra NMR Spectroscopy (7) Description (NMR Spectroscopy)

Nucleus (NMR Spectroscopy)

Solvents (NMR Spectroscopy)

Chemical shifts

1H

Chemical shifts Spectrum

Temperature (NMR Spectroscopy)

Frequency (NMR Spectroscopy)

water-d2

1H

water-d2

Chemical shifts Spectrum

13C

Chemical shifts Spectrum

Location

Reference

300 MHz

supporting information

Rival, Nicolas; Hazelard, Damien; Hanquet, Gilles; Kreuzer, Thomas; Bensoussan, Charlelie; Reymond, Sébastien; Cossy, Janine; Colobert, Françoise

Organic and Biomolecular Chemistry, 2012 , vol. 10, # 47 p. 9418 - 9428 Title/Abstract Full Text View citing articles Show Details

Zhai, Duanting; Tan, Yong Qiao Elton; Xu, Wang; Chang, Young-Tae

Chemical Communications, 2014 , vol. 50, # 22 p. 2904 - 2906 Title/Abstract Full Text View citing articles Show Details

400 MHz

supporting information

Lemoine, Hugues; Marković, Dean; Deguin, Brigitte

Journal of Organic Chemistry, 2014 , vol. 79, # 10 p. 4358 4366 Title/Abstract Full Text View citing articles Show Details

water-d2

100 MHz

supporting information

Lemoine, Hugues; Marković, Dean; Deguin, Brigitte

Journal of Organic Chemistry, 2014 , vol. 79, # 10 p. 4358 4366 Title/Abstract Full Text View citing articles Show Details

1H

deuteromethanol

25 °C

400 MHz

supporting information

Smeenk, Linde E. J.; Dailly, Nicolas; Hiemstra, Henk; Van Maarseveen, Jan H.; Timmerman, Peter

Organic Letters, 2012 , vol. 14, # 5 p. 1194 - 1197 Title/Abstract Full Text View citing articles Show Details

Chemical shifts Spectrum

13C

deuteromethanol

25 °C

100 MHz

supporting information

Smeenk, Linde E. J.; Dailly, Nicolas; Hiemstra, Henk; Van Maarseveen, Jan H.; Timmerman, Peter

Organic Letters, 2012 , vol. 14, # 5 p. 1194 - 1197 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

water-d2

75 MHz

supporting information

Rival, Nicolas; Hazelard, Damien; Hanquet, Gilles; Kreuzer, Thomas; Bensoussan, Charlelie; Reymond, Sébastien; Cossy, Janine; Colobert, Françoise

Organic and Biomolecular Chemistry, 2012 , vol. 10, # 47 p. 9418 - 9428 Title/Abstract Full Text View citing articles Show Details


Chemical shifts

13C

D2O aq. NaOH

25 °C

Simkovic, Ivan; Alfoeldi, Juraj; Matulova, Maria

Carbohydrate Research, 1986 , vol. 152, p. 137 - 142 Title/Abstract Full Text View citing articles Show Details

IR Spectroscopy (6) Description (IR Spectroscopy)

Solvent (IR Spectroscopy)

Location

Comment (IR Spectroscopy)

ATR (attenuated total reflectance) Bands

Lemoine, Hugues; Marković, Dean; Deguin, Brigitte

Journal of Organic Chemistry, 2014 , vol. 79, # 10 p. 4358 - 4366 Title/Abstract Full Text View citing articles Show Details

Bands

supporting information

Smeenk, Linde E. J.; Dailly, Nicolas; Hiemstra, Henk; Van Maarseveen, Jan H.; Timmerman, Peter

Organic Letters, 2012 , vol. 14, # 5 p. 1194 - 1197 Title/Abstract Full Text View citing articles Show Details

ATR (attenuated total reflectance) Intensity of IR bands Bands

neat (no solvent, solid phase)

supporting information

Rival, Nicolas; Hazelard, Damien; Hanquet, Gilles; Kreuzer, Thomas; Bensoussan, Charlelie; Reymond, Sébastien; Cossy, Janine; Colobert, Françoise

Organic and Biomolecular Chemistry, 2012 , vol. 10, # 47 p. 9418 - 9428 Title/Abstract Full Text View citing articles Show Details

Spectrum

solid

4000 - 200 cm** (-1)

Morssli, M.; Cassanas, G.; Bardet, L.; Pauvert, B.; Terol, A.

Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy, 1991 , vol. 47, # 5 p. 529 - 541 Title/Abstract Full Text View citing articles Show Details

Bands

H2O

1560 - 910 cm** (-1)

Morssli, M.; Cassanas, G.; Bardet, L.; Pauvert, B.; Terol, A.

Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy, 1991 , vol. 47, # 5 p. 529 - 541 Title/Abstract Full Text View citing articles Show Details

Bands

solid

3340 - 320 cm** (-1)

Morssli, M.; Cassanas, G.; Bardet, L.; Pauvert, B.; Terol, A.

Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy, 1991 , vol. 47, # 5 p. 529 - 541 Title/Abstract Full Text View citing articles Show Details

Reference

Mass Spectrometry (3) Description (Mass Spectrometry)

Reference

electrospray ionisation (ESI) time-of-flight mass spectra (TOFMS) spectrum

Lemoine, Hugues; Marković, Dean; Deguin, Brigitte

Journal of Organic Chemistry, 2014 , vol. 79, # 10 p. 4358 - 4366 Title/Abstract Full Text View citing articles Show Details

high resolution mass spectrometry (HRMS) electrospray ionisation (ESI) time-of-flight mass spectra (TOFMS) spectrum

Lemoine, Hugues; Marković, Dean; Deguin, Brigitte

Journal of Organic Chemistry, 2014 , vol. 79, # 10 p. 4358 - 4366 Title/Abstract Full Text View citing articles Show Details

spectrum time-of-flight mass spectra (TOFMS)

Cody, Robert B.; Laramee, James A.; Durst, H. Dupont

Analytical Chemistry, 2005 , vol. 77, # 8 p. 2297 - 2302 Title/Abstract Full Text View citing articles Show Details

Raman Spectroscopy (5) Description (Raman Spectroscopy)

Comment (Raman Spectroscopy)

Spectrum

D2O

Morssli, M.; Cassanas, G.; Bardet, L.; Pauvert, B.; Terol, A.

Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy, 1991 , vol. 47, # 5 p. 529 - 541 Title/Abstract Full Text View citing articles Show Details

Spectrum

H2O

Morssli, M.; Cassanas, G.; Bardet, L.; Pauvert, B.; Terol, A.

Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy, 1991 , vol. 47, # 5 p. 529 - 541 Title/Abstract Full Text View citing articles Show Details

Spectrum

neat (no solvent, solid phase)

Morssli, M.; Cassanas, G.; Bardet, L.; Pauvert, B.; Terol, A.

Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy, 1991 , vol. 47, # 5 p. 529 - 541 Title/Abstract Full Text View citing articles Show Details

Reference


Bands

H2O

Morssli, M.; Cassanas, G.; Bardet, L.; Pauvert, B.; Terol, A.

Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy, 1991 , vol. 47, # 5 p. 529 - 541 Title/Abstract Full Text View citing articles Show Details

Bands

neat (no solvent, solid phase)

Morssli, M.; Cassanas, G.; Bardet, L.; Pauvert, B.; Terol, A.

Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy, 1991 , vol. 47, # 5 p. 529 - 541 Title/Abstract Full Text View citing articles Show Details

Bioactivity Pharmacological Data (76) 1 of 76

Comment (Pharmacological Data)

Bioactivities present

Reference

HOWARD FLOREY INSTITUTE OF, EXPERIMENTAL PHYSIOLOGY AND MEDICINE

Patent: EP972779 A2, 2000 ; Title/Abstract Full Text Show Details

Kricheldorf,H.R.; Kaschig,J.

Justus Liebigs Annalen der Chemie, 1976 , p. 882 - 890 Full Text View citing articles Show Details

Laboratorio Farmaceutico C.T. S.r.l.

Patent: US4983632 A1, 1991 ; Title/Abstract Full Text Show Details

Fuji Photo Film Co., Ltd.

Patent: US5436221 A1, 1995 ; Title/Abstract Full Text Show Details

Sterling Winthrop Inc.

Patent: US5512589 A1, 1996 ; Title/Abstract Full Text Show Details

Eli Lilly and Company

Patent: US6040442 A1, 2000 ; Title/Abstract Full Text Show Details

Drug Delivery System Institute, Ltd.

Patent: US6057431 A1, 2000 ; Title/Abstract Full Text Show Details

Eli Lilly and Company

Patent: US4038275 A1, 1977 ; Title/Abstract Full Text Show Details

Wise, Alan; Brown, Andrew James

Patent: US2003/113810 A1, 2003 ; Title/Abstract Full Text Show Details

Koppel,G.A.; Nummy,L.J.

Tetrahedron Letters, 1978 , p. 25 - 28 Full Text View citing articles Show Details

Bernasconi,S. et al.

Gazzetta Chimica Italiana, 1979 , vol. 109, p. 5 - 8 Full Text View citing articles Show Details

HOWARD FLOREY INSTITUTE OF EXPERIMENTAL PHYSIOLOGY AND MEDICINE

Patent: EP383803 B1, 2000 ; Title/Abstract Full Text Show Details

Brookhaven Science Associates

Patent: EP1481668 A1, 2004 ; Title/Abstract Full Text Show Details

Wright, Emma Jayne; Huckle, James William; Ali, Saad Aboul Majeed

Patent: US2004/265282 A1, 2004 ; Title/Abstract Full Text Show Details

Ayala, William J.

Patent: US2005/31688 A1, 2005 ; Title/Abstract Full Text Show Details

ORPHAN MEDICAL, INC.

Patent: WO2006/29155 A2, 2006 ; Title/Abstract Full Text Show Details

Liang, Likan; Shah, Niraj; Bhatt, Padmanabh P.; Ibrahim, Scott

Patent: US2006/210630 A1, 2006 ; Title/Abstract Full Text Show Details


JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

THERAQUEST BIOSCIENCES, INC.

Patent: WO2008/33351 A2, 2008 ; Title/Abstract Full Text Show Details

2 of 76

3 of 76

Comment (Pharmacological Data)

Bioactivities present

Reference

Nelson; Cretcher

Journal of the American Chemical Society, 1930 , vol. 52, p. 3702 Full Text View citing articles Show Details

Paulssen et al.

Journal of Organic Chemistry, 1969 , vol. 34, p. 2097 Full Text View citing articles Show Details

Haralambidis; Duncan; Tregear

Tetrahedron Letters, 1987 , vol. 28, # 43 p. 5199 - 5202 Title/Abstract Full Text View citing articles Show Details

Weber; Halgren; Doyle; Lynch; Siegl; Parsons; Greenlee; Patchett

Journal of Medicinal Chemistry, 1991 , vol. 34, # 9 p. 2692 - 2701 Title/Abstract Full Text View citing articles Show Details

Morssli, M.; Cassanas, G.; Bardet, L.; Pauvert, B.; Terol, A.

Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy, 1991 , vol. 47, # 5 p. 529 - 541 Title/Abstract Full Text View citing articles Show Details

Dardoize; Goasdoue; Goadoue; Laborit; Topall

Tetrahedron, 1989 , vol. 45, # 24 p. 7783 - 7794 Title/Abstract Full Text View citing articles Show Details

Sugawara; Irie; Iwasawa; Yoshikawa; Okuno; Watanabe; Kato; Shibukawa; Ito

Carbohydrate Research, 1992 , vol. 230, # 1 p. 117 - 149 Title/Abstract Full Text View citing articles Show Details

Simkovic, Ivan; Alfoeldi, Juraj; Matulova, Maria

Carbohydrate Research, 1986 , vol. 152, p. 137 - 142 Title/Abstract Full Text View citing articles Show Details

Goto; Okamoto; Okutani; Imada

Chemical and Pharmaceutical Bulletin, 1985 , vol. 33, # 10 p. 4422 - 4431 Title/Abstract Full Text View citing articles Show Details

Binns, Falmai; Roberts, Stanley M.; Taylor, Alan; Williams, Charles F.

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Saratikov; Zamoshchina

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Arena; Fung

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Hovinen; Guzaev; Azhayev; Lonnberg

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Ochiai, Masahito; Ito, Takao; Takahashi, Hideo; Nakanishi, Akinobu; Toyonari, Mika; Sueda, Takuya; Goto, Satoru; Shiro, Motoo

Journal of the American Chemical Society, 1996 , vol. 118, # 33 p. 7716 - 7730 Title/Abstract Full Text View citing articles Show Details

Manclus, Juan J.; Primo, Jaime; Montoya, Angel

Journal of Agricultural and Food Chemistry, 1996 , vol. 44, # 12 p. 4052 - 4062 Title/Abstract Full Text View citing articles Show Details

Hassan, Abdi; Wang, Suning

Journal of the Chemical Society - Dalton Transactions, 1997 , # 12 p. 2009 - 2017 Title/Abstract Full Text View citing articles Show Details

Tomchin; Kropotov

Pharmaceutical Chemistry Journal, 1998 , vol. 32, # 1 p. 20 - 25 Title/Abstract Full Text View citing articles Show Details

Tomchin; Velezheva; Shustov

Pharmaceutical Chemistry Journal, 1998 , vol. 32, # 2 p. 59 - 63 Title/Abstract Full Text View citing articles Show Details

Gatley, S. John; Ding, Yu-Shin; Volkow, Nora D.; Chen, Ruoyan; Sugano, Yuichi; Fowler, Joanna S.

European Journal of Pharmacology, 1995 , vol. 281, # 2 p. 141 - 149 Title/Abstract Full Text View citing articles Show Details

Clive, Derrick L. J.; Zhang, Junhu

Tetrahedron, 1999 , vol. 55, # 41 p. 12059 - 12068 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

Bioactivities present

Reference

Antopolsky, Maxim; Azhayev, Alex

Helvetica Chimica Acta, 1999 , vol. 82, # 12 p. 2130 - 2140


Title/Abstract Full Text View citing articles Show Details

Janssen; Hulst; Kellogg; Hendriks; Ensing; De Zeeuw

Pharmazie, 2000 , vol. 55, # 1 p. 42 - 48 Title/Abstract Full Text View citing articles Show Details

Kavanagh; Kenny; Feely

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McMahon, Lance R.; France, Charles P.

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Borgen, Lowell A.; Okerholm, Richard; Morrison, Dennis; Lai, Allen

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Borgen, Lowell A.; Okerholm, Richard A.; Lai, Allen; Scharf, Martin B.

Journal of Clinical Pharmacology, 2004 , vol. 44, # 3 p. 253 - 257 Title/Abstract Full Text View citing articles Show Details

Ottani, Alessandra; Vergoni, Anna Valeria; Saltini, Sabrina; Mioni, Chiara; Giuliani, Daniela; Bartiromo, Marta; Zaffe, Davide; Botticelli, Annibale R.; Ferrari, Anna; Bertolini, Alfio; Genedani, Susanna

European Journal of Pharmacology, 2004 , vol. 485, # 1-3 p. 183 - 191 Title/Abstract Full Text View citing articles Show Details

Carter; Unzeitig; Wu; Chen; Coop; Koek; France, Charles P.

Journal of Pharmacology and Experimental Therapeutics, 2004 , vol. 309, # 2 p. 540 - 547 Title/Abstract Full Text View citing articles Show Details

Morris, Marilyn E.; Hu, Ke; Wang, Qi

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Bhattacharya, Indranil; Boje, Kathleen M. K.

Journal of Pharmacology and Experimental Therapeutics, 2004 , vol. 311, # 1 p. 92 - 98 Title/Abstract Full Text View citing articles Show Details

Iliev, Boyan; Linden, Anthony; Heimgartner, Heinz

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Sevak, Rajkumar J.; Koek, Wouter; Galli, Aurelio; France, Charles P.

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4 of 76

Comment (Pharmacological Data)

Bioactivities present

Reference

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Life Sciences, 2007 , vol. 80, # 11 p. 1046 - 1050 Title/Abstract Full Text View citing articles Show Details

Cody, Robert B.; Laramee, James A.; Durst, H. Dupont

Analytical Chemistry, 2005 , vol. 77, # 8 p. 2297 - 2302 Title/Abstract Full Text View citing articles Show Details

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COOK, HARRY N.; HAMILTON, MARTHA; DANIELSON, DOUG; GODERSTAD, COLETTE; REARDAN, DAYTON

Patent: US2002/77334 A1, 2002 ; Title/Abstract Full Text Show Details

THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK

Patent: WO2006/53186 A2, 2006 ; Title/Abstract Full Text Show Details

Isupov; Chupakhina

Russian Journal of Inorganic Chemistry, 1998 , vol. 43, # 1 p. 51 - 56 Title/Abstract Full Text View citing articles Show Details

Andjelkovic, Mirjana; Ceccarelli, Simona M.; Chomienne, Odile; Kaplan, Gerald Lewis; Mattei, Patrizio; Tilley, Jefferson Wright


Patent: US2009/270505 A1, 2009 ; Title/Abstract Full Text Show Details

NORAC, INC.

Patent: WO2009/129350 A2, 2009 ; Title/Abstract Full Text Show Details

Sankyo Company, Limited

Patent: EP1362856 A1, 2003 ; Title/Abstract Full Text Show Details

Fuji Photo Film Co., Ltd.

Patent: EP1466893 A1, 2004 ; Title/Abstract Full Text Show Details

PFIZER LIMITED; PFIZER INC.

Patent: WO2005/9966 A1, 2005 ; Title/Abstract Full Text Show Details

Kagoshima, Yoshiko; Mori, Makoto; Suzuki, Eiko; Kobayashi, Nobue; Shibayama, Takahiro; Kubota, Mikie; Kamai, Yasuki; Konosu, Toshiyuki

Chemical and Pharmaceutical Bulletin, 2010 , vol. 58, # 6 p. 794 - 804 Title/Abstract Full Text View citing articles Show Details

Luchi, James; Levin, Daniel

Patent: US2011/34727 A1, 2011 ; Title/Abstract Full Text Show Details

Lam, Wing Ki; Felmlee, Melanie A.; Morris, Marilyn E.

