(S)-1-Phenylpropan-2-amine (Dextroamphetamine; (S)-Amphetamine)

Reaxys

PubChem

eMolecules

Reactions (362)

Substances (1)

Structure

Citations (570)

Structure/Compound Data Chemical Name: dexamfetamine Reaxys Registry Number: 2205872

CAS Registry Number: 51-64-9 Type of Substance: isocyclic Molecular Formula: C9H13N Linear Structure Formula: NH2CH(CH3)CH2(C6H5) Molecular Weight: 135.209 InChI Key: KWTSXDURSIMDCE-QMMMGPOBSA-N

1

N° of preparations All Preps | All Reactions 97 prep out of 362 reactions.

Available Data

N° of ref.

Identification Physical Data (53) Spectra (21) Bioactivity (303) Other Data (178)

570

Synthesize | Hide Details Find similar Chemical Names and Synonyms dexamfetamine, d-amphetamine Identification Substance Label (43) Label

Reference

AMP

Ichikawa; Kurok; Kitchen; Meltzer

European Journal of Pharmacology, 1995 , vol. 287, # 2 p. 179 - 184 Title/Abstract Full Text View citing articles Show Details

Yamamoto, Yoshiko; Yamamoto, Keiichi; Hayase, Tamaki; Fukui, Yuko; Shiota, Kohei

Reproductive Toxicology, 1998 , vol. 12, # 2 p. 133 - 137 Title/Abstract Full Text View citing articles Show Details

Shi Wei-Xing; Nathaniel; Bunney

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 274, # 2 p. 735 - 740 Title/Abstract Full Text View citing articles Show Details

Chłoń-Rzepa, Grażyna; Zagórska, Agnieszka; Żmudzki, Paweł; Bucki, Adam; Kołaczkowski, Marcin; Partyka, Anna; Wesołowska, Anna; Kazek, Grzegorz;

Głuch-Lutwin, Monika; Siwek, Agata; Starowicz, Gabriela; Pawłowski, Maciej

Archiv der Pharmazie, 2016 , vol. 349, # 12 p. 889 - 903 Title/Abstract Full Text Show Details

AMPH

Sulzer, David; Remy, Carl St.; Rayport, Stephen

Molecular Pharmacology, 1996 , vol. 49, # 2 p. 338 - 342 Title/Abstract Full Text View citing articles Show Details

Wang; McGinty

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 273, # 2 p. 909 - 917 Title/Abstract Full Text View citing articles Show Details

Dluzen, Dean E.; Anderson, Linda I.

European Journal of Pharmacology, 1998 , vol. 341, # 1 p. 23 - 32 Title/Abstract Full Text View citing articles Show Details

Liu, Pei-Shan; Liaw, Chwen-Tzy; Lin, Meng-Kai; Shin, Song-Huah; Kao, Lung-Sen; Lin, Lih-Fang

European journal of pharmacology, 2003 , vol. 460, # 1 p. 9 - 17 Title/Abstract Full Text View citing articles Show Details

Riddle, Evan L.; Hanson, Glen R.; Fleckenstein, Annette E.

European Journal of Pharmacology, 2007 , vol. 571, # 1 p. 25 - 28 Title/Abstract Full Text View citing articles Show Details

Harvey, Eric L.; Baker, Lisa E.

Psychopharmacology, 2016 , vol. 233, # 4 p. 673 - 680 Title/Abstract Full Text View citing articles Show Details

amphetamine

Martella; Madeo; Maltese; Vanni; Puglisi; Ferraro; Schirinzi; Valente; Bonanni; Shen; Mandolesi; Mercuri; Bonsi; Pisani

Neurobiology of Disease, 2016 , vol. 91, p. 21 - 36 Title/Abstract Full Text View citing articles Show Details

1

Decker, Ann M.; Partilla, John S.; Baumann, Michael H.; Rothman, Richard B.; Blough, Bruce E.

MedChemComm, 2016 , vol. 7, # 8 p. 1657 - 1663 Title/Abstract Full Text View citing articles Show Details

13

Hale, Lillian V. A.; Szymczak, Nathaniel K.

Journal of the American Chemical Society, 2016 , vol. 138, # 41 p. 13489 - 13492 Title/Abstract Full Text Show Details

14b

Martínez-Montero, Lía; Gotor, Vicente; Gotor-Fernández, Vicente; Lavandera, Iván

Advanced Synthesis and Catalysis, 2016 , vol. 358, # 10 p. 1618 - 1624 Title/Abstract Full Text Show Details

7

CHEMAPOTHECA, LLC; Meckler, Harold; Gregg, Brian Thomas; Yang, Jie

Patent: US2015/183716 A1, 2015 ; Title/Abstract Full Text Show Details

A

Molnr, Borbla; Fodor, Blanka; Boldizsr, Imre; Molnr-Perl, Ibolya

Analytical Chemistry, 2015 , vol. 87, # 20 p. 10188 - 10192 Title/Abstract Full Text View citing articles Show Details

AM

Earla, Ravinder; Kumar, Santosh; Wang, Lei; Bosinger, Steven; Li, Junhao; Shah, Ankit; Gangwani, Mohitkumar; Nookala, Anantha; Liu, Xun; Cao, Lu; Jackson, Austin; Silverstein, Peter S.; Fox, Howard S.; Li, Weihua; Kumar, Anil

Drug Metabolism and Disposition, 2014 , vol. 42, # 12 p. 2097 - 2108 Title/Abstract Full Text Show Details

Formula V

IND-SWIFT LABORATORIES LIMITED; BHIRUD Shekhar Bhaskar; SARIN GURDEEP, Singh; KUMAR, Rajiv

Patent: WO2013/11526 A1, 2013 ; Title/Abstract Full Text Show Details

Amp

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

5

Li, Bryan; Samp, Lacey; Sagal, John; Hayward, Cheryl M.; Yang, Christine; Zhang, Zhijun

Journal of Organic Chemistry, 2013 , vol. 78, # 3 p. 1273 - 1277 Title/Abstract Full Text View citing articles Show Details

(S)-3d

Fesko, Kateryna; Steiner, Kerstin; Breinbauer, Rolf; Schwab, Helmut; Schuermann, Martin; Strohmeier, Gernot A.

Journal of Molecular Catalysis B: Enzymatic, 2013 , vol. 96, p. 103 - 110 Title/Abstract Full Text View citing articles Show Details

2a

Colucid Pharmaceuticals, Inc.

Patent: US2010/256229 A1, 2010 ; Title/Abstract Full Text Show Details

III

ARCHIMICA, INC.; MEUDT, Andreas; WISDOM, Richard; HELMKE, Jason; QIU, Guofang; MEENK, Paul

Patent: WO2010/42120 A1, 2010 ;

Title/Abstract Full Text Show Details

(+)AM

Holt, Andrew; Smith, David J.; Cendron, Laura; Zanotti, Giuseppe; Rigo, Adelio; Di Paolo, Maria Luisa

Molecular Pharmacology, 2008 , vol. 73, # 2 p. 525 - 538 Title/Abstract Full Text View citing articles Show Details

9

Routaboul, Lucie; Vanthuyne, Nicolas; Gastaldi, Stephane; Gil, Gerard; Bertrand, Michele

Journal of Organic Chemistry, 2008 , vol. 73, # 2 p. 364 - 368 Title/Abstract Full Text View citing articles Show Details

47

Lewin, Anita H.; Navarro, Hernan A.; Wayne Mascarella

Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 15 p. 7415 - 7423 Title/Abstract Full Text View citing articles Show Details

(S)-9

Nechab, Malek; Azzi, Nadia; Vanthuyne, Nicolas; Bertrand, Michele; Gastaldi, Stephane; Gil, Gerard

Journal of Organic Chemistry, 2007 , vol. 72, # 18 p. 6918 - 6923 Title/Abstract Full Text View citing articles Show Details

L-amph

Botta, Bruno; D'Acquarica, Ilaria; Nevola, Laura; Sacco, Fabiola; Lopez, Zara Valbuena; Zappia, Giovanni; Fraschetti, Caterina; Speranza, Maurizio; Tafi, Andrea; Caporuscio, Fabiana; Letzel, Matthias C.; Mattay, Jochen

European Journal of Organic Chemistry, 2007 , # 36 p. 5995 - 6002 Title/Abstract Full Text View citing articles Show Details

Show next 20

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Label

Reference

(+)-AMPH

Cashman, John R.; Xiong, Yeng N.; Lifen, Xu; Janowsky, Aaron

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 288, # 3 p. 1251 - 1260 Title/Abstract Full Text View citing articles Show Details

Reviriego, Felipe; Rodriguez-Franco, Maria Isabel; Navarro, Pilar; Garcia-Espana, Enrique; Liu-Gonzalez, Malva; Verdejo, Begona; Domenech, Antonio

Journal of the American Chemical Society, 2006 , vol. 128, # 51 p. 16458 - 16459 Title/Abstract Full Text View citing articles Show Details

Amph

Casis, Oscar; Espina, Laura; Gallego, Monica

Journal of Cardiovascular Pharmacology, 2000 , vol. 36, # 3 p. 390 - 395 Title/Abstract Full Text View citing articles Show Details

Zolkowska, Dorota; Rothman, Richard B.; Baumann, Michael H.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 2 p. 604 - 610 Title/Abstract Full Text View citing articles Show Details

16'

Fecik, Robert A.; Devasthale, Pratik; Pillai, Segaran; Keschavarz-Shokri, Ali; Shen, Linus; Mitscher, Lester A.

Journal of Medicinal Chemistry, 2005 , vol. 48, # 4 p. 1229 - 1236 Title/Abstract Full Text View citing articles Show Details

3d

Yang, Bo; Zhang, Yanjun; Zhang, Shusheng; Izumi

Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 2005 , vol. 44, # 6 p. 1312 - 1316 Title/Abstract Full Text View citing articles Show Details

D-amph

Pascoli, Vincent; Valjent, Emmanuel; Corbille, Anne-Gaelle; Corvol, Jean-Christophe; Tassin, Jean-Pol; Girault, Jean-Antoine; Herve, Denis

Molecular Pharmacology, 2005 , vol. 68, # 2 p. 421 - 429 Title/Abstract Full Text View citing articles Show Details

13a-(S)

Sayyed, Iliyas Ali; Sudalai, Arumugam

Tetrahedron Asymmetry, 2004 , vol. 15, # 19 p. 3111 - 3116 Title/Abstract Full Text View citing articles Show Details

11

Shi, Xiao-Xin; Yao, Jian-Zhong; Kang, Li; Shen, Chun-Li; Yi, Fei

Journal of Chemical Research, 2004 , # 10 p. 681 - 683 Title/Abstract Full Text View citing articles Show Details

Merck 587

Byrnes-Blake, Kelly A.; Laurenzana, Elizabeth M.; Carroll, F. Ivy; Abraham, Philip; Gentry, W. Brooks; Landes, Reid D.; Owens, S. Michael

European Journal of Pharmacology, 2003 , vol. 461, # 2-3 p. 119 - 128 Title/Abstract Full Text View citing articles Show Details

(S)-1

Gonzalez-Sabin, Javier; Gotor, Vicente; Rebolledo, Francisca

Tetrahedron Asymmetry, 2002 , vol. 13, # 12 p. 1315 - 1320 Title/Abstract Full Text View citing articles Show Details

(S)-7

Pallavicini, Marco; Bolchi, Cristiano; Fumagalli, Laura; Valoti, Ermanno; Villa, Luigi

Tetrahedron Asymmetry, 2002 , vol. 13, # 20 p. 2277 - 2282 Title/Abstract Full Text View citing articles Show Details

Merck 623

Poerzgen, Peter; Park, Sang Ki; Hirsh, Jay; Sonders, Mark S.; Amara, Susan G.

Molecular Pharmacology, 2001 , vol. 59, # 1 p. 83 - 95 Title/Abstract Full Text View citing articles Show Details

M12: 2996, AMPH

Kuo, Dong-Yih; Hsu, Chao-Tien; Cheng, Juei-Tang

Life Sciences, 2001 , vol. 70, # 3 p. 243 - 251 Title/Abstract Full Text View citing articles Show Details

S(+)-amph

Bunzow; Sonders; Arttamangkul; Harrison; Zhang; Quigley; Darland; Suchland; Pasumamula; Kennedy; Olson; Magenis; Amara; Grandy

Molecular Pharmacology, 2001 , vol. 60, # 6 p. 1181 - 1188 Title/Abstract Full Text View citing articles Show Details

(+)-AMP

Riviere, Gilles J.; Gentry, W. Brooks; Owens, S. Michael

Journal of Pharmacology and Experimental Therapeutics, 2000 , vol. 292, # 3 p. 1042 - 1047 Title/Abstract Full Text View citing articles Show Details

Riviere, Gilles J.; Byrnes, Kelly A.; Gentry, W. Brooks; Owens, S. Michael

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 291, # 3 p. 1220 - 1226 Title/Abstract Full Text View citing articles Show Details

S-23

Grunewald, Gary L.; Caldwell, Timothy M.; Li, Qifang; Criscione, Kevin R.

Bioorganic and Medicinal Chemistry, 1999 , vol. 7, # 5 p. 869 - 880 Title/Abstract Full Text View citing articles Show Details

4

Blagg, Julian; Davies, Stephen G.

Tetrahedron, 1987 , vol. 43, # 19 p. 4463 - 4472 Title/Abstract Full Text View citing articles Show Details

Hegedues, H.; Gergely, A.; Horvath, P.; Noszal, B.

Journal of Chemical Research, Miniprint, 1999 , # 5 p. 1331 - 1342 Title/Abstract Full Text Show Details

amp

Maes, J.H. Roald; Vossen, Jo M.H.

European Journal of Pharmacology, 1997 , vol. 319, # 1 p. 5 - 11 Title/Abstract Full Text View citing articles Show Details

Merck 12,2996

Schad, Christina A.; Justice, Joseph B.; Holtzmann, Stephen G.

European Journal of Pharmacology, 1995 , vol. 275, # 1 p. 9 - 16 Title/Abstract Full Text View citing articles Show Details

(S)-(+)-AMPH

Florin; Kuczenski; Segal

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 274, # 1 p. 231 - 241 Title/Abstract Full Text View citing articles Show Details

d-AM

Pugsley; Davis; Akunne; Mackenzie; Shih; Damsma; Wikstrom; Whetzel; Georgic; Cooke; Demattos; Corbin; Glase; Wise; Dijkstra; Heffner

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 275, # 3 p. 1355 - 1366 Title/Abstract Full Text View citing articles Show Details

(S)(+)-2

Harsche; Oelschlaeger; Engel

Archiv der Pharmazie, 1992 , vol. 325, # 9 p. 593 - 595 Title/Abstract Full Text View citing articles Show Details

15a

Ikota; Achiwa; Yamada

Chemical and Pharmaceutical Bulletin, 1983 , vol. 31, # 3 p. 887 - 894 Title/Abstract Full Text View citing articles Show Details

(S)-(+)-4

Glennon; Liebowitz; Anderson III

Journal of Medicinal Chemistry, 1980 , vol. 23, # 3 p. 294 - 299 Title/Abstract Full Text View citing articles Show Details

Patent-Specific Data (7) Prophetic Compound

Related Markush Structure (RN)

Location in Patent

Reference

Page/Page column

Mickle, Travis

Patent: US2014/171510 A1, 2014 ; Title/Abstract Full Text Show Details

CHEMAPOTHECA, LLC; Meckler, Harold; Gregg, Brian Thomas; Yang, Jie

Patent: US2015/183716 A1, 2015 ; Title/Abstract Full Text Show Details

22528436

BASF SE

Patent: US2012/123155 A1, 2012 ; Title/Abstract Full Text Show Details

20353528

Johnson Matthey Public Limited Company

Patent: US2010/125146 A1, 2010 ;

Title/Abstract Full Text Show Details

19731841

Cambrex Charles City

Patent: US2009/292143 A1, 2009 ; Title/Abstract Full Text Show Details

11337200

Caron, Marc G.; Sotnikova, Tatyana D.; Gainetdinov, Raul R.

Patent: US2007/27208 A1, 2007 ; Title/Abstract Full Text Show Details

prophetic product

BOEHRINGER INGELHEIM CHEMICALS INC

Patent: JP2005/507936 A, 2005 ; Title/Abstract Full Text Show Details

19815298

Yamakawa Chemical Industry Co., Ltd.

Patent: US6342636 B1, 2002 ; Title/Abstract Full Text Show Details

Related Structure (2) Related Structure

Reference

Configuration.

Karrer; Ehrhardt

Helvetica Chimica Acta, 1951 , vol. 34, p. 2202,2208 Full Text Show Details

Herbert

Acta Crystallographica, Section B: Structural Crystallography and Crystal Chemistry, 1978 , vol. 34, p. 611 Full Text Show Details

Schrecker

Journal of Organic Chemistry, 1957 , vol. 22, p. 33 Full Text View citing articles Show Details

Cervinka et al.

Zeitschrift fuer Chemie (Stuttgart, Germany), 1968 , vol. 8, p. 24 Full Text Show Details

Busser,U.; Haller,R.

Tetrahedron Letters, 1973 , p. 231 - 232 Full Text View citing articles Show Details

Derivative (10)

Derivative

Comment (Derivative)

Reference

(S)-(+)-amphetamine hydrochloride

Davies, Stephen G.; Dixon, Darren J.

Journal of the Chemical Society. Perkin Transactions 1, 2002 , # 16 p. 1869 - 1876 Title/Abstract Full Text View citing articles Show Details

Fecik, Robert A.; Devasthale, Pratik; Pillai, Segaran; Keschavarz-Shokri, Ali; Shen, Linus; Mitscher, Lester A.

Journal of Medicinal Chemistry, 2005 , vol. 48, # 4 p. 1229 - 1236 Title/Abstract Full Text View citing articles Show Details

Shi, Xiao-Xin; Yao, Jian-Zhong; Kang, Li; Shen, Chun-Li; Yi, Fei

Journal of Chemical Research, 2004 , # 10 p. 681 - 683 Title/Abstract Full Text View citing articles Show Details

dextroamphetamine sulfate

Grunewald, Gary L.; Caldwell, Timothy M.; Li, Qifang; Criscione, Kevin R.

Bioorganic and Medicinal Chemistry, 1999 , vol. 7, # 5 p. 869 - 880 Title/Abstract Full Text View citing articles Show Details

(S)-(+)-amphetamine hydrochloride

Rozwadowska

Tetrahedron Asymmetry, 1993 , vol. 4, # 7 p. 1619 - 1624 Title/Abstract Full Text View citing articles Show Details

(S)-(+)-amphetamine hydrochloride; Damphetamine sulfate

Buckley, Thomas F.; Rapoport, Henry

Journal of the American Chemical Society, 1981 , vol. 103, # 20 p. 6157 - 6163 Title/Abstract Full Text View citing articles Show Details

Hydrochlorid (R)-5a: UV, CD

Smith et al.

Journal of the American Chemical Society, 1978 , vol. 100, p. 3714,3715 Full Text Show Details

Sulfat: F>300grad, α(D)=20.1grad

Repke et al.

Journal of Pharmaceutical Sciences, 1978 , vol. 67, p. 1167,1168 Full Text Show Details

<α>(D)25:

Smith et al.

Journal of the American Chemical Society, 1978 , vol. 100, p. 3714,3715 Full Text Show Details

Hydrochlorid (S)-5a: +21.6grad

Hydrochlorid: CD

Smith; Burrows; Marks; Lynch; Chen

Journal of the American Chemical Society, 1977 , vol. 99, # 3 p. 707 - 713 Title/Abstract Full Text View citing articles Show Details

*HCl: <α>(D)16: +1.55grad <W>

Busser,U.; Haller,R.

Tetrahedron Letters, 1973 , p. 231 - 232 Full Text View citing articles Show Details

Hydrochlorid: <α>(D)15: +1.55grad

Busser,U.; Haller,R.

Tetrahedron Letters, 1973 , p. 231 - 232 Full Text View citing articles Show Details

Physical Data Melting Point (1) Melting Point

Comment (Melting Point)

Reference

27.5 °C

nach Erweichen.

Jaeger; van Dijk

Proceedings of the Koninklijke Nederlandse Akademie van Wetenschappen, Series B: Physical Sciences, 1941 , vol. 44, p. 26,36,37 Full Text Show Details

Boiling Point (8) Boiling Point

Pressure (Boiling Point)

Reference

83 - 86 °C

15 Torr

Ikota; Achiwa; Yamada

Chemical and Pharmaceutical Bulletin, 1983 , vol. 31, # 3 p. 887 - 894 Title/Abstract Full Text View citing articles Show Details

40 - 60 °C

0.05 Torr

Repke et al.