Drug Metabolism and Disposition, 2010 , vol. 38, # 3 p. 441 - 447 Title/Abstract Full Text View citing articles Show Details

Kambe, Tohru; Maruyama, Toru; Nakano, Masayuki; Nakai, Yoshihiko; Yoshida, Tadahiro; Matsunaga, Naoki; Oida, Hiroji; Konaka, Akira; Maruyama, Takayuki; Nakai, Hisao; Toda, Masaaki

Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 1 p. 396 - 401 Title/Abstract Full Text View citing articles Show Details

Smeenk, Linde E. J.; Dailly, Nicolas; Hiemstra, Henk; Van Maarseveen, Jan H.; Timmerman, Peter

Organic Letters, 2012 , vol. 14, # 5 p. 1194 - 1197 Title/Abstract Full Text View citing articles Show Details

Kambe, Tohru; Maruyama, Toru; Nakai, Yoshihiko; Yoshida, Hideyuki; Oida, Hiroji; Maruyama, Takayuki; Abe, Nobutaka; Nishiura, Akio; Nakai, Hisao; Toda, Masaaki

Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 7 p. 2235 - 2251 Title/Abstract Full Text View citing articles Show Details

Lamarche, Matthew J.; Leeds, Jennifer A.; Amaral, Adam; Brewer, Jason T.; Bushell, Simon M.; Deng, Gejing; Dewhurst, Janetta M.; Ding, Jian; Dzink-Fox, Joanne; Gamber, Gabriel; Jain, Akash; Lee, Kwangho; Lee, Lac; Lister, Troy; McKenney, David; Mullin, Steve; Osborne, Colin; Palestrant, Deborah; Patane, Michael A.; Rann, Elin M.; Sachdeva, Meena; Shao, Jian; Tiamfook, Stacey; Trzasko, Anna; Whitehead, Lewis; Yifru, Aregahegn; Yu, Donghui; Yan, Wanlin; Zhu, Qingming

Journal of Medicinal Chemistry, 2012 , vol. 55, # 5 p. 2376 - 2387 Title/Abstract Full Text View citing articles Show Details

Rival, Nicolas; Hazelard, Damien; Hanquet, Gilles; Kreuzer, Thomas; Bensoussan, Charlelie; Reymond, Sébastien; Cossy, Janine; Colobert, Françoise

Organic and Biomolecular Chemistry, 2012 , vol. 10, # 47 p. 9418 - 9428 Title/Abstract Full Text View citing articles Show Details

INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM); MAITRE, Michel; BOURGUIGNON, JeanJacques; SCHMITT, Martine; KLEIN, Christian; MENSAH-NYAGAN, Ayikoe, Guy; MATHIS, Chantal; CASSEL, Jean-Christophe

Patent: WO2013/24028 A1, 2013 ; Title/Abstract Full Text Show Details

5 of 76

Comment (Pharmacological Data)

Bioactivities present

Reference

Renton; Shen; Eckert; Lee; Gala; Chen; Pramanik; Schumacher

Organic Process Research and Development, 2002 , vol. 6, # 1 p. 36 - 41 Title/Abstract Full Text View citing articles Show Details

Lee, Gary M.; Eckert, Jefrey; Gala, Dinesh; Schwartz, Martin; Renton, Paul; Pergamen, Edward; Whttington, Michael; Schumacher, Doris; Heimark, Larry; Shipkova, Petia

Organic Process Research and Development, 2001 , vol. 5, # 6 p. 622 - 629 Title/Abstract Full Text View citing articles Show Details

Zhai, Duanting; Tan, Yong Qiao Elton; Xu, Wang; Chang, Young-Tae

Chemical Communications, 2014 , vol. 50, # 22 p. 2904 - 2906 Title/Abstract Full Text View citing articles Show Details

CONCERT PHARMACEUTICALS, INC.; TUNG, Roger D.; SILVERMAN, I. Robert

Patent: WO2014/31840 A1, 2014 ; Title/Abstract Full Text Show Details

Lemoine, Hugues; Marković, Dean; Deguin, Brigitte

Journal of Organic Chemistry, 2014 , vol. 79, # 10 p. 4358 - 4366 Title/Abstract Full Text View citing articles Show Details

Jazz Pharmaceuticals, Inc.; Eller, Mark

Patent: US8772306 B1, 2014 ; Title/Abstract Full Text Show Details

ONYX THERAPEUTICS, INC.; MCMINN, Dustin; JOHNSON, Henry; MOEBIUS, David, C.

Patent: WO2014/152127 A1, 2014 ; Title/Abstract Full Text Show Details


PTM Biolabs, Inc.; Zhao, Yingming; Xie, Zhongyu

Patent: US2015/51093 A1, 2015 ; Title/Abstract Full Text Show Details

Soyka; Lieb

Pharmacopsychiatry, 2015 , vol. 48, # 4-5 p. 123 - 135 Title/Abstract Full Text View citing articles Show Details

Pross, Nathalie; Patat, Alain; Vivet, Philippe; Bidaut, Michelle; Fauchoux, Nicolas

British Journal of Clinical Pharmacology, 2015 , vol. 80, # 3 p. 480 - 492 Title/Abstract Full Text View citing articles Show Details

Stratton, Christopher F.; Newman, David J.; Tan, Derek S.

Bioorganic and Medicinal Chemistry Letters, 2015 , vol. 25, # 21 p. 4802 - 4807 Title/Abstract Full Text View citing articles Show Details

Evren, Cuneyt; Bozkurt, Muge

Dusunen Adam, 2015 , vol. 28, # 4 p. 283 - 300 Title/Abstract Full Text View citing articles Show Details

Salminen, Antero; Jouhten, Paula; Sarajärvi, Timo; Haapasalo, Annakaisa; Hiltunen, Mikko

Neurochemistry International, 2016 , vol. 92, p. 13 - 24 Title/Abstract Full Text View citing articles Show Details

Liebenthal, Jennifer; Valerio, Jason; Ruoff, Chad; Mahowald, Mark

JAMA Neurology, 2016 , vol. 73, # 1 p. 126 - 127 Title/Abstract Full Text View citing articles Show Details

Liu, Albert Y.; Cohen, Stephanie E.; Vittinghoff, Eric; Anderson, Peter L.; Doblecki-Lewis, Susanne; Bacon, Oliver; Chege, Wairimu; Postle, Brian S.; Matheson, Tim; Rivet Amico; Liegler, Teri; Keith Rawlings; Trainor, Nikole; Blue, Robert Wilder; Estrada, Yannine; Coleman, Megan E.; Cardenas, Gabriel; Feaster, Daniel J.; Grant, Robert; Philip, Susan S.; Elion, Richard; Buchbinder, Susan; Kolber, Michael A.

JAMA Internal Medicine, 2016 , vol. 176, # 1 p. 75 - 84 Title/Abstract Full Text View citing articles Show Details

Gitto, Stefano; Golfieri, Lucia; Caputo, Fabio; Grandi, Silvana; Andreone, Pietro

Biomolecules, 2016 , vol. 6, # 1 Title/Abstract Full Text Show Details

Rosato; Abenavoli; Federico; Masarone; Persico

International Journal of Clinical Practice, 2016 , vol. 70, # 2 p. 119 - 131 Title/Abstract Full Text View citing articles Show Details

Deftereos, Spyros N.; Vernon, Suzanne D.; Persidis, Andreas

Fatigue: Biomedicine, Health and Behavior, 2016 , vol. 4, # 1 p. 39 - 51 Title/Abstract Full Text Show Details

Cochen De Cock, Valérie

Current Treatment Options in Neurology, 2016 , vol. 18, # 2 art. no. 6, p. 1 - 9 Title/Abstract Full Text View citing articles Show Details

Chinn, Steven; Caldwell, William; Gritsenko, Karina

Current Pain and Headache Reports, 2016 , vol. 20, # 4 art. no. 25, p. 1 - 10 Title/Abstract Full Text View citing articles Show Details

6 of 76

Comment (Pharmacological Data)

Bioactivities present

Reference

Sarkanen, Tomi; Alakuijala, Anniina; Partinen, Markku

Sleep Medicine, 2016 , vol. 19, p. 17 - 22 Title/Abstract Full Text View citing articles Show Details

Caputo, Fabio; Vignoli, Teo; Tarli, Claudia; Domenicali, Marco; Zoli, Giorgio; Bernardi, Mauro; Addolorato, Giovanni

International Journal of Environmental Research and Public Health, 2016 , vol. 13, # 3 art. no. 290 Title/Abstract Full Text View citing articles Show Details

Busardò, Francesco Paolo; Bertol, Elisabetta; Mannocchi, Giulio; Tittarelli, Roberta; Pantano, Flaminia; Vaiano, Fabio; Baglio, Giovanni; Kyriakou, Chrystalla; Marinelli, Enrico

Forensic Science International, 2016 , vol. 265, p. 172 - 181 Title/Abstract Full Text View citing articles Show Details

Barateau, Lucie; Jaussent, Isabelle; Lopez, Régis; Boutrel, Benjamin; Leu-Semenescu, Smaranda; Arnulf, Isabelle; Dauvilliers, Yves

Sleep, 2016 , vol. 39, # 3 p. 573 - 580 Title/Abstract Full Text View citing articles Show Details

Pal, Nabhendu; Majumdar, Amit

Inorganic Chemistry, 2016 , vol. 55, # 6 p. 3181 - 3191 Title/Abstract Full Text View citing articles Show Details

Hintze, Jonathan P.; Paruthi, Shalini

Sleep Medicine Clinics, 2016 , vol. 11, # 1 p. 91 - 103 Title/Abstract Full Text View citing articles Show Details

BAYER PHARMA AKTIENGESELLSCHAFT; BOTHE, Ulrich; CANCHO GRANDE, Yolanda; IRLBACHER, Horst; RAY, Nicholas Charles

Patent: WO2016/37956 A1, 2016 ; Title/Abstract Full Text Show Details

Maitre, Michel; Klein, Christian; Mensah-Nyagan, Ayikoe G.

Medicinal Research Reviews, 2016 , vol. 36, # 3 p. 363 - 388 Title/Abstract Full Text View citing articles Show Details

Jazz Pharmaceuticals, Inc.; Cook, Harry; Hamilton, Martha; Danielson, Douglas; Goderstad, Colette; Reardan, Dayton T.

Patent: US2016/58862 A1, 2016 ; Title/Abstract Full Text Show Details

Gulyani; Salas; Mari; Choi; Mahajan; Gamaldo

Basal Ganglia, 2016 , vol. 6, # 3 p. 165 - 172 Title/Abstract Full Text View citing articles Show Details

Filardi, Marco; Pizza, Fabio; Bruni, Oliviero; Natale, Vincenzo; Plazzi, Giuseppe

Sleep, 2016 , vol. 39, # 6 p. 1241 - 1247 Title/Abstract Full Text View citing articles Show Details


Park, Eu Gene; Lee, Jiwon; Joo, Eun Yeon; Lee, Munhyang; Lee, Jeehun

Brain and Development, 2016 , vol. 38, # 1 p. 139 - 141 Title/Abstract Full Text View citing articles Show Details

Gashlin, Lauren Z.; Sullo, David; Lawrence, Ruth A.; Rosen-Carole, Casey

Breastfeeding Medicine, 2016 , vol. 11, # 5 p. 261 - 263 Title/Abstract Full Text View citing articles Show Details

Leu-Semenescu, Smaranda; Louis, Pauline; Arnulf, Isabelle

Sleep Medicine, 2016 , vol. 17, p. 38 - 44 Title/Abstract Full Text Show Details

Rocca, Francesca Letizia; Finotti, Elena; Pizza, Fabio; Ingravallo, Francesca; Gatta, Michela; Bruni, Oliviero; Plazzi, Giuseppe Sleep, 2016 , vol. 39, # 7 p. 1389 - 1398 Title/Abstract Full Text View citing articles Show Details

Testino, Gianni; Leone, Silvia; Borro, Paolo

Minerva Medica, 2016 , vol. 107, # 4 p. 223 - 238 Title/Abstract Full Text View citing articles Show Details

Okifuji, Akiko; Gao, Jeff; Bokat, Christina; Hare, Bradford D.

Pain Management, 2016 , vol. 6, # 4 p. 383 - 400 Title/Abstract Full Text Show Details

Ablin, Jacob N.; Häuser, Winfried

Pain Management, 2016 , vol. 6, # 4 p. 371 - 381 Title/Abstract Full Text Show Details

Choy, Ernest H.

Pain Management, 2016 , vol. 6, # 4 p. 339 - 346 Title/Abstract Full Text Show Details

Soyka, Michael; Mutschler, Jochen

Progress in Neuro-Psychopharmacology and Biological Psychiatry, 2016 , vol. 70, p. 148 - 161 Title/Abstract Full Text View citing articles Show Details

7 of 76

Comment (Pharmacological Data)

Bioactivities present

Reference

Jennum, Poul; Christensen, Julie A.E.; Zoetmulder, Marielle

Nature and Science of Sleep, 2016 , vol. 8, p. 107 - 120 Title/Abstract Full Text View citing articles Show Details

Weingarten, Jeremy A.; Dubrovsky, Boris; Basner, Robert C.; Redline, Susan; George, Liziamma; Lederer, David J.

Sleep, 2016 , vol. 39, # 8 p. 1583 - 1589 Title/Abstract Full Text View citing articles Show Details

Shanker, Vicki; Bressman, Susan B.

CONTINUUM Lifelong Learning in Neurology, 2016 , vol. 22, # 4,MovementDisorders p. 1227 - 1245 Title/Abstract Full Text View citing articles Show Details

Ooms, Sharon; Ju, Yo-El

Current Treatment Options in Neurology, 2016 , vol. 18, # 9 art. no. 40 Title/Abstract Full Text View citing articles Show Details

Sharpless, Brian A.

Neuropsychiatric Disease and Treatment, 2016 , vol. 12, p. 1761 - 1767 Title/Abstract Full Text View citing articles Show Details

Syed, Yahiya Y.

Drugs, 2016 , vol. 76, # 13 p. 1313 - 1318 Title/Abstract Full Text Show Details

Barateau, Lucie; Lopez, Régis; Dauvilliers, Yves

Current Treatment Options in Neurology, 2016 , vol. 18, # 10 art. no. 43 Title/Abstract Full Text Show Details

Black, Jed; Swick, Todd; Bogan, Richard; Lai, Chinglin; Carter, Lawrence P.

Sleep Medicine, 2016 , vol. 24, p. 57 - 62 Title/Abstract Full Text Show Details

Bennett, Robert

Nature Reviews Rheumatology, 2016 , vol. 12, # 10 p. 568 - 569 Title/Abstract Full Text Show Details

Bosch, Oliver G.; Seifritz, Erich

Brain Research Bulletin, 2016 , vol. 126, p. 47 - 60 Title/Abstract Full Text Show Details

Kleczkowska, Patrycja; Smaga, Irena; Filip, Małgorzata; Bujalska-Zadrozny, Magdalena

Neurotoxicity Research, 2016 , vol. 30, # 4 p. 698 - 714 Title/Abstract Full Text Show Details

Maski, Kiran; Owens, Judith A

The Lancet Neurology, 2016 , vol. 15, # 11 p. 1170 - 1181 Title/Abstract Full Text Show Details

Adis Medical Writers

Drugs and Therapy Perspectives, 2016 , vol. 32, # 11 p. 470 - 475 Title/Abstract Full Text Show Details

Addolorato, Giovanni; Mirijello, Antonio; Barrio, Pablo; Gual, Antoni

Journal of Hepatology, 2016 , vol. 65, # 3 p. 618 - 630 Title/Abstract Full Text Show Details

Berkowski, Joseph Andrew; Shelgikar, Anita Valanju

Sleep Medicine Clinics, 2016 , vol. 11, # 3 p. 365 - 378 Title/Abstract Full Text Show Details

Snell, Terry W.; Johnston, Rachel K.; Srinivasan, Bharath; Zhou, Hongyi; Gao, Mu; Skolnick, Jeffrey

Biogerontology, 2016 , vol. 17, # 5-6 p. 907 - 920 Title/Abstract Full Text Show Details

Muza, Rexford; Lawrence, Madeleine; Drakatos, Panagis

Current Opinion in Pulmonary Medicine, 2016 , vol. 22, # 6 p. 576 - 582 Title/Abstract Full Text Show Details

Jung, Youngsin; St. Louis, Erik K.

Current Treatment Options in Neurology, 2016 , vol. 18, # 11 art. no. 50


Title/Abstract Full Text Show Details

Ng, Lee-Mei; Sudesh, Kumar

Journal of Bioscience and Bioengineering, 2016 , vol. 122, # 5 p. 550 - 557 Title/Abstract Full Text Show Details

Maitre, Michel; Klein, Christian; Mensah-Nyagan, Ayikoe G.

Alzheimer's Research and Therapy, 2016 , vol. 8, # 1 art. no. 37 Title/Abstract Full Text Show Details

8 of 76

9 of 76

Comment (Pharmacological Data)

Bioactivities present

Reference

Van Der Heide, Astrid; Werth, Esther; Donjacour, Claire E. H. M.; Reijntjes, Robert H. A. M.; Lammers, Gert Jan; Van Someren, Eus J. W.; Baumann, Christian R.; Fronczek, Rolf

Sleep, 2016 , vol. 39, # 11 p. 1941 - 1949 Title/Abstract Full Text Show Details

Kelberman, Michael A.; Vazey, Elena M.

Current Pharmacology Reports, 2016 , vol. 2, # 6 p. 253 - 261 Title/Abstract Full Text Show Details

Blumenthal, David E.; Malemud, Charles J.

Expert Review of Neurotherapeutics, 2016 , vol. 16, # 12 p. 1407 - 1411 Title/Abstract Full Text Show Details

Kacar Bayram, Ayşe; Per, Hüseyin; Ismailoǧullari, Sevda; Canpolat, Mehmet; Gumus, Hakan; Aksu, Murat

Neuropediatrics, 2016 , vol. 47, # 6 p. 380 - 387 Title/Abstract Full Text Show Details

Maresova, Petra; Novotny, Michal; Klímová, Blanka; Kuča, Kamil

Therapeutics and Clinical Risk Management, 2016 , vol. 12, p. 1709 - 1715 Title/Abstract Full Text Show Details

Bogan, Richard; Swick, Todd; Mamelak, Mortimer; Kovacevic-Ristanovic, Ruzica; Lai, Chinglin; Black, Jed; Villa, Kathleen F.; Montplaisir, Jacques

Neurology and Therapy, 2016 , vol. 5, # 2 p. 203 - 213 Title/Abstract Full Text Show Details

Ainslie, Garrett R.; Gibson, K. Michael; Vogel, Kara R.

Pharmacology Research and Perspectives, 2016 , vol. 4, # 6 art. no. E00265 Title/Abstract Full Text Show Details

Jesse; Bråthen; Ferrara; Keindl; Ben-Menachem; Tanasescu; Brodtkorb; Hillbom; Leone; Ludolph

Acta Neurologica Scandinavica, 2017 , vol. 135, # 1 p. 4 - 16 Title/Abstract Full Text Show Details

Calandre, Elena P.; Rico-Villademoros, Fernando; Slim, Mahmoud

Pain Management, 2017 , vol. 7, # 1 p. 5 - 10 Title/Abstract Full Text Show Details

Mayer, Geert

Neurology, 2016 , vol. 87, # 24 p. 2594 - 2595 Title/Abstract Full Text Show Details

Taddei, Raquel N.; Werth, Esther; Poryazova, Rositsa; Baumann, Christian R.; Valko, Philipp O.

Journal of Sleep Research, 2016 , vol. 25, # 6 p. 709 - 715 Title/Abstract Full Text Show Details

Ponziani, Virginia; Gennari, Monia; Pizza, Fabio; Balsamo, Antonio; Bernardi, Filippo; Plazzi, Giuseppe

Journal of Clinical Sleep Medicine, 2016 , vol. 12, # 12 p. 1649 - 1657 Title/Abstract Full Text Show Details

Wairkar, Sarika; Gaud, Ram; Raghavan, Adhithi

Recent Patents on Drug Delivery and Formulation, 2016 , vol. 10, # 3 p. 184 - 191 Title/Abstract Full Text Show Details

Moghadam, Keivan Kaveh; Pizza, Fabio; Primavera, Alberto; Ferri, Raffaele; Plazzi, Giuseppe

Sleep Medicine, 2017 , vol. 32, p. 16 - 21 Title/Abstract Full Text Show Details

Kamal, Rama M.; van Noorden, Martijn S.; Wannet, Wim; Beurmanjer, Harmen; Dijkstra, Boukje A. G.; Schellekens, Arnt

CNS Drugs, 2017 , vol. 31, # 1 p. 51 - 64 Title/Abstract Full Text Show Details

Neikrug, Ariel B.; Crawford, Megan R.; Ong, Jason C.

Behavioral Sleep Medicine, 2017 , vol. 15, # 2 p. 158 - 171 Title/Abstract Full Text Show Details

Susta, Marek; Nemcova, Veronika; Bizik, Gustav; Sonka, Karel

Journal of Sleep Research, 2017 , vol. 26, # 1 p. 30 - 37 Title/Abstract Full Text Show Details

Busardò, Francesco Paolo; Kyriakou, Chrystalla; Marchei, Emilia; Pacifici, Roberta; Pedersen, Daniel Sejer; Pichini, Simona

Journal of Pharmaceutical and Biomedical Analysis, 2017 , vol. 137, p. 123 - 131 Title/Abstract Full Text Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Jazz Pharmaceuticals, Inc.; Cook, Harry; Hamilton, Martha; Danielson, Douglas; Goderstad, Colette; Reardan, Dayton T.

Patent: US2016/58862 A1, 2016 ; Title/Abstract Full Text Show Details

10 of 76

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Pross, Nathalie; Patat, Alain; Vivet, Philippe; Bidaut, Michelle; Fauchoux, Nicolas

British Journal of Clinical Pharmacology, 2015 , vol. 80, # 3 p. 480 - 492 Title/Abstract Full Text View citing articles Show Details


11 of 76

Location

Paragraph

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

CONCERT PHARMACEUTICALS, INC.; TUNG, Roger D.; SILVERMAN, I. Robert

Patent: WO2014/31840 A1, 2014 ; Title/Abstract Full Text Show Details

12 of 76

Location

Page/Page column

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Jazz Pharmaceuticals, Inc.; Eller, Mark

Patent: US8772306 B1, 2014 ; Title/Abstract Full Text Show Details

13 of 76

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM); MAITRE, Michel; BOURGUIGNON, JeanJacques; SCHMITT, Martine; KLEIN, Christian; MENSAH-NYAGAN, Ayikoe, Guy; MATHIS, Chantal; CASSEL, Jean-Christophe

Patent: WO2013/24028 A1, 2013 ; Title/Abstract Full Text Show Details

14 of 76

15 of 76

Effect (Pharmacological Data)

cell uptake; inhibition of

Species or TestSystem (Pharmacological Data)

human

Concentration (Pharmacological Data)

0.5 mmol/l

Kind of Dosing (Pharmacological Data)

incubation of 3H-labeled title comp. (0.1 mmol/l) in presence of title compound

Type (Pharmacological Data)

effective concentration

Value of Type (Pharmacological Data)

0.5 mmol/l

Reference

Lam, Wing Ki; Felmlee, Melanie A.; Morris, Marilyn E.

Drug Metabolism and Disposition, 2010 , vol. 38, # 3 p. 441 - 447 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

intestinal Caco-2 cells of human

Concentration (Pharmacological Data)

0.01 - 80 mmol/l

Kind of Dosing (Pharmacological Data)

title comp. used as sodium salt

Further Details (Pharmacological Data)

Michaelis-Menten constant (Km)

Type (Pharmacological Data)

Km


16 of 76

17 of 76

18 of 76

Value of Type (Pharmacological Data)

17.6 mmol/l

Reference

Lam, Wing Ki; Felmlee, Melanie A.; Morris, Marilyn E.

Drug Metabolism and Disposition, 2010 , vol. 38, # 3 p. 441 - 447 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

intestinal Caco-2 cells of human

Concentration (Pharmacological Data)

0.01 - 80 mmol/l

Kind of Dosing (Pharmacological Data)

title comp. used as sodium salt

Type (Pharmacological Data)

Vmax

Value of Type (Pharmacological Data)

17.3 nmol/min/mg

Reference

Lam, Wing Ki; Felmlee, Melanie A.; Morris, Marilyn E.

Drug Metabolism and Disposition, 2010 , vol. 38, # 3 p. 441 - 447 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

intestinal Caco-2 cells of human

Concentration (Pharmacological Data)

0.01 - 80 mmol/l

Kind of Dosing (Pharmacological Data)

title comp. used as sodium salt

Type (Pharmacological Data)

P

Value of Type (Pharmacological Data)

0.38 μl/min/mg

Reference

Lam, Wing Ki; Felmlee, Melanie A.; Morris, Marilyn E.

Drug Metabolism and Disposition, 2010 , vol. 38, # 3 p. 441 - 447 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

cataleptic

Species or TestSystem (Pharmacological Data)

rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

56 - 1000 mg/kg

Kind of Dosing (Pharmacological

solution in 0.9percent saline (1 ml/kg); title comp. was administered in 6 cumulative doses with 25-min intervals


Data)

19 of 76

20 of 76

Method (Pharmacological Data)

rats were rendered diabetic with 50 mg/kg streptozotocin (STZ) i.p. on d 1 or were injected with saline; STZ-treated rats were injected with 1.78 mg/kg amphetamine i.p. 4 times during days 9 - 16 and insulin-releasing pellets were implanted s.c. on d 28

Further Details (Pharmacological Data)

title comp. was administered to rats treated with only STZ or saline, on days 24 and 26 (after amphetamine), and on days 44 and 46 (after insulin replacement); catalepsy was estimated 25 min after each title comp. injection using a bar test

Results

title comp. induced catalepsy; title comp. dose-response curve was shifted to the left in STZ-treated compared to normal rats, but was shifted to the right in STZ-treated rats with insulin replacement; amphetamine did not change title comp. effect

Reference

Sevak, Rajkumar J.; Koek, Wouter; Galli, Aurelio; France, Charles P.

Journal of Pharmacology and Experimental Therapeutics, 2007 , vol. 320, # 3 p. 1216 - 1223 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

glucose level; effect on

Species or TestSystem (Pharmacological Data)

rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

56 - 1000 mg/kg

Kind of Dosing (Pharmacological Data)

solution in 0.9percent saline (1 ml/kg); 6 cumulative title comp. doses were administered daily on 2 days

Method (Pharmacological Data)

rats were rendered diabetic by i.p. injection of 50 mg/kg streptozotocin on day 1; title comp. treatment on days 24 and 26; blood glucose level was determined on days 1, 8, 17, and 28 to estimate title comp. effect on it

Further Details (Pharmacological Data)

4 doses of amphetamine (1.78 mg/kg i.p.) were injected every other day on days 9 to 16; quinpirole (0.0178 - 0.178 mg/kg i.p.) was administered on days 18, 20, and 22

Comment (Pharmacological Data)

No effect

Reference

Sevak, Rajkumar J.; Koek, Wouter; Galli, Aurelio; France, Charles P.

Journal of Pharmacology and Experimental Therapeutics, 2007 , vol. 320, # 3 p. 1216 - 1223 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

body weight; effect on

Species or TestSystem (Pharmacological Data)

rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

56 - 1000 mg/kg

Kind of Dosing (Pharmacological Data)

solution in 0.9percent saline (1 ml/kg); 6 cumulative title comp. doses were administered daily on 2 days

Method (Pharmacological Data)

rats were rendered diabetic by i.p. injection of 50 mg/kg streptozotocin on day 1; title comp. treatment on days 24 and 26; body weight was determined on days 1, 8, 17, and 28 to estimate title comp. effect on streptozotocin-induced weight loss

Further Details (Pharmacological Data)

4 doses of amphetamine (1.78 mg/kg i.p.) were injected every other day on days 9 to 16; quinpirole (0.0178 - 0.178 mg/kg i.p.) was administered on days 18, 20, and 22

Comment (Pharmacological Data)

No effect


Reference

Show next 20

21 of 76

22 of 76

23 of 76

Sevak, Rajkumar J.; Koek, Wouter; Galli, Aurelio; France, Charles P.

Journal of Pharmacology and Experimental Therapeutics, 2007 , vol. 320, # 3 p. 1216 - 1223 Title/Abstract Full Text View citing articles Show Details

Hide facts

Effect (Pharmacological Data)

tranquilizing

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

548 mg/kg

Kind of Dosing (Pharmacological Data)

dose per day

Method (Pharmacological Data)

acute or chronic (for 5 days) administration of title comp.; sedative/hypnotic effect was assessed by time of loss righting reflex (LRR; onset) and time of regaining righting reflex (RRR: ofset)

Results

title comp. at chronic exposure decreased sedative/hypnotic effect on day 5 compared with either 1st day of exposure or acute dose on 5th day; figure

Reference

Raybon, Joseph J.; Boje, Kathleen M. K.

Journal of Pharmacology and Experimental Therapeutics, 2007 , vol. 320, # 3 p. 1252 - 1260 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

548 mg/kg

Method (Pharmacological Data)

acute administration of title comp.; blood samples were collected over 5 h; concentration of title comp. in plasma was measured; LC/MS/MS assay; noncompartmental parmacokinetic parameters were assessed

Further Details (Pharmacological Data)

LC: liquid chromatography; MS/MS: tandem mass spectrometry

Results

AUC0-290=84.8 mg/min/ml, Cmax=479 μg/ml, Tmax=50.0 min, V/F=225 ml/kg, CL/F=6.52 ml/min/kg, t1/2=24.3 min; table

Reference

Raybon, Joseph J.; Boje, Kathleen M. K.

Journal of Pharmacology and Experimental Therapeutics, 2007 , vol. 320, # 3 p. 1252 - 1260 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

548 mg/kg


24 of 76

25 of 76

26 of 76

Method (Pharmacological Data)

administration of title comp. for 5 days; blood samples were collected over 5 h; concentration of title comp. in plasma was measured; LC/MS/MS assay; noncompartmental parmacokinetic parameters were assessed

Further Details (Pharmacological Data)

LC: liquid chromatography; MS/MS: tandem mass spectrometry

Results

AUC0-290=91.3 mg/min/ml, Cmax=602 μg/ml, Tmax=50.0 min, V/F=159 ml/kg, CL/F=6.05 ml/min/kg, t1/2=18.8 min; table

Reference

Raybon, Joseph J.; Boje, Kathleen M. K.

Journal of Pharmacology and Experimental Therapeutics, 2007 , vol. 320, # 3 p. 1252 - 1260 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

548 mg/kg

Method (Pharmacological Data)

acute administration of title comp.; extracellular brain concentration of title comp. was measured using microdialysis sampling for 5 h; LC/MS/MS assay; noncompartmental parmacokinetic parameters were assessed

Further Details (Pharmacological Data)

LC: liquid chromatography; MS/MS: tandem mass spectrometry

Results

AUC0-290=11.4 mg/min/ml, Cmax=66.0 μg/ml, Tmax=120 min; table

Reference

Raybon, Joseph J.; Boje, Kathleen M. K.

Journal of Pharmacology and Experimental Therapeutics, 2007 , vol. 320, # 3 p. 1252 - 1260 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

548 mg/kg

Kind of Dosing (Pharmacological Data)

dose per day

Method (Pharmacological Data)

administration of title comp. for 5 days; extracellular brain concentration of title comp. was measured using microdialysis sampling for 5 h; LC/MS/MS assay; noncompartmental parmacokinetic parameters were assessed

Further Details (Pharmacological Data)

LC: liquid chromatography; MS/MS: tandem mass spectrometry

Results

AUC0-290=10.3 mg/min/ml, Cmax=63.3 μg/ml, Tmax=106 min; table

Reference

Raybon, Joseph J.; Boje, Kathleen M. K.

Journal of Pharmacology and Experimental Therapeutics, 2007 , vol. 320, # 3 p. 1252 - 1260 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transmitter release; inhibition of

Species or TestSystem

Sprague-Dawley rat


(Pharmacological Data)

27 of 76

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

548 mg/kg

Kind of Dosing (Pharmacological Data)

dose per day

Method (Pharmacological Data)

acute or chronic (for 5 days) administration of title comp.; extracellular striatal dopamine level was measured for 360 min by microdialysis; HPLC-electrochemical detection

Further Details (Pharmacological Data)

HPLC: high-performance liquid chromatography

Results

title comp. at acute, but not at chronic treatment decreased striatal dopamine level; figure

Reference

Raybon, Joseph J.; Boje, Kathleen M. K.

Journal of Pharmacology and Experimental Therapeutics, 2007 , vol. 320, # 3 p. 1252 - 1260 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

dog

Sex

male and female

Route of Application

peroral

Method (Pharmacological Data)

Four prototypes were used in the cross-over dog PK study, including an immediate release core (as the immediate release component in the current invention, IR) (see Ex. 2), an Eudragit L 30 D-55 coated delayed release prototype (DR2) (see Ex. 6a), an Eudragit FS 30 D coated delayed release prototype (DR1-no acid) (see Ex. 6c) and an Eudragit FS 30 D coated delayed release prototype with malic acid as the neutralizing agent in the barrier coats (DR1-with acid) (see Ex. 6d). A total of 6 dogs (3 males and 3 females) were given two oral capsules of one of the prototypes containing 1 g of sodium gamma-hydroxybutyrate per capsule. There was a minimum of a 2-day washout between each dose. Blood was collected at the following time points: 0 (pre-dose), 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, and 14 Hrs post dose (for atotal of 312 samples). Plasma samples were analyzed using a verified LC/MS/MS method. Relative bioavailability was determined by comparing the AUC from the delayed release prototype group to the AUC of the immediate release prototype group. The results show that the lower in the GI, the lower the bioavailability (BA); i.e., absorption is higher at upper GI. The immediate release component has the highest BA, so GHB may be absorbed better in its acid form. The BAs for the delayed release components with or without an neutralizer in the barrier coat do not very much so the neutralizer helps the coating-in turn the gastro-stability-but does not affect the BA. See Table 3 and FIG. 7.

Results

The immediate release component has the highest bioavailability BA, so test compound may be absorbed better in its acid form. The BAs for the delayed release components with or without an neutralizer in the barrier coat do not very much so the neutralizer helps the coatingin turn the gastro-stability, but does not affect the BA. Tmax (hr): 1.2-5.2; Cmax (μg/mL): 38.77-249.5; AUClast: 134.3-601.0; Rel BA: 22100percent; figure given.

Location

Page/Page column 2; 8-9; sheet 7

Reference

Liang, Likan; Shah, Niraj; Bhatt, Padmanabh P.; Ibrahim, Scott

Patent: US2006/210630 A1, 2006 ; Title/Abstract Full Text Show Details

28 of 76

Effect (Pharmacological Data)

anti-myoclonic

Species or TestSystem (Pharmacological Data)

human

Sex

female

Route of Application

peroral

Method (Pharmacological Data)

0070] A single patient clinical trial of Xyrem.(R). for severe posthypoxic myoclonus was performed. The patient was a 37-year-old woman who suffered an anesthesia accident. After remaining in a coma, she awakened and gradually recovered, however she was completely disabled by severe myoclonic jerks that affected her voice, head, proximal arms, legs and trunk. By clinical examination she had both positive myoclonus (active jerks) and negative myoclonus (postural lapses). Her myoclonus had been treated with phenobarbital, zonisamide, clonazepam and levetiracetam, without significant improvement. Prior to the trial she was treated with clonazepam and


levetiracetam. She is allergic to penicillin, has no other known drug allergies, and is otherwise in good general health. 0074] Given the lack of significant benefit from treatment with standard anti- myoclonic agents, it was felt that empiric trials of other anti-epileptic agents were unlikely to improve her condition. She had not received piracetam; however, based on her lack of response to levetiracetam, the difficulty in obtaining piracetam, and her examination (suggesting a prominent subcortical component of myoclonus), it was not expected that she would respond well with this agent. After obtaining verbal consent from the patient and her husband, she was given approximately six ounces of wine to drink (alcohol content 14percent by volume). Within 30 minutes, dramatic improvement in myoclonus was obvious to the patient and her family. She was able to speak, to use her hands, to feed herself, and even walk with mild assistance. She was videotaped before and after the trial with alcohol. Resting myoclonic jerks resolved, her speech returned to near normal, and she was able to use her arms in fluid gestures for the first time in three years. Mild positive and negative myoclonic jerks were still present on forward arm extension, although both were improved. She was able to stand with assistance and even walk with gentle guidance. She appeared slightly euphoric from the alcohol, but was not sedated. The anti-myoclonic effect of alcohol resolved in several hours.[0075] Given the dramatic response to alcohol, a single-patient, open-label, dose- ranging trial to assess the tolerability and efficacy of GHB (Xyrem.(R)., Orphan Medical, Inc.) as a treatment for alcohol-responsive posthypoxic myoclonus was designed, which was approved by The Columbia University Medical Center Institutional Review Board. After obtaining informed consent, she was videotaped during performance of the Unified Myoclonus Rating Scale (UMRS). The UMRS is a validated clinical rating instrument that measures the severity and intensity of myoclonus and has been used in other trials of anti- myoclonic agents. Frucht S.J., et ah, Adv Neurology Vol. 89 Lippincott Williams and Wilkins, Philadelphia, 2002:361-376. The scale consists of eight sections: section I: patient questionnaire (11 items); section II: myoclonus at rest (frequency and amplitude, 16 items); EPO section III: stimulus-sensitive myoclonus (17 items); section IV: severity of myoclonus with action (frequency and amplitude, 20 items); section V: performance on functional tests (5 items); section VI: physician rating of patient's global disability (1 item); section VII: presence of negative myoclonus (1 item); section VIII: severity of negative myoclonus (1 item). Each item is rated on a scale of 0 to 4, with higher scores assigned to myoclonus of greater severity or frequency. For section III stimulus-sensitivity is either present (1) or absent (0); section VII negative myoclonus either present (1) or absent (0); and section VIII negative myoclonus absent (0) to severe (3).[0076] AU office visits and the UMRS scale were performed by the supervisory physician. The patient came to the office for five visits, each separated by two weeks (time 0, 2 weeks, 4 weeks, 6 weeks and 8 weeks). At each visit, the physician examined the Results

UMRS subscores before and during treatment wirh test compound (0-4 mg): I. Self Assessment: 15-33 (Max. UMRS score - 44); I. Global Disability: 2-3 (4); II. Myoclonic @ Rest: 1-8 (128); III. Stimulus-Sens.: 1-12 (17); IV. Action Myoclonus: 53-108 (160); V. Funct. Performance: 4-20 (20); VI. MD Global Disab.: 2-3 (4); VII. Neg. Myoclonus: 1 (1); VIII. Severity: 2 (3); figure is given.