Journal of Pharmaceutical Sciences, 1978 , vol. 67, p. 1167,1168 Full Text Show Details

83.5 - 84 °C

13 Torr

Pratesi; La Manna

Farmaco, Edizione Scientifica, 1956 , vol. 11, p. 33,41 Full Text Show Details

65 °C

5 Torr

Murakami; Akagi

Nippon Kagaku Zasshi, 1954 , vol. 75, p. 532,534 Chem.Abstr., 1957 , p. 11242 Full Text Show Details

80 °C

12 Torr

Jaeger; van Dijk

Proceedings of the Koninklijke Nederlandse Akademie van Wetenschappen, Series B: Physical Sciences, 1941 , vol. 44, p. 26,36,37 Full Text Show Details

70 °C

8 Torr

Jaeger; van Dijk

Proceedings of the Koninklijke Nederlandse Akademie van Wetenschappen, Series B: Physical Sciences, 1941 , vol. 44, p. 26,36,37 Full Text Show Details

68 °C

7 Torr

Jaeger; van Dijk

Proceedings of the Koninklijke Nederlandse Akademie van Wetenschappen, Series B: Physical Sciences, 1941 , vol. 44, p. 26,36,37 Full Text Show Details

60 °C

4 Torr

Jaeger; van Dijk

Proceedings of the Koninklijke Nederlandse Akademie van Wetenschappen, Series B: Physical Sciences, 1941 , vol. 44, p. 26,36,37 Full Text Show Details

Density (3) Density

Reference Temperature

Measurement Temperature

Type (Density)

0.949 g·cm-3

4 °C

20 °C

Smith, Howard E.; Neergaard, Jon R.; Paulis, Tomas de; Chen, Fu-Ming

Journal of the American Chemical Society, 1983 , vol. 105, # 6 p. 1578 - 1584 Title/Abstract Full Text View citing articles Show Details

0.9337 g·cm-3

18 °C

crystallographic

Jaeger; van Dijk

Reference

Proceedings of the Koninklijke Nederlandse Akademie van Wetenschappen, Series B: Physical Sciences, 1941 , vol. 44, p. 26,36,37 Full Text Show Details

15 °C

Leithe

Chemische Berichte, 1932 , vol. 65, p. 660,665 Full Text Show Details

0.94 g·cm-3

4 °C

Association (MCS) (3) Description (Association (MCS))

Partner (Association (MCS))

Stability constant of the complex with ...

sodium 3,5bis(ethoxycarbonyl)pyrazolate

Stability constant of the complex with ...

sodium 3,5bis(ethoxycarbonyl)pyrazolate

Further physical properties of the complex

bilirubin

Solvent (Association (MCS))

Temperature (Association (MCS))

dimethylsulfoxided6

25 °C

Reviriego, Felipe; Rodriguez-Franco, Maria Isabel; Navarro, Pilar; Garcia-Espana, Enrique; Liu-Gonzalez, Malva; Verdejo, Begona; Domenech, Antonio

Journal of the American Chemical Society, 2006 , vol. 128, # 51 p. 16458 - 16459 Title/Abstract Full Text View citing articles Show Details

H2O

24.95 °C

Reviriego, Felipe; Rodriguez-Franco, Maria Isabel; Navarro, Pilar; Garcia-Espana, Enrique; Liu-Gonzalez, Malva; Verdejo, Begona; Domenech, Antonio

Journal of the American Chemical Society, 2006 , vol. 128, # 51 p. 16458 - 16459 Title/Abstract Full Text View citing articles Show Details

benzene

25 °C

Lightner, David A.; An, Jing-Yi

Tetrahedron, 1987 , vol. 43, # 19 p. 4287 - 4296 Title/Abstract Full Text View citing articles Show Details

Reference

Chromatographic Data (1) Chromatographic data

Reference

HPLC (High performance liquid chromatography)

Taschwer, Magdalena; Seidl, Yvonne; Mohr, Stefan; Schmid, Martin G.

Chirality, 2014 , vol. 26, # 8 p. 411 - 418 Title/Abstract Full Text View citing articles Show Details

Circular Dichroism (4) Solvent (Circular Dichroism)

Comment (Circular Dichroism)

Reference

H2O various solvent(s)

Hegedues, H.; Gergely, A.; Horvath, P.; Noszal, B.

Journal of Chemical Research, Miniprint, 1999 , # 5 p. 1331 - 1342 Title/Abstract Full Text Show Details

cyclohexane

268 - 255 nm

Smith, Howard E.; Neergaard, Jon R.; Paulis, Tomas de; Chen, Fu-Ming

Journal of the American Chemical Society, 1983 , vol. 105, # 6 p. 1578 - 1584 Title/Abstract Full Text View citing articles Show Details

methanol

269 - 257 nm

Smith, Howard E.; Neergaard, Jon R.; Paulis, Tomas de; Chen, Fu-Ming

Journal of the American Chemical Society, 1983 , vol. 105, # 6 p. 1578 - 1584 Title/Abstract Full Text View citing articles Show Details

Smith et al.

Journal of the American Chemical Society, 1978 , vol. 100, p. 3714,3715 Full Text Show Details

Crystal Property Description (1) Colour & Other Properties

Location

Reference

colourless

Paragraph 0123; 0140; 0144; 0148

CHEMAPOTHECA, LLC; Meckler, Harold; Gregg, Brian Thomas; Yang, Jie

Patent: US2015/183716 A1, 2015 ; Title/Abstract Full Text Show Details

Electrochemical Behaviour (1) Description (Electrochemical Behaviour)

Comment (Electrochemical Behaviour)

Reference

Protonation

pH dependence

Hegedues, H.; Gergely, A.; Horvath, P.; Noszal, B.

Journal of Chemical Research, Miniprint, 1999 , # 5 p. 1331 - 1342 Title/Abstract Full Text Show Details

Further Information (3) Description (Further Information)

Reference

Further information

Smith et al.

Journal of the American Chemical Society, 1978 , vol. 100, p. 3714,3715 Full Text Show Details

Further information

Smith; Burrows; Marks; Lynch; Chen

Journal of the American Chemical Society, 1977 , vol. 99, # 3 p. 707 - 713 Title/Abstract Full Text View citing articles Show Details

Further information

Warren,M.E.; Smith,H.E.

Journal of the American Chemical Society, 1965 , vol. 87, p. 1757 - 1764 Full Text View citing articles Show Details

Optical Rotatory Dispersion (1) Comment (Optical Rotatory Dispersion)

Reference

438 - 728 nm

Jaeger; van Dijk

Proceedings of the Koninklijke Nederlandse Akademie van Wetenschappen, Series B: Physical Sciences, 1941 , vol. 44, p. 26,36,37 Full Text Show Details

Optical Rotatory Power (25) Type (Optical Rotatory Power)

Concentration (Optical Rotatory Power)

Enantiomeric excess

[alpha]

1.2 g/100ml

96 %ee

[alpha]

1 g/100ml

[alpha]

Solvent (Optical Rotatory Power)

Optical Rotatory Power

Wavelength (Optical Rotatory Power)

Temperature (Optical Rotatory Power)

chloroform

27.5 deg

589 nm

20 °C

Munoz, Lourdes; Rodriguez, Anna M.; Rosell, Gloria; Bosch, M. Pilar; Guerrero, Angel

Organic and Biomolecular Chemistry, 2011 , vol. 9, # 23 p. 8171 - 8177 Title/Abstract Full Text View citing articles Show Details

CHCl3

40 deg

589 nm

25 °C

Nechab, Malek; Azzi, Nadia; Vanthuyne, Nicolas; Bertrand, Michele; Gastaldi, Stephane; Gil, Gerard

Journal of Organic Chemistry, 2007 , vol. 72, # 18 p. 6918 - 6923 Title/Abstract Full Text View citing articles Show Details

3.5 g/100ml

methanol

33 deg

589 nm

20 °C

Shi, Xiao-Xin; Yao, Jian-Zhong; Kang, Li; Shen, Chun-Li; Yi, Fei

Journal of Chemical Research, 2004 , # 10 p. 681 683 Title/Abstract Full Text View citing articles Show Details

[alpha]

22.4 deg

589 nm

20 °C

Van der Wenden; Von Frijtag Drabbe Kunzel; Mathot; Danhof; Ijzerman; Soudijn

Journal of Medicinal Chemistry, 1995 , vol. 38, # 20 p. 4000 - 4006 Title/Abstract Full Text View citing articles Show Details

[alpha]

neat (no solvent)

37.1 deg

589 nm

24 °C

Grishina, G. V.; Gaidarova, E. L.

Chemistry of Heterocyclic Compounds (New York, NY, United States), 1992 , vol. 28, # 8 p. 898 - 904 Khimiya Geterotsiklicheskikh Soedinenii, 1992 , # 8 p. 1072 - 1078 Title/Abstract Full Text View citing articles Show Details

[alpha]

2.09 g/100ml

methanol

29.2 deg

589 nm

21 °C

Smith, Roger A.; White, Robert L.; Krantz, Allen

Journal of Medicinal Chemistry, 1988 , vol. 31, # 8 p. 1558 - 1566 Title/Abstract Full Text View citing articles Show Details

[alpha]

neat (no solvent)

36 deg

589 nm

Jaeger; van Dijk

Proceedings of the Koninklijke Nederlandse Akademie van Wetenschappen, Series B: Physical Sciences, 1941 , vol. 44, p. 26,36,37

Length of Path

Reference

Full Text Show Details

Lightner, David A.; An, Jing-Yi

Tetrahedron, 1987 , vol. 43, # 19 p. 4287 - 4296 Title/Abstract Full Text View citing articles Show Details

[alpha]

100 weightpercent

36.6 deg

589 nm

20 °C

Leshcheva, I. F.; Sergeev, N. M.; Grishina, G. V.; Potapov, V. M.

Chemistry of Heterocyclic Compounds (New York, NY, United States), 1986 , vol. 22, # 11 p. 1214 - 1225 Khimiya Geterotsiklicheskikh Soedinenii, 1986 , vol. 22, # 11 p. 1503 - 1515 Title/Abstract Full Text View citing articles Show Details

[alpha]

5 cm

neat (no solvent)

33.1 deg

589 nm

22 °C

Smith, Howard E.; Neergaard, Jon R.; Paulis, Tomas de; Chen, Fu-Ming

Journal of the American Chemical Society, 1983 , vol. 105, # 6 p. 1578 - 1584 Title/Abstract Full Text View citing articles Show Details

[alpha]

37.1 deg

589 nm

20 °C

Solov'eva, L. D.; Dem'yanovich, V. M.; Potapov, V. M.

Journal of Organic Chemistry USSR (English Translation), 1981 , vol. 17, # 6 p. 1099 - 1105 Zhurnal Organicheskoi Khimii, 1981 , vol. 17, # 6 p. 1241 - 1248 Title/Abstract Full Text Show Details

[alpha]

34.1 deg

589 nm

Smith et al.

Journal of Organic Chemistry, 1974 , vol. 39, p. 2309 Full Text View citing articles Show Details

[alpha]

neat (no solvent)

36.3 deg

589 nm

19 °C

Potapow; Terentew

Zhurnal Obshchei Khimii, 1958 , vol. 28, p. 3323,3325 Anm. J. Gen. Chem. USSR (Engl. Transl.), 1958 , vol. 28, p. 3349,3351 Anm. Full Text Show Details

[alpha]

c=9

benzene

40.2 deg

589 nm

15 °C

Pratesi; La Manna

Farmaco, Edizione Scientifica, 1956 , vol. 11, p. 33,41 Full Text Show Details

[alpha]

c=9

ethanol

37.4 deg

589 nm

22 °C

Murakami; Akagi

Nippon Kagaku Zasshi, 1954 , vol. 75, p. 532,534 Chem.Abstr., 1957 , p. 11242 Full Text Show Details

[alpha]

neat (no solvent)

35.6 deg

589 nm

15 °C

Leithe

Chemische Berichte, 1932 , vol. 65, p. 660,665 Full Text Show Details

[alpha]

c=9

cyclohexane

35.8 deg

589 nm

15 °C

Leithe

Chemische Berichte, 1932 , vol. 65, p. 660,665 Full Text Show Details

[alpha]

c=9

benzene

37.6 deg

589 nm

15 °C

Leithe

Chemische Berichte, 1932 , vol. 65, p. 660,665 Full Text Show Details

[alpha]

c=12

CCl4

54.3 deg

589 nm

15 °C

Leithe

Chemische Berichte, 1932 , vol. 65, p. 660,665 Full Text Show Details

[alpha]

c=11

CHCl3

36.2 deg

589 nm

15 °C

Leithe

Chemische Berichte, 1932 , vol. 65, p. 660,665 Full Text Show Details

[alpha]

c=11

diethyl ether

29.9 deg

589 nm

15 °C

Leithe

Chemische Berichte, 1932 , vol. 65, p. 660,665 Full Text Show Details

Hide facts Type (Optical

Concentration (Optical

Solvent (Optical

Optical Rotatory

Wavelength (Optical

Temperature (Optical

Reference

Rotatory Power)

Rotatory Power)

Rotatory Power)

Rotatory Power)

Rotatory Power)

[alpha]

c=11

ethanol

34.5 deg

589 nm

15 °C

Leithe

Chemische Berichte, 1932 , vol. 65, p. 660,665 Full Text Show Details

[alpha]

c=9

methanol

29.4 deg

589 nm

15 °C

Leithe

Chemische Berichte, 1932 , vol. 65, p. 660,665 Full Text Show Details

[alpha]

neat (no solvent)

37.7 deg

578 nm

15 °C

Leithe

Chemische Berichte, 1932 , vol. 65, p. 660,665 Full Text Show Details

[alpha]

neat (no solvent)

43.6 deg

546 nm

15 °C

Leithe

Chemische Berichte, 1932 , vol. 65, p. 660,665 Full Text Show Details

[alpha]

neat (no solvent)

80.3 deg

436 nm

15 °C

Leithe

Chemische Berichte, 1932 , vol. 65, p. 660,665 Full Text Show Details

Power

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

Reference

1.81

Costentin

Annales Pharmaceutiques Francaises, 2006 , vol. 64, # 3 p. 148 - 159 Title/Abstract Full Text View citing articles Show Details

Vapour Pressure (1) Vapour Pressure

Temperature (Vapour Pressure)

Reference

0.24 Torr

20 °C

Lawrence; Elias; Authier-Martin

Canadian Journal of Chemistry, 1984 , vol. 62, # 10 p. 1886 - 1888 Title/Abstract Full Text View citing articles Show Details

Spectra NMR Spectroscopy (13) Description (NMR Spectroscopy)

Frequency (NMR Spectroscopy)

Original Text (NMR Spectroscopy)

dichloromethaned2

supporting information

Hale, Lillian V. A.; Szymczak, Nathaniel K.

Journal of the American Chemical Society, 2016 , vol. 138, # 41 p. 13489 - 13492 Title/Abstract Full Text Show Details

chloroform-d1

300 MHz

‘H NMR (300 MHz, CDC13) ö 7.36 -7.26 (m, 2H), 7.23-7.13 (m, 3H), 3.263.03 (m, 1H), 2.72 (dd, J=13.2, 5.4 Hz, 1H), 2.53 (dd, J=13.2, 8.0 Hz, 1H), 1.20 (br s, 2H), 1.13 (d, J=6.3 Hz, 3H).

Paragraph 0140

CHEMAPOTHECA, LLC; Meckler, Harold; Gregg, Brian Thomas; Yang, Jie

Patent: US2015/183716 A1, 2015 ;

400 MHz 1H NMR (CDCl3) 7.34-7.20 (m, 5), 3.22-3.17 (m, 1), 2.762.72 (d of d, J=13.2 Hz,

Page/Page column 3

Nucleus (NMR Spectroscopy)

Coupling Nuclei

Solvents (NMR Spectroscopy)

Chemical shifts Spectrum

1H

Chemical shifts

1H

1H

chloroform-d1

400 MHz

Location

Comment (NMR Spectroscopy)

Reference

Title/Abstract Full Text Show Details

Signals given

Johnson Matthey Public Limited Company

Patent: US2010/125146 A1, 2010 ; Title/Abstract Full Text Show Details

J'=5.4 Hz, 1), 2.57-2.52 (d of d, J=13.2 Hz, J'=8.1 Hz, 1), 1.16-1.14 (d, J=6.3 Hz, 3). Spectrum

13C

75 MHz

Routaboul, Lucie; Vanthuyne, Nicolas; Gastaldi, Stephane; Gil, Gerard; Bertrand, Michele

Journal of Organic Chemistry, 2008 , vol. 73, # 2 p. 364 - 368 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

1H

CDCl3

Nordlander, J. Eric; Njoroge, F. George; Payne, Mark J.; Warman, Dhiraj

Journal of Organic Chemistry, 1985 , vol. 50, # 19 p. 3481 - 3484 Title/Abstract Full Text View citing articles Show Details

Yang, Bo; Zhang, Yanjun; Zhang, Shusheng; Izumi

Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 2005 , vol. 44, # 6 p. 1312 - 1316 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

CDCl3

Yang, Bo; Zhang, Yanjun; Zhang, Shusheng; Izumi

Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 2005 , vol. 44, # 6 p. 1312 - 1316 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

1H

CDCl3

200 MHz

Gonzalez-Sabin, Javier; Gotor, Vicente; Rebolledo, Francisca

Tetrahedron Asymmetry, 2002 , vol. 13, # 12 p. 1315 - 1320 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

CDCl3

75.5 MHz

Gonzalez-Sabin, Javier; Gotor, Vicente; Rebolledo, Francisca

Tetrahedron Asymmetry, 2002 , vol. 13, # 12 p. 1315 - 1320 Title/Abstract Full Text View citing articles Show Details

1H

1H

CDCl3

200 MHz

Gonzalez-Sabin, Javier; Gotor, Vicente; Rebolledo, Francisca

Tetrahedron Asymmetry, 2002 , vol. 13, # 12 p. 1315 - 1320 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

1H

CDCl3

300 MHz

Pallavicini, Marco; Bolchi, Cristiano; Fumagalli, Laura; Valoti, Ermanno; Villa, Luigi

Tetrahedron Asymmetry, 2002 , vol. 13, # 20 p. 2277 - 2282 Title/Abstract Full Text View citing articles Show Details

Spin-spin coupling constants

CDCl3

1H-1H

Nordlander, J. Eric; Njoroge, F. George; Payne, Mark J.; Warman, Dhiraj

Journal of Organic Chemistry, 1985 , vol. 50, # 19 p. 3481 - 3484 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

Δν(Me) (in Anw. v. PEA)

Jennison,C.P.R.; Mackay,D.

Canadian Journal of Chemistry, 1973 , vol. 51, p. 3726 - 3732 Full Text View citing articles Show Details

NMR with shift reagents

Jennison,C.P.R.; Mackay,D.

Canadian Journal of Chemistry, 1973 ,

vol. 51, p. 3726 - 3732 Full Text View citing articles Show Details

IR Spectroscopy (1)

Description (IR Spectroscopy)

Solvent (IR Spectroscopy)

Reference

Bands

KBr

Yang, Bo; Zhang, Yanjun; Zhang, Shusheng; Izumi

Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 2005 , vol. 44, # 6 p. 1312 - 1316 Title/Abstract Full Text View citing articles Show Details

Mass Spectrometry (3) Description (Mass Spectrometry)

Location

Reference

electrospray ionisation (ESI) liquid chromatography mass spectrometry (LCMS) tandem mass spectrometry spectrum

supporting information

Earla, Ravinder; Kumar, Santosh; Wang, Lei; Bosinger, Steven; Li, Junhao; Shah, Ankit; Gangwani, Mohitkumar; Nookala, Anantha; Liu, Xun; Cao, Lu; Jackson, Austin; Silverstein, Peter S.; Fox, Howard S.; Li, Weihua; Kumar, Anil

Drug Metabolism and Disposition, 2014 , vol. 42, # 12 p. 2097 - 2108 Title/Abstract Full Text Show Details

Page/Page column 11

BASF SE

Patent: US2012/123155 A1, 2012 ;

spectrum

Title/Abstract Full Text Show Details

Gonzalez-Sabin, Javier; Gotor, Vicente; Rebolledo, Francisca

Tetrahedron Asymmetry, 2002 , vol. 13, # 12 p. 1315 - 1320 Title/Abstract Full Text View citing articles Show Details

UV/VIS Spectroscopy (3) Description (UV/VIS Spectroscopy)

Solvent (UV/VIS Spectroscopy)

Absorption Maxima (UV/VIS)

Ext./Abs. Coefficient

Reference

Absorption maxima

cyclohexane

268 nm 262 nm 259 nm 253 nm

150 l·mol-1cm-1

200 l·mol-1cm-1

210 l·mol-1cm-1

170 l·mol-1cm-1

Smith, Howard E.; Neergaard, Jon R.; Paulis, Tomas de; Chen, Fu-Ming

Journal of the American Chemical Society, 1983 , vol. 105, # 6 p. 1578 - 1584 Title/Abstract Full Text View citing articles Show Details

Absorption maxima

methanol

268 nm 264 nm 261 nm 259 nm

140 l·mol-1cm-1

160 l·mol-1cm-1

180 l·mol-1cm-1

200 l·mol-1cm-1

Smith, Howard E.; Neergaard, Jon R.; Paulis, Tomas de; Chen, Fu-Ming

Journal of the American Chemical Society, 1983 , vol. 105, # 6 p. 1578 - 1584 Title/Abstract Full Text View citing articles Show Details

UV/VIS

Smith et al.