Location

Page/Page column sheet 1; 17-23

Reference

THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK

Patent: WO2006/53186 A2, 2006 ; Title/Abstract Full Text Show Details

29 of 76

Effect (Pharmacological Data)

anti-myoclonic

Species or TestSystem (Pharmacological Data)

human

Sex

male and female

Route of Application

peroral

Method (Pharmacological Data)

Patients and Methods[0095] Five patients were enrolled in a trial from the Movement Disorders Division of Columbia University Medical Center during the fall of 2004. All patients were EPO afflicted with hyperkinetic movement disorders that responded to ethanol (defined as a noticeable change to the patient), and all were refractory to treatment with conventional medications or could not tolerate them. The Medical Center's Institutional Review Board approved the trial, and written and verbal informed consent were obtained from all patients prior to enrollment. Salient clinical features appear below and are summarized in Table 1. Table 1: Clinical features of patients with ethanolresponsive movement disorders t~duration of symptoms in years on enrollment in the trial; Dx - diagnosis; Current Rx - current medications during the trial; Past Rx - past medication exposures; PHM- -posthypoxic myoclonus; MD~myoclonus-dystonia; ET - essential tremor[0096] Patient 1 : A 37-year-old woman with a history of asthma suffered a cardiopulmonary arrest after a drug overdose at age 31, emerging from coma with severe PHM. On initial evaluation at our center at age 33, action and intention myoclonus were severe, with prominent vocal myoclonus and disabling negative myoclonic jerks of the trunk and legs. Her mother noted that ingestion of two glasses of wine noticeably improved her myoclonus, allowing her to assist in daily hygiene activities. Nine months prior to enrollment she sustained a subcortical infarct during a hospitalization for pneumonia, leaving her with a i residual left hemiparesis.[0097] Patient 2: A 25 -year-old man presented to our medical center for evaluation of a seven-year history of myoclonic jerks. His family history was notable for a paternal grandmother with torticollis and two paternal first cousins with myoclonus, all ethanol-responsive; the patient however never consumed ethanol. Genetic testing revealed a EPO mutation in the epsilon-sarcoglycan gene, confirming the diagnosis of MD. Klein C, et al. Am J Hum Genet 67:1314-9 (2000). Prominent proximal myoclonic jerks of the head, neck, and arms were triggered by voluntary actions such as pouring or writing. [0098] Patient 3: A 20-year-old man presented at age 11 to our center for initial evaluation of myoclonus that began at age 2 1A in his right foot. Myoclonic jerks of the trunk and proximal arms interfered with writing, pouring and using utensils. At age 17 he developed obsessivecompulsive symptoms that were successfully treated with paroxetine. Genetic testing revealed a mutation in the epsilon-sarcoglycan gene, confirming the diagnosis of MD. Klein C, et al. Am J Hum Genet 67:1314-9 (2000) On several occasions he consumed ethanol, observing a dose-dependent improvement in myoclonus (requiring 80 gm of alcohol to reach maximal improvement).[0099] Patient 4: A 67-year-old man with a family history of ET developed mild kinetic tremor of his hands in high school. Tremor progressively affected his ability to eat with utensils, hold a cup and write. His tremor was exquisitely alcohol-responsive with moderate tremor relief fifteen minutes after ingestion of one glass of wine, and near-complete tremor relief from two glasses. He chose not to take daily medication for his ET. Three years prior to enrollment he developed cervical dystonia that also responded to ethanol, and began receiving botulinum toxin injections. The last injection was performed seven weeks prior to enrollment.[00100] Patient 5: A 75-year-old retired general surgeon developed a kinetic tremor of his hands at age 62, forcing him to retire. Action tremor of the hands became progressively severe, causing social embarrassment when eating in public. Because of severe chronic obstructive pulmonary disease, treatment with propranolol was contraindicated, and primidone was too sedating. He was not currently taking any medications for his pulmonary disease, which might wor

Results

Myoclonus at rest and stimulus-sensitive myoclonus improved in dose-dependent fashion. Action myoclonus improved by 50percent, 57percent and 88percent respectively; the functional performance improved by 40percent, 60percent and 25percent. Patient selfassessment scores improved for patients #2 and 3, and were unchanged for patient #1. Physician global assessment scores were "mild" for patients #2 and 3 and remained unchanged, while scores decreased from severe disability (4) to moderate impairment (2) in patient #1.

Location

Page/Page column 24-34


Reference

THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK

Patent: WO2006/53186 A2, 2006 ; Title/Abstract Full Text Show Details

30 of 76

Effect (Pharmacological Data)

sustention tremor and action tremor; improvement in

Species or TestSystem (Pharmacological Data)

human

Sex

male

Route of Application

peroral

Method (Pharmacological Data)

Patients and Methods[0095] Five patients were enrolled in a trial from the Movement Disorders Division of Columbia University Medical Center during the fall of 2004. All patients were EPO afflicted with hyperkinetic movement disorders that responded to ethanol (defined as a noticeable change to the patient), and all were refractory to treatment with conventional medications or could not tolerate them. The Medical Center's Institutional Review Board approved the trial, and written and verbal informed consent were obtained from all patients prior to enrollment. Salient clinical features appear below and are summarized in Table 1. Table 1: Clinical features of patients with ethanolresponsive movement disorders t~duration of symptoms in years on enrollment in the trial; Dx - diagnosis; Current Rx - current medications during the trial; Past Rx - past medication exposures; PHM- -posthypoxic myoclonus; MD~myoclonus-dystonia; ET - essential tremor[0096] Patient 1 : A 37-year-old woman with a history of asthma suffered a cardiopulmonary arrest after a drug overdose at age 31, emerging from coma with severe PHM. On initial evaluation at our center at age 33, action and intention myoclonus were severe, with prominent vocal myoclonus and disabling negative myoclonic jerks of the trunk and legs. Her mother noted that ingestion of two glasses of wine noticeably improved her myoclonus, allowing her to assist in daily hygiene activities. Nine months prior to enrollment she sustained a subcortical infarct during a hospitalization for pneumonia, leaving her with a i residual left hemiparesis.[0097] Patient 2: A 25 -year-old man presented to our medical center for evaluation of a seven-year history of myoclonic jerks. His family history was notable for a paternal grandmother with torticollis and two paternal first cousins with myoclonus, all ethanol-responsive; the patient however never consumed ethanol. Genetic testing revealed a EPO mutation in the epsilon-sarcoglycan gene, confirming the diagnosis of MD. Klein C, et al. Am J Hum Genet 67:1314-9 (2000). Prominent proximal myoclonic jerks of the head, neck, and arms were triggered by voluntary actions such as pouring or writing. [0098] Patient 3: A 20-year-old man presented at age 11 to our center for initial evaluation of myoclonus that began at age 2 1A in his right foot. Myoclonic jerks of the trunk and proximal arms interfered with writing, pouring and using utensils. At age 17 he developed obsessivecompulsive symptoms that were successfully treated with paroxetine. Genetic testing revealed a mutation in the epsilon-sarcoglycan gene, confirming the diagnosis of MD. Klein C, et al. Am J Hum Genet 67:1314-9 (2000) On several occasions he consumed ethanol, observing a dose-dependent improvement in myoclonus (requiring 80 gm of alcohol to reach maximal improvement).[0099] Patient 4: A 67-year-old man with a family history of ET developed mild kinetic tremor of his hands in high school. Tremor progressively affected his ability to eat with utensils, hold a cup and write. His tremor was exquisitely alcohol-responsive with moderate tremor relief fifteen minutes after ingestion of one glass of wine, and near-complete tremor relief from two glasses. He chose not to take daily medication for his ET. Three years prior to enrollment he developed cervical dystonia that also responded to ethanol, and began receiving botulinum toxin injections. The last injection was performed seven weeks prior to enrollment.[00100] Patient 5: A 75-year-old retired general surgeon developed a kinetic tremor of his hands at age 62, forcing him to retire. Action tremor of the hands became progressively severe, causing social embarrassment when eating in public. Because of severe chronic obstructive pulmonary disease, treatment with propranolol was contraindicated, and primidone was too sedating. He was not currently taking any medications for his pulmonary disease, which might wor

Results

The dose-dependent improvement in sustention tremor and action tremor of 79percent in patient #4, and 48percent in patient #5 was obtained. Blinded rating of the severity of torticollis in patient #4 decreased from "moderate" to "mild" at the 1 gm twice-daily dose. After 2 gm dose, tremor amplitude was markedly diminished. Patient #5's kinetic tremor were more severe. Although still present after receiving 2 gm dose, the amplitude has diminished and voluntary movements are more fluid.

Location

Page/Page column 24-34

Reference

THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK

Patent: WO2006/53186 A2, 2006 ; Title/Abstract Full Text Show Details

31 of 76

Effect (Pharmacological Data)

myoclonus; effect on

Species or TestSystem (Pharmacological Data)

human

Sex

male and female

Route of Application

peroral

Method (Pharmacological Data)

Clinical trial[00117] Twenty patients age 18 or older were recruited from a clinical practice at the Movement Disorders Division of Columbia University Medical Center. Eligible patients with medication-refractory, ethanol-responsive myoclonus (6 PHM, 3 MD, 2 PME) or ET (9 patients) (Table 1) were offered enrollment from February 2004 to March 2005. The medical center's institutional review board approved the protocol, and written informed consent was obtained from all participants. AU had myoclonus or ET that improved (by self-report) with ingestion of ethanol. All patients were medication-refractory, defined as obtaining inadequate benefit from best medical treatment or being unable to tolerate treatment. The dose and timing of other medications were kept constant before and during the trial. Table 1 : Clinical features of the twenty patients are summarized in this table. Dx: diagnosis; Age: in years at time of enrollment1 Sx1 symptom duration in years at time of enrollment; Current meds: continued at time of enrollment; Past meds: medications taken in the past for treatment of involuntary movements (excluding those currently being administered), Rx?: decision (Yes or No) to continue treatment with sodium oxybate after completion of the trial; Dose: total daily dose of sodium oxybate on completion of the trial[00118] Twelve men and 8 women enrolled. Results from patients No.6, and No.s 1, 2, 7, 12, and 13 were reported previously. Frucht, SJ., et al. Mov Disord 20:745-51(2005); Frucht, SJ., et al. Mov Disord 20:1330-7(2005). Mean age/symptom duration was 43.9 yrs/12.3 yrs (myoclonus) and 71.2 yrs/26.7 yrs (ET).


Patients with myoclonus were examined and videotaped at each visit using the Unified Myoclonus Rating Scale (UMRS), and patients with ET were examined and videotaped using the modified Washington Heights hrwood Genetic Essential Tremor Rating Scale (WHIGET; Appendix I). Frucht, SJ., et al. Mov Disord 20: 1330-7(2005). After initial baseline examination and videotaping, patients took 1 gm of sodium oxybate by mouth (2 ml of the standard 0.5 gm/ml solution dissolved in 60 ml of water), and one hour later the videotaped examination was repeated. Patients were maintained on a dose of 1 gm T.I.D. (taken before meals) until their next office visit two weeks later, when the examination and videotaping were repeated one hour after receiving 1.5 gm of sodium oxybate. Subsequent visits and dose titrations at two-week intervals were EPO repeated until the maximum dose was reached (3 gm T.I.D), patients were satisfied with the results of treatment, or until they developed side effects that they viewed as troublesome. Dosing for patients No. 1, 2, 6, 7, 12, and 13 was slightly different (1 gm BID, with dose increments of 2 gm to maximum dose of 4 gm BID), but office visits and videotaping protocol were otherwise identical. Sections 1-6 of the UMRS appear above. Full details regarding the scale are available in reference 16. Higher scores indicate more severe involuntary movements. The range for each section appears in brackets { } .Ratings and data analyses[00119] The entire videotape segments and writing samples from each visit were copied and randomly ordered, and identifying features that might reveal trial order or drug dose were removed. A blinded movement disorder neurologist scored each videotape segment using the UMRS or the WHIGET. Subscores for each visit were calculated as described previously. Frucht, S.J., et al. Mov Disord 20: 1330-7(2005). Based on data from the first two ET cases, and assuming alpha = 0.05, power = 80percent, and a 25percent reduction in post-treatment tremor severity, we calculated that eight ET cases were required. A similar number of myoclonus patients would provide > 80percent power to detect a 25percent reduction in the severity of post-treatment action myoclonus. Paired t tests were performed for scores pre- and posttreatment.Results[00120] A patient with ET (patient No.15) Results

Individ. dose, mg - 0 - 3.0. Myoclonus at rest score: 0.6 - 7.4; Stimulus-sensitive myoclonus score: 1.0 - 5.8; Action myoclonus score: 26.2 - 45.3; Functional performanc score: 6.0 - 12.9. Maximal improvement occurred at dose 2.5 gm.

Location

Page/Page column 34-40

Reference

THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK

Patent: WO2006/53186 A2, 2006 ; Title/Abstract Full Text Show Details

32 of 76

Effect (Pharmacological Data)

essential tremor (ET); effect on

Species or TestSystem (Pharmacological Data)

human

Sex

male and female

Route of Application

peroral

Method (Pharmacological Data)

Clinical trial[00117] Twenty patients age 18 or older were recruited from a clinical practice at the Movement Disorders Division of Columbia University Medical Center. Eligible patients with medication-refractory, ethanol-responsive myoclonus (6 PHM, 3 MD, 2 PME) or ET (9 patients) (Table 1) were offered enrollment from February 2004 to March 2005. The medical center's institutional review board approved the protocol, and written informed consent was obtained from all participants. AU had myoclonus or ET that improved (by self-report) with ingestion of ethanol. All patients were medication-refractory, defined as obtaining inadequate benefit from best medical treatment or being unable to tolerate treatment. The dose and timing of other medications were kept constant before and during the trial. Table 1 : Clinical features of the twenty patients are summarized in this table. Dx: diagnosis; Age: in years at time of enrollment1 Sx1 symptom duration in years at time of enrollment; Current meds: continued at time of enrollment; Past meds: medications taken in the past for treatment of involuntary movements (excluding those currently being administered), Rx?: decision (Yes or No) to continue treatment with sodium oxybate after completion of the trial; Dose: total daily dose of sodium oxybate on completion of the trial[00118] Twelve men and 8 women enrolled. Results from patients No.6, and No.s 1, 2, 7, 12, and 13 were reported previously. Frucht, SJ., et al. Mov Disord 20:745-51(2005); Frucht, SJ., et al. Mov Disord 20:1330-7(2005). Mean age/symptom duration was 43.9 yrs/12.3 yrs (myoclonus) and 71.2 yrs/26.7 yrs (ET). Patients with myoclonus were examined and videotaped at each visit using the Unified Myoclonus Rating Scale (UMRS), and patients with ET were examined and videotaped using the modified Washington Heights hrwood Genetic Essential Tremor Rating Scale (WHIGET; Appendix I). Frucht, SJ., et al. Mov Disord 20: 1330-7(2005). After initial baseline examination and videotaping, patients took 1 gm of sodium oxybate by mouth (2 ml of the standard 0.5 gm/ml solution dissolved in 60 ml of water), and one hour later the videotaped examination was repeated. Patients were maintained on a dose of 1 gm T.I.D. (taken before meals) until their next office visit two weeks later, when the examination and videotaping were repeated one hour after receiving 1.5 gm of sodium oxybate. Subsequent visits and dose titrations at two-week intervals were EPO repeated until the maximum dose was reached (3 gm T.I.D), patients were satisfied with the results of treatment, or until they developed side effects that they viewed as troublesome. Dosing for patients No. 1, 2, 6, 7, 12, and 13 was slightly different (1 gm BID, with dose increments of 2 gm to maximum dose of 4 gm BID), but office visits and videotaping protocol were otherwise identical. Sections 1-6 of the UMRS appear above. Full details regarding the scale are available in reference 16. Higher scores indicate more severe involuntary movements. The range for each section appears in brackets { } .Ratings and data analyses[00119] The entire videotape segments and writing samples from each visit were copied and randomly ordered, and identifying features that might reveal trial order or drug dose were removed. A blinded movement disorder neurologist scored each videotape segment using the UMRS or the WHIGET. Subscores for each visit were calculated as described previously. Frucht, S.J., et al. Mov Disord 20: 1330-7(2005). Based on data from the first two ET cases, and assuming alpha = 0.05, power = 80percent, and a 25percent reduction in post-treatment tremor severity, we calculated that eight ET cases were required. A similar number of myoclonus patients would provide > 80percent power to detect a 25percent reduction in the severity of post-treatment action myoclonus. Paired t tests were performed for scores pre- and posttreatment.Results[00120] A patient with ET (patient No.15)

Results

Individ. dose, mg: 0 - 2. Kinetic tremor score: 8.8 - 15.4; postural tremor score: 1.1 - 2.4. Maximal improvement occurred at dose 1,5 mg; figure is given.

Location

Page/Page column sheet 4; 34-40

Reference

THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK

Patent: WO2006/53186 A2, 2006 ; Title/Abstract Full Text Show Details

33 of 76

Effect (Pharmacological Data)

patient with ARG; effect on


Species or TestSystem (Pharmacological Data)

human

Method (Pharmacological Data)

Example 54A patient with ARG was chronically treated with the Class III GABAnergic agent alprazolam 3 mg, the Class IV agent Zolpidem 10 mg, the Class V agent gabapentin 300 mg, and either the Class II agent NaGHB 5.25 grams or the Class I agent red wine about 1000 ml prior to sleep on a nightly basis and had marked reduction in fatigue and markedly increased motivation on these regimens. The patient was then switched to monotherapy using only NaGHB 4.5 grams prior to the intended sleep time and a second dose of 4.5 grams four hours after the first. The patient complained that the first dose did not induce sleep at all but did induce a state of near stupor until the second dose, and the second dose induced sleep for only two hours. There was no improvement on monotherapy with NaGHB. The patient was EPO switched back to treatment with multiple GABAnergic agents and again had dramatic reduction in fatigue. On a scale from 0 to 10 where 10 is the most tired, the patient rated the fatigue at 10 without treatment, 3 to 4 with treatment on multiple GABAnergic agents, and 10 on monotherapy with NaGHB.; Example 86A patient had a sleeping disorder. Overnight polysomnography had shown minimal obstructive sleep apnea with 2 apneas per hour of sleep. The patient was placed on a regimen of the Class III agent alprazolam, the Class IV agent Zolpidem, the Class V agent gabapentin, and the Class II agent the sodium salt of gamma- hydroxyl butyric acid (GHB), which were administered prior to sleep for the treatment of sleeping disorders. The initial dose of GHB was prescribed as 2.25 grams prior to sleep and repeat dose of 2.25 grams to be taken 2.5 to 4 hours after sleep onset. Doses were slowly increased to a regimen of 3 mg alprazolam, 10 mg Zolpidem, 200 mg gabapentin, and 5.25 grams NaGHB prior to sleep. However, the patient found that he slept roughly six hours when given the alprazolam, Zolpidem, gabapentin, and 3 grams of NaGHB, and he instead took the second GHB dose upon awakening, not 2.5 to 4 hours after sleep onset as prescribed. The patient eventually increased the first dose of NaGHB to 5.25 grams prior to sleep, and sometimes took a second dose of 3.75 grams upon awakening. The second dose usually did not induce sleep.

Results

The patient complained that the first dose did not induce sleep at all but did induce a state of near stupor until the second dose, and the second dose induced sleep for only two hours. There was no improvement on monotherapy with NaGHB. The patient eventually increased the first dose of NaGHB to 5.25 grams prior to sleep, and sometimes took a second dose of 3.75 grams upon awakening. The second dose usually did not induce sleep.

Location

Page/Page column 79-80; 91-92

Reference

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

34 of 76

35 of 76

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intravenous

Kind of Dosing (Pharmacological Data)

dissolved in water; loading dose 100-400 mg/kg followed by infusion of 108-208 mg/h/kg for 3 h

Method (Pharmacological Data)

animals with chronic cannulaes into jugular and femoral veins and bladders were treated with title comp.; blood and urine samples collected; title comp. levels assayed using LC/MS/MS; CL and CLR calculated

Further Details (Pharmacological Data)

LC/MS/MS: liquid chromatography-tandem mass spectrometry; CL and CLR: total and renal clearances, respectively

Results

CLR and CL were dose-dependent, CLR values of medium (51.8 ml/h/kg) and high (97.1 ml/h/kg) doses were significantly higher than that of low dose (14.9 ml/h/kg), whereas CL values were significantly lower than that of low dose (table, figure)

Reference

Morris, Marilyn E.; Hu, Ke; Wang, Qi

Journal of Pharmacology and Experimental Therapeutics, 2005 , vol. 313, # 3 p. 1194 - 1202 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intravenous

Kind of Dosing (Pharmacological Data)

dissolved in water; loading dose 200 mg/kg followed by infusion of 128 mg/h/kg for 3 h

Method (Pharmacological

animals with chronic cannulaes into jugular and femoral veins and bladders were treated with title comp.; blood and urine samples collected; title comp. levels (CSS) assayed using LC/MS/MS; CL and CLR calculated


Data)

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Further Details (Pharmacological Data)

in absence or presence of various modulators (L-lactate, pyruvate, D-mannitol, sodium bicarbonate) or normal saline; LC/MS/MS: liquid chromatography-tandem mass spectrometry; CL and CLR: total and renal clearances, respectively

Results

CSS, CL and CLR values for title comp. were 0.37 mg/ml, 342 ml/h/kg and 63.3 ml/h/kg, respectively; in presence of all tested modulators except normal saline these values were significantly increased (table, figure)

Reference

Morris, Marilyn E.; Hu, Ke; Wang, Qi

Journal of Pharmacology and Experimental Therapeutics, 2005 , vol. 313, # 3 p. 1194 - 1202 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pH levels; induction of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intravenous

Concentration (Pharmacological Data)

200 mg/kg

Kind of Dosing (Pharmacological Data)

dissolved in water; loading dose 200 mg/gk followed by infusion of 128 mg/h/kg for 3 h

Method (Pharmacological Data)

animals with chronic cannulaes into jugular and femoral veins and bladders were treated with title comp.; urine samples collected; changes in pH determined over time interval of 4-6 h

Further Details (Pharmacological Data)

in absence or presence various modulators (L-lactate, pyruvate, D-mannitol, sodium bicarbonate) or normal saline

Results

title comp. increased urine pH value from 6.54 at 1 h to 8.27 at 6 h in presence or absence of tested modulators (figure)

Reference

Morris, Marilyn E.; Hu, Ke; Wang, Qi

Journal of Pharmacology and Experimental Therapeutics, 2005 , vol. 313, # 3 p. 1194 - 1202 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics; effect on

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intravenous

Concentration (Pharmacological Data)

100 - 400 mg/kg

Kind of Dosing (Pharmacological Data)

dissolved in water; loading dose 100-400 mg/kg followed by 108-208 mg/h/kg for 3 h

Method (Pharmacological Data)

animals were treated with inulin (60 mg/kg followed by 100 mg/kg/h for 3 h) and title comp.; blood and urine samples collected; changes in inulin concentrations determined by colorimetry

Comment (Pharmacological Data)

No effect

Reference

Morris, Marilyn E.; Hu, Ke; Wang, Qi

Journal of Pharmacology and Experimental Therapeutics, 2005 , vol. 313, # 3 p. 1194 - 1202 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or Test-

Sprague-Dawley rat


System (Pharmacological Data)

39 of 76

40 of 76

Sex

male

Route of Application

intravenous

Kind of Dosing (Pharmacological Data)

dissolved in water; loading dose 100, 200, 400 mg/kg followed by infusion of 108, 128, 208 mg/h/kg, resp., for 3 h

Method (Pharmacological Data)

animals with chronic cannulaes into jugular and femoral veins and bladders were treated with title comp.; blood samples collected; title comp. levels assayed using LC/MS/MS

Further Details (Pharmacological Data)

LC/MS/MS: liquid chromatography-tandem mass spectrometry

Results

steady-state plasma concentrations of title comp. were 0.22, 0.43 and 0.68 mg/ml at low, medium and high doses, respectively (table)

Reference

Morris, Marilyn E.; Hu, Ke; Wang, Qi

Journal of Pharmacology and Experimental Therapeutics, 2005 , vol. 313, # 3 p. 1194 - 1202 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

human

Sex

male and female

Route of Application

peroral

Concentration (Pharmacological Data)

4.5 g

Kind of Dosing (Pharmacological Data)

given in 120 ml of water as single dose only or after 8-wk treatment with title comp. twice daily (2.25 g at bedtime and 4 h later)

Method (Pharmacological Data)

title comp. given to 13 patients with narcolepsy at bedtime as acute dose (AD) or after chronic dosing (CD); plasma title comp. conc. measured up to 7 h with LC/MS/MS; Cmax, tmax, AUC, CL/F, and Vz/F determined by noncompartmental analysis

Further Details (Pharmacological Data)

Cmax: peak concentration; tmax: time to Cmax; AUC: area under the curve from 0 to infinity; CL/F: plasma clearance; Vz/F: volume of distribution; LC/MS/MS: liquid chromatography/tandem mass-spectrometry

Half-life Time (Pharmacological Data)

0.72 h

Results

Cmax of title comp. at AD was 90.0 mg/ml, tmax 0.87 h, AUC 225.6 mg*h/ml, CL/F 4.0 ml/min/kg, and Vz/F 225.9 ml/kg; after CD, Cmax increased to 103.5 mg/ml and AUC to 253.8 mg*h/ml; other parameters unchanged

Reference

Borgen, Lowell A.; Okerholm, Richard A.; Lai, Allen; Scharf, Martin B.

Journal of Clinical Pharmacology, 2004 , vol. 44, # 3 p. 253 - 257 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

toxicity

Species or TestSystem (Pharmacological Data)

human

Sex

male and female

Route of Application

peroral

Concentration (Pharmacological Data)

4.5 g

Kind of Dosing (Pharmacological

given in 120 ml of water as single dose only or after 8-wk treatment with title comp. twice daily (2.25 g at bedtime and 4 h later)


Data)

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43 of 76

Method (Pharmacological Data)

title comp. given to 13 patients with narcolepsy at bedtime (21:00 h) as acute dose (AD) or after chronic dosing (CD); vital signs (VSs) monitored and adverse events (AEs) recorded

Results

title comp. was well tolerated: no serious AEs (headache in 3 patients, enuresis in 2 ones, leg cramps in one); no changes in VSs

Reference

Borgen, Lowell A.; Okerholm, Richard A.; Lai, Allen; Scharf, Martin B.

Journal of Clinical Pharmacology, 2004 , vol. 44, # 3 p. 253 - 257 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

SPF Wistar rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

100 - 300 mg/kg

Kind of Dosing (Pharmacological Data)

300 mg/kg 2 h after ischemia-reperfusion followed by 100 mg/kg twice daily for the following 10 d; dissolved in saline, injected in volume of 2 ml/kg

Method (Pharmacological Data)

rats subjected to 30-min global cerebral ischemia (four vessel occlusion model) followed by reperfusion and treated witht title comp.; sensory-motor performance (orientation, limb reflexes, coordinated limb) determined 51 and 63 d after ischemia

Further Details (Pharmacological Data)

control: saline

Results

title comp. afforded protection either 51 or 63 d after ischemia

Reference

Ottani, Alessandra; Vergoni, Anna Valeria; Saltini, Sabrina; Mioni, Chiara; Giuliani, Daniela; Bartiromo, Marta; Zaffe, Davide; Botticelli, Annibale R.; Ferrari, Anna; Bertolini, Alfio; Genedani, Susanna

European Journal of Pharmacology, 2004 , vol. 485, # 1-3 p. 183 - 191 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

SPF Wistar rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

100 - 300 mg/kg

Kind of Dosing (Pharmacological Data)

300 mg/kg 2 h after ischemia-reperfusion followed by 100 mg/kg twice daily for 10 d; dissolved in saline, injected in volume of 2 ml/kg

Method (Pharmacological Data)

rats subjected to 30-min global cerebral ischemia (four vessels occlusion model) followed by reperfusion and treated with title comp.; spatial learning and memory determined using Morris water maze test

Further Details (Pharmacological Data)

control: saline

Results

performance of treated rats was better than control from 2 to 5 d of acquisition session; similar results obtained for reversal learning, lasting 3 d and started 10 d after the termination of the first 5-d acquisition session

Reference

Ottani, Alessandra; Vergoni, Anna Valeria; Saltini, Sabrina; Mioni, Chiara; Giuliani, Daniela; Bartiromo, Marta; Zaffe, Davide; Botticelli, Annibale R.; Ferrari, Anna; Bertolini, Alfio; Genedani, Susanna

European Journal of Pharmacology, 2004 , vol. 485, # 1-3 p. 183 - 191 Title/Abstract Full Text View citing articles Show Details

Effect

neuroprotective


(Pharmacological Data)

44 of 76

45 of 76

Species or TestSystem (Pharmacological Data)

SPF Wistar rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

100 - 300 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline, injected in volume of 2 ml/kg; administered at 300 mg/kg 2 h after ischemia-reperfusion, then 100 mg/kg twice daily for 10 d

Method (Pharmacological Data)

rats subjected to 30-min global cerebral ischemia (four vessels occlusion model) followed by reperfusion; title comp. administered; rats killed 63 d after; brain sectioned; hippocampal slides examined by histological and immunohistochemical methods

Further Details (Pharmacological Data)

control: saline

Results

treated rats had moderate degree of ischemic area with the presence of living neurons among necrotic ones; predominant glial element in ischemic areas was protoplasmic astrocyte; ischemic area was decreased

Reference

Ottani, Alessandra; Vergoni, Anna Valeria; Saltini, Sabrina; Mioni, Chiara; Giuliani, Daniela; Bartiromo, Marta; Zaffe, Davide; Botticelli, Annibale R.; Ferrari, Anna; Bertolini, Alfio; Genedani, Susanna

European Journal of Pharmacology, 2004 , vol. 485, # 1-3 p. 183 - 191 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

56 - 560 mg/kg

Kind of Dosing (Pharmacological Data)

administered in a volume of 0.1 to 1 ml

Method (Pharmacological Data)

substitutional assay; rats trained to discriminate baclofen vs saline and to press appropriate lever; the level of pressing on drug-associated lever determined 15 min after administration of title comp. during a 15-min test session

Further Details (Pharmacological Data)

3.2 mg/kg dose of baclofen occasioned 81.2 percent of drug-associated lever responding

Results

title comp. dose-dependently increased responding on drug-associated lever (76.5 percent maximum for 320 mg/kg dose); 560 mg/kg dose markedly decreased the average response rate

Reference

Carter; Unzeitig; Wu; Chen; Coop; Koek; France, Charles P.

Journal of Pharmacology and Experimental Therapeutics, 2004 , vol. 309, # 2 p. 540 - 547 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration

56 - 320 mg/kg


(Pharmacological Data)

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47 of 76

Kind of Dosing (Pharmacological Data)

administered in a volume of 0.1 to 1 ml

Method (Pharmacological Data)

substitutional assay; rats trained to discriminate diazepam vs saline and to press appropriate lever; the level of pressing on drug-associated lever determined 15 min after administration of title comp. during a 15-min test session

Further Details (Pharmacological Data)

1.0 mg/kg dose of diazepam occasioned 93.0 percent of drug-associated lever responding

Results

title comp. occasioned less than 5 percent of drug-appropriate responding

Reference

Carter; Unzeitig; Wu; Chen; Coop; Koek; France, Charles P.

Journal of Pharmacology and Experimental Therapeutics, 2004 , vol. 309, # 2 p. 540 - 547 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transport

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Concentration (Pharmacological Data)

2.8E-05 - 40 mmol/l

Method (Pharmacological Data)

250-250 g adult rats anesthetized; in situ brain perfusion performed with physiological perfusate containing 3H-labeled title comp. for 1560 s (pH ca. 7.4, O2:CO2 = 95:5, 37 deg C), then rats sacrificed by decapitation; dissected brains analyzed by LSC

Further Details (Pharmacological Data)

LSC: liquid scintillation counting; Km: Michaelis-Menten half-saturation const.; Vmax: max. transport rate of title comp. influx; CLns: nonsaturable clearance representing passive diffusion

Type (Pharmacological Data)

Km

Value of Type (Pharmacological Data)

11.0 mmol/l

Results

title comp. exhibited carrier-mediated transport across the blood-brain barrier consistent with high-capacity, low-affinity transporter; Vmax = 709 nmol/min/g; CLns = 0.019 cm3/min/g

Reference

Bhattacharya, Indranil; Boje, Kathleen M. K.

Journal of Pharmacology and Experimental Therapeutics, 2004 , vol. 311, # 1 p. 92 - 98 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transport

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Concentration (Pharmacological Data)

0.028 μmol/l

Method (Pharmacological Data)

250-250 g adult rats anesthetized; in situ brain perfusion performed with physiological perfusate containing 3H-labeled title comp. for 1560 s (pH ca. 7.4, O2:CO2 = 95:5, 37 deg C), then rats sacrificed by decapitation; dissected brains analyzed by LSC

Further Details (Pharmacological Data)

LSC: liquid scintillation counting; further investigation on mechanism of transport by substrate inhibitor studies (coperfusion with shortand medium-chain fatty acids, organic anions, dicarboxylic acids)

Results

carrier-mediated transport of title comp. through the blood-brain barrier suggested to proceed via monocarboxylate transporter isoform

Reference

Bhattacharya, Indranil; Boje, Kathleen M. K.

Journal of Pharmacology and Experimental Therapeutics, 2004 , vol. 311, # 1 p. 92 - 98 Title/Abstract Full Text View citing articles Show Details


48 of 76

49 of 76

50 of 76

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

100 - 560 mg/kg

Kind of Dosing (Pharmacological Data)

dissolved in saline

Method (Pharmacological Data)

adult animals trained to respond under fixed-ratio schedule of food presentation administered with cumulative doses of title comp.; relative potency to decrease rate of responding evaluated over 6 months; dose-effect curves constructed

Further Details (Pharmacological Data)

reference comp.: diazepam, baclofen, γ-butyrolactone (GBL), 1,4-butanediol (1,4-BDL)

Type (Pharmacological Data)

ED50

Value of Type (Pharmacological Data)

213.4 - 218.4 mg/kg

Results

similarly with reference compounds, title comp. dose-dependently decreased rate of responding; rank-order potency of rate decreasing effects was: diazepam = baclofen > GBL > 1,4-BDL = title comp. (figure, table)

Reference

Carter, Lawrence P.; Wu, Huifang; Chen, Weibin; Cruz, Christopher M.; Lamb; Koek, Wouter; Coop, Andy; France, Charles P.

Journal of Pharmacology and Experimental Therapeutics, 2004 , vol. 308, # 1 p. 182 - 188 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

100 - 320 mg/kg

Kind of Dosing (Pharmacological Data)

dissolved in saline

Method (Pharmacological Data)

adult animals trained to respond under fixed-ratio schedule of food presentation administered with title comp.; time course of ratedecreasing effects determined over 120 min

Further Details (Pharmacological Data)

reference comp.: diazepam, baclofen, γ-butyrolactone (GBL), 1,4-butanediol (1,4-BDL)

Results

similarly with reference compounds, title comp. decreased responding 20 min after administration; duration of action of title comp., diazepam and GBL was shorter than that of 1,4-BDL and baclofen (figure)

Reference

Carter, Lawrence P.; Wu, Huifang; Chen, Weibin; Cruz, Christopher M.; Lamb; Koek, Wouter; Coop, Andy; France, Charles P.

Journal of Pharmacology and Experimental Therapeutics, 2004 , vol. 308, # 1 p. 182 - 188 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological

Sprague-Dawley rat


Data)

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52 of 76

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

100 - 560 mg/kg

Kind of Dosing (Pharmacological Data)

dissolved in saline

Method (Pharmacological Data)

adult animals trained to respond under fixed-ratio schedule of food presentation administered with title comp. alone or in combinations with different antagonists; changes in rate of responding evaluated

Further Details (Pharmacological Data)

antagonists: (2E)-(5-hydroxy-5,7,8,9-tetrahydro-6H-benzo<a><7>annulen-6-ylidene ethanoic acid, p-3-aminopropyl-p-diethoxymethyl phosphinic acid (CGP35348) and flumazenil; reference comp.: baclofen and diazepam

Results

title comp. alone and in combinations with antagonists dose-dependently decreased rate of responding; rate-decreasing effects of baclofen and diazepam were attenuated in combinations with CGP35348 and flumazenil, respectively (figure, table)

Reference

Carter, Lawrence P.; Wu, Huifang; Chen, Weibin; Cruz, Christopher M.; Lamb; Koek, Wouter; Coop, Andy; France, Charles P.

Journal of Pharmacology and Experimental Therapeutics, 2004 , vol. 308, # 1 p. 182 - 188 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Concentration (Pharmacological Data)

200 mg/kg

Kind of Dosing (Pharmacological Data)

dissolved in sterile water

Method (Pharmacological Data)

rats were trained to discriminate title comp. from saline using two-lever food-reinforced procedure under fixed ratio schedule; the role of GABAA, GABAB and other receptors in the discriminative stimulus effect of title comp. investigated

Further Details (Pharmacological Data)

GABAA and GABAB agonists, μ-opioid agonist, N-methyl-D-aspartate agonist, GHB antagonist (NCB-382), and GABAB antagonist (CGP 35348) were used; GHB: γ-hydroxybutyrate; GABA: γ-aminobutyric acid; pretreatment time up to 90 min

Results

rats discriminated title comp. from saline after a 23-41 training sessions; 83.1 percent title comp.-appropriate responding observed; effect evident at 15 min; no effect at 60 min; GABAB mechanism in discriminative stimulus effect of title comp. established

Reference

Carter, Lawrence P.; Flores, Lauren R.; Wu, Huifang; Chen, Weibin; Unzeitig, Andrew W.; Coop, Andy; France, Charles P.