Journal of the American Chemical Society, 1978 , vol. 100, p. 3714,3715 Full Text Show Details

Rotational Spectroscopy (1) Description (Rotational Spectroscopy)

Reference

Microwave spectrum

Godfrey, Peter D.; McGlone, Shane J.; Brown, Ronald D.

Journal of Molecular Structure, 2001 , vol. 599, p. 139 - 152 Title/Abstract Full Text View citing articles Show Details

Bioactivity Pharmacological Data (303) 1 of 303

Comment (Pharmacological Data)

Bioactivities present

Reference

John Wyeth and Brother Limited

Patent: US3931244 A1, 1976 ; Title/Abstract Full Text Show Details

Jennison,C.P.R.; Mackay,D.

Canadian Journal of Chemistry, 1973 , vol. 51, p. 3726 - 3732 Full Text View citing articles Show Details

Warren,M.E.; Smith,H.E.

Journal of the American Chemical Society, 1965 , vol. 87, p. 1757 - 1764 Full Text View citing articles Show Details

Smith; Burrows; Marks; Lynch; Chen

Journal of the American Chemical Society, 1977 , vol. 99, # 3 p. 707 - 713 Title/Abstract Full Text View citing articles Show Details

Holland,G.F. et al.

Journal of Medicinal Chemistry, 1963 , vol. 6, p. 519 - 524 Full Text View citing articles Show Details

Boissier; Ratouis; Dumont; Taliani; Forest

Journal of medicinal chemistry, 1967 , vol. 10, # 1 p. 86 - 91 Title/Abstract Full Text View citing articles Show Details

Howe,R.; Rao,B.S.

Journal of Medicinal Chemistry, 1968 , vol. 11, p. 1118 - 1121 Full Text View citing articles Show Details

Verbiscar,A.J.; Abood,L.G.

Journal of Medicinal Chemistry, 1970 , vol. 13, p. 1176 - 1179 Full Text View citing articles Show Details

Mazur,R.H. et al.

Journal of Medicinal Chemistry, 1970 , vol. 13, p. 1217 - 1221 Full Text View citing articles Show Details

Edwards,J.A. et al.

Journal of Medicinal Chemistry, 1974 , vol. 17, p. 200 - 203 Full Text View citing articles Show Details

Matin,S.B. et al.

Journal of Medicinal Chemistry, 1974 , vol. 17, p. 877 - 882 Full Text View citing articles Show Details

Najjar; Blake; Benoit; Lu

Journal of Medicinal Chemistry, 1978 , vol. 21, # 6 p. 555 - 558 Title/Abstract Full Text View citing articles Show Details

Beckett,A.H. et al.

Tetrahedron, 1975 , vol. 31, p. 1531 - 1535 Full Text View citing articles Show Details

Beckett,A.H. et al.

Tetrahedron, 1976 , vol. 32, p. 1267 - 1276 Full Text View citing articles Show Details

Gacek,M.; Undheim,K.

Acta Chemica Scandinavica, Series B: Organic Chemistry and Biochemistry, 1975 , vol. 29, p. 206 - 212 Full Text View citing articles Show Details

Merrell Dow Pharmaceuticals Inc.

Patent: US5426101 A1, 1995 ; Title/Abstract Full Text Show Details

University of Kentucky Research Foundation

Patent: US6087376 A1, 2000 ; Title/Abstract Full Text Show Details

Piccariello, Thomas; Olon, Lawrence P.; Kirk, Randal J.

Patent: US2002/99013 A1, 2002 ; Title/Abstract Full Text Show Details

Pazos,J.F. et al.

Journal of Organic Chemistry, 1974 , vol. 39, p. 1990 - 1995 Full Text View citing articles Show Details

Lederman, Seth; Levensr, Steve; Kucharik JR., Robert

Patent: US2003/96004 A1, 2003 ; Title/Abstract Full Text Show Details

2 of 303

Comment (Pharmacological Data)

Bioactivities present

Reference

Synpatic Pharmaceutical Corporation

Patent: US2003/105318 A1, 2003 ; Title/Abstract Full Text Show Details

Busser,U.; Haller,R.

Tetrahedron Letters, 1973 , p. 231 - 232 Full Text View citing articles Show Details

THE GOVERNMENT OF THE UNITED STATES OF AMERICA as represented by THE DEPARTMENT OF HEALTH AND HUMAN SERVICES

Patent: WO1993/8281 A1, 1993 ; Title/Abstract Full Text Show Details

SHAPIRO; BAZGA; FREEDMAN

Journal of pharmaceutical sciences, 1962 , vol. 51, p. 582 - 584 Title/Abstract Full Text View citing articles Show Details

Schaeffer; Cho; Fischer

Journal of Pharmaceutical Sciences, 1976 , vol. 65, # 1 p. 122 - 126 Title/Abstract Full Text View citing articles Show Details

PSYCHOGENICS INC.

Patent: WO2004/69339 A1, 2004 ; Title/Abstract Full Text Show Details

PREDIX PHARMACEUTICALS HOLDINGS, INC.

Patent: WO2004/69794 A2, 2004 ; Title/Abstract Full Text Show Details

PediaMed Pharmaceuticals, Inc.

Patent: US2004/259809 A1, 2004 ; Title/Abstract Full Text Show Details

ELI LILLY AND COMPANY

Patent: WO2005/19180 A1, 2005 ; Title/Abstract Full Text Show Details

BOEHRINGER INGELHEIM CHEMICALS INC

Patent: JP2005/507936 A, 2005 ; Title/Abstract Full Text Show Details

CNS Response

Patent: US2005/96311 A1, 2005 ; Title/Abstract Full Text Show Details

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Lemaire, Marc; Abraini, Jacques

Patent: US2005/152988 A1, 2005 ; Title/Abstract Full Text Show Details

Celltech Pharma Europe Limited

Patent: EP1185268 B1, 2005 ; Title/Abstract Full Text Show Details

Saegis Pharmaceuticals, Inc.

Patent: US2005/187196 A1, 2005 ; Title/Abstract Full Text Show Details

Novo Nordisk, A/S

Patent: US6972294 B1, 2005 ; Title/Abstract Full Text Show Details

Andersen, Denise Lyn; Frohn, Michael J.; Hong, Fang-Tsao; Liu, Longbin; Lopez, Patricia

Patent: US2005/288502 A1, 2005 ; Title/Abstract Full Text Show Details

Washburn, William; Meng, Wei

Patent: US2006/63722 A1, 2006 ; Title/Abstract Full Text Show Details

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

KETOCYTONYX INC.

Patent: WO2006/34361 A2, 2006 ; Title/Abstract Full Text Show Details

3 of 303

Comment (Pharmacological Data)

Bioactivities present

Reference

Davis, Michael; Ressler, Kerry J.; Chhatwal, Jasmeer P.; McDevitt, Jason P.

Patent: US2006/84659 A1, 2006 ; Title/Abstract Full Text Show Details

NOVO NORDISK A/S

Patent: WO2006/40329 A1, 2006 ; Title/Abstract Full Text Show Details

Searle u. Co.

Patent: US3803223 , 1974 ; Chem.Abstr., 1974 , vol. 80, # 146537 Full Text Show Details

CYPRESS BIOSCIENCE, INC.

Patent: WO2006/55854 A2, 2006 ; Title/Abstract Full Text Show Details

Meng, Wei; Hamann, Lawrence G.; Brigance, Robert

Patent: US2006/142576 A1, 2006 ; Title/Abstract Full Text Show Details

NEW RIVER PHARMACEUTICALS INC.

Patent: WO2006/121552 A2, 2006 ; Title/Abstract Full Text Show Details

Caron, Marc G.; Sotnikova, Tatyana D.; Gainetdinov, Raul R.

Patent: US2007/27208 A1, 2007 ; Title/Abstract Full Text Show Details

Hellstrom, Harold Richard

Patent: US2007/37797 A1, 2007 ; Title/Abstract Full Text Show Details

Maibach, Todd

Patent: US2007/59346 A1, 2007 ; Title/Abstract Full Text Show Details

NOVARTIS AG; NOVARTIS PHARMA GmbH

Patent: WO2007/41366 A1, 2007 ; Title/Abstract Full Text Show Details

CAMBREX CHARLES CITY, INC.

Patent: WO2007/41571 A1, 2007 ; Title/Abstract Full Text Show Details

Bristol-Myers Squibb Company

Patent: US2007/99913 A1, 2007 ; Title/Abstract Full Text Show Details

WYETH

Patent: WO2007/50353 A2, 2007 ; Title/Abstract Full Text Show Details

IRM LLC

Patent: WO2007/89557 A2, 2007 ; Title/Abstract Full Text Show Details

IRM LLC

Patent: WO2007/89667 A1, 2007 ; Title/Abstract Full Text Show Details

BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG

Patent: WO2007/93624 A2, 2007 ; Title/Abstract Full Text Show Details

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

Stoll; Hofmann

Helvetica Chimica Acta, 1955 , vol. 38, p. 421,432 Full Text Show Details

Shapiro et al.

Journal of the American Chemical Society, 1958 , vol. 80, p. 6060,6063 Journal of the American Chemical Society, 1959 , vol. 81, p. 203,207 Full Text Show Details

Karrer; Ehrhardt

Helvetica Chimica Acta, 1951 , vol. 34, p. 2202,2208 Full Text Show Details

4 of 303

Comment (Pharmacological Data)

Bioactivities present

Reference

Leonard et al.

Journal of the American Chemical Society, 1958 , vol. 80, p. 4858,4859 Journal of the American Chemical Society, 1954 , vol. 76, p. 5708,5709,5713 Full Text Show Details

Johns; Burch

Journal of the American Chemical Society, 1938 , vol. 60, p. 919 Full Text View citing articles Show Details

Maguire; Shaw

Journal of the Chemical Society, 1957 , p. 2713 Full Text Show Details

Leaper; Bishop

Pr. Symp. Chem. Mode Action Plant Growth Subst. Wye 1955 S. 211, 213 Full Text Show Details

Shapiro et al.

Journal of the American Chemical Society, 1959 , vol. 81, p. 5646,5648 Full Text Show Details

Matell

Acta Chemica Scandinavica (1947-1973), 1953 , vol. 7, p. 698 Full Text Show Details

Matell

Arkiv foer Kemi, 1956 , vol. 8, p. 79,81, 83 Full Text Show Details

Matell

Arkiv foer Kemi, 1954 , vol. 6, p. 375,378 Full Text Show Details

Magidson; Garkuscha

Zhurnal Obshchei Khimii, 1941 , vol. 11, p. 339,341 Chem.Abstr., 1941 , p. 5868

Full Text Show Details

Parham et al.

Journal of the American Chemical Society, 1952 , vol. 74, p. 5646 Full Text View citing articles Show Details

Leithe

Chemische Berichte, 1932 , vol. 65, p. 660,665 Full Text Show Details

Jaeger; van Dijk

Proceedings of the Koninklijke Nederlandse Akademie van Wetenschappen, Series B: Physical Sciences, 1941 , vol. 44, p. 26,36,37 Full Text Show Details

Potapow; Terentew

Zhurnal Obshchei Khimii, 1958 , vol. 28, p. 3323,3325 Anm. J. Gen. Chem. USSR (Engl. Transl.), 1958 , vol. 28, p. 3349,3351 Anm. Full Text Show Details

Kerwin et al.

Journal of the American Chemical Society, 1950 , vol. 72, p. 3983,3985 Full Text Show Details

FISCHER; PLEIN

Journal of the American Pharmaceutical Association. American Pharmaceutical Association, 1955 , vol. 44, # 5 p. 313 - 316 Title/Abstract Full Text View citing articles Show Details

Gruber; Gunsalus

Journal of Organic Chemistry, 1956 , vol. 21, p. 1024 Full Text View citing articles Show Details

Pratesi; La Manna

Farmaco, Edizione Scientifica, 1956 , vol. 11, p. 33,41 Full Text Show Details

Murakami; Akagi

Nippon Kagaku Zasshi, 1954 , vol. 75, p. 532,534 Chem.Abstr., 1957 , p. 11242 Full Text Show Details

Herbert

Acta Crystallographica, Section B: Structural Crystallography and Crystal Chemistry, 1978 , vol. 34, p. 611 Full Text Show Details

Chatten; Levi

Analytical Chemistry, 1959 , vol. 31, p. 1581,1582,1585 Full Text View citing articles Show Details

5 of 303

Comment (Pharmacological Data)

Bioactivities present

Reference

Temmler-Werke

Patent: DE871155 , 1938 ; Full Text Show Details

Wallis; Nagel

Journal of the American Chemical Society, 1931 , vol. 53, p. 2787,2790 Full Text Show Details

Schrecker

Journal of Organic Chemistry, 1957 , vol. 22, p. 33 Full Text View citing articles Show Details

v. Braun; Friehmelt

Chemische Berichte, 1933 , vol. 66, p. 684 Full Text Show Details

Repke et al.

Journal of Pharmaceutical Sciences, 1978 , vol. 67, p. 1167,1168 Full Text Show Details

Smith et al.

Journal of Organic Chemistry, 1974 , vol. 39, p. 2309 Full Text View citing articles Show Details

Smith et al.

Journal of the American Chemical Society, 1978 , vol. 100, p. 3714,3715 Full Text Show Details

Cervinka et al.

Zeitschrift fuer Chemie (Stuttgart, Germany), 1968 , vol. 8, p. 24 Full Text Show Details

Sarges, Reinhard; Howard, Harry R.; Browne, Ronald G.; Lebel, Lorraine A.; Seymour, Patricia A.; Koe, B. Kenneth

Journal of Medicinal Chemistry, 1990 , vol. 33, # 8 p. 2240 - 2254 Title/Abstract Full Text View citing articles Show Details

Galen, Philip J. M. van; Nissen, Peter; Wijngaarden, Ineke van; IJzerman, Adriaan P.; Soudijn, Willem

Journal of Medicinal Chemistry, 1991 , vol. 34, # 3 p. 1202 - 1206 Title/Abstract Full Text View citing articles Show Details

Glennon, Richard A.; Smith, J. Doyle; Ismaiel, Abd M.; El-Ashmawy, Mahmoud; Battaglia, George; Fisher, James B.

Journal of Medicinal Chemistry, 1991 , vol. 34, # 3 p. 1094 - 1098 Title/Abstract Full Text View citing articles Show Details

Johnson; Frescas; Oberlender; Nichols

Journal of Medicinal Chemistry, 1991 , vol. 34, # 5 p. 1662 - 1668 Title/Abstract Full Text View citing articles Show Details

Brine; Boldt; Huang; Sawyer; Carroll

Journal of Heterocyclic Chemistry, 1989 , vol. 26, # 3 p. 677 - 686 Title/Abstract Full Text View citing articles Show Details

Leshcheva, I. F.; Sergeev, N. M.; Grishina, G. V.; Potapov, V. M.

Chemistry of Heterocyclic Compounds (New York, NY, United States), 1986 , vol. 22, # 11 p. 1214 - 1225 Khimiya Geterotsiklicheskikh Soedinenii, 1986 , vol. 22, # 11 p. 1503 - 1515 Title/Abstract Full Text View citing articles Show Details

Rogalska, Ewa; Belzecki, Czeslaw

Journal of Organic Chemistry, 1984 , vol. 49, p. 1397 - 1402 Title/Abstract Full Text View citing articles Show Details

Thompson, Robert D.; Secunda, Sherrie; Daly, John W.; Olsson, Ray A.

Journal of Medicinal Chemistry, 1991 , vol. 34, # 9 p. 2877 - 2882 Title/Abstract Full Text View citing articles Show Details

Thompson; Secunda; Daly; Olsson

Journal of medicinal chemistry, 1991 , vol. 34, # 12 p. 3388 - 3390 Title/Abstract Full Text View citing articles Show Details

Blagg, Julian; Davies, Stephen G.

Tetrahedron, 1987 , vol. 43, # 19 p. 4463 - 4472 Title/Abstract Full Text View citing articles Show Details

Lightner, David A.; An, Jing-Yi

Tetrahedron, 1987 , vol. 43, # 19 p. 4287 - 4296 Title/Abstract Full Text View citing articles Show Details

Coote, Steven J.; Davies, Stephen G.; Sutton, Kevin H.

Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999), 1988 , p. 1481 - 1488 Title/Abstract Full Text Show Details

6 of 303

Comment (Pharmacological Data)

Bioactivities present

Reference

Landor, Stephen R.; Chan, Yuet M.; Sonola, Olutunji O.; Tatchell, Austin R.

Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999), 1984 , # 3 p. 493 - 496 Title/Abstract Full Text View citing articles Show Details

Buckley, Thomas F.; Rapoport, Henry

Journal of the American Chemical Society, 1981 , vol. 103, # 20 p. 6157 - 6163 Title/Abstract Full Text View citing articles Show Details

Solov'eva, L. D.; Dem'yanovich, V. M.; Potapov, V. M.

Journal of Organic Chemistry USSR (English Translation), 1981 , vol. 17, # 6 p. 1099 - 1105 Zhurnal Organicheskoi Khimii, 1981 , vol. 17, # 6 p. 1241 - 1248 Title/Abstract Full Text Show Details

Grunewald, Gary L.; Monn, James A.; Rafferty, Michael F,; Borchardt, Ronald T.; Krass, Polina

Journal of Medicinal Chemistry, 1982 , vol. 25, # 10 p. 1248 - 1250 Title/Abstract Full Text View citing articles Show Details

Harsche; Oelschlaeger; Engel

Archiv der Pharmazie, 1992 , vol. 325, # 9 p. 593 - 595 Title/Abstract Full Text View citing articles Show Details

Ikota; Achiwa; Yamada

Chemical and Pharmaceutical Bulletin, 1983 , vol. 31, # 3 p. 887 - 894 Title/Abstract Full Text View citing articles Show Details

Lawrence; Elias; Authier-Martin

Canadian Journal of Chemistry, 1984 , vol. 62, # 10 p. 1886 - 1888 Title/Abstract Full Text View citing articles Show Details

Smith, Howard E.; Neergaard, Jon R.; Paulis, Tomas de; Chen, Fu-Ming

Journal of the American Chemical Society, 1983 , vol. 105, # 6 p. 1578 - 1584 Title/Abstract Full Text View citing articles Show Details

Mautner; Lorenc; Quain; Marquis; Tasaki

Journal of Medicinal Chemistry, 1980 , vol. 23, # 3 p. 282 - 285 Title/Abstract Full Text View citing articles Show Details

Glennon; Liebowitz; Anderson III

Journal of Medicinal Chemistry, 1980 , vol. 23, # 3 p. 294 - 299 Title/Abstract Full Text View citing articles Show Details

Hamilton; Bristol

Journal of medicinal chemistry, 1983 , vol. 26, # 11 p. 1601 - 1606 Title/Abstract Full Text View citing articles Show Details

Nordlander, J. Eric; Njoroge, F. George; Payne, Mark J.; Warman, Dhiraj

Journal of Organic Chemistry, 1985 , vol. 50, # 19 p. 3481 - 3484 Title/Abstract Full Text View citing articles Show Details

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Bioactivities present

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Comment (Pharmacological Data)

Bioactivities present

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Bioactivities present

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Park, Hye-Yeon; Ryu, Young-Kyoung; Kim, Yong-Hoon; Park, Tae-Shin; Go, Jun; Hwang, Jung Hwan; Choi, Dong-Hee; Rhee, Myungchull; Lee, Chul-Ho; Kim, Kyoung-Shim

Neurobiology of Disease, 2016 , vol. 89, p. 169 - 179 Title/Abstract Full Text View citing articles Show Details

Ahlner, Johan; Holmgren, Anita; Jones, Alan Wayne

Forensic Science International, 2016 , vol. 265, p. 138 - 143 Title/Abstract Full Text View citing articles Show Details

Penttinen, Anna-Maija; Suleymanova, Ilida; Albert, Katrina; Anttila, Jenni; Voutilainen, Merja H.; Airavaara, Mikko

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Gidaro, Maria Concetta; Astorino, Christian; Petzer, Anél; Carradori, Simone; Alcaro, Francesca; Costa, Giosuè; Artese, Anna; Rafele, Giancarlo; Russo, Francesco M.; Petzer, Jacobus P.; Alcaro, Stefano

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Ahn, James; Ahn, Hyung Seok; Cheong, Jae Hoon; Dela Peña, Ike

Neural Plasticity, 2016 , vol. 2016, art. no. 1320423

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Nichols, David E.

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Klima, Miriam; Altenburger, Markus J.; Kempf, Jürgen; Auwärter, Volker; Neukamm, Merja A.

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McKay, Mary Pat; Groff, Loren

Accident Analysis and Prevention, 2016 , vol. 90, p. 108 - 117 Title/Abstract Full Text View citing articles Show Details

Yang, Chunsong; Hao, Zilong; Zhu, Cairong; Guo, Qin; Mu, Dezhi; Zhang, Lingli

Neuroscience and Biobehavioral Reviews, 2016 , vol. 63, p. 239 - 255 Title/Abstract Full Text View citing articles Show Details

Lavreysen, Hilde; Langlois, Xavier; Donck, Luc Ver; Nuñez, José María Cid; Pype, Stefan; Lütjens, Robert; Megens, Anton

Pharmacology Research and Perspectives, 2015 , vol. 3, # 2 p. 1 - 14 Title/Abstract Full Text Show Details

Johnson-Davis, Kamisha L.; Sadler, Aaron J.; Genzen, Jonathan R.