Journal of Pharmacology and Experimental Therapeutics, 2003 , vol. 305, # 2 p. 668 - 674 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Endpoint of Effect (Pharmacological Data)

discriminative stimulus effects

Species or TestSystem (Pharmacological Data)

Macaca mulatta, rhesus monkey

Sex

male and female

Route of Application

subcutaneous

Concentration (Pharmacological Data)

100 - 1000 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. was dissolved in sterile distilled water


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Method (Pharmacological Data)

diazepam-treated flumazenil discriminating monkeys (training cycles) injected with title comp. during first minute of first test cycle followed by cumulative doses of flumazenil during subsequent cycles; percent DR and response rate ( percent of control) calculated

Further Details (Pharmacological Data)

DR: drug responding ( percent responding on flumazenil lever); control response rate represents average of five saline sessions immediately preceding a test; flumazenil 0.32 mg/kg for three monkeys or 0.1 mg/kg for two monkeys, s.c.

Results

title comp. did not substitute for flumazenil and did not substantially modify response rate; title comp. did not modify the discriminative stimulus effects of flumazenil

Reference

McMahon, Lance R.; France, Charles P.

Journal of Pharmacology and Experimental Therapeutics, 2003 , vol. 304, # 1 p. 109 - 120 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Endpoint of Effect (Pharmacological Data)

discriminative stimulus effects

Species or TestSystem (Pharmacological Data)

Macaca mulatta, rhesus monkey

Sex

male and female

Route of Application

subcutaneous

Concentration (Pharmacological Data)

100 - 560 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. was dissolved in sterile distilled water

Method (Pharmacological Data)

midazolam discriminating monkeys (midazolam training cycles) injected with title comp. during first minute of first test cycle followed by cumulative doses of midazolam during subsequent cycles; percent DR and response rate ( percent of control) calculated

Further Details (Pharmacological Data)

DR: drug responding ( percent responding on midazolam lever); control response rate represents average of five saline sessions immediately preceding a test; substitution for midazolam was defined as >= 80 percent responding on midazolam-appropriate lever

Results

title comp. (560 mg/kg) shifted the midazolam dose-effect curve leftward in two monkeys (including monkey that responded on midazolam after title comp. alone) and disrupted responding in third monkey, and decreased group average response rate

Reference

McMahon, Lance R.; France, Charles P.

Journal of Pharmacology and Experimental Therapeutics, 2003 , vol. 304, # 1 p. 109 - 120 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Endpoint of Effect (Pharmacological Data)

discriminative stimulus effects

Species or TestSystem (Pharmacological Data)

Macaca mulatta, rhesus monkey

Sex

male and female

Route of Application

subcutaneous

Concentration (Pharmacological Data)

560 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. was dissolved in sterile distilled water

Method (Pharmacological Data)

midazolam discriminating monkeys (midazolam training cycles) injected with title comp. during first minute of first test cycle followed by saline or sham injection on subsequent cycles; percent DR and response rate ( percent of control) calculated

Further Details (Pharmacological

DR: drug responding ( percent responding on midazolam lever); control response rate represents average of five saline sessions immediately preceding a test; substitution for midazolam was defined as >= 80 percent responding on midazolam-appropriate lever


Data)

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Results

single dose of title comp. occasioned saline-lever responding in two monkeys and a maximum of 70 percent midazolam-lever responding 75 to 90 min after injection in third, and did not systematically alter response rate in any monkey

Reference

McMahon, Lance R.; France, Charles P.

Journal of Pharmacology and Experimental Therapeutics, 2003 , vol. 304, # 1 p. 109 - 120 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

human

Sex

male and female

Route of Application

peroral

Concentration (Pharmacological Data)

4.5 g

Kind of Dosing (Pharmacological Data)

500 mg/ml of title comp. oral solution in overnight fasted condition or with breakfast (high-fat meal)

Method (Pharmacological Data)

title comp. administered after an overnight fast or 30 min after a standardized high-fat meal; blood samples collected before and 10 min 10 h after dosing and urine at 1 to 10 h after dosing; serum and urine conc. of title comp. measured by LC/MS/MS

Further Details (Pharmacological Data)

pharmacokinetic parameters were calculated; healthy volunteers; Cmax: maximum conc.; AUC: area under conc.-time curve; RC: renal clearance

Half-life Time (Pharmacological Data)

0.57 - 0.68 h

Results

food significantly affected systemic exposure of title comp.: absorption and peak plasma conc. were slower and observed later, Cmax decreased more than 2-fold, mean AUC0-infinite was significantly lower; RC tended to be higher after fat meal (table)

Reference

Borgen, Lowell A.; Okerholm, Richard; Morrison, Dennis; Lai, Allen

Journal of Clinical Pharmacology, 2003 , vol. 43, # 1 p. 59 - 65 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

human

Sex

male and female

Route of Application

peroral

Concentration (Pharmacological Data)

4.5 g

Kind of Dosing (Pharmacological Data)

500 mg/ml oral solution of title comp.; 2 h after light meal

Method (Pharmacological Data)

title comp. administered; blood samples collected before and 10 min - 8 h after title comp. dosing; urine was collected before and during 8 h after title comp. dosing; serum and urine conc. of title comp. were measured by LC/MS/MS

Further Details (Pharmacological Data)

pharmacokinetic parameters were calculated; healthy volunteers; data from male and female (18/18) compared; Cmax: maximum conc.; AUC: area under conc.-time curve; CLR: renal clearance

Half-life Time (Pharmacological Data)

0.61 - 0.65 h

Results

parameters for male/female: Cmax = 88.3/83 μg/ml, CLR = 484/510 ml/h, AUC0-infinite = 241/233 μg*h/ml; there were no differences between male and female subjects for any pharmacokinetic parameter; urinary excretion ranged from 1 percent to 7 percent

Reference

Borgen, Lowell A.; Okerholm, Richard; Morrison, Dennis; Lai, Allen

Journal of Clinical Pharmacology, 2003 , vol. 43, # 1 p. 59 - 65


Title/Abstract Full Text View citing articles Show Details

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Effect (Pharmacological Data)

toxicity

Species or TestSystem (Pharmacological Data)

human

Sex

male and female

Route of Application

peroral

Concentration (Pharmacological Data)

4.5 g

Kind of Dosing (Pharmacological Data)

500 mg/ml of oral solution in overnight fasted condition or 30 min later breakfast (standardized high-fat meal)

Method (Pharmacological Data)

after title comp. administration, adverse events were studied and vital signs including blood pressure (BP), heart rate (HR) and respiratory rate (RR) were recorded within 1 h before and 2, 6, and 10 h after the treatment

Further Details (Pharmacological Data)

healthy volunteers

Results

no changes in vital signs during the study; 86 not serious adverse events including nausea, vomiting and various CNS symptoms were reported; most (79 percent) after overnight fast and most (more than 70 percent) reported by females

Reference

Borgen, Lowell A.; Okerholm, Richard; Morrison, Dennis; Lai, Allen

Journal of Clinical Pharmacology, 2003 , vol. 43, # 1 p. 59 - 65 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Endpoint of Effect (Pharmacological Data)

urinary excretion

Species or TestSystem (Pharmacological Data)

human

Sex

male

Route of Application

peroral

Concentration (Pharmacological Data)

1 - 2 g

Kind of Dosing (Pharmacological Data)

doses administered one week apart, dissolved in 30 ml water; 1-g dose equivalent to 10 mg/kg, 2-g dose equivalent to 20 mg/kg

Method (Pharmacological Data)

title comp. was given to healthy volunteer; ca. 100 kg body wt; volunteer consumed ca. 1.5 l water in 30 min immediately before administration; urine samples collected with intervals during 36 h; then extracted; GC/MS

Results

title comp. excreted very quickly; title comp. was detectable for up to 10 h at 1-g dose and only up to 2 h at 2-g dose; table representation

Reference

Kavanagh; Kenny; Feely

Journal of Pharmacy and Pharmacology, 2001 , vol. 53, # 3 p. 399 - 402 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

human

Sex

male

Route of Application

peroral


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Concentration (Pharmacological Data)

1 - 2 g

Kind of Dosing (Pharmacological Data)

doses administered one week apart, dissolved in 30 ml water; 1-g dose equivalent to 10 mg/kg, 2-g dose equivalent to 20 mg/kg

Method (Pharmacological Data)

title comp. was given to healthy volunteer; ca. 100 kg body wt; volunteer consumed ca. 1.5 l water in 30 min immediately before administration; urine samples collected with intervals during 36 h; then extracted; GC/MS

Results

euphoric effect making volunteer feel relaxed and open to increased social interaction; title conp. did not induce sleep

Reference

Kavanagh; Kenny; Feely

Journal of Pharmacy and Pharmacology, 2001 , vol. 53, # 3 p. 399 - 402 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

male

Route of Application

intravenous

Concentration (Pharmacological Data)

150 - 600 mg/kg

Kind of Dosing (Pharmacological Data)

total doses of 150-300 mg/kg infused via femoral vein over 5 min; total dose of 600 mg/kg infused over 45 or 60 min

Method (Pharmacological Data)

after overnight fasting, 15 restrained rats (280-420 g) received title comp. between 0800 and 0900 h; arterial blood samples taken at regular time intervals and replaced with isotonic saline; plasma conc. of title comp. measured by HPLC

Further Details (Pharmacological Data)

data fitted to two-compartment open model with Michaelis-Menten elimination kinetics; Vmax, theoretical maximum rate of elimination; Km, Michaelis-Menten constant; Vd, apparent volume of distribution

Results

plasma conc.-time curves; Vmax: from 1889 (150 mg/kg/5 min) to 2703 μg/min/kg (600 mg/kg/45 min); Km: from 35 (200 mg/kg/5 min) to 370 μg/ml (600 mg/kg/45 min); Vd: from 439 (150 mg/kg/5 min) to 565 ml/kg (600 mg/kg/60 min)

Reference

Van Sassenbroeck; De Paepe; Belpaire; Rosseel; Martens; Boon; Buylaert

Journal of Pharmacy and Pharmacology, 2001 , vol. 53, # 12 p. 1687 - 1696 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

electroencephalographic amplitude; inhibition of

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

male

Route of Application

intravenous

Concentration (Pharmacological Data)

150 - 600 mg/kg

Kind of Dosing (Pharmacological Data)

total doses of 150-300 mg/kg infused via femoral vein over 5 min, followed by 450 mg/kg/5 min after 3 h; total dose of 600 mg/kg infused over 45 or 60 min; between 0800 and 0900 h

Method (Pharmacological Data)

15 rats (280-420 g); epidural EEG electrodes implanted in frontal, central and occipital positions on both sides of skull; 1 week later, rats received title comp.; EEG continuously recorded; amplitude in 15.5-30 Hz band quantified using aperiodic anal.

Further Details (Pharmacological Data)

rats fasted overnight and placed in restraining cage before experiment; plasma conc. of title comp. determined simultaneously by HPLC; EEG, electroencephalo(gram/graph/graphic)

Results

EEG amplitude (15.5-30 Hz) vs. time curves; monophasic inhibition of EEG amplitude was maximal at >=200 mg/kg; EEG effect vs. plasma conc. curves showed hysteresis for 150-300 mg/kg doses


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Reference

Van Sassenbroeck; De Paepe; Belpaire; Rosseel; Martens; Boon; Buylaert

Journal of Pharmacy and Pharmacology, 2001 , vol. 53, # 12 p. 1687 - 1696 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

electroencephalographic amplitude; inhibition of

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

male

Route of Application

intravenous

Kind of Dosing (Pharmacological Data)

total doses of 150-300 mg/kg infused via femoral vein over 5 min, followed by 450 mg/kg/5 min after 3 h; total dose of 600 mg/kg infused over 45 or 60 min; between 0800 and 0900 h

Method (Pharmacological Data)

15 rats (280-420 g); epidural EEG electrodes implanted in frontal, central and occipital positions on both sides of skull; 1 week later, rats received title comp.; EEG continuously recorded; amplitude in 15.5-30 Hz band quantified using aperiodic anal.

Further Details (Pharmacological Data)

rats fasted overnight and restrained before exp.; plasma conc. measured by HPLC; EEG, electroencephalo(gram/graph/graphic); EEG effect vs. effect-site conc. curve fitted to sigmoid inhibitory Emax model; EC50, effect-site conc. to reach 50 percent of maximum

Type (Pharmacological Data)

EC50

Value of Type (Pharmacological Data)

269 - 468 mg/l

Results

max. depression of EEG amplitude: 502-644 μV/s (1st infusion) and 645-799 μV/s (2nd infusion); baseline value: 834-1066 μV/s; distribution from central compartment to effect-site, first-order rate constant: 0.12-8.01 1/min, half-life: 0.37-5.78 min

Reference

Van Sassenbroeck; De Paepe; Belpaire; Rosseel; Martens; Boon; Buylaert

Journal of Pharmacy and Pharmacology, 2001 , vol. 53, # 12 p. 1687 - 1696 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

tranquilizing

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

male

Route of Application

intravenous

Concentration (Pharmacological Data)

150 - 600 mg/kg

Kind of Dosing (Pharmacological Data)

total doses of 150-300 mg/kg infused via femoral vein over 5 min, followed by 450 mg/kg/5 min after 3 h; total dose of 600 mg/kg infused over 45 or 60 min; between 0800 and 0900 h

Method (Pharmacological Data)

15 rats (280-420 g); epidural EEG electrodes implanted in frontal, central and occipital positions on both sides of skull; 1 week later, rats received title comp.; EEG assessed continuously; return of righting reflex measured every 5 min

Further Details (Pharmacological Data)

rats fasted overnight and placed in restraining cage before experiment; electroencephalo(gram/graphic)

Results

infusion of title comp. caused sedation in each dose group; righting reflex returned at 27, 51, 146 and 166 min in 200/5, 300/5, 600/45 and 600/60 mg/kg/min group, resp.; rats in 150/5 mg/kg/min group slightly sedated and did not lose righting reflex

Reference

Van Sassenbroeck; De Paepe; Belpaire; Rosseel; Martens; Boon; Buylaert

Journal of Pharmacy and Pharmacology, 2001 , vol. 53, # 12 p. 1687 - 1696 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

immunostimulant

Species or TestSystem

BALB/c mouse splenic B cells


(Pharmacological Data)

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Sex

female

Concentration (Pharmacological Data)

0.8 mmol/l

Method (Pharmacological Data)

in vitro; effect on anti-TNP PFC response and histone H4 acetylation assayed; 3.5E6 cells/well cultured with 5 μg/ml TNP-LPS in RPMI 1640 with 10 percent heat inactivated FCS; 100 U/ml IL-2; 5 percent CO2/95 percent air; 37 deg C; 5 d incub.

Further Details (Pharmacological Data)

number of anti-TNP PFC determined; 15 μg of histones isolated after 12 h of incubation; level of histone H4 acetylation analyzed by densitometry; TNP: trinitrophenyl; PFC: plaque-forming cells

Comment (Pharmacological Data)

No effect

Reference

Okamura, Takayuki; Gohda, Eiichi; Kohge, Takashi; Yamamoto, Itaru

Biological and Pharmaceutical Bulletin, 1999 , vol. 22, # 12 p. 1288 - 1292 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

membranotropic

Species or TestSystem (Pharmacological Data)

rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

250 mg/kg

Method (Pharmacological Data)

on rats; 180-200 g body wt; on acute pulmonary edema models (induced by adrenaline or nitrogen oxides); in 10-20 min after introduction of adrenaline; in 60-120 min after withdraval from inhalation chamber; in lipids from blood serum and lung tissues

Results

ability to decrease the level of phospholipid lysoforms and increase the total phospholipid fraction in the total lung lipids in the state of developed pathology

Reference

Tomchin; Kropotov

Pharmaceutical Chemistry Journal, 1998 , vol. 32, # 1 p. 20 - 25 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

membranotropic

Species or TestSystem (Pharmacological Data)

mice erythrocytes

Method (Pharmacological Data)

in vitro; method of acid and osmotic hemolysis; acid erythrogram technique; 0.024 M HCl as a hemolytic agent; osmotic strength studied in buffered hypotonic solutions of NaCl

Results

title compound inhibited process of osmotic and oxygen-induced hemolysis of erythrocytes

Reference

Tomchin; Kropotov

Pharmaceutical Chemistry Journal, 1998 , vol. 32, # 1 p. 20 - 25 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

membranotropic

Species or TestSystem (Pharmacological Data)

mitochondria

Method (Pharmacological Data)

in vitro; mitochondrial model of nonenzymatic and enzymatic lipid peroxidation; preliminary introduction of title compound into suspension of mitochondria

Results

accumulation of malonic dialdehyde prevented


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Reference

Tomchin; Kropotov

Pharmaceutical Chemistry Journal, 1998 , vol. 32, # 1 p. 20 - 25 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

anti-inflammatory

Endpoint of Effect (Pharmacological Data)

action on toxic pulmonary edema

Species or TestSystem (Pharmacological Data)

white mongrel mice

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

125 - 500 mg/kg

Method (Pharmacological Data)

in 20-40 mice; 18-24 g body wt; acute toxic pulmonary edema model; in inhalation chamber with nitrogen oxides at concentration 4.3 mg/l for 10 min; test compound was introduced 30 min before modeling edema; histological methods; control (intact mice)

Further Details (Pharmacological Data)

percentage survival of test mice during one day; protection coefficient - PC; lung coefficient (lungs wt/total body wt) - LC; dry residue (mass ratio of dry and raw lung tissues) - DR

Results

20-30 percent survival; PC = 1.03-1.11; LC = 1.50-2.04 percent (0.92 percent in control); DR = 12.2-14.9 percent (22.3 percent in control)

Reference

Tomchin; Kropotov

Pharmaceutical Chemistry Journal, 1998 , vol. 32, # 1 p. 20 - 25 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

anti-inflammatory

Endpoint of Effect (Pharmacological Data)

action on hydrodynamic edema

Species or TestSystem (Pharmacological Data)

white mongrel mice

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

62.5 - 500 mg/kg

Method (Pharmacological Data)

in 20 mice; 18-24 g body weight; acute adrenaline-induced (i.p.) pulmonary edema model; test compound was introduced 30 min before modeling edema; histological methods; control (intact mice)

Further Details (Pharmacological Data)

percentage survival of test mice during one day; protection coefficient - PC; lung coefficient (lungs wt/total body wt) - LC; dry residue (mass ratio of dry and raw lung tissues) - DR

Results

40-60 percent survival; PC = 1.27-1.39; LC = 1.25-1.66 percent (0.92 percent in control); DR = 15.8-17.4 percent (22.3 percent in control)

Reference

Tomchin; Kropotov

Pharmaceutical Chemistry Journal, 1998 , vol. 32, # 1 p. 20 - 25 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

anti-inflammatory

Endpoint of Effect (Pharmacological Data)

survival

Species or TestSystem (Pharmacological

mice


Data)

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Route of Application

intraperitoneal

Concentration (Pharmacological Data)

125 - 500 mg/kg

Kind of Dosing (Pharmacological Data)

test comp. injected in physiological soln. with Tween-80 additives

Method (Pharmacological Data)

20-40 mice; acute toxic (nitrogen dioxide induced) pulmonary edema model; control

Results

survival 20-30 percent; protection coefficient 1.03-1.11; test compound normalized gravimetric parameters of lungs

Reference

Tomchin; Velezheva; Shustov

Pharmaceutical Chemistry Journal, 1998 , vol. 32, # 2 p. 59 - 63 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

anti-inflammatory

Endpoint of Effect (Pharmacological Data)

survival

Species or TestSystem (Pharmacological Data)

mice

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

62.5 - 500 mg/kg

Kind of Dosing (Pharmacological Data)

test comp. injected in physiological soln. with Tween-80 additives

Method (Pharmacological Data)

20 mice; acute adrenaline-induced pulmonary edema model; control

Results

survival 40-60 percent; protection coefficient 1.27-1.39; test compound normalized gravimetric parameters of lungs

Reference

Tomchin; Velezheva; Shustov

Pharmaceutical Chemistry Journal, 1998 , vol. 32, # 2 p. 59 - 63 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

anxiolytic

Species or TestSystem (Pharmacological Data)

Long-Evans rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

75 - 600 mg/kg

Kind of Dosing (Pharmacological Data)

75, 150 mg/kg

Method (Pharmacological Data)

injected rat placed in activity meter compartment, movements detected every 5 min for 1 h with 150 mg/kg title comp. or measurement at 30 min after injection with all doses

Results

no reduction of spontaneous activity, slight hyperactivity even 35 min after injection with 75, 150 mg/kg; no sedation up to 150 mg/kg; sedative effect at 300-600 mg/kg

Reference

Schmidt-Mutter, Catherine; Pain, Laure; Sandner, Guy; Gobaille, Serge; Maitre, Michel

European Journal of Pharmacology, 1998 , vol. 342, # 1 p. 21 - 27 Title/Abstract Full Text View citing articles Show Details


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Effect (Pharmacological Data)

anxiolytic

Species or TestSystem (Pharmacological Data)

Long-Evans rat

Sex

male

Route of Application

intraperitoneal

Kind of Dosing (Pharmacological Data)

50, 150, 250 mg/kg

Method (Pharmacological Data)

title comp. injected 30 min before testing; rat placed in maze with 2-2 open-enclosed arms, elevated to 50 cm above ground; behavior recorded on videotape for 5 min

Results

150, 250 mg/kg sign. increased percentage of entries into and percentage of time spent in open arms; 250 mg/kg sign. increased total number of arm entries, no sedative effect at this dose

Reference

Schmidt-Mutter, Catherine; Pain, Laure; Sandner, Guy; Gobaille, Serge; Maitre, Michel

European Journal of Pharmacology, 1998 , vol. 342, # 1 p. 21 - 27 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

drug interaction

Species or TestSystem (Pharmacological Data)

Papio anubis baboon

Sex

female

Route of Application

intravenous

Concentration (Pharmacological Data)

200 mg/kg

Exposure Period (Pharmacological Data)

30 - 90 min

Method (Pharmacological Data)

two sequential i.v. of <11>d-threo-methylphenidate in same scanning session; followed by 1 h dynamic PET scan; effect of title comp. administered before second scan

Further Details (Pharmacological Data)

PET: positron emission tomography; effect on methylphenidate distribution between striatum and cerebellum

Comment (Pharmacological Data)

No effect

Reference

Gatley, S. John; Ding, Yu-Shin; Volkow, Nora D.; Chen, Ruoyan; Sugano, Yuichi; Fowler, Joanna S.

European Journal of Pharmacology, 1995 , vol. 281, # 2 p. 141 - 149 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

influence on liability and excitability of nerve elements of rabbits like lithium hydroxybutyrate but weaker by 30-50percent

Reference

Saratikov; Zamoshchina

Arzneimittel-Forschung/Drug Research, 1986 , vol. 36, # 10 p. 1448 - 1451 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

intestinal transport through the everted rat gut

Reference

Arena; Fung

Journal of Pharmaceutical Sciences, 1980 , vol. 69, # 3 p. 356 - 358 Title/Abstract Full Text View citing articles Show Details

Other Data


Use (237) Use Pattern

Location

Reference

Pharmaceuticals

Page/Page column 34

Jazz Pharmaceuticals, Inc.; Cook, Harry; Hamilton, Martha; Danielson, Douglas; Goderstad, Colette; Reardan, Dayton T.

Patent: US2016/58862 A1, 2016 ; Title/Abstract Full Text Show Details

active agent

Page/Page column 34

Jazz Pharmaceuticals, Inc.; Cook, Harry; Hamilton, Martha; Danielson, Douglas; Goderstad, Colette; Reardan, Dayton T.

Patent: US2016/58862 A1, 2016 ; Title/Abstract Full Text Show Details

pharmaceutical composition, chemically stable and resistant to microbial growth

Page/Page column 34

Jazz Pharmaceuticals, Inc.; Cook, Harry; Hamilton, Martha; Danielson, Douglas; Goderstad, Colette; Reardan, Dayton T.

Patent: US2016/58862 A1, 2016 ; Title/Abstract Full Text Show Details

active ingredient of multimodal abuse resistant pharmaceutical composition

THERAQUEST BIOSCIENCES, INC.

Patent: WO2008/33351 A2, 2008 ; Title/Abstract Full Text Show Details

active ingredient of multimodal extended release pharmaceutical composition

THERAQUEST BIOSCIENCES, INC.

Patent: WO2008/33351 A2, 2008 ; Title/Abstract Full Text Show Details

active ingredient of multimodal extended release abuse resistant pharmaceutical composition

THERAQUEST BIOSCIENCES, INC.

Patent: WO2008/33351 A2, 2008 ; Title/Abstract Full Text Show Details

drug addiction

Brookhaven Science Associates

Patent: EP1481668 A1, 2004 ; Title/Abstract Full Text Show Details

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

modulation of cannabinoid recptors; HMG-CoA reductase inhibition; regulation of triglyceride levels in the blood plasma; modulation of cannabinoid-receptors; cannabinoid 1 (CB1) receptors; aldehyde dehydrogenase inhibition; GABA(A) BZ site receptors agonist; sodium channels blockage; μ-opioid receptors antagonist; GABA aminotransferase inhibition; metabotropic glutamate receptors inhibition; 5-HT3 receptors antagonist; κ-opioid-receptors antagonist; 5-HT1A receptors partial antagonist

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details


Coronary heart disease

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

myocardial ischemia

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

angina pectoris

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

atherosclerosis

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

hypertension

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

hyperlipidemia

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

Lipoprotein disorders

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

Hypercholesterolemia

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

lowering of cardiac risk

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

future adverse cardiac event

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details


myocardial infarction

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

cardiac arrest

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

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Use Pattern

Reference

cardiac failure

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

cardiac ischemia

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

disorders of the central nervous system

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

disorders of the cardiovascular system

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

disorders of the immune system

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

disorders of the endocrinous system

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

disorders of the respiratory system

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

disorders of the gastrointestinal tract

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

reproductive disorders

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

food intake disorders

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

bulimia

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

anorexia

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ;


Title/Abstract Full Text Show Details

cachexia

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

type Il diabetes mellitus

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

non-insuline dependent diabetes mellitus

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

psychosis

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

alcohol abuse

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

Alcohol addiction

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

nicotine abuse

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

nicotine addiction

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

drug abuse

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

medicament abuse

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

medicament addiction

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

schizophrenia

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

anxiety

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

depression

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

epilepsy

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details


neurodegenerative disorders

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

Morbus Parkinson

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

Morbus Huntington

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

Morbus Alzheimer

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

Multiple Sclerosis

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

cerebellar disorders

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

spinocerebellar disorders

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

cognitive disorders

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

cranial trauma

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

panic attacks

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

peripheric neuropathy

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

glaucoma

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

migraine

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

Raynaud's disease

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

tremblement disorders

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

compulsive disorders

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ;


Title/Abstract Full Text Show Details

senile dementia

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

thymic disorders

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

tardive dyskinesia

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

bipolar disorders

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

bone disorders

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

osteoporosis

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

Paget's disease of bone

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

cancer

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

brain cancer

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

bone cancer

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

lip cancer

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

mouth cancer

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

esophageal cancer

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

stomach cancer

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

liver cancer

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details


bladder cancer

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

pancreas cancer

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

ovary cancer

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

cervical cancer

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

lung cancer

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

breast cancer

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

skin cancer

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

colon cancer

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

Bowel cancer

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

prostate cancer

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

medicament-induced movement disorders

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

dystonia

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

endotoxemic shock

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

stroke

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

hemorrhagic shock

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

hypotension

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ;


Title/Abstract Full Text Show Details

insomnia

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

immunologic disorders

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

sclerotic plaques

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

vomiting

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

diarrhoea

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

asthma

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

memory disorders

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

pruritus

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

pain

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

potentiation of the analgesic effect of narcotic

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

potentiation of the analgesic effect of non-narcotic analgesics

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

for influencing intestinal transit

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

dementia

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

memory loss

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

vascular dementia

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details


mild cognitive impairment

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

frontotemporal dementia

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

Pick's disease

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

binge eating disorders

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

juvenile obesity

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

drug induced obesity

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

atypical depression

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

behavioural addictions

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

attention deficit disorders

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

Tourette's syndrome

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

suppression of reward-related behaviours

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

suppression of cocaine induced conditioned place preference

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

suppression of morphine induced conditioned place preference

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

impulsivity

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

sexual dysfunction

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

erectile difficulty

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ;


Title/Abstract Full Text Show Details

female sexual dysfunction

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

seizure disorders

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

nausea

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

emesis

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

neuroinflammatory disease

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

demyelinisation related disorders

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

Guillan-Barre syndrome

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

viral encephalitis

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

cerebrovascular accidents

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

neurological disorders

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

muscle spasticity

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

traumatic brain injury

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

spinal cord injury

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

inflammation disorders

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

immunomodulatory disorders

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details


cutaneous T-cell lymphoma

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

rheumatoid arthritis

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

systemic lupus erythematosus

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

sepsis

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

sarcoidosis

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

idiopathic pulmonary fibrosis

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

bronchopulmonary dysplasia

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

retinal disease

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

scleroderma

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

renal ischemia

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

mycocardial infarction

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

cerebral ischemia

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

nephritis

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

hepatitis

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

glomerulonephritis

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

cryptogenic fibrosing aveolitis

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ;


Title/Abstract Full Text Show Details

psoriasis

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

transplant rejection

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

atopic dermatitis

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

vasculitis

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

allergy

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

seasonal allergic rhinitis

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

Crohn's disease

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

inflammatory bowel disease

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

reversible airway obstruction

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

adult respiratory distress syndrome

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

chronic obstructive pulmonary disease

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

bronchitis

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

cerebral apoplexy

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

craniocerebral trauma

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

neuropathic pain disorders

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details


gastric ulcers

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

atheriosclerosis

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

liver cirrhosis

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

Anti-alcohol-addictive agent

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: WO2007/9691 A2, 2007 ; Title/Abstract Full Text Show Details

a central nervous system depressant with anti-cataplectic activity

THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK

Patent: WO2006/53186 A2, 2006 ; Title/Abstract Full Text Show Details

anti-myoclonic agent

THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK

Patent: WO2006/53186 A2, 2006 ; Title/Abstract Full Text Show Details

binding gamma-aminobutyric acid (GABA) receptor or augmenting the actions of GABA and its cogeners

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ;

Sleeping disorders

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ;

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

Insomnia

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Drug abuse

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Alcohol and opiate withdrawal

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Reduced level of growth hormone

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Anxiety

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Analgesia

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Acquired resistance to GABAnergic agents(ARG)

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details


Effects in certain neurological disorders

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Parkinson's disease

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Depression

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Obesity

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Certain endocrine disturbances

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Tissue protection following hypoxia/anoxia such as in stroke or myocardial infarction

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Increased level of intracranial pressure

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Hyperactivity

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Attention deficit hyperactivity disorder

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Decreased concentration

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Mania

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Hypomania

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Bipolar disorder

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Cyclothymia

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Sleepiness during waking hours

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Narcolepsy major

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ;


Title/Abstract Full Text Show Details

Narcolepsy minor

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Restless legs syndrome

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Periodic limb movement disorder

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Subclinical restless legs syndrome

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Subclinical periodic limb movement disorder

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Obstructive sleep apnea

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Symptoms associated with acquired resistance to GABAminergic agents

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Fatigue(the feeling of tiredness)

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Unrestful sleep

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Difficulty dealing with stress

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Arthralgias (joint pain)

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Myalgias (muscle aching)

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Tense muscles

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Difficulty concentrating(brain fog)

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Impaired memory

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details


Sleepiness

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Tender trigger points

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Periodic limb movement disorder of sleep

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

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Reference

Interstitial cystitis

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Irritable bowel syndrome

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Rheumatoid arthritis

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Lupus erythematosus

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Multiple sclerosis

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

Treating ARG or related conditions

JOHNSON, Joseph

Patent: WO2006/124609 A2, 2006 ; Title/Abstract Full Text Show Details

energizer

Ayala, William J.

Patent: US2005/31688 A1, 2005 ; Title/Abstract Full Text Show Details

invigorant

Ayala, William J.

Patent: US2005/31688 A1, 2005 ; Title/Abstract Full Text Show Details

nervous system stimulant

Ayala, William J.

Patent: US2005/31688 A1, 2005 ; Title/Abstract Full Text Show Details

psychostimulant

Ayala, William J.

Patent: US2005/31688 A1, 2005 ; Title/Abstract Full Text Show Details

angiogenic material

Wright, Emma Jayne; Huckle, James William; Ali, Saad Aboul Majeed

Patent: US2004/265282 A1, 2004 ; Title/Abstract Full Text Show Details

fixation devices for tissue repair

Wright, Emma Jayne; Huckle, James William; Ali, Saad Aboul Majeed

Patent: US2004/265282 A1, 2004 ;


Title/Abstract Full Text Show Details

enhance the production or release of gamma amino butyric acid (GABA) in the central nervous system (CNS) and/or increase GABAergic transmission

Brookhaven Science Associates

Patent: EP1481668 A1, 2004 ;

anti-glaucoma drugs

Brookhaven Science Associates

Patent: EP1481668 A1, 2004 ;

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

Brookhaven Science Associates

Patent: EP1481668 A1, 2004 ;

retinal perfusion

Title/Abstract Full Text Show Details

Brookhaven Science Associates

Patent: EP1481668 A1, 2004 ;

visual field defects

Title/Abstract Full Text Show Details

Brookhaven Science Associates

Patent: EP1481668 A1, 2004 ;

seizure disorder

Title/Abstract Full Text Show Details

Chemical Name: sodium 3,3-d2-4-hydroxybutanoate

1 prep out of 1 reactions.

Physical Data (1) Spectra (2)

Reaxys Registry Number: 20833179

Molecular Formula: C4H7O3*Na Linear Structure Formula: C4H5(2)H2O3(1-)*Na(1+)

3

Molecular Weight: 128.072

InChI Key: XYGBKMMCQDZQOZ-CUOKRTIESA-M

13

Synthesize | Hide Details Find similar Chemical Names and Synonyms sodium 3,3-d2-4-hydroxybutanoate, sodium 3,3-dideuterio-4-hydroxybutanoate, sodium 3,3-dideuterium-4-hydroxybutyrate Physical Data Crystal Property Description (1) Colour & Other Properties

Location

Reference

white

Paragraph 187

CONCERT PHARMACEUTICALS, INC.; TUNG, Roger D.; SILVERMAN, I. Robert

Patent: WO2014/31840 A1, 2014 ; Title/Abstract Full Text Show Details

Spectra NMR Spectroscopy (2) Description (NMR Spectroscopy)

Nucleus (NMR Spectroscopy)

Solvents (NMR Spectroscopy)

Frequency (NMR Spectroscopy)

Chemical shifts

1H

chloroform-d1

400 MHz

Original Text (NMR Spectroscopy) H NMR (CDCI3, 400 MHz) δ 6.17 (s, 1 H), 3.38 (s, 2H), 2.01 (s, 2H).

Location Paragraph 187

Comment (NMR Spectroscopy)

Reference CONCERT PHARMACEUTICALS, INC.; TUNG, Roger D.; SILVERMAN, I. Robert

Patent: WO2014/31840 A1, 2014 ; Title/Abstract Full Text Show Details


1H

chloroform-d1

400 MHz

H NMR (CDCI3, 400 MHz) δ 6.17 (s, 1 H), 3.38 (s, 2H), 2.01 (s, 2H).

Page/Page column 43

Signals given

CONCERT PHARMACEUTICALS INC.; TUNG, Roger, D.; MORGAN, Adam; SILVERMAN, I., Robert

Patent: WO2012/112492 A1, 2012 ; Title/Abstract Full Text Show Details

Chemical Name: 2,2-dideutero-4-hydroxybutanoic acid sodium salt

2 prep out of 2 reactions.

Reaxys Registry Number: 20833180

Molecular Formula: C4H7O3*Na Linear Structure Formula: C4H5(2)H2O3(1-)*Na(1+)

Physical Data (2) Spectra (2) Bioactivity (2)

3

Molecular Weight: 128.072

InChI Key: XYGBKMMCQDZQOZ-IYPYQTRPSA-M

14

Synthesize | Hide Details Find similar Chemical Names and Synonyms 2,2-dideutero-4-hydroxybutanoic acid sodium salt, sodium 2,2-d2-4-hydroxybutanoate, sodium 2,2-dideuterio-4-hydroxybutanoate, sodium 2,2dideuterium-4-hydroxybutyrate Physical Data Crystal Property Description (2) Colour & Other Properties

Location

Reference

white

Paragraph 183

CONCERT PHARMACEUTICALS, INC.; TUNG, Roger D.; SILVERMAN, I. Robert

Patent: WO2014/31840 A1, 2014 ; Title/Abstract Full Text Show Details

white

Page/Page column 42

CONCERT PHARMACEUTICALS INC.; TUNG, Roger, D.; MORGAN, Adam; SILVERMAN, I., Robert

Patent: WO2012/112492 A1, 2012 ; Title/Abstract Full Text Show Details

Spectra NMR Spectroscopy (2) Description (NMR Spectroscopy)

Nucleus (NMR Spectroscopy)

Solvents (NMR Spectroscopy)

Frequency (NMR Spectroscopy)

Chemical shifts

1H

chloroform-d1

400 MHz

Original Text (NMR Spectroscopy) H NMR (CDCI3, 400 MHz) δ 3.38 (t, J = 5.8 Hz, 2H), 1 .55 (t, J = 5.8 Hz, 2H).