Journal of Analytical Toxicology, 2016 , vol. 40, # 2 art. no. BKV133, p. 97 - 107 Title/Abstract Full Text View citing articles Show Details

Gul, Waseem; Stamper, Brandon J.; Godfrey, Murrell; ElSohly, Mahmoud A.

Journal of Analytical Toxicology, 2016 , vol. 40, # 2 art. no. BKV124, p. 124 - 132 Title/Abstract Full Text View citing articles Show Details

Schweren; Hartman; Zwiers; Heslenfeld; Franke; Oosterlaan; Buitelaar; Hoekstra

European Neuropsychopharmacology, 2016 , vol. 26, # 4 p. 674 - 683 Title/Abstract Full Text View citing articles Show Details

Martella; Madeo; Maltese; Vanni; Puglisi; Ferraro; Schirinzi; Valente; Bonanni; Shen; Mandolesi; Mercuri; Bonsi; Pisani

Neurobiology of Disease, 2016 , vol. 91, p. 21 - 36 Title/Abstract Full Text View citing articles Show Details

Meyer, Golo M.; Maurer, Hans H.; Meyer, Markus R.

Bioanalysis, 2016 , vol. 8, # 5 p. 457 - 481 Title/Abstract Full Text View citing articles Show Details

Farrell, Martilias S.; McCorvy, John D.; Huang, Xi-Ping; Urban, Daniel J.; White, Kate L.; Giguere, Patrick M.; Doak, Allison K.; Bernstein, Alison I.; Stout, Kristen A.; Park, Su Mi; Rodriguiz, Ramona M.; Gray, Bradley W.; Hyatt, William S.; Norwood, Andrew P.; Webster, Kevin A.; Gannon, Brenda M.; Miller, Gary W.; Porter, Joseph H.; Shoichet, Brian K.; Fantegrossi, William E.; Wetsel, William C.; Roth, Bryan L.

PLoS ONE, 2016 , vol. 11, # 3 art. no. E0150602 Title/Abstract Full Text View citing articles Show Details

Zawilska, Jolanta B.; Andrzejczak, Dariusz

Drug and Alcohol Dependence, 2015 , vol. 157, p. 1 - 17 Title/Abstract Full Text View citing articles Show Details

Nugteren-van Lonkhuyzen, Johanna J.; van Riel, Antoinette J.H.P.; Brunt, Tibor M.; Hondebrink, Laura

Drug and Alcohol Dependence, 2015 , vol. 157, p. 18 - 27 Title/Abstract Full Text View citing articles Show Details

Winkler, David A.; Thornton, Aaron; Farjot, Géraldine; Katz, Ira

Pharmacology and Therapeutics, 2016 , vol. 160, p. 44 - 64 Title/Abstract Full Text View citing articles Show Details

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Journal of Medical Hypotheses and Ideas, 2015 , vol. 9, # 2 p. S24 - S30 Title/Abstract Full Text View citing articles Show Details

Kim, Eunmi; Choe, Sanggil; Lee, Juseon; Jang, Moonhee; Choi, Hyeyoung; Chung, Heesun

Forensic Science International, 2016 , vol. 265, p. 186 - 192 Title/Abstract Full Text View citing articles Show Details

Czoty; Blough; Fennell; Snyder; Nader

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Behavioral and Brain Functions, 2016 , vol. 12, # 1 art. no. 12 Title/Abstract Full Text View citing articles Show Details

Furlong, Teri M.; Leavitt, Lee S.; Keefe, Kristen A.; Son, Jong-Hyun

Neurotoxicity Research, 2016 , vol. 29, # 4 p. 569 - 582 Title/Abstract Full Text View citing articles Show Details

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Journal of Integrative Neuroscience, 2016 , vol. 15, # 1 p. 109 - 122 Title/Abstract Full Text View citing articles Show Details

Kantak, Kathleen M.; Dwoskin, Linda P.

Pharmacology Biochemistry and Behavior, 2016 , vol. 145, p. 24 - 26 Title/Abstract Full Text View citing articles Show Details

McCall, Ann-Kathrin; Bade, Richard; Kinyua, Juliet; Lai, Foon Yin; Thai, Phong K.; Covaci, Adrian; Bijlsma, Lubertus; van Nuijs, Alexander L.N.; Ort, Christoph

Water Research, 2016 , vol. 88, p. 933 - 947 Title/Abstract Full Text View citing articles Show Details

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Clinical Drug Investigation, 2016 , vol. 36, # 5 p. 341 - 356 Title/Abstract Full Text View citing articles Show Details

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Medizinische Monatsschrift fur Pharmazeuten, 2016 , vol. 39, # 4 p. 174 - 174 Title/Abstract Full Text View citing articles Show Details

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Sleep Medicine, 2016 , vol. 17, p. 38 - 44 Title/Abstract Full Text View citing articles Show Details

The Board of Trustees of the University of Arkansas; Owens, Samuel M.; Carroll, Frank Ivy; Abraham, Philip

Patent: US9303092 B2, 2016 ; Title/Abstract Full Text Show Details

Lie, Celia; Macaskill, Anne C.; Harper, David N.

Behavioral Neuroscience, 2016 , vol. 130, # 2 p. 243 - 251 Title/Abstract Full Text View citing articles Show Details

Bespalov, Anton; Müller, Reinhold; Relo, Ana-Lucia; Hudzik, Thomas

Trends in Pharmacological Sciences, 2016 , vol. 37, # 5 p. 364 - 378 Title/Abstract Full Text View citing articles Show Details

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Psychopharmacology, 2016 , vol. 233, # 10 p. 1845 - 1866 Title/Abstract Full Text View citing articles Show Details

Marks, Katherine R.; Lile, Joshua A.; Stoops, William W.; Glaser, Paul E. A.; Hays, Lon R.; Rush, Craig R.

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Emmanouilidou, Evangelia; Minakaki, Georgia; Keramioti, Maria V.; Xylaki, Mary; Balafas, Evangelos; Chrysanthou-Piterou, Margarita; Kloukina, Ismini; Vekrellis, Kostas

Brain, 2016 , vol. 139, # 3 p. 871 - 890 Title/Abstract Full Text View citing articles Show Details

Yazdani, Farzane; Naghshvarian, Mojtaba; Salehi, Alireza; Marzban, Maryam

Iranian Journal of Psychiatry and Behavioral Sciences, 2016 , vol. 10, # 1 art. no. E3483 Title/Abstract Full Text View citing articles Show Details

Huss, Michael; Sikirica, Vanja; Hervas, Amaia; Newcorn, Jeffrey H.; Harpin, Valerie; Robertson, Brigitte

Neuropsychiatric Disease and Treatment, 2016 , vol. 12, p. 1085 - 1101 Title/Abstract Full Text View citing articles Show Details

Czoty, Paul W.; Stoops, William W.; Rush, Craig R.

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Reference

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Nature Reviews Endocrinology, 2016 , vol. 12, # 6 p. 319 - 336 Title/Abstract Full Text View citing articles Show Details

Reed, Stephanie Collins; Evans, Suzette M.

Drug and Alcohol Dependence, 2016 , vol. 163, p. 141 - 152 Title/Abstract Full Text View citing articles Show Details

Lloyd, Kevin; Dayan, Peter

Behavioral and Brain Functions, 2016 , vol. 12, # 1 art. no. 15 Title/Abstract Full Text View citing articles Show Details

Roila, Fausto; Fumi, Guglielmo; Fatigoni, Sonia

Breast Cancer Management, 2016 , vol. 5, # 2 p. 79 - 87 Title/Abstract Full Text Show Details

Booij; Welfeld; Leyton; Dagher; Boileau; Sibon; Baker; Diksic; Soucy; Pruessner; Cawley-Fiset; Casey; Benkelfat

Translational Psychiatry, 2016 , vol. 6, # 2 p. e740 - e740 Title/Abstract Full Text View citing articles Show Details

España, Rodrigo A.; Schmeichel, Brooke E.; Berridge, Craig W.

Brain Research, 2016 , vol. 1641, p. 207 - 216 Title/Abstract Full Text View citing articles Show Details

Winstein, Carolee J.; Stein, Joel; Arena, Ross; Bates, Barbara; Cherney, Leora R.; Cramer, Steven C.; Deruyter, Frank; Eng, Janice J.; Fisher, Beth; Harvey, Richard L.; Lang, Catherine E.; MacKay-Lyons, Marilyn; Ottenbacher, Kenneth J.; Pugh, Sue; Reeves, Mathew J.; Richards, Lorie G.; Stiers, William; Zorowitz, Richard D.

Stroke, 2016 , vol. 47, # 6 p. e98 - e169 Title/Abstract Full Text View citing articles Show Details

Comiran, Eloisa; Kessler, Félix Henrique; Fröehlich, Pedro Eduardo; Limberger, Renata Pereira

European Journal of Pharmaceutical Sciences, 2016 , vol. 89, p. 172 - 179 Title/Abstract Full Text View citing articles Show Details

Asherson, Philip; Buitelaar, Jan; Faraone, Stephen V.; Rohde, Luis A.

The Lancet Psychiatry, 2016 , vol. 3, # 6 p. 568 - 578 Title/Abstract Full Text View citing articles Show Details

Fakhoury, Marc

Journal of Psychiatric Research, 2016 , vol. 80, p. 14 - 21 Title/Abstract Full Text View citing articles Show Details

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Australian Prescriber, 2016 , vol. 39, # 3 p. 96 - 100 Title/Abstract Full Text View citing articles Show Details

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Journal of Pediatrics, 2016 , vol. 173, p. 254 - 257 Title/Abstract Full Text View citing articles Show Details

Geryk, Radim; Kalíková, Květa; Schmid, Martin G.; Tesařová, Eva

Analytica Chimica Acta, 2016 , vol. 932, p. 98 - 105 Title/Abstract Full Text View citing articles Show Details

Skelley, Jessica W.; Carpenter, P. Chase; Morehead, M. Shawn; Murphy, Patrick L.

Southern Medical Journal, 2016 , vol. 109, # 6 p. 331 - 337 Title/Abstract Full Text View citing articles Show Details

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Journal of Addiction Medicine, 2016 , vol. 10, # 3 p. 156 - 165 Title/Abstract Full Text View citing articles Show Details

Spronk, Desirée B.; Verkes, Robbert J.; Cools, Roshan; Franke, Barbara; Van Wel, Janelle H. P.; Ramaekers, Johannes G.; De Bruijn, Ellen R.A.

European Neuropsychopharmacology, 2016 , vol. 26, # 7 p. 1127 - 1139 Title/Abstract Full Text View citing articles Show Details

Moscoso-Castro, Maria; Gracia-Rubio, Irene; Ciruela, Francisco; Valverde, Olga

European Neuropsychopharmacology, 2016 , vol. 26, # 7 p. 1227 - 1240 Title/Abstract Full Text View citing articles Show Details

Collatz, Ansel; Johnston, Samantha C.; Staines, Donald R.; Marshall-Gradisnik, Sonya M.

Clinical Therapeutics, 2016 , vol. 38, # 6 p. 1263 - 9,1271 Title/Abstract Full Text View citing articles Show Details

Beau-Lejdstrom, Raphaelle; Douglas, Ian; Evans, Stephen J.W.; Smeeth, Liam

BMJ Open, 2016 , vol. 6, # 6 art. no. 010508 Title/Abstract Full Text View citing articles Show Details

Green, Rachael

Drugs: Education, Prevention and Policy, 2016 , vol. 23, # 3 p. 202 - 211 Title/Abstract Full Text View citing articles Show Details

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Osteoporosis International, 2016 , vol. 27, # 7 p. 2223 - 2227 Title/Abstract Full Text View citing articles Show Details

Singh, Kanwaljit; Morse, Anne Marie; Tkachenko, Nataliya; Kothare, Sanjeev V.

Pediatric Neurology, 2016 , vol. 60, p. 30 - 36 Title/Abstract Full Text View citing articles Show Details

Heal, David J.; Goddard, Simon; Brammer, Richard J.; Hutson, Peter H.; Vickers, Steven P.

Journal of Psychopharmacology, 2016 , vol. 30, # 7 p. 662 - 675 Title/Abstract Full Text View citing articles Show Details

Saroja, Sivaprakasam R.; Aher, Yogesh D.; Kalaba, Predrag; Aher, Nilima Y.; Zehl, Martin; Korz, Volker; Subramaniyan, Saraswathi; Miklosi, Andras G.; Zanon, Lisa; Neuhaus, Winfried; Höger, Harald; Langer, Thierry; Urban, Ernst; Leban, Johann; Lubec, Gert

Behavioural Brain Research, 2016 , vol. 312, p. 127 - 137 Title/Abstract Full Text View citing articles Show Details

Maincent, Julien; Zhang, Feng

International Journal of Pharmaceutics, 2016 , vol. 510, # 1 p. 57 - 72 Title/Abstract Full Text View citing articles Show Details

Besag, Frank; Gobbi, Giuseppe; Caplan, Rochelle; Sillanpää, Matti; Aldenkamp, Albert; Dunn, David W.

Epileptic Disorders, 2016 , vol. 18, p. S8 - S15 Title/Abstract Full Text View citing articles Show Details

Besag, Frank; Aldenkamp, Albert; Caplan, Rochelle; Dunn, David W.; Gobbi, Giuseppe; Sillanpää, Matti

Epileptic Disorders, 2016 , vol. 18, p. S77 - S86 Title/Abstract Full Text View citing articles Show Details

Molina-Carballo, Antonio; Checa-Ros, Ana; Muñoz-Hoyos, Antonio

Expert Opinion on Therapeutic Patents, 2016 , vol. 26, # 7 p. 799 - 814 Title/Abstract Full Text View citing articles Show Details

Ganos, Christos

Current Opinion in Neurology, 2016 , vol. 29, # 4 p. 513 - 518 Title/Abstract Full Text View citing articles Show Details

Hassamal, Sameer; Haglund, Margaret; Wittnebel, Karl; Danovitch, Itai

Scandinavian Journal of Pain, 2016 , vol. 13, p. 27 - 31 Title/Abstract Full Text View citing articles Show Details

Roy, Dijendra Nath; Goswami, Ritobrata

Chemico-Biological Interactions, 2016 , vol. 255, p. 92 - 105 Title/Abstract Full Text View citing articles Show Details

Hatch-Maillette, Mary; Wells, Elizabeth A.; Doyle, Suzanne R.; Brigham, Gregory S.; Daley, Dennis; DiCenzo, Jessica; Donovan, Dennis; Garrett, Sharon; Horigian, Viviana E.; Jenkins, Lindsay; Killeen, Therese; Owens, Mandy; Perl, Harold I.

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Leu-Semenescu, Smaranda; Louis, Pauline; Arnulf, Isabelle

Sleep Medicine, 2016 , vol. 17, p. 38 - 44 Title/Abstract Full Text Show Details

Aldrin-Kirk, Patrick; Heuer, Andreas; Wang, Gang; Mattsson, Bengt; Lundblad, Martin; Parmar, Malin; Björklund, Tomas

Neuron, 2016 , vol. 90, # 5 p. 955 - 968 Title/Abstract Full Text View citing articles Show Details

Weber; Beck-Schimmer; Kajdi; Müller; Tobler; Quednow

Translational Psychiatry, 2016 , vol. 6, # 7 art. no. E850 Title/Abstract Full Text View citing articles Show Details

Scofield; Heinsbroek; Gipson; Kupchik; Spencer; Smith; Roberts-Wolfe; Kalivas

Pharmacological Reviews, 2016 , vol. 68, # 3 p. 816 - 871 Title/Abstract Full Text View citing articles Show Details

Ennaceur, Abdelkader; Chazot, Paul L.

Pharmacology Research and Perspectives, 2016 , vol. 4, # 2 art. no. E00223 Title/Abstract Full Text Show Details

García-Cabrerizo, Rubén; García-Fuster, M. Julia

NeuroToxicology, 2016 , vol. 56, p. 29 - 39 Title/Abstract Full Text View citing articles Show Details

Ruoff, Chad; Swick , Todd J.; Doekel, Robert; Emsellem, Helene A.; Feldman, Neil T.; Rosenberg, Russell; Bream, Gary; Khayrallah, Moise A.; Lu , Yuan; Black, Jed

Sleep, 2016 , vol. 39, # 7 p. 1379 - 1387 Title/Abstract Full Text View citing articles Show Details

Sobolewski, Marissa; Allen, Joshua L.; Morris-Schaffer, Keith; Klocke, Carolyn; Conrad, Katherine; Cory-Slechta, Deborah A.

Neurotoxicology and Teratology, 2016 , vol. 56, p. 75 - 80 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

Bioactivities present

Reference

Cooper, Stephen J.; Reynolds, Gavin P.; Barnes; England; Haddad; Heald; Holt; Lingford-Hughes; Osborn; McGowan; Patel; Paton; Reid;

Shiers; Smith

Journal of Psychopharmacology, 2016 , vol. 30, # 8 p. 717 - 748 Title/Abstract Full Text View citing articles Show Details

McElroy, Susan L.; Guerdjikova, Anna I.; Mori, Nicole; Keck, Paul E.

Expert Opinion on Pharmacotherapy, 2016 , vol. 17, # 12 p. 1599 - 1610 Title/Abstract Full Text View citing articles Show Details

Atmaca, Murad

Progress in Neuro-Psychopharmacology and Biological Psychiatry, 2016 , vol. 70, p. 127 - 133 Title/Abstract Full Text View citing articles Show Details

Koek, Ralph J.; Schwartz, Holly N.; Scully, Stephenie; Langevin, Jean-Philippe; Spangler, Shana; Korotinsky, Arkady; Jou, Kevin; Leuchter, Andrew

Progress in Neuro-Psychopharmacology and Biological Psychiatry, 2016 , vol. 70, p. 170 - 218 Title/Abstract Full Text View citing articles Show Details

Ryu, Yeonsuk; Barceló, Damià; Barron, Leon P.; Bijlsma, Lubertus; Castiglioni, Sara; de Voogt, Pim; Emke, Erik; Hernández, Félix; Lai, Foon Yin; Lopes, Alvaro; de Alda, Miren López; Mastroianni, Nicola; Munro, Kelly; O'Brien, Jake; Ort, Christoph; Plósz, Benedek G.; Reid, Malcolm J.; Yargeau, Viviane; Thomas, Kevin V.

Science of the Total Environment, 2016 , vol. 565, p. 977 - 983 Title/Abstract Full Text View citing articles Show Details

Bolin, B. Levi; Alcorn, Joseph L.; Reynolds, Anna R.; Lile, Joshua A.; Rush, Craig R.

Experimental and Clinical Psychopharmacology, 2016 , vol. 24, # 4 p. 214 - 228 Title/Abstract Full Text View citing articles Show Details

McCarter, Stuart J.; St. Louis, Erik K.; Boeve, Bradley F.

Current Neurology and Neuroscience Reports, 2016 , vol. 16, # 9 art. no. 85 Title/Abstract Full Text View citing articles Show Details

Page, Robert L.; O'bryant, Cindy L.; Cheng, Davy; Dow, Tristan J.; Ky, Bonnie; Stein, C. Michael; Spencer, Anne P.; Trupp, Robin J.; Lindenfeld, JoAnn

Circulation, 2016 , vol. 134, # 6 p. e32 - e69 Title/Abstract Full Text View citing articles Show Details

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THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS; KOZIKOWSKI, Alan; CHENG, Jianjun

Patent: WO2016/123164 A1, 2016 ; Title/Abstract Full Text Show Details

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van Lieshout, Marloes; Luman, Marjolein; Twisk, Jos W. R.; van Ewijk, Hanneke; Groenman, Annabeth P.; Thissen, Andrieke J. A. M.; Faraone, Stephen V.; Heslenfeld, Dirk J.; Hartman, Catharina A.; Hoekstra, Pieter J.; Franke, Barbara; Buitelaar, Jan K.; Rommelse, Nanda N. J.; Oosterlaan, Jaap

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Íbias, Javier; Miguéns, Miguel; Pellón, Ricardo

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Barateau, Lucie; Lopez, Régis; Dauvilliers, Yves

Current Treatment Options in Neurology, 2016 , vol. 18, # 10 art. no. 43 Title/Abstract Full Text Show Details

Ogrim, Geir; Aasen, Ida Emilia; Brunner, Jan Ferenc

Clinical Neurophysiology, 2016 , vol. 127, # 10 p. 3277 - 3287 Title/Abstract Full Text Show Details

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CNS and Neurological Disorders - Drug Targets, 2016 , vol. 15, # 7 p. 777 - 801 Title/Abstract Full Text Show Details

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Reference

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Martínez-Montero, Lía; Gotor, Vicente; Gotor-Fernández, Vicente; Lavandera, Iván

Advanced Synthesis and Catalysis, 2016 , vol. 358, # 10 p. 1618 - 1624 Title/Abstract Full Text Show Details

Fischer, Bo; Herberholz, Nicola

Paediatrics and Child Health (United Kingdom), 2016 , vol. 26, # 10 p. 464 - 467 Title/Abstract Full Text Show Details

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Physician Assistant Clinics, 2016 , vol. 1, # 4 p. 683 - 699 Title/Abstract Full Text Show Details

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Medicine (United Kingdom), 2016 , vol. 44, # 11 p. 683 - 686 Title/Abstract Full Text Show Details

Sanchez; Valverde; Sinclair; Mosley; Singh; Mutsaers; Hanna; Gu; Johnson

Journal of Veterinary Pharmacology and Therapeutics, 2016 , vol. 39, # 5 p. 452 - 459 Title/Abstract Full Text Show Details

van der Schans, Jurjen; Pleiter, Janine C.; de Vries, Tjalling W.; Schuiling-Veninga, Catharina C.M.; Bos, Jens H.J.; Hoekstra, Pieter J.; Hak, Eelko

Annals of Allergy, Asthma and Immunology, 2016 , vol. 117, # 2 p. 186 - 191 Title/Abstract Full Text Show Details

Bui, Quan M.; Allen, Larry A.; Monte, Andrew A.; Page, Robert L.; McIlvennan, Colleen K.

Journal of Heart and Lung Transplantation, 2016 , vol. 35, # 8 p. 1045 - 1048 Title/Abstract Full Text Show Details

Swedberg, Michael D.B.

Journal of Pharmacological and Toxicological Methods, 2016 , vol. 81, p. 295 - 305 Title/Abstract Full Text Show Details

26 of 303

Comment (Pharmacological Data)

Bioactivities present

Reference

Hale, Lillian V. A.; Szymczak, Nathaniel K.

Journal of the American Chemical Society, 2016 , vol. 138, # 41 p. 13489 - 13492 Title/Abstract Full Text Show Details

SK Biopharmaceuticals Co., Ltd.; Khayrallah, Moise A.; Bream, Gary; Butts, Stephen E.; Melnick, Susan Marie; Taylor, Duncan

Patent: US9464041 B2, 2016 ; Title/Abstract Full Text Show Details

Ramakrishnan, Sridhar; Wesensten, Nancy J.; Kamimori, Gary H.; Moon, James E.; Balkin, Thomas J.; Reifman, Jaques

Sleep, 2016 , vol. 39, # 10 p. 1827 - 1841 Title/Abstract Full Text Show Details

Zhang, Ji-Chun; Yao, Wei; Hashimoto, Kenji

Current Neuropharmacology, 2016 , vol. 14, # 7 p. 721 - 731 Title/Abstract Full Text Show Details

Zhu, Qingfu; Scriba, Gerhard K. E.

Chromatographia, 2016 , vol. 79, # 21-22 p. 1403 - 1435 Title/Abstract Full Text Show Details

Biezonski; Shah; Krivko; Cha; Guilfoyle; Hrabe; Gerum; Xie; Duan; Bansal; Leventhal; Peterson; Kellendonk; Posner

Translational Psychiatry, 2016 , vol. 6, # 9 art. no. E884 Title/Abstract Full Text Show Details

Asherson, Philip; Manor, Iris; Huss, Michael

Neuropsychiatry, 2014 , vol. 4, # 1 p. 109 - 128 Title/Abstract Full Text Show Details

Ahn, Sungwoo; Rubchinsky, Leonid L.; Lapish, Christopher C.

Cerebral cortex (New York, N.Y. : 1991), 2014 , vol. 24, # 10 p. 2553 - 2561 Title/Abstract Full Text Show Details

Arbo, Marcelo Dutra; Melega, Simone; Stöber, Regina; Schug, Markus; Rempel, Eugen; Rahnenführer, Jörg; Godoy, Patricio; Reif, Raymond; Cadenas, Cristina; de Lourdes Bastos, Maria; Carmo, Helena; Hengstler, Jan G.

Archives of Toxicology, 2016 , vol. 90, # 12 p. 3045 - 3060 Title/Abstract Full Text Show Details

Jordan, Chloe J.; Lemay, Carley; Dwoskin, Linda P.; Kantak, Kathleen M.

Psychopharmacology, 2016 , vol. 233, # 23-24 p. 3891 - 3903 Title/Abstract Full Text Show Details

Kölch; Plener

Pharmacopsychiatry, 2016 , vol. 49, # 6 p. 219 - 225 Title/Abstract Full Text Show Details

Olsen, Rebecca A.; Macaskill, Anne C.; Harper, David N.

Pharmacology Biochemistry and Behavior, 2016 , vol. 150-151, p. 170 - 181 Title/Abstract Full Text Show Details

Sever, Melike; Turkyilmaz, Mesut; Sevinc, Cansu; Cakir, Aysen; Ocalan, Busra; Cansev, Mehmet; Guler, Mustafa O.; Tekinay, Ayse B.

Acta Biomaterialia, 2016 , vol. 46, p. 79 - 90 Title/Abstract Full Text Show Details

Jenkins, Peter O.; Mehta, Mitul A.; Sharp, David J.

Brain, 2016 , vol. 139, # 9 p. 2345 - 2371 Title/Abstract Full Text Show Details

Tyagi, Mudit; Bukrinsky, Michael; Simon, Gary L.

Current HIV Research, 2016 , vol. 14, # 5 p. 442 - 454 Title/Abstract Full Text Show Details

Notzon, Daniel P.; Mariani, John J.; Pavlicova, Martina; Glass, Andrew; Mahony, Amy L.; Brooks, Daniel J.; Grabowski, John; Levin, Frances R.

American Journal on Addictions, 2016 , vol. 25, # 8 p. 666 - 672 Title/Abstract Full Text Show Details

Michelis, Joan Philipp; Zimmermann, Julian; Bedarf, Janis Rebecca; Bundschuh, Ralph; Gaertner, Florian C.; Paus

Parkinsonism and Related Disorders, 2016 , vol. 31, p. 153 - 155 Title/Abstract Full Text Show Details

Clark, Glenn T.; Ram, Saravanan

Oral and Maxillofacial Surgery Clinics of North America, 2016 , vol. 28, # 3 p. 397 - 407 Title/Abstract Full Text Show Details

Erland, Lauren A E; Turi, Christina E; Saxena, Praveen K.

Biotechnology Advances, 2016 , vol. 34, # 8 p. 1347 - 1361 Title/Abstract Full Text Show Details

Liepert, Joachim

Current Opinion in Neurology, 2016 , vol. 29, # 6 p. 700 - 705 Title/Abstract Full Text Show Details

27 of 303

Comment (Pharmacological Data)

Bioactivities present

Reference

Kooij, J. J. Sandra; Michielsen, Marieke; Kruithof, Henk; Bijlenga, Denise

Expert Review of Neurotherapeutics, 2016 , vol. 16, # 12 p. 1371 - 1381 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

Ermer, James; Corcoran, Mary; Lasseter, Kenneth; Martin, Patrick T.

Therapeutic Drug Monitoring, 2016 , vol. 38, # 6 p. 769 - 776 Title/Abstract Full Text Show Details

Maddry, Joseph K.; Ng, Patrick C.; Sessions, Daniel; Bebarta, Vikhyat S.

Military Medicine, 2016 , vol. 181, # 11 p. e1666 - e1668 Title/Abstract Full Text Show Details

Erhardt, Sophie; Schwieler, Lilly; Imbeault, Sophie; Engberg, Göran

Neuropharmacology, 2017 , vol. 112, p. 297 - 306 Title/Abstract Full Text Show Details

Osunsanmi, Sunkanmi; Turk, Jeremy

Journal of Child and Adolescent Psychopharmacology, 2016 , vol. 26, # 9 p. 828 - 834 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

Wendler, Etieli; de Souza, Camila Pasquini; Vecchia, Debora Dalla; Kanazawa, Luiz Kae Sales; de Almeida Soares Hocayen, Palloma; Wöhr, Markus; Schwarting, Rainer K.W.; Andreatini, Roberto

European Neuropsychopharmacology, 2016 , vol. 26, # 12 p. 1900 - 1908 Title/Abstract Full Text Show Details

Blum, Kenneth; Febo, Marcelo; Badgaiyan, Rajendra D.; Braverman, Eric R.; Dushaj, Kristina; Li, Mona; Demetrovics, Zsolt

Scientific Reports, 2016 , vol. 22, # 999 p. 1 - 18 Title/Abstract Full Text Show Details

Chłoń-Rzepa, Grażyna; Zagórska, Agnieszka; Żmudzki, Paweł; Bucki, Adam; Kołaczkowski, Marcin; Partyka, Anna; Wesołowska, Anna; Kazek, Grzegorz; Głuch-Lutwin, Monika; Siwek, Agata; Starowicz, Gabriela; Pawłowski, Maciej

Archiv der Pharmazie, 2016 , vol. 349, # 12 p. 889 - 903 Title/Abstract Full Text Show Details

Higashida, Haruhiro; Yokoyama, Shigeru; Tsuji, Chiharu; Muramatsu, Shin-ichi

Journal of Physiological Sciences, 2017 , vol. 67, # 1 p. 11 - 17 Title/Abstract Full Text Show Details

Blecher, Gregory; Wainbergas, Natalie; McGlynn, Michael; Teng, Arthur

Respirology Case Reports, 2014 , vol. 2, # 3 p. 111 - 112 Title/Abstract Full Text Show Details

De Rosa, Nicholas; Glanville, Allan

Respirology Case Reports, 2015 , vol. 3, # 4 p. 138 - 140

Title/Abstract Full Text Show Details

Bozkurt, Biykem; Colvin, Monica; Cook, Jennifer; Cooper, Leslie T.; Deswal, Anita; Fonarow, Gregg C.; Francis, Gary S.; Lenihan, Daniel; Lewis, Eldrin F.; McNamara, Dennis M.; Pahl, Elfriede; Vasan, Ramachandran S.; Ramasubbu, Kumudha; Rasmusson, Kismet; Towbin, Jeffrey A.; Yancy, Clyde

Circulation, 2016 , vol. 134, # 23 p. e579 - e646 Title/Abstract Full Text Show Details

Blake, Timothy K.

Nursing, 2016 , vol. 46, # 12 p. 60 - 64 Title/Abstract Full Text Show Details

Harvanko, Arit; Martin, Catherine; Lile, Joshua; Kryscio, Richard; Kelly, Thomas H.

Experimental and Clinical Psychopharmacology, 2016 , vol. 24, # 6 p. 436 - 446 Title/Abstract Full Text Show Details

Luks, Andrew M.; Grissom, Colin; Freer, Luanne; Hackett, Peter

High Altitude Medicine and Biology, 2016 , vol. 17, # 4 p. 315 - 322 Title/Abstract Full Text Show Details

Levy, Florence

Therapeutic Advances in Psychopharmacology, 2016 , vol. 6, # 6 p. 382 - 383 Title/Abstract Full Text Show Details

Stępnik, Katarzyna E.

Biomedical Chromatography, 2017 , vol. 31, # 1 art. no. E3741 Title/Abstract Full Text Show Details

Kordower, Jeffrey H.; Vinuela, Angel; Chu, Yaping; Isacson, Ole; Redmond, D. Eugene

Journal of Comparative Neurology, 2017 , vol. 525, # 3 p. 498 - 512 Title/Abstract Full Text Show Details

28 of 303

Comment (Pharmacological Data)

Bioactivities present

Reference

Carlos, Graciela; Comiran, Eloisa; de Oliveira, Marcella Herbstrith; Limberger, Renata Pereira; Bergold, Ana Maria; Fröehlich, Pedro Eduardo

Arabian Journal of Chemistry, 2016 , vol. 9, p. S1905 - S1914 Title/Abstract Full Text Show Details

Fogel, Jessica S.; Kelly, Thomas H.; Westgate, Philip M.; Lile, Joshua A.

Pharmacology Biochemistry and Behavior, 2017 , vol. 152, p. 44 - 51 Title/Abstract Full Text Show Details

Bade, Richard; Bijlsma, Lubertus; Sancho, Juan V.; Gracia-Lor, Emma; Hernández, Félix; Baz-Lomba, Jose A.; Ryu, Yeonsuk; Thomas, Kevin V.; Castiglioni, Sara; Rousis, Nikolaos I.; Zuccato, Ettore; Castrignanò, Erika; Kasprzyk-Hordern, Barbara; Causanilles, Ana; de Voogt, Pim; Kinyua, Juliet; van Nuijs, Alexander L.N.; McCall, Ann-Kathrin; Ort, Christoph; Plósz, Benedek G.; Ramin, Pedram

Chemosphere, 2017 , vol. 168, p. 1032 - 1041 Title/Abstract Full Text Show Details

Camkurt, Mehmet Akif; Gunes, Serkan; Tecimer, Ergün

Journal of Child and Adolescent Psychopharmacology, 2016 , vol. 26, # 10 p. 953 - 954 Title/Abstract Full Text Show Details

McGrane, Ian R.; Loveland, Joshua G.; Zaluski, Heather J.

Journal of Child and Adolescent Psychopharmacology, 2016 , vol. 26, # 10 p. 935 - 938 Title/Abstract Full Text Show Details

Westover, Arthur N.; Nakonezny, Paul A.; Adinoff, Bryon; Brown, Edson Sherwood; Halm, Ethan A.

Journal of Child and Adolescent Psychopharmacology, 2016 , vol. 26, # 10 p. 889 - 899 Title/Abstract Full Text Show Details

Zhang, Yan; Zhang, Tingting; Guo, Changsheng; Lv, Jiapei; Hua, Zhendong; Hou, Song; Zhang, Yuan; Meng, Wei; Xu, Jian

Science of the Total Environment, 2017 , vol. 579, p. 305 - 313 Title/Abstract Full Text Show Details

Petrenko, Christie L.M.; Alto, Michelle E.

European Journal of Medical Genetics, 2017 , vol. 60, # 1 p. 79 - 91 Title/Abstract Full Text Show Details

Bogale, Tegegne; Engidawork, Epherm; Yisma, Engida

BMC Complementary and Alternative Medicine, 2016 , vol. 16, # 1 art. no. 153 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

Moeller, Kim; Sandberg, Sveinung

Justice Quarterly, 2017 , vol. 34, # 2 p. 272 - 296 Title/Abstract Full Text Show Details

Cortese, Samuele; Adamo, Nicoletta; Mohr-Jensen, Christina; Hayes, Adrian J.; Bhatti, Sahar; Carucci, Sara; Del Giovane, Cinzia; Atkinson, Lauren Z.; Banaschewski, Tobias; Simonoff, Emily; Zuddas, Alessandro; Barbui, Corrado; Purgato, Marianna; Steinhausen, Hans-Christoph; Shokraneh, Farhad; Xia, Jun; Cipriani, Andrea; Coghill, David

BMJ Open, 2017 , vol. 7, # 1 art. no. E013967 Title/Abstract Full Text Show Details

Banks, Matthew L.; Negus, S. Stevens

Trends in Pharmacological Sciences, 2017 , vol. 38, # 2 p. 181 - 194 Title/Abstract Full Text Show Details

Alvanzo, Anika A. H.; Wand, Gary S.; Kuwabara, Hiroto; Wong, Dean F.; Xu, Xiaoqiang; McCaul, Mary E.

Addiction Biology, 2017 , vol. 22, # 1 p. 218 - 228 Title/Abstract Full Text Show Details

Rodríguez-Arias, Marta; Montagud-Romero, Sandra; Rubio-Araiz, Ana; Aguilar, María A.; Martín-García, Elena; Cabrera, Roberto; Maldonado, Rafael; Porcu, Francesca; Colado, María Isabel; Miñarro, José

Addiction Biology, 2017 , vol. 22, # 1 p. 129 - 141 Title/Abstract Full Text Show Details

Maroteaux, Luc; Ayme-Dietrich, Estelle; Aubertin-Kirch, Gaëlle; Banas, Sophie; Quentin, Emily; Lawson, Roland; Monassier, Laurent

Pharmacology and Therapeutics, 2017 , vol. 170, p. 14 - 36 Title/Abstract Full Text Show Details

Guarnieri, Regina V.; Buratto, Luciano G.; Gomes, Carlos F.A.; Ribeiro, Rafaela L.; de Souza, Altay A. Lino; Stein, Lilian M.; Galduróz, José C.; Bueno, Orlando F.A.

Human Psychopharmacology, 2017 , vol. 32, # 1 art. no. E2563

Title/Abstract Full Text Show Details

Grecu, Iulia; Ionica, Mihai; Vladescu, Marian; Truta, Elena; Sultan, Carmen; Viscol, Oana; Horhota, Luminita; Radu, Simona

Proceedings of SPIE - The International Society for Optical Engineering, 2016 , vol. 10010, art. no. 100103H Title/Abstract Full Text Show Details

Eshleman, Amy J.; Wolfrum, Katherine M.; Reed, John F.; Kim, Sunyoung O.; Swanson, Tracy; Johnson, Robert A.; Janowsky, Aaron

Journal of Pharmacology and Experimental Therapeutics, 2017 , vol. 360, # 1 p. 33 - 47 Title/Abstract Full Text Show Details

McDonnell-Dowling, Kate; Kelly, John P.

Current Neuropharmacology, 2017 , vol. 15, # 2 p. 300 - 314 Title/Abstract Full Text Show Details

29 of 303

Comment (Pharmacological Data)

Bioactivities present

Reference

Ryu, Young-Kyoung; Kang, Young; Go, Jun; Park, Hye-Yeon; Noh, Jung-Ran; Kim, Yong-Hoon; Hwang, Jung Hwan; Choi, Dong-Hee; Han, Sang-Seop; Oh, Won-Keun; Lee, Chul-Ho; Kim, Kyoung-Shim

Journal of Medicinal Food, 2017 , vol. 20, # 2 p. 116 - 123 Title/Abstract Full Text Show Details

Archer, Edward; Petrie, Bruce; Kasprzyk-Hordern, Barbara; Wolfaardt, Gideon M.

Chemosphere, 2017 , vol. 174, p. 437 - 446 Title/Abstract Full Text Show Details

Ding, Catherine; Palmer, Colin J.; Hohwy, Jakob; Youssef, George J.; Paton, Bryan; Tsuchiya, Naotsugu; Stout, Julie C.; Thyagarajan, Dominic

Neuropsychologia, 2017 , vol. 97, p. 38 - 45 Title/Abstract Full Text Show Details

Carradori, Dario; Eyer, Joel; Saulnier, Patrick; Préat, Véronique; des Rieux, Anne

Biomaterials, 2017 , vol. 123, p. 77 - 91 Title/Abstract Full Text Show Details

Cappelle, Delphine; De Doncker, Mireille; Gys, Celine; Krysiak, Kamelia; De Keukeleire, Steven; Maho, Walid; Crunelle, Cleo L.; Dom, Geert; Covaci, Adrian; van Nuijs, Alexander L.N.; Neels, Hugo

Analytica Chimica Acta, 2017 , vol. 960, p. 101 - 109 Title/Abstract Full Text Show Details

Hao, Fei; Yang, Chun; Chen, Sha-Sha; Wang, Yan-Yan; Zhou, Wei; Hao, Qiang; Lu, Tao; Hoffer, Barry; Zhao, Li-Ru; Duan, Wei-Ming; Xu, Qun-Yuan

Experimental Neurology, 2017 , vol. 291, p. 120 - 133 Title/Abstract Full Text Show Details

Jhanda, Soumya; Singla, Neha; Grover, Sandeep

Journal of Pediatric Neurosciences, 2016 , vol. 11, # 4 p. 316 - 318 Title/Abstract Full Text Show Details

Moreno-Paublete, Rocio; Canlon, Barbara; Cederroth, Christopher R.

Frontiers in Cellular Neuroscience, 2017 , vol. 11, art. no. 19 Title/Abstract Full Text Show Details

Punia, Bhupinder Singh; Yadav, Praveen Kumar; Bumbrah, Gurvinder Singh; Sharma, Rakesh Mohan

Journal of AOAC International, 2017 , vol. 100, # 1 p. 109 - 125 Title/Abstract Full Text Show Details

CONCERT PHARMACEUTICALS, INC.; TUNG, Roger D.; GRAHAM, Philip B.

Patent: WO2017/20016 A1, 2017 ; Title/Abstract Full Text Show Details

30 of 303

31 of 303

32 of 303

33 of 303

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Moreno-Paublete, Rocio; Canlon, Barbara; Cederroth, Christopher R.

Frontiers in Cellular Neuroscience, 2017 , vol. 11, art. no. 19 Title/Abstract Full Text Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Lotfizadeh, Amin D.; Zimmermann, Zachary J.; Watkins, Erin E.; Edwards, Timothy L.; Poling, Alan

Pharmacology Biochemistry and Behavior, 2014 , vol. 125, p. 65 - 69 Title/Abstract Full Text View citing articles Show Details

Harvey, Eric L.; Baker, Lisa E.

Psychopharmacology, 2016 , vol. 233, # 4 p. 673 - 680 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Banks, Matthew L.; Smith, Douglas A.; Kisor, David F.; Poklis, Justin L.