Location Paragraph 183

Comment (NMR Spectroscopy)

Reference CONCERT PHARMACEUTICALS, INC.; TUNG, Roger D.; SILVERMAN, I. Robert

Patent: WO2014/31840 A1, 2014 ; Title/Abstract Full Text Show Details

1H

chloroform-d1

400 MHz

H NMR (CDCI3, 400 MHz) δ 3.38 (t, J = 5.8 Hz, 2H), 1 .55 (t, J = 5.8 Hz, 2H).

Page/Page column 42

Signals given

CONCERT PHARMACEUTICALS INC.; TUNG, Roger, D.; MORGAN, Adam; SILVERMAN, I., Robert

Patent: WO2012/112492 A1, 2012 ; Title/Abstract Full Text Show Details


Bioactivity Pharmacological Data (2) 1 of 2

Comment (Pharmacological Data)

Bioactivities present

Reference

CONCERT PHARMACEUTICALS, INC.; TUNG, Roger, D.

Patent: WO2010/124046 A1, 2010 ; Title/Abstract Full Text Show Details

CONCERT PHARMACEUTICALS INC.; TUNG, Roger, D.; MORGAN, Adam; SILVERMAN, I., Robert

Patent: WO2012/112492 A1, 2012 ; Title/Abstract Full Text Show Details

CONCERT PHARMACEUTICALS, INC.; TUNG, Roger D.; SILVERMAN, I. Robert

Patent: WO2014/31840 A1, 2014 ; Title/Abstract Full Text Show Details

2 of 2

Location

Paragraph

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

CONCERT PHARMACEUTICALS, INC.; TUNG, Roger D.; SILVERMAN, I. Robert

Patent: WO2014/31840 A1, 2014 ; Title/Abstract Full Text Show Details

Chemical Name: Sodium oxybate Reaxys Registry Number: 24193564

Molecular Formula: C4H8O3*HNa Linear Structure Formula: C4H8O3*HNa Molecular Weight: 128.103

InChI Key: PILWMQBFGACQJS-UHFFFAOYSA-N

15

Synthesize | Hide Details Find similar Chemical Names and Synonyms Sodium oxybate Bioactivity Pharmacological Data (2) 1 of 2

Comment (Pharmacological Data)

Bioactivities present

Reference

Liang, Likan; Shah, Niraj; Bhatt, Padmanabh P.; Ibrahim, Scott

Patent: US2006/210630 A1, 2006 ; Title/Abstract Full Text Show Details

Bourguignon; Schoenfelder; Schmitt; Wermuth; Hechler; Charlier; Maitre

Journal of Medicinal Chemistry, 1988 , vol. 31, # 5 p. 893 - 897 Title/Abstract Full Text View citing articles Show Details

Saratikov; Zamoshchina

Arzneimittel-Forschung/Drug Research, 1986 , vol. 36, # 10 p. 1448 - 1451 Title/Abstract Full Text View citing articles Show Details

Arena; Fung

Journal of Pharmaceutical Sciences, 1980 , vol. 69, # 3 p. 356 - 358 Title/Abstract Full Text View citing articles Show Details

Tomchin; Kropotov

Pharmaceutical Chemistry Journal, 1998 , vol. 32, # 1 p. 20 - 25 Title/Abstract Full Text View citing articles Show Details

Tomchin; Velezheva; Shustov

Pharmaceutical Chemistry Journal, 1998 , vol. 32, # 2 p. 59 - 63

no reactions.

Bioactivity (2)

28


Title/Abstract Full Text View citing articles Show Details

Kavanagh; Kenny; Feely

Journal of Pharmacy and Pharmacology, 2001 , vol. 53, # 3 p. 399 - 402 Title/Abstract Full Text View citing articles Show Details

Schmidt-Mutter, Catherine; Pain, Laure; Sandner, Guy; Gobaille, Serge; Maitre, Michel

European Journal of Pharmacology, 1998 , vol. 342, # 1 p. 21 - 27 Title/Abstract Full Text View citing articles Show Details

Van Sassenbroeck; De Paepe; Belpaire; Rosseel; Martens; Boon; Buylaert

Journal of Pharmacy and Pharmacology, 2001 , vol. 53, # 12 p. 1687 - 1696 Title/Abstract Full Text View citing articles Show Details

Okamura, Takayuki; Gohda, Eiichi; Kohge, Takashi; Yamamoto, Itaru

Biological and Pharmaceutical Bulletin, 1999 , vol. 22, # 12 p. 1288 - 1292 Title/Abstract Full Text View citing articles Show Details

Carter, Lawrence P.; Flores, Lauren R.; Wu, Huifang; Chen, Weibin; Unzeitig, Andrew W.; Coop, Andy; France, Charles P.

Journal of Pharmacology and Experimental Therapeutics, 2003 , vol. 305, # 2 p. 668 - 674 Title/Abstract Full Text View citing articles Show Details

Wu, Huifang; Zink, Nick; Carter, Lawrence P.; Mehta, Ashok K.; Hernandez, R. Jason; Ticku, Maharaj K.; Lamb, Richard; France, Charles P.; Coop, Andrew

Journal of Pharmacology and Experimental Therapeutics, 2003 , vol. 305, # 2 p. 675 - 679 Title/Abstract Full Text View citing articles Show Details

McMahon, Lance R.; France, Charles P.

Journal of Pharmacology and Experimental Therapeutics, 2003 , vol. 304, # 1 p. 109 - 120 Title/Abstract Full Text View citing articles Show Details

Borgen, Lowell A.; Okerholm, Richard; Morrison, Dennis; Lai, Allen

Journal of Clinical Pharmacology, 2003 , vol. 43, # 1 p. 59 - 65 Title/Abstract Full Text View citing articles Show Details

Borgen, Lowell A.; Okerholm, Richard A.; Lai, Allen; Scharf, Martin B.

Journal of Clinical Pharmacology, 2004 , vol. 44, # 3 p. 253 - 257 Title/Abstract Full Text View citing articles Show Details

Ottani, Alessandra; Vergoni, Anna Valeria; Saltini, Sabrina; Mioni, Chiara; Giuliani, Daniela; Bartiromo, Marta; Zaffe, Davide; Botticelli, Annibale R.; Ferrari, Anna; Bertolini, Alfio; Genedani, Susanna

European Journal of Pharmacology, 2004 , vol. 485, # 1-3 p. 183 - 191 Title/Abstract Full Text View citing articles Show Details

Carter; Unzeitig; Wu; Chen; Coop; Koek; France, Charles P.

Journal of Pharmacology and Experimental Therapeutics, 2004 , vol. 309, # 2 p. 540 - 547 Title/Abstract Full Text View citing articles Show Details

Morris, Marilyn E.; Hu, Ke; Wang, Qi

Journal of Pharmacology and Experimental Therapeutics, 2005 , vol. 313, # 3 p. 1194 - 1202 Title/Abstract Full Text View citing articles Show Details

Bhattacharya, Indranil; Boje, Kathleen M. K.

Journal of Pharmacology and Experimental Therapeutics, 2004 , vol. 311, # 1 p. 92 - 98 Title/Abstract Full Text View citing articles Show Details

Carter, Lawrence P.; Wu, Huifang; Chen, Weibin; Cruz, Christopher M.; Lamb; Koek, Wouter; Coop, Andy; France, Charles P.

Journal of Pharmacology and Experimental Therapeutics, 2004 , vol. 308, # 1 p. 182 - 188 Title/Abstract Full Text View citing articles Show Details

2 of 2

Comment (Pharmacological Data)

Bioactivities present

Reference

Raybon, Joseph J.; Boje, Kathleen M. K.

Journal of Pharmacology and Experimental Therapeutics, 2007 , vol. 320, # 3 p. 1252 - 1260 Title/Abstract Full Text View citing articles Show Details

THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK

Patent: WO2006/53186 A2, 2006 ; Title/Abstract Full Text Show Details

Lam, Wing Ki; Felmlee, Melanie A.; Morris, Marilyn E.

Drug Metabolism and Disposition, 2010 , vol. 38, # 3 p. 441 - 447 Title/Abstract Full Text View citing articles Show Details

Gatley; Ding; Volkow; Chen; Sugano; Fowler

European Journal of Pharmacology, 1995 , vol. 281, # 2 p. 141 - 149 Title/Abstract Full Text Show Details

JOHNSON, Joseph

Patent: WO2006/124609 , 2006 ; Title/Abstract Full Text Show Details

Borgen LA, Morrison D, Lai A

Clinical pharmacology and therapeutics, 2004 , vol. 75 Title/Abstract Full Text Show Details

Type: Review, Lab: EFF_071212, Owner: EFFECT, Number: 000, Revision: 07.12.2012 00:00:00 2012 Full Text Show Details

Type: Clinical Pharmacology Biopharmaceutics Review, Lab: NDA021196, Owner: JAZZ, Number: 000, Revision: 17.07.2002 00:00:00 2002 Title/Abstract Full Text Show Details

Chemical Name: sodium 2,2,3,3-d4-4-hydroxybutanoate Reaxys Registry Number: 20833181

Molecular Formula: C4H7O3*Na Linear Structure Formula: C4H3(2)H4O3(1-)*Na(1+)

Molecular Weight: 130.056

InChI Key: XYGBKMMCQDZQOZ-PBCJVBLFSA-M

2 prep out of 2 reactions.

Physical Data (1) Spectra (2)

3


16

Synthesize | Hide Details Find similar Chemical Names and Synonyms sodium 2,2,3,3-d4-4-hydroxybutanoate, sodium 2,2,3,3-tetradeuterio-4-hydroxybutanoate, sodium 2,2,3,3-tetradeuterium-4-hydroxybutyrate Physical Data Crystal Property Description (1) Colour & Other Properties

Location

Reference

white

Paragraph 191

CONCERT PHARMACEUTICALS, INC.; TUNG, Roger D.; SILVERMAN, I. Robert

Patent: WO2014/31840 A1, 2014 ; Title/Abstract Full Text Show Details

Spectra NMR Spectroscopy (2) Description (NMR Spectroscopy)

Nucleus (NMR Spectroscopy)

Solvents (NMR Spectroscopy)

Frequency (NMR Spectroscopy)

Original Text (NMR Spectroscopy)

Chemical shifts

1H

chloroform-d1

400 MHz

H NMR (CDCI3, 400 MHz) δ 3.38 (s, 2H).

Paragraph 191

H NMR (CDCI3, 400 MHz) δ 3.38 (s, 2H).

Page/Page column 43

1H

chloroform-d1

400 MHz

Location

Comment (NMR Spectroscopy)

Reference CONCERT PHARMACEUTICALS, INC.; TUNG, Roger D.; SILVERMAN, I. Robert

Patent: WO2014/31840 A1, 2014 ; Title/Abstract Full Text Show Details

Signals given

CONCERT PHARMACEUTICALS INC.; TUNG, Roger, D.; MORGAN, Adam; SILVERMAN, I., Robert

Patent: WO2012/112492 A1, 2012 ; Title/Abstract Full Text Show Details

Chemical Name: sodium 2,2,4,4-d4-4-hydroxybutanoate Reaxys Registry Number: 22826703

CAS Registry Number: 1393801-57-4 Molecular Formula: C4H7O3*Na Linear Structure Formula: C4H3(2)H4O3(1-)*Na(1+)

Molecular Weight: 130.056

InChI Key: XYGBKMMCQDZQOZ-DAHDXRBSSA-M

17

Synthesize | Hide Details Find similar Chemical Names and Synonyms sodium 2,2,4,4-d -4-hydroxybutanoate, sodium 2,2,4,4-tetradeuterio-4-hydroxybutanoate

1 prep out of 1 reactions.

Identification Physical Data (2) Spectra (2) Bioactivity (2)

2


4

Identification Substance Label (2) Label

Reference

IV-b sodium salt

CONCERT PHARMACEUTICALS, INC.; TUNG, Roger D.; SILVERMAN, I. Robert

Patent: WO2014/31840 A1, 2014 ; Title/Abstract Full Text Show Details

CONCERT PHARMACEUTICALS INC.; TUNG, Roger, D.; MORGAN, Adam; SILVERMAN, I., Robert

Patent: WO2012/112492 A1, 2012 ;

IVb sodium salt

Title/Abstract Full Text Show Details

Patent-Specific Data (1) Related Markush Structure (RN)

Reference

22826687; 22826688

CONCERT PHARMACEUTICALS INC.; TUNG, Roger, D.; MORGAN, Adam; SILVERMAN, I., Robert

Patent: WO2012/112492 A1, 2012 ; Title/Abstract Full Text Show Details

Physical Data Crystal Property Description (2) Colour & Other Properties

Location

Reference

white

Paragraph 195

CONCERT PHARMACEUTICALS, INC.; TUNG, Roger D.; SILVERMAN, I. Robert

Patent: WO2014/31840 A1, 2014 ; Title/Abstract Full Text Show Details

white

CONCERT PHARMACEUTICALS INC.; TUNG, Roger, D.; MORGAN, Adam; SILVERMAN, I., Robert

Patent: WO2012/112492 A1, 2012 ;

Page/Page column 45

Title/Abstract Full Text Show Details

Spectra NMR Spectroscopy (2) Description (NMR Spectroscopy)

Nucleus (NMR Spectroscopy)

Solvents (NMR Spectroscopy)

Frequency (NMR Spectroscopy)

Original Text (NMR Spectroscopy)

Chemical shifts

1H

chloroform-d1

400 MHz

H NMR (CDCI3, 400 MHz) δ 1 .53 (s, 2H).

Paragraph 195

H NMR (CDCI3, 400 MHz) 5D 1 .53(s, 2H).

Page/Page column 45

1H

chloroform-d1

400 MHz

Location

Comment (NMR Spectroscopy)

Reference CONCERT PHARMACEUTICALS, INC.; TUNG, Roger D.; SILVERMAN, I. Robert

Patent: WO2014/31840 A1, 2014 ; Title/Abstract Full Text Show Details

Signals given

CONCERT PHARMACEUTICALS INC.; TUNG, Roger, D.; MORGAN, Adam; SILVERMAN, I., Robert

Patent: WO2012/112492 A1, 2012 ; Title/Abstract Full Text Show Details

Bioactivity Pharmacological Data (2) 1 of 2

Comment (Pharmacological Data)

Bioactivities present

Reference

CONCERT PHARMACEUTICALS INC.; TUNG, Roger, D.; MORGAN, Adam; SILVERMAN, I., Robert

Patent: WO2012/112492 A1, 2012 ; Title/Abstract Full Text Show Details


CONCERT PHARMACEUTICALS, INC.; TUNG, Roger D.; SILVERMAN, I. Robert

Patent: WO2014/31840 A1, 2014 ; Title/Abstract Full Text Show Details

2 of 2

Location

Paragraph

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

CONCERT PHARMACEUTICALS, INC.; TUNG, Roger D.; SILVERMAN, I. Robert

Patent: WO2014/31840 A1, 2014 ; Title/Abstract Full Text Show Details

Chemical Name: potassium salt of gamma-hydroxy butyric acid

2 prep out of 4 reactions.

Reaxys Registry Number: 13959855

CAS Registry Number: 57769-01-4 Molecular Formula: C4H7O3*K Linear Structure Formula: C4H7O3(1-)*K(1+)

Identification Physical Data (1) Spectra (3) Other Data (2)

Molecular Weight: 142.196

InChI Key: TXSIWDVUJVMMKM-UHFFFAOYSA-M

18

Synthesize | Hide Details Find similar Chemical Names and Synonyms potassium salt of gamma-hydroxy butyric acid, 4-hydroxybutyrate pottasium salt, potassium 4-(hydroxy)butanoate, potassium 4-hydroxybutanoate, potassium 4-hydroxybutyrate, sodium hydroxybutyrate Identification Patent-Specific Data (1) Location in Patent

Reference

Claim

Laboratorio Farmaceutico C.T. S.r.l.

Patent: US4983632 A1, 1991 ; Title/Abstract Full Text Show Details

Physical Data Crystal Property Description (1) Colour & Other Properties

Reference

light-yellow

NICOX S.A.

Patent: WO2005/54175 A2, 2005 ; Title/Abstract Full Text Show Details

Spectra IR Spectroscopy (1) Description (IR Spectroscopy)

Original Text (IR Spectroscopy)

Reference

in KBr

IR(KBr)cm-1: 2958, 1653, 1562 (C=O), 1403,1305, 1059

NICOX S.A.

Patent: WO2005/54175 A2, 2005 ; Title/Abstract Full Text Show Details

Mass Spectrometry (1) Description (Mass Spectrometry)

Comment (Mass Spectrometry)

Reference

5


ESI (Electrospray ionisation)

NICOX S.A.

Patent: WO2005/54175 A2, 2005 ;

Molecular peak

Title/Abstract Full Text Show Details

UV/VIS Spectroscopy (1) Description (UV/VIS Spectroscopy)

Absorption Maxima (UV/VIS)

Reference

Spectrum

362 nm

Zhang, Jiong; Huo, Shuying; Shi, Hongmei; Shen, Shigang; Shang, Yanli

Transition Metal Chemistry, 2013 , vol. 38, # 1 p. 15 - 20 Title/Abstract Full Text View citing articles Show Details

Other Data Use (2) Use Pattern

Reference

angiogenic material

Wright, Emma Jayne; Huckle, James William; Ali, Saad Aboul Majeed

Patent: US2004/265282 A1, 2004 ; Title/Abstract Full Text Show Details

fixation devices for tissue repair

Wright, Emma Jayne; Huckle, James William; Ali, Saad Aboul Majeed

Patent: US2004/265282 A1, 2004 ; Title/Abstract Full Text Show Details

Chemical Name: silver 4-hydroxybutyrate Reaxys Registry Number: 3708529

CAS Registry Number: 193960-46-2 Type of Substance: acyclic Molecular Formula: Ag*C4H7O3

Linear Structure Formula: Ag(1+)*O2CCH2CH2CH2OH(1-) =

1 prep out of 3 reactions.

AgO2CCH2CH2CH2OH Molecular Weight: 210.966

InChI Key: AINPQCTYYCCWKG-UHFFFAOYSA-M

19

Synthesize | Hide Details Find similar Chemical Names and Synonyms silver 4-hydroxybutyrate, 4-hydroxy-butyric acid ; silver (I)-compound, 4-Hydroxy-buttersaeure; Silber(I)-Verbindung Physical Data Melting Point (1) Melting Point

Solvent (Melting Point)

Reference

178 - 180 °C

aq. ethanol

Paul; Tchelitcheff

Bulletin de la Societe Chimique de France, 1948 , p. 197,202 Full Text Show Details

Physical Data (1)

2


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