Pharmacology Biochemistry and Behavior, 2016 , vol. 141, p. 58 - 65 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

The Board of Trustees of the University of Arkansas; Owens, Samuel M.; Carroll, Frank Ivy; Abraham, Philip

Patent: US9303092 B2, 2016 ;

Title/Abstract Full Text Show Details

34 of 303

35 of 303

36 of 303

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Decker, Ann M.; Partilla, John S.; Baumann, Michael H.; Rothman, Richard B.; Blough, Bruce E.

MedChemComm, 2016 , vol. 7, # 8 p. 1657 - 1663 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Saroja, Sivaprakasam R.; Aher, Yogesh D.; Kalaba, Predrag; Aher, Nilima Y.; Zehl, Martin; Korz, Volker; Subramaniyan, Saraswathi; Miklosi, Andras G.; Zanon, Lisa; Neuhaus, Winfried; Höger, Harald; Langer, Thierry; Urban, Ernst; Leban, Johann; Lubec, Gert

Behavioural Brain Research, 2016 , vol. 312, p. 127 - 137 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS; KOZIKOWSKI, Alan; CHENG, Jianjun

Patent: WO2016/123164 A1, 2016 ; Title/Abstract Full Text Show Details

37 of 303

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

SK Biopharmaceuticals Co., Ltd.; Khayrallah, Moise A.; Bream, Gary; Butts, Stephen E.; Melnick, Susan Marie; Taylor, Duncan

Patent: US9464041 B2, 2016 ; Title/Abstract Full Text Show Details

38 of 303

39 of 303

40 of 303

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Chłoń-Rzepa, Grażyna; Zagórska, Agnieszka; Żmudzki, Paweł; Bucki, Adam; Kołaczkowski, Marcin; Partyka, Anna; Wesołowska, Anna; Kazek, Grzegorz; Głuch-Lutwin, Monika; Siwek, Agata; Starowicz, Gabriela; Pawłowski, Maciej

Archiv der Pharmazie, 2016 , vol. 349, # 12 p. 889 - 903 Title/Abstract Full Text Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Wang, Kevin H.; Penmatsa, Aravind; Gouaux, Eric

Nature, 2015 , vol. 521, # 7552 p. 322 - 327 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Randox Laboratories Ltd.; Benchik, Elouard; Fitzgerald, Peter; Lowry, Philip; McConnell, Ivan

Patent: EP2950104 A1, 2015 ; Title/Abstract Full Text Show Details

41 of 303

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

SHIRE AG; WHOMSLEY, Rhys; ALLAN, Christine Elizabeth; LUKER, Timothy Jon

Patent: WO2014/2039 A1, 2014 ; Title/Abstract Full Text Show Details

42 of 303

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Sandtner, Walter; Schmid, Diethart; Schicker, Klaus; Gerstbrein, Klaus; Koenig, Xaver; Mayer, Felix P.; Boehm, Stefan; Freissmuth, Michael; Sitte, Harald H.

British Journal of Pharmacology, 2014 , vol. 171, # 4 p. 1007 - 1018 Title/Abstract Full Text View citing articles Show Details

43 of 303

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Mickle, Travis

Patent: US2014/171510 A1, 2014 ; Title/Abstract Full Text Show Details

44 of 303

45 of 303

46 of 303

47 of 303

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Ash, Elizabeth S.; Heal, David J.; Clare Stanford

Neuropharmacology, 2014 , vol. 87, p. 180 - 187 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Atack, John R.; Shook, Brian C.; Rassnick, Stefanie; Jackson, Paul F.; Rhodes, Kenneth; Drinkenburg, Wilhelmus H.; Ahnaou, Abdallah; Te Riele, Paula; Langlois, Xavier; Hrupka, Brian; De Haes, Patrick; Hendrickx, Herman; Aerts, Nancy; Hens, Koen; Wellens, Annemie; Vermeire, Jef; Megens, Anton A. H. P.

ACS Chemical Neuroscience, 2014 , vol. 5, # 10 p. 1005 - 1019 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Earla, Ravinder; Kumar, Santosh; Wang, Lei; Bosinger, Steven; Li, Junhao; Shah, Ankit; Gangwani, Mohitkumar; Nookala, Anantha; Liu, Xun; Cao, Lu; Jackson, Austin; Silverstein, Peter S.; Fox, Howard S.; Li, Weihua; Kumar, Anil

Drug Metabolism and Disposition, 2014 , vol. 42, # 12 p. 2097 - 2108 Title/Abstract Full Text Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

peroral

Concentration (Pharmacological Data)

1.5 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. administered as l-homoarginine d-amphetamine dihydrochloride prodrug

Method (Pharmacological Data)

name of method/assay: ELISA

Further Details (Pharmacological Data)

peak plasma concentration (Cmax); Cmax related to: plasma

Type (Pharmacological Data)

Cmax

Value of Type (Pharmacological Data)

44 ng/ml

Location

Paragraph 129-135

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

48 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or Test-

Sprague-Dawley rat

System (Pharmacological Data) Sex

male

Route of Application

peroral

Concentration (Pharmacological Data)

1.5 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. administered as l-homoarginine d-amphetamine dihydrochloride prodrug

Method (Pharmacological Data)

name of method/assay: ELISA

Further Details (Pharmacological Data)

time to Cmax (tmax); tmax related to: plasma

Type (Pharmacological Data)

tmax

Value of Type (Pharmacological Data)

2 - 4 h

Location

Paragraph 129-135

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

49 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

peroral

Concentration (Pharmacological Data)

1.5 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. administered as l-lysine-d-amphetamine prodrug (Vyvanse™)

Method (Pharmacological Data)

name of method/assay: ELISA

Further Details (Pharmacological Data)

peak plasma concentration (Cmax); Cmax related to: plasma

Type (Pharmacological Data)

Cmax

Value of Type (Pharmacological Data)

44 ng/ml

Location

Paragraph 129-135

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

50 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or Test-

Sprague-Dawley rat

System (Pharmacological Data) Sex

male

Route of Application

peroral

Concentration (Pharmacological Data)

1.5 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. administered as l-lysine-d-amphetamine prodrug (Vyvanse™)

Method (Pharmacological Data)

name of method/assay: ELISA

Further Details (Pharmacological Data)

time to Cmax (tmax); tmax related to: plasma

Type (Pharmacological Data)

tmax

Value of Type (Pharmacological Data)

1 - 3 h

Location

Paragraph 129-135

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

51 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

nasal

Concentration (Pharmacological Data)

1.5 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. administered as l-homoarginine d-amphetamine dihydrochloride prodrug

Method (Pharmacological Data)

name of method/assay: ELISA

Further Details (Pharmacological Data)

peak plasma concentration (Cmax); Cmax related to: plasma

Type (Pharmacological Data)

Cmax

Value of Type (Pharmacological Data)

71 ng/ml

Location

Paragraph 136

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

52 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or Test-

Sprague-Dawley rat

System (Pharmacological Data) Sex

male

Route of Application

nasal

Concentration (Pharmacological Data)

1.5 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. administered as l-homoarginine d-amphetamine dihydrochloride prodrug

Method (Pharmacological Data)

name of method/assay: ELISA

Further Details (Pharmacological Data)

time to Cmax (tmax); tmax related to: plasma

Type (Pharmacological Data)

tmax

Value of Type (Pharmacological Data)

0.5 h

Location

Paragraph 136

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

53 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

nasal

Concentration (Pharmacological Data)

1.5 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. administered as l-lysine-d-amphetamine prodrug (Vyvanse™)

Method (Pharmacological Data)

name of method/assay: ELISA

Further Details (Pharmacological Data)

peak plasma concentration (Cmax); Cmax related to: plasma

Type (Pharmacological Data)

Cmax

Value of Type (Pharmacological Data)

79 ng/ml

Location

Paragraph 136

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

54 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or Test-

Sprague-Dawley rat

System (Pharmacological Data) Sex

male

Route of Application

nasal

Concentration (Pharmacological Data)

1.5 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. administered as l-lysine-d-amphetamine prodrug (Vyvanse™)

Method (Pharmacological Data)

name of method/assay: ELISA

Further Details (Pharmacological Data)

time to Cmax (tmax); tmax related to: plasma

Type (Pharmacological Data)

tmax

Value of Type (Pharmacological Data)

3 h

Location

Paragraph 136

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

55 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

nasal

Concentration (Pharmacological Data)

1.5 mg/kg

Method (Pharmacological Data)

name of method/assay: ELISA

Further Details (Pharmacological Data)

peak plasma concentration (Cmax); Cmax related to: plasma

Type (Pharmacological Data)

Cmax

Value of Type (Pharmacological Data)

779 ng/ml

Location

Paragraph 136

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

56 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

male

Sex Route of Application

nasal

Concentration (Pharmacological Data)

1.5 mg/kg

Method (Pharmacological Data)

name of method/assay: ELISA

Further Details (Pharmacological Data)

time to Cmax (tmax); tmax related to: plasma

Type (Pharmacological Data)

tmax

Value of Type (Pharmacological Data)

5 min

Location

Paragraph 136

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

57 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intravenous

Concentration (Pharmacological Data)

1.5 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. administered as l-homoarginine d-amphetamine dihydrochloride prodrug

Method (Pharmacological Data)

name of method/assay: ELISA

Further Details (Pharmacological Data)

peak plasma concentration (Cmax); Cmax related to: plasma

Type (Pharmacological Data)

Cmax

Value of Type (Pharmacological Data)

68 ng/ml

Location

Paragraph 137

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

58 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intravenous

Concentration

1.5 mg/kg

(Pharmacological Data) Kind of Dosing (Pharmacological Data)

title comp. administered as l-homoarginine d-amphetamine dihydrochloride prodrug

Method (Pharmacological Data)

name of method/assay: ELISA

Further Details (Pharmacological Data)

time to Cmax (tmax); tmax related to: plasma

Type (Pharmacological Data)

tmax

Value of Type (Pharmacological Data)

5 min

Location

Paragraph 137

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

59 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intravenous

Concentration (Pharmacological Data)

1.5 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. administered as l-lysine-d-amphetamine prodrug (Vyvanse™)

Method (Pharmacological Data)

name of method/assay: ELISA

Further Details (Pharmacological Data)

peak plasma concentration (Cmax); Cmax related to: plasma

Type (Pharmacological Data)

Cmax

Value of Type (Pharmacological Data)

79 ng/ml

Location

Paragraph 137

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

60 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intravenous

Concentration

1.5 mg/kg

(Pharmacological Data) Kind of Dosing (Pharmacological Data)

title comp. administered as l-lysine-d-amphetamine prodrug (Vyvanse™)

Method (Pharmacological Data)

name of method/assay: ELISA

Further Details (Pharmacological Data)

time to Cmax (tmax); tmax related to: plasma

Type (Pharmacological Data)

tmax

Value of Type (Pharmacological Data)

15 min

Location

Paragraph 137

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

61 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intravenous

Concentration (Pharmacological Data)

1.5 mg/kg

Method (Pharmacological Data)

name of method/assay: ELISA

Further Details (Pharmacological Data)

peak plasma concentration (Cmax); Cmax related to: plasma

Type (Pharmacological Data)

Cmax

Value of Type (Pharmacological Data)

554 ng/ml

Location

Paragraph 137

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

62 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intravenous

Concentration (Pharmacological Data)

1.5 mg/kg

Method

name of method/assay: ELISA

(Pharmacological Data) Further Details (Pharmacological Data)

time to Cmax (tmax); tmax related to: plasma

Type (Pharmacological Data)

tmax

Value of Type (Pharmacological Data)

5 min

Location

Paragraph 137

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

63 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

rat

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

title comp. administered as l-homoarginine d-amphetamine dihydrochloride prodrug solution at a dose of 4.20 mg/kg

Further Details (Pharmacological Data)

area under the curve (AUC); AUC related to: plasma

Type (Pharmacological Data)

AUC

Value of Type (Pharmacological Data)

447.2 ng*h/ml

Location

Paragraph 140; 141

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

64 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

rat

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

title comp. administered as l-homoarginine d-amphetamine dihydrochloride prodrug solution at a dose of 4.20 mg/kg

Further Details (Pharmacological Data)

peak plasma concentration (Cmax); Cmax related to: plasma

Type (Pharmacological Data)

Cmax

Value of Type (Pharmacological Data)

43.2 ng/ml

Location

Paragraph 140; 141

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ;

Title/Abstract Full Text Show Details

65 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

rat

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

title comp. administered as l-homoarginine d-amphetamine dihydrochloride prodrug solution at a dose of 4.20 mg/kg

Further Details (Pharmacological Data)

time to Cmax (tmax); tmax related to: plasma

Type (Pharmacological Data)

tmax

Value of Type (Pharmacological Data)

3 h

Location

Paragraph 140; 141

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

66 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

rat

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

title comp. administered as l-lysine-d-amphetamine prodrug (Vyvanse™)solution at a dose of 5.05 mg/kg

Further Details (Pharmacological Data)

area under the curve (AUC); AUC related to: plasma

Type (Pharmacological Data)

AUC

Value of Type (Pharmacological Data)

596.4 ng*h/ml

Location

Paragraph 140; 141

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

67 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

rat

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

title comp. administered as l-lysine-d-amphetamine prodrug (Vyvanse™)solution at a dose of 5.05 mg/kg

Further Details (Pharmacological

peak plasma concentration (Cmax); Cmax related to: plasma

Data) Type (Pharmacological Data)

Cmax

Value of Type (Pharmacological Data)

71.5 ng/ml

Location

Paragraph 140; 141

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

68 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

rat

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

title comp. administered as l-lysine-d-amphetamine prodrug (Vyvanse™)solution at a dose of 5.05 mg/kg

Further Details (Pharmacological Data)

time to Cmax (tmax); tmax related to: plasma

Type (Pharmacological Data)

tmax

Value of Type (Pharmacological Data)

2 h

Location

Paragraph 140; 141

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

69 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

dog

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

title comp. administered as l-homoarginine d-amphetamine dihydrochloride prodrug at a dose of 1.5 mg/kg

Further Details (Pharmacological Data)

area under the curve (AUC); AUC related to: plasma

Type (Pharmacological Data)

AUC

Value of Type (Pharmacological Data)

706.2 ng*h/ml

Location

Paragraph 140; 142

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

70 of 303

Effect (Pharmacological

pharmacokinetics

Data) Species or TestSystem (Pharmacological Data)

dog

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

title comp. administered as l-homoarginine d-amphetamine dihydrochloride prodrug at a dose of 1.5 mg/kg

Further Details (Pharmacological Data)

peak plasma concentration (Cmax); Cmax related to: plasma

Type (Pharmacological Data)

Cmax

Value of Type (Pharmacological Data)

94.3 ng/ml

Location

Paragraph 140; 142

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

71 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

dog

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

title comp. administered as l-homoarginine d-amphetamine dihydrochloride prodrug at a dose of 1.5 mg/kg

Further Details (Pharmacological Data)

time to Cmax (tmax); tmax related to: plasma

Type (Pharmacological Data)

tmax

Value of Type (Pharmacological Data)

2 h

Location

Paragraph 140; 142

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

72 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

dog

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

title comp. administered as l-lysine-d-amphetamine prodrug (Vyvanse™) at a dose of 1.8 mg/kg

Further Details (Pharmacological Data)

area under the curve (AUC); AUC related to: plasma

Type (Pharmacological Data)

AUC

Value of Type (Pharmacological Data)

775 ng*h/ml

Location

Paragraph 140; 142

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

73 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

dog

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

title comp. administered as l-lysine-d-amphetamine prodrug (Vyvanse™) at a dose of 1.8 mg/kg

Further Details (Pharmacological Data)

peak plasma concentration (Cmax); Cmax related to: plasma

Type (Pharmacological Data)

Cmax

Value of Type (Pharmacological Data)

95.4 ng/ml

Location

Paragraph 140; 142

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

74 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

dog

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

title comp. administered as l-lysine-d-amphetamine prodrug (Vyvanse™) at a dose of 1.8 mg/kg

Further Details (Pharmacological Data)

time to Cmax (tmax); tmax related to: plasma

Type (Pharmacological Data)

tmax

Value of Type (Pharmacological Data)

2 h

Location

Paragraph 140; 142

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

75 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

human

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

title comp. administered as l-homoarginine d-amphetamine dihydrochloride prodrug solution at a dose of 25 mg

Further Details (Pharmacological Data)

area under the curve (AUC); AUC related to: plasma

Type (Pharmacological Data)

AUC

Value of Type (Pharmacological Data)

282.7 ng*h/ml

Location

Paragraph 143; 144; 145

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

76 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

human

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

title comp. administered as l-homoarginine d-amphetamine dihydrochloride prodrug solution at a dose of 25 mg

Further Details (Pharmacological Data)

peak plasma concentration (Cmax); Cmax related to: plasma

Type (Pharmacological Data)

Cmax

Value of Type (Pharmacological Data)

20.7 ng/ml

Location

Paragraph 143; 144; 145

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

77 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

human

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

title comp. administered as l-homoarginine d-amphetamine dihydrochloride prodrug solution at a dose of 25 mg

Further Details (Pharmacological Data)

time to Cmax (tmax); tmax related to: plasma

Type (Pharmacological Data)

tmax

Value of Type (Pharmacological Data)

3.15 h

Location

Paragraph 143; 144; 145 KEMPHARM, INC.; MICKLE, Travis

Reference

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

78 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

human

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

title comp. administered as l-lysine-d-amphetamine prodrug (Vyvanse™)solution at a dose of 30 mg

Further Details (Pharmacological Data)

area under the curve (AUC); AUC related to: plasma

Type (Pharmacological Data)

AUC

Value of Type (Pharmacological Data)

421.9 ng*h/ml

Location

Paragraph 143; 144; 145

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

79 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

human

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

title comp. administered as l-lysine-d-amphetamine prodrug (Vyvanse™)solution at a dose of 30 mg

Further Details (Pharmacological Data)

peak plasma concentration (Cmax); Cmax related to: plasma

Type (Pharmacological Data)

Cmax

Value of Type (Pharmacological Data)

30 ng/ml

Location

Paragraph 143; 144; 145

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

80 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

human

Route of Application

peroral

Kind of Dosing (Pharmacological Data)

title comp. administered as l-lysine-d-amphetamine prodrug (Vyvanse™)solution at a dose of 30 mg

Further Details (Pharmacological Data)

time to Cmax (tmax); tmax related to: plasma

Type (Pharmacological Data)

tmax

Value of Type (Pharmacological Data)

2.85 h

Location

Paragraph 143; 144; 145

Reference

KEMPHARM, INC.; MICKLE, Travis

Patent: WO2013/19187 A1, 2013 ; Title/Abstract Full Text Show Details

81 of 303

82 of 303

Effect (Pharmacological Data)

protein binding affinity

Species or TestSystem (Pharmacological Data)

cells; genetically modified/infected with: DAT transporter

Kind of Dosing (Pharmacological Data)

comparative comp. dissolved in buffer containing a cell-impermeant fluorescence quencher

Method (Pharmacological Data)

name of assay/method: DAT uptake assay

Further Details (Pharmacological Data)

affinity constant (Ki); Ki related to: DAT transporter

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

109 nmol/l

Location

supporting information

Reference

Arunotayanun, Warunya; Dalley, Jeffrey W.; Huang, Xi-Ping; Setola, Vincent; Treble, Ric; Iversen, Leslie; Roth, Bryan L.; Gibbons, Simon

Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 11 p. 3411 - 3415 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein binding affinity

Species or TestSystem (Pharmacological Data)

cells; genetically modified/infected with: DAT transporter

Kind of Dosing (Pharmacological Data)

comparative comp. dissolved in buffer containing a cell-impermeant fluorescence quencher

Method (Pharmacological Data)

name of assay/method: DAT uptake assay

Further Details (Pharmacological Data)

pIC50 related to: DAT transporter

Type (Pharmacological Data)

pIC50

Value of Type (Pharmacological Data)

6.54

Location

supporting information

Reference

Arunotayanun, Warunya; Dalley, Jeffrey W.; Huang, Xi-Ping; Setola, Vincent; Treble, Ric; Iversen, Leslie; Roth, Bryan L.; Gibbons, Simon

Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 11 p. 3411 - 3415 Title/Abstract Full Text View citing articles Show Details

83 of 303

84 of 303

85 of 303

86 of 303

87 of 303

Effect (Pharmacological Data)

protein binding affinity

Species or TestSystem (Pharmacological Data)

cells; genetically modified/infected with: DAT transporter

Kind of Dosing (Pharmacological Data)

comparative comp. dissolved in buffer containing a cell-impermeant fluorescence quencher

Method (Pharmacological Data)

name of assay/method: DAT uptake assay

Results

molecular target: DAT transporter

Location

supporting information

Reference

Arunotayanun, Warunya; Dalley, Jeffrey W.; Huang, Xi-Ping; Setola, Vincent; Treble, Ric; Iversen, Leslie; Roth, Bryan L.; Gibbons, Simon

Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 11 p. 3411 - 3415 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Broadley, Kenneth J.; Fehler, Martina; Ford, William R.; Kidd, Emma J.

European Journal of Pharmacology, 2013 , vol. 715, # 1-3 p. 370 - 380 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

5-hydroxytryptamine transporter-mediated release; effect on

Species or TestSystem (Pharmacological Data)

brain synaptosomes of Sprague-Dawley rat

Sex

male

Further Details (Pharmacological Data)

transporter-mediated release assay; radioligand: 5 nM [3H]5-hydroxytryptamine; synaptosomal preparation from whole brain minus cerebellum and caudate used

Results

molecular target: rat 5-hydroxytryptamine transporter

Reference

Rothman, Richard B.; Partilla, John S.; Baumann, Michael H.; Lightfoot-Siordia, Catrissa; Blough, Bruce E.

Journal of Pharmacology and Experimental Therapeutics, 2012 , vol. 341, # 1 p. 251 - 262 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

5-hydroxytryptamine transporter-mediated release; effect on

Species or TestSystem (Pharmacological Data)

brain synaptosomes of Sprague-Dawley rat

Sex

male

Further Details (Pharmacological Data)

transporter-mediated release assay; radioligand: 5 nM [3H]5-hydroxytryptamine; synaptosomal preparation from whole brain minus cerebellum and caudate used; effective concentration (EC)

Type (Pharmacological Data)

EC50

Value of Type (Pharmacological Data)

1960 nmol/l

Reference

Rothman, Richard B.; Partilla, John S.; Baumann, Michael H.; Lightfoot-Siordia, Catrissa; Blough, Bruce E.

Journal of Pharmacology and Experimental Therapeutics, 2012 , vol. 341, # 1 p. 251 - 262 Title/Abstract Full Text View citing articles Show Details

Effect

5-hydroxytryptamine transporter-mediated release; effect on

(Pharmacological Data)

88 of 303

89 of 303

90 of 303

Species or TestSystem (Pharmacological Data)

brain synaptosomes of Sprague-Dawley rat

Sex

male

Further Details (Pharmacological Data)

transporter-mediated release assay; radioligand: 5 nM [3H]5-hydroxytryptamine; synaptosomal preparation from whole brain minus cerebellum and caudate used; maximal release rate (Emax)

Type (Pharmacological Data)

Emax

Value of Type (Pharmacological Data)

104 percent

Reference

Rothman, Richard B.; Partilla, John S.; Baumann, Michael H.; Lightfoot-Siordia, Catrissa; Blough, Bruce E.

Journal of Pharmacology and Experimental Therapeutics, 2012 , vol. 341, # 1 p. 251 - 262 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

dopamine transporter-mediated release; effect on

Species or TestSystem (Pharmacological Data)

brain synaptosomes of Sprague-Dawley rat

Sex

male

Further Details (Pharmacological Data)

transporter-mediated release assay; radioligand: 5 nM [3H]1-methyl-4-phenylpyridinium; synaptosomal preparation from caudate used

Results

molecular target: rat dopamine transporter

Reference

Rothman, Richard B.; Partilla, John S.; Baumann, Michael H.; Lightfoot-Siordia, Catrissa; Blough, Bruce E.

Journal of Pharmacology and Experimental Therapeutics, 2012 , vol. 341, # 1 p. 251 - 262 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

dopamine transporter-mediated release; effect on

Species or TestSystem (Pharmacological Data)

brain synaptosomes of Sprague-Dawley rat

Sex

male

Further Details (Pharmacological Data)

transporter-mediated release assay; radioligand: 5 nM [3H]1-methyl-4-phenylpyridinium; synaptosomal preparation from caudate used; effective concentration (EC)

Type (Pharmacological Data)

EC50

Value of Type (Pharmacological Data)

6.4 nmol/l

Reference

Rothman, Richard B.; Partilla, John S.; Baumann, Michael H.; Lightfoot-Siordia, Catrissa; Blough, Bruce E.

Journal of Pharmacology and Experimental Therapeutics, 2012 , vol. 341, # 1 p. 251 - 262 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

dopamine transporter-mediated release; effect on

Species or TestSystem (Pharmacological Data)

brain synaptosomes of Sprague-Dawley rat

Sex

male

Further Details (Pharmacological

transporter-mediated release assay; radioligand: 5 nM [3H]1-methyl-4-phenylpyridinium; synaptosomal preparation from caudate used; maximal release rate (Emax)

Data)

91 of 303

92 of 303

93 of 303

Type (Pharmacological Data)

Emax

Value of Type (Pharmacological Data)

103 percent

Reference

Rothman, Richard B.; Partilla, John S.; Baumann, Michael H.; Lightfoot-Siordia, Catrissa; Blough, Bruce E.

Journal of Pharmacology and Experimental Therapeutics, 2012 , vol. 341, # 1 p. 251 - 262 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

norepinephrine transporter-mediated release; effect on

Species or TestSystem (Pharmacological Data)

brain synaptosomes of Sprague-Dawley rat

Sex

male

Further Details (Pharmacological Data)

transporter-mediated release assay; radioligand: 5 nM [3H]1-methyl-4-phenylpyridinium; synaptosomal preparation from whole brain minus cerebellum and caudate used

Results

molecular target: rat norepinephrine transporter

Reference

Rothman, Richard B.; Partilla, John S.; Baumann, Michael H.; Lightfoot-Siordia, Catrissa; Blough, Bruce E.

Journal of Pharmacology and Experimental Therapeutics, 2012 , vol. 341, # 1 p. 251 - 262 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

norepinephrine transporter-mediated release; effect on

Species or TestSystem (Pharmacological Data)

brain synaptosomes of Sprague-Dawley rat

Sex

male

Further Details (Pharmacological Data)

transporter-mediated release assay; radioligand: 5 nM [3H]1-methyl-4-phenylpyridinium; synaptosomal preparation from whole brain minus cerebellum and caudate used; effective concentration (EC)

Type (Pharmacological Data)

EC50

Value of Type (Pharmacological Data)

7.4 nmol/l

Reference

Rothman, Richard B.; Partilla, John S.; Baumann, Michael H.; Lightfoot-Siordia, Catrissa; Blough, Bruce E.

Journal of Pharmacology and Experimental Therapeutics, 2012 , vol. 341, # 1 p. 251 - 262 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

norepinephrine transporter-mediated release; effect on

Species or TestSystem (Pharmacological Data)

brain synaptosomes of Sprague-Dawley rat

Sex

male

Further Details (Pharmacological Data)

transporter-mediated release assay; radioligand: 5 nM [3H]1-methyl-4-phenylpyridinium; synaptosomal preparation from whole brain minus cerebellum and caudate used; maximal release rate (Emax)

Type (Pharmacological Data)

Emax

Value of Type (Pharmacological Data)

101 percent

Reference

Rothman, Richard B.; Partilla, John S.; Baumann, Michael H.; Lightfoot-Siordia, Catrissa; Blough, Bruce E.

Journal of Pharmacology and Experimental Therapeutics, 2012 , vol. 341, # 1 p. 251 - 262 Title/Abstract Full Text View citing articles Show Details

94 of 303

95 of 303

96 of 303

97 of 303

Effect (Pharmacological Data)

parasite growth; inhibition of

Species or TestSystem (Pharmacological Data)

Plasmodium falciparum

Kind of Dosing (Pharmacological Data)

title comp. used as saccharate

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

352 μmol/l

Reference

Yuan, Jing; Cheng, Ken Chih-Chien; Johnson, Ronald L.; Huang, Ruili; Pattaradilokrat, Sittiporn; Liu, Anna; Guha, Rajarshi; Fidock, David A.; Inglese, James; Wellems, Thomas E.; Austin, Christopher P.; Su, Xin-Zhuan

Science, 2011 , vol. 333, # 6043 p. 724 - 729 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; activation of

Species or TestSystem (Pharmacological Data)

RD-HGA16 cells; genetically modified/infected with: recombinant human TAAR1

Further Details (Pharmacological Data)

TAAR1: trace amine-associated receptor 1; effective concentration (EC); EC50 related to: human TAAR1

Type (Pharmacological Data)

EC50

Value of Type (Pharmacological Data)

0.6 μmol/l

Reference

Lewin, Anita H.; Miller, Gregory M.; Gilmour, Brian

Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 23 p. 7044 - 7048 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; activation of

Species or TestSystem (Pharmacological Data)

RD-HGA16 cells; genetically modified/infected with: recombinant human TAAR1

Further Details (Pharmacological Data)

TAAR1: trace amine-associated receptor 1

Results

molecular target: human TAAR1

Reference

Lewin, Anita H.; Miller, Gregory M.; Gilmour, Brian

Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 23 p. 7044 - 7048 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; activation of

Species or TestSystem (Pharmacological Data)

RD-HGA16 cells; genetically modified/infected with: recombinant rhesus monkey TAAR1

Further Details (Pharmacological Data)

TAAR1: trace amine-associated receptor 1; effective concentration (EC); EC50 related to: monkey TAAR1

Type (Pharmacological

EC50

Data)

98 of 303

99 of 303

100 of 303

Value of Type (Pharmacological Data)

1.01 μmol/l

Reference

Lewin, Anita H.; Miller, Gregory M.; Gilmour, Brian

Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 23 p. 7044 - 7048 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; activation of

Species or TestSystem (Pharmacological Data)

RD-HGA16 cells; genetically modified/infected with: recombinant rhesus monkey TAAR1

Further Details (Pharmacological Data)

TAAR1: trace amine-associated receptor 1

Results

molecular target: monkey TAAR1

Reference

Lewin, Anita H.; Miller, Gregory M.; Gilmour, Brian

Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 23 p. 7044 - 7048 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neurotransmitter level; increase of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

1 mg/kg

Kind of Dosing (Pharmacological Data)

comparative comp. dissolved in saline

Further Details (Pharmacological Data)

microdialysis; mass of species: 300 - 350 g; dopamine extracellular level increase rate related to: nucleus accumbens

Type (Pharmacological Data)

dopamine extracellular level increase rate

Value of Type (Pharmacological Data)

412 percent

Reference

Kehr; Ichinose; Yoshitake; Goiny; Sievertsson; Nyberg

British Journal of Pharmacology, 2011 , vol. 164, # 8 p. 1949 - 1958 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neurotransmitter level; increase of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

1 mg/kg

Kind of Dosing (Pharmacological Data)

comparative comp. dissolved in saline

Further Details

microdialysis; mass of species: 300 - 350 g; serotonin extracellular level increase rate related to: nucleus accumbens

(Pharmacological Data)

101 of 303

102 of 303

Type (Pharmacological Data)

serotonin extracellular level increase rate

Value of Type (Pharmacological Data)

165 percent

Reference

Kehr; Ichinose; Yoshitake; Goiny; Sievertsson; Nyberg

British Journal of Pharmacology, 2011 , vol. 164, # 8 p. 1949 - 1958 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neurotransmitter metabolite level; decrease of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

1 mg/kg

Kind of Dosing (Pharmacological Data)

comparative comp. dissolved in saline

Further Details (Pharmacological Data)

microdialysis; DOPAC: 3,4-dihydroxyphenylacetic acid; 5-HIAA: 5-hydroxyindolacetic acid; mass of species: 300 - 350 g; 5-HIAA extracellular level decrease rate related to: nucleus accumbens

Type (Pharmacological Data)

5-HIAA extracellular level decrease rate

Value of Type (Pharmacological Data)

32.9 percent

Reference

Kehr; Ichinose; Yoshitake; Goiny; Sievertsson; Nyberg

British Journal of Pharmacology, 2011 , vol. 164, # 8 p. 1949 - 1958 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neurotransmitter metabolite level; decrease of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

1 mg/kg

Kind of Dosing (Pharmacological Data)

comparative comp. dissolved in saline

Further Details (Pharmacological Data)

microdialysis; DOPAC: 3,4-dihydroxyphenylacetic acid; 5-HIAA: 5-hydroxyindolacetic acid; mass of species: 300 - 350 g; DOPAC extracellular level decrease rate related to: nucleus accumbens

Type (Pharmacological Data)

DOPAC extracellular level decrease rate

Value of Type (Pharmacological Data)

42.5 percent

Reference

Kehr; Ichinose; Yoshitake; Goiny; Sievertsson; Nyberg

British Journal of Pharmacology, 2011 , vol. 164, # 8 p. 1949 - 1958 Title/Abstract Full Text View citing articles Show Details

103 of 303

104 of 303

105 of 303

Effect (Pharmacological Data)

dopamine level; increase of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

4 - 10 mg/kg

Further Details (Pharmacological Data)

microdialysis from dorsal limit of the left striatum; mass of species: 300 - 350 g; increasing rate related to: striatal extracellular compartment

Type (Pharmacological Data)

increasing rate

Value of Type (Pharmacological Data)

464 - 791 percent

Reference

Aluf; Vaya; Khatib; Finberg

Neuropharmacology, 2011 , vol. 61, # 1-2 p. 87 - 94 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

extracellular oxidative stress level in the striatum; decrease of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

4 mg/kg

Further Details (Pharmacological Data)

microdialysis from dorsal limit of the left striatum; LT: sensitive oxidative stress marker molecule was constructed from linoleic acid combined covalently with tyrosine; mass of species: 300 - 350 g; decreasing rate related to: LT-OOH

Type (Pharmacological Data)

decreasing rate

Value of Type (Pharmacological Data)

28 percent

Reference

Aluf; Vaya; Khatib; Finberg

Neuropharmacology, 2011 , vol. 61, # 1-2 p. 87 - 94 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

extracellular oxidative stress level in the striatum; increase of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

10 mg/kg

Further Details (Pharmacological Data)

microdialysis from dorsal limit of the left striatum; LT: sensitive oxidative stress marker molecule was constructed from linoleic acid combined covalently with tyrosine; mass of species: 300 - 350 g; increasing rate related to: LT-OOH

Type

increasing rate

(Pharmacological Data)

106 of 303

107 of 303

108 of 303

Value of Type (Pharmacological Data)

38 percent

Reference

Aluf; Vaya; Khatib; Finberg

Neuropharmacology, 2011 , vol. 61, # 1-2 p. 87 - 94 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

intracellular oxidative stress level in the striatum; decrease of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

4 - 10 mg/kg

Further Details (Pharmacological Data)

GC/MS assay; mass of species: 300 - 350 g; decreasing rate related to: 7-ketocholesterol

Type (Pharmacological Data)

decreasing rate

Value of Type (Pharmacological Data)

50 - 57 percent

Reference

Aluf; Vaya; Khatib; Finberg

Neuropharmacology, 2011 , vol. 61, # 1-2 p. 87 - 94 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

level of oxidized dopamine metabolites in the striatum; decrease of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

4 - 10 mg/kg

Further Details (Pharmacological Data)

HPLC analysis of striatal homogenate; DOPAC: 3,4-dihydroxyphenylacetic acid; mass of species: 300 - 350 g; decreasing rate related to: DOPAC

Type (Pharmacological Data)

decreasing rate

Value of Type (Pharmacological Data)

39 - 60 percent

Reference

Aluf; Vaya; Khatib; Finberg

Neuropharmacology, 2011 , vol. 61, # 1-2 p. 87 - 94 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

dopamine fractional release; stimulation of

Species or TestSystem (Pharmacological Data)

pheochromocytoma PC-12 cells of rat

Concentration

5 μmol/l

(Pharmacological Data)

109 of 303

110 of 303

111 of 303

112 of 303

Type (Pharmacological Data)

stimulation rate

Value of Type (Pharmacological Data)

45.6 percent

Reference

Abdelhafez, Omaima M.; Amin, Kamelia M.; Ali, Hamed I.; Maher, Timothy J.; Batran, Rasha Z.

Neurochemistry International, 2011 , vol. 59, # 6 p. 906 - 912 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein binding affinity

Species or TestSystem (Pharmacological Data)

embryonic kidney HEK293 cells of human; genetically modified/infected with: human DAT

Further Details (Pharmacological Data)

[3H]2β-carbomethoxy-3β-(4-fluorophenyl)-tropane used as radioligand; DAT: dopamine transporter;; inhibition constant (Ki); Ki related to: dopamine transporter

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

592.8 nmol/l

Reference

Schmitt, Kyle C.; Mamidyala, Sreeman; Biswas, Swati; Dutta, Aloke K.; Reith, Maarten E. A.

Journal of Neurochemistry, 2010 , vol. 112, # 6 p. 1605 - 1618 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein binding affinity

Species or TestSystem (Pharmacological Data)

embryonic kidney HEK293 cells of human; genetically modified/infected with: human DAT

Further Details (Pharmacological Data)

[3H]2β-carbomethoxy-3β-(4-fluorophenyl)-tropane used as radioligand; DAT: dopamine transporter;

Results

molecular target: dopamine transporter

Reference

Schmitt, Kyle C.; Mamidyala, Sreeman; Biswas, Swati; Dutta, Aloke K.; Reith, Maarten E. A.

Journal of Neurochemistry, 2010 , vol. 112, # 6 p. 1605 - 1618 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein binding affinity

Species or TestSystem (Pharmacological Data)

embryonic kidney HEK293 cells of human; genetically modified/infected with: mutant human DAT W84L

Further Details (Pharmacological Data)

[3H]2β-carbomethoxy-3β-(4-fluorophenyl)-tropane used as radioligand; DAT: dopamine transporter; Ki related to: dopamine transporter W84L

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

1486 nmol/l

Reference

Schmitt, Kyle C.; Mamidyala, Sreeman; Biswas, Swati; Dutta, Aloke K.; Reith, Maarten E. A.

Journal of Neurochemistry, 2010 , vol. 112, # 6 p. 1605 - 1618 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological

protein binding affinity

Data)

113 of 303

114 of 303

115 of 303

116 of 303

Species or TestSystem (Pharmacological Data)

embryonic kidney HEK293 cells of human; genetically modified/infected with: mutant human DAT W84L

Further Details (Pharmacological Data)

[3H]2β-carbomethoxy-3β-(4-fluorophenyl)-tropane used as radioligand; DAT: dopamine transporter

Results

molecular target: dopamine transporter W84L

Reference

Schmitt, Kyle C.; Mamidyala, Sreeman; Biswas, Swati; Dutta, Aloke K.; Reith, Maarten E. A.

Journal of Neurochemistry, 2010 , vol. 112, # 6 p. 1605 - 1618 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein binding affinity

Species or TestSystem (Pharmacological Data)

embryonic kidney HEK293 cells of human; genetically modified/infected with: mutant human DAT D313N

Further Details (Pharmacological Data)

[3H]2β-carbomethoxy-3β-(4-fluorophenyl)-tropane used as radioligand; DAT: dopamine transporter; Ki related to: dopamine transporter D313N

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

7534 nmol/l

Reference

Schmitt, Kyle C.; Mamidyala, Sreeman; Biswas, Swati; Dutta, Aloke K.; Reith, Maarten E. A.

Journal of Neurochemistry, 2010 , vol. 112, # 6 p. 1605 - 1618 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein binding affinity

Species or TestSystem (Pharmacological Data)

embryonic kidney HEK293 cells of human; genetically modified/infected with: mutant human DAT D313N

Further Details (Pharmacological Data)

[3H]2β-carbomethoxy-3β-(4-fluorophenyl)-tropane used as radioligand; DAT: dopamine transporter

Results

molecular target: dopamine transporter D313N

Reference

Schmitt, Kyle C.; Mamidyala, Sreeman; Biswas, Swati; Dutta, Aloke K.; Reith, Maarten E. A.

Journal of Neurochemistry, 2010 , vol. 112, # 6 p. 1605 - 1618 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

[3H]dopamine uptake; inhibition of

Species or TestSystem (Pharmacological Data)

embryonic kidney HEK293 cells of human; genetically modified/infected with: human DAT

Further Details (Pharmacological Data)

DAT: dopamine transporter; apparent affinity constant (Kapp); Kapp related to: dopamine transporter

Type (Pharmacological Data)

Kapp

Value of Type (Pharmacological Data)

163.5 nmol/l

Reference

Schmitt, Kyle C.; Mamidyala, Sreeman; Biswas, Swati; Dutta, Aloke K.; Reith, Maarten E. A.

Journal of Neurochemistry, 2010 , vol. 112, # 6 p. 1605 - 1618 Title/Abstract Full Text View citing articles Show Details

[3H]dopamine uptake; inhibition of

Effect (Pharmacological Data)

117 of 303

118 of 303

119 of 303

Species or TestSystem (Pharmacological Data)

embryonic kidney HEK293 cells of human; genetically modified/infected with: human DAT

Further Details (Pharmacological Data)

DAT: dopamine transporter

Results

molecular target: dopamine transporter

Reference

Schmitt, Kyle C.; Mamidyala, Sreeman; Biswas, Swati; Dutta, Aloke K.; Reith, Maarten E. A.

Journal of Neurochemistry, 2010 , vol. 112, # 6 p. 1605 - 1618 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

OCT3-mediated dopamine uptake; inhibition of

Species or TestSystem (Pharmacological Data)

HEK293 cells; genetically modified/infected with: human OCT3

Kind of Dosing (Pharmacological Data)

title comp. administered as sulfate salt

Further Details (Pharmacological Data)

OCT: organic cation transporter; confluent cells used; inhibitory concentration (IC)

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

41.5 μmol/l

Reference

Zhu, Hao-Jie; Appel, David I.; Gruendemann, Dirk; Markowitz, John S.

Journal of Neurochemistry, 2010 , vol. 114, # 1 p. 142 - 149 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

OCT3-mediated serotonin uptake; inhibition of

Species or TestSystem (Pharmacological Data)

HEK293 cells; genetically modified/infected with: human OCT3

Kind of Dosing (Pharmacological Data)

title comp. administered as sulfate salt

Further Details (Pharmacological Data)

OCT: organic cation transporter; confluent cells used; inhibitory concentration (IC)

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

24.1 μmol/l

Reference

Zhu, Hao-Jie; Appel, David I.; Gruendemann, Dirk; Markowitz, John S.

Journal of Neurochemistry, 2010 , vol. 114, # 1 p. 142 - 149 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

OCT3-mediated norepinephrine uptake; inhibition of

Species or TestSystem (Pharmacological Data)

HEK293 cells; genetically modified/infected with: human OCT3

Concentration

<= 100 μmol/l

(Pharmacological Data)

120 of 303

121 of 303

Kind of Dosing (Pharmacological Data)

title comp. administered as sulfate salt

Further Details (Pharmacological Data)

OCT: organic cation transporter; confluent cells used; inhibitory concentration (IC)

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

> 100 μmol/l

Reference

Zhu, Hao-Jie; Appel, David I.; Gruendemann, Dirk; Markowitz, John S.

Journal of Neurochemistry, 2010 , vol. 114, # 1 p. 142 - 149 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

OCT3-mediated 4-Di-1-ASP uptake; inhibition of

Species or TestSystem (Pharmacological Data)

HEK293 cells; genetically modified/infected with: human OCT3

Concentration (Pharmacological Data)

<= 100 μmol/l

Kind of Dosing (Pharmacological Data)

title comp. administered as sulfate salt

Further Details (Pharmacological Data)

OCT: organic cation transporter; 4-Di-1-ASP: 4-(4-(dimethylamino)styryl)-N-methylpyridinium iodide; confluent cells used; inhibitory concentration (IC)

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

> 100 μmol/l

Reference

Zhu, Hao-Jie; Appel, David I.; Gruendemann, Dirk; Markowitz, John S.

Journal of Neurochemistry, 2010 , vol. 114, # 1 p. 142 - 149 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein expression; effect on

Species or TestSystem (Pharmacological Data)

mouse

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

0.5 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline solution (NaCl 0.9percent) and administered as sulfate salt; given as commercial product: Parafarm.(R).

Further Details (Pharmacological Data)

Western blotting

Results

no effect (related to striatum-caudate putamen tyrosine hydroxylase); insignificant effect(s) discussed

Reference

Krapacher, Favio Ariel; Mlewski, Estela Cecilia; Ferreras, Soledad; Pisano, Victoria; Paolorossi, Mariana; Hansen, Cristian; Paglini, Gabriela

Journal of Neurochemistry, 2010 , vol. 114, # 1 p. 203 - 214 Title/Abstract Full Text View citing articles Show Details

122 of 303

123 of 303

124 of 303

Effect (Pharmacological Data)

D2 receptor-activated GIRK currents; decrease of

Species or TestSystem (Pharmacological Data)

substantia nigra pars compacta dopaminergic neurones of mouse

Concentration (Pharmacological Data)

30 μmol/l

Kind of Dosing (Pharmacological Data)

title comp administered as sulphate salt

Further Details (Pharmacological Data)

voltage clamp experiment; GIRK: G protein-gated inward rectifier K+ channel; (-)-quinpirole hydrochloride used to induce GIRK activation; reduction rate related to: G protein-gated inward rectifier K+ channel

Type (Pharmacological Data)

reduction rate

Value of Type (Pharmacological Data)

41.2 percent

Reference

Ledonne, Ada; Federici, Mauro; Giustizieri, Michela; Pessia, Mauro; Imbrici, Paola; Millan, Mark J; Bernardi, Giorgio; Mercuri, Nicola B

British Journal of Pharmacology, 2010 , vol. 160, # 6 p. 1509 - 1520 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pre-weaning body weight; effect on

Species or TestSystem (Pharmacological Data)

pup of Sprague-Dawley rat

Sex

male and female

Route of Application

intragastric

Concentration (Pharmacological Data)

5 - 25 mg/kg

Kind of Dosing (Pharmacological Data)

sulfate salt of title comp. administered twice daily

Further Details (Pharmacological Data)

effect determined at postnatal days 9-15; lowest observed effect dose (LOED)

Type (Pharmacological Data)

LOED

Value of Type (Pharmacological Data)

15 mg/kg

Reference

Smith, Andrew M.; Chen, Wei-Jung A.

Life Sciences, 2010 , vol. 86, # 13-14 p. 482 - 487 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

post-weaning body weight; effect on

Species or TestSystem (Pharmacological Data)

pup of Sprague-Dawley rat

Sex

male and female

Route of Application

intragastric

Concentration (Pharmacological Data)

5 - 25 mg/kg

Kind of Dosing

sulfate salt of title comp. administered twice daily

(Pharmacological Data)

125 of 303

126 of 303

127 of 303

Results

no effect; insignificant effect(s) discussed

Reference

Smith, Andrew M.; Chen, Wei-Jung A.

Life Sciences, 2010 , vol. 86, # 13-14 p. 482 - 487 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

organ weight; effect on

Species or TestSystem (Pharmacological Data)

pup of Sprague-Dawley rat

Sex

male and female

Route of Application

intragastric

Concentration (Pharmacological Data)

5 - 25 mg/kg

Kind of Dosing (Pharmacological Data)

sulfate salt of title comp. administered twice daily

Further Details (Pharmacological Data)

effect determined at postnatal day 9 and 68

Results

no effect (related to cortex); insignificant effect(s) discussed

Reference

Smith, Andrew M.; Chen, Wei-Jung A.

Life Sciences, 2010 , vol. 86, # 13-14 p. 482 - 487 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

organ weight; effect on

Species or TestSystem (Pharmacological Data)

pup of Sprague-Dawley rat

Sex

male and female

Route of Application

intragastric

Concentration (Pharmacological Data)

5 - 25 mg/kg

Kind of Dosing (Pharmacological Data)

sulfate salt of title comp. administered twice daily

Further Details (Pharmacological Data)

effect determined at postnatal day 9 and 68

Results

no effect (related to cerebellum); insignificant effect(s) discussed

Reference

Smith, Andrew M.; Chen, Wei-Jung A.

Life Sciences, 2010 , vol. 86, # 13-14 p. 482 - 487 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

organ weight; effect on

Species or TestSystem (Pharmacological Data)

pup of Sprague-Dawley rat

Sex

male and female

Route of Application

intragastric

Concentration (Pharmacological Data)

5 - 25 mg/kg

128 of 303

129 of 303

130 of 303

Kind of Dosing (Pharmacological Data)

sulfate salt of title comp. administered twice daily

Further Details (Pharmacological Data)

effect determined at postnatal day 9 and 68

Results

no effect (related to brainstem); insignificant effect(s) discussed

Reference

Smith, Andrew M.; Chen, Wei-Jung A.

Life Sciences, 2010 , vol. 86, # 13-14 p. 482 - 487 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pre-weaning body weight; effect on

Species or TestSystem (Pharmacological Data)

pup of Sprague-Dawley rat

Sex

male and female

Route of Application

intragastric

Concentration (Pharmacological Data)

5 - 25 mg/kg

Kind of Dosing (Pharmacological Data)

sulfate salt of title comp. administered twice daily

Further Details (Pharmacological Data)

effect determined at postnatal day 7, 8, 17, 19 and 21; lowest observed effect dose (LOED)

Type (Pharmacological Data)

LOED

Value of Type (Pharmacological Data)

25 mg/kg

Reference

Smith, Andrew M.; Chen, Wei-Jung A.

Life Sciences, 2010 , vol. 86, # 13-14 p. 482 - 487 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pre-weaning body weight; effect on

Species or TestSystem (Pharmacological Data)

pup of Sprague-Dawley rat

Sex

male and female

Route of Application

intragastric

Concentration (Pharmacological Data)

5 - 25 mg/kg

Kind of Dosing (Pharmacological Data)

sulfate salt of title comp. administered twice daily

Further Details (Pharmacological Data)

effect determined at postnatal days 1-7

Results

no effect; insignificant effect(s) discussed

Reference

Smith, Andrew M.; Chen, Wei-Jung A.

Life Sciences, 2010 , vol. 86, # 13-14 p. 482 - 487 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem

pup of Sprague-Dawley rat

(Pharmacological Data)

131 of 303

132 of 303

133 of 303

Sex

male and female

Route of Application

intragastric

Concentration (Pharmacological Data)

5 - 25 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. administered as sulfate salt; title comp. administered twice daily for 9 days

Further Details (Pharmacological Data)

concentration related to: serum

Type (Pharmacological Data)

concentration

Value of Type (Pharmacological Data)

170 - 489.7 ng/ml

Reference

Smith, Andrew M.; Chen, Wei-Jung A.

Life Sciences, 2010 , vol. 86, # 13-14 p. 482 - 487 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

latent inhibition expression; induction of

Species or TestSystem (Pharmacological Data)

C57BL/6J mouse

Sex

male

Kind of Dosing (Pharmacological Data)

title compound dissolved in saline

Type (Pharmacological Data)

effective dose

Value of Type (Pharmacological Data)

0.5 - 1 mg/kg

Reference

Lipina, Tatiana; Roder, John

Psychopharmacology, 2010 , vol. 208, # 3 p. 487 - 498 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

latent inhibition expression; induction of

Species or TestSystem (Pharmacological Data)

C57BL/6J mouse

Sex

male

Concentration (Pharmacological Data)

2.5 mg/kg

Kind of Dosing (Pharmacological Data)

title compound dissolved in saline

Results

no effect

Reference

Lipina, Tatiana; Roder, John

Psychopharmacology, 2010 , vol. 208, # 3 p. 487 - 498 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

latent inhibition expression; induction of

Species or Test-

C57BL/6J mouse

System (Pharmacological Data)

134 of 303

135 of 303

136 of 303

Sex

male

Kind of Dosing (Pharmacological Data)

title compound dissolved in saline; with 40 whitenoise presentations

Type (Pharmacological Data)

effective dose

Value of Type (Pharmacological Data)

2.5 mg/kg

Reference

Lipina, Tatiana; Roder, John

Psychopharmacology, 2010 , vol. 208, # 3 p. 487 - 498 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

[3H]MK-801 binding to NMDA receptor; inhibition of

Species or TestSystem (Pharmacological Data)

cerebral membranes of rat

Further Details (Pharmacological Data)

NMDA: N-methyl-D-aspartate; MK-801: 5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine; test membranes prepared from cerebral cortex and CA1 and dentate gyrus part of hippocampus; inhibition constant (Ki); Ki related to: NMDA receptor

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

300 μmol/l

Reference

Berger, Michael L.; Schweifer, Anna; Rebernik, Patrick; Hammerschmidt, Friedrich

Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 9 p. 3456 - 3462 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

[3H]MK-801 binding to NMDA receptor; inhibition of

Species or TestSystem (Pharmacological Data)

cerebral membranes of rat

Further Details (Pharmacological Data)

NMDA: N-methyl-D-aspartate; MK-801: 5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine; test membranes prepared from cerebral cortex and CA1 and dentate gyrus part of hippocampus

Results

molecular target: NMDA receptor

Reference

Berger, Michael L.; Schweifer, Anna; Rebernik, Patrick; Hammerschmidt, Friedrich

Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 9 p. 3456 - 3462 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Method (Pharmacological Data)

EXAMPLE 10Intranasal Study of Amp, hAr-Amp, Orn-AmpMale Sprague-Dawley rats were fasted overnight and dosed by intranasal administration with either hArg-Amp, Orn-Amp or d-amphetamine. Doses were calculated at an equivalent 1.5 mg/kg freebase equivalent of d-amphetamine. Plasma concentrations of d-amphetamine were measured using ELISA. Mean plasma concentration curves (n=5) of d-amphetamine released by hArg-Amp or Orn-Amp are shown in FIG. 8. Pharmacokinetic parameters of this study are listed in Table 6. No significant release (<25percent) was observed in either hArg-Amp or Orn-Amp.

Results

title compound treatment showed percentAUC: 100percent; Tmax: 15min; Cmax: 53ng/ml; percentTmax: 100percent; percentCmax: 100percent; figure is given

Location

Page/Page column 3; 15; Sheet 4

Reference

Mickle, Travis C.

Patent: US2008/139653 A1, 2008 ; Title/Abstract Full Text Show Details

137 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intravenous

Method (Pharmacological Data)

EXAMPLE 11Intravenous Study of Amp, hAr-Amp, Orn-AmpMale Sprague-Dawley rats were dosed by intravenous administration through the tail vein with hArg-Amp, Orn-Amp or d-amphetamine. Doses were calculated at an equivalent 1.5 mg/kg freebase equivalent of d-amphetamine. Plasma concentrations of d-amphetamine were measured using ELISA. Mean plasma concentration curves (n=5) of d-amphetamine released by hArg-Amp or Orn-Amp are shown in FIG. 9. Pharmacokinetic parameters of this study are listed in Table 7. No significant release (max (earlier or later), modify curve shape, lower Cmax, and raise Cmax. In addition, the shift in Tmax for hArg-Amp may be clinically significant in that many of the cardiovascular side effects and toxicity are related to Tmax and Cmax. The results demonstrate that by using non-standard amino acids a shift in the Tmax, with a lower Cmax occurs without changing AUC significantly. In addition, the slope of uptake of hArg-Amp vs. Lys-Amp appears to be more gradual thus leading to a slower onset which could further alleviate side effects.The amphetamine conjugate, hArg-Amp, of the present technology demonstrates that by using non-standard amino acids, a shift in the Tmax occurs while still retaining AUC and potential clinical effect. By using non-standard amino acids, we are able to demonstrate that both hArg-Amp and Orn-Amp show little release via the IN and IV route yet still maintain a similar AUC.

Results

title compound treatment showed an percentAUC: 100percent; Tmax: 15min; Cmax: 396ng/ml; percentTmax: 100percent; percentCmax: 100percent; figure is given

Location

Page/Page column 4; 15; Sheet 5

Reference

Mickle, Travis C.

Patent: US2008/139653 A1, 2008 ; Title/Abstract Full Text Show Details

138 of 303

Effect (Pharmacological Data)

dopamine function; effect on

Species or TestSystem (Pharmacological Data)

6-hydroxydopmaine model of Wistar mouse

Sex

male

Method (Pharmacological Data)

EXAMPLE 86-Hydroxydopamine Model6-Hydroxydopamine (6-OHDA) is a neurotoxin which causes a unilateral lesion of the dopaminergic nigrostriatal pathway that induces hypersensitivity of the post synaptic dopaminergic receptor in the striatum of the lesioned side. An indirect acting compound like amphetamine is administered the mice rotate toward the lesioned side (ipsilateral) as opposed to when a direct acting dopaminergic drug is administered which causes then to rotate contra laterally. Therefore, this test can be used for the study of central dopamine function and the evaluation of dopamine antagonists and agonists, particularly the activity of novel anti-parkinsonian drugs. This test clearly distinguishes drugs with predominantly dopamine receptor agonist activity from those with predominantly dopamine releasing activity of the drug.Procedure: Male Wistar mice weighing 200-250 grams at the time of surgery are used. They are housed individually in a controlled environment with free access to food and water. The animals are anaesthetized with sodium pentobarbital. The head is placed in a stereotaxic device (DKI 900) and positioned according to the atlas of Konig and Klippel. After a sagittal cut is made in the skin of the skull, a 2 mm wide hole is drilled with an electrical trepan drill. Care is taken not to lesion the meninges. A 30 gauge stainless-steel cannula connected to a Hamilton syringe is aimed at the anterior zona compacta of the substantia nigra (coordinates anterior 1.88 mm, lateral 2.0 mm and dorso-ventral-8.2 mm from instrument zero). A total of 8 μg of 6-HAD in 4 γ/L of saline is injected at a rate of 1 γ/L/min. After the intra-cranial injection, the wound is closed.The animal is allowed several weeks for recovery and for development of the lesion. Specially constructed opaque plastic spheres attached to solid state programming equipment serve as test chambers. The number of full turns, either ipsilateral or contra lateral to the lesion, are recorded on an automatic printout counter every 15 min for one or two hours test sessions. To determine the control values for ipsilateral turning, each subject is administered 2.5 mg/kg of d amphetamine and immediately placed in the circling chamber for 2 hours Control values for contra lateral circling are determined by injecting apomorphine at 1 mg/kg s.c. and recording the rat's circling for 1 hour. Test compounds are given i.p or sc. And the animals placed into the circling chambers. Circling is recorded over a 1 hour period. This experiment is conducted in 30 animals and the average is represented in the tableThe test drug induced significant ipsilateral rotations at dose 30 mg/kg (P<0.001) and 10 mg/kg (P<0.05). This test mimics dopamine depletion and consequently Parkinson's disease. Anti-Parkinson's compounds may have contralateral or ipsilateral rotation. Drugs like Amphetamine induce ipsilateral rotation. Whereas drugs like L-Dopa, Apomorphine, Bromocriptine induce contralateral rotation. Monoamine Oxidase B inhibitors like Selgiline induces ipsilateral rotation. COMT inhibitors induce contra-lateral rotation.The test drug behaves like Amphetamine or Monoamine Oxidase (MAO-B) inhibitor. Hence the test drug may have the dopamine releasing property that is significant as compared to control at these doses.This model is an important one to determine whether a compound is a dopaminergic one or one that acts on the dopamine receptors. The ipsilateral rotation with the test compound shows its dopaminergic activity. Unlike the current class of drugs which show a contralateral rotation the test compound is a dopaminergic agent and not a receptor agonist.This experiment proves the exclusive dopaminergic activity of the test drug. Hence this dopaminergic composition can find applications related to increase of levels of dopamine. Increased levels of dopamine have an inhibitory effect on prolactin levels. Increased prolactin levels are one of the causes of P

Results

title compound treatment at 2.5 mg/kg induced ipsilateral rotation indicating dopaminergic activity

Location

Page/Page column 9

Reference

Indus Biotech Pvt. Ltd.

Patent: US2008/221173 A1, 2008 ; Title/Abstract Full Text Show Details

139 of 303

Effect (Pharmacological Data)

attention-deficit hyperactivity disorder; improvement of

Species or TestSystem (Pharmacological Data)

with attention-deficit hyperactivity disorder (ADHD) of human

Sex

male and female

Method (Pharmacological Data)

Example 1 - Treatment of adult ADHD sufferers with a combination of psychostimulant and mood stabiliserIn the clinical setting where this study has originated from, a number of adults with ADHD (who had previously demonstrated significant improvements on stimulants alone) began a dual regime of stimulant medication (dexamphetamine) augmented with sodium valproate (VPA), primarily as an agent to improve mood stability. The dosages used were from 15 to 70 mg/day of dexamphetamine and from 200 to 700 mg/day of VPA (Epilim) (= approximately 2 to 10 mg/kg/day). The Epilim product information supplied by Sanofi-Aventis for the treatment of mania (e.g. bipolar disorder) in adults suggests that control of symptoms occurs within the range of 1 ,000 to 2,000 mg/day, (i.e. 20 to 30 mg/kg/day). The dosages used in this trial were therefore substantially lower than the dosages required for treating mania.The determination of the dose for the dexamphetamine was undertaken in a clinical sensitive open label manner. The dose was titrated upwards dependent on the clinical response and the freedom from side-effects. The dose range was between 15 and 70 mg a day. The frequency of the dosing also varied dependent upon the clinical response. The usual dose interval was between two to four hours. This dosing adjustment took place prior to the commencement of the sodium valproate. The sodium valproate medication was initiated once a day at 50 mg tablet or elixir and titrated upwards dependent on response, but not more than one increase every three days. The dose was given as a once or twice a day regime. During the titration phase, if clinically possible, no other adjustments to the pharmacotherapy were undertaken. The dosages of sodium valproate, after adjustment, varied between 100 mg/day, 200 mg/day, 500 mg/day or 700 mg/day (number of patients - 71), with the majority of patients receiving either 200 mg/day or 500 mg/day.Results and DiscussionWhen VPA was integrated into the pharmacological approach, patients often described their thoughts as slowing to a rate that was more manageable and less chaotic. This seemed to allow for more temporal sequencing of ideas, with a resulting overall improvement in psychosocial functioning. The interesting dimension to this argument of pharmacological approach is that a large number of these patients had no evidence to suggest a personal or family history of a bipolar disorder and were benefiting from a dose of VPA below the initiation dose recommended for bipolar disorder, and significantly below the dose typically required to achieve control of symptoms of mania.A significant number of patients who reported a subjective improvement in ADHD symptoms also described an improvement in their reading and verbal comprehension abilities. They were more able to attend to the content of both the text and conversation, which was in direct contrast to their previously frustrating experiences of needing to put most of their mental effort into either reading or listening with relatively little comprehension occurring. We have been able to assess objectively oculomotor function with the Developmental Eye Movement Test (DEM): this has shown improvement consistent with that of the patient's own subjective experience, with less mental effort required to follow written text. This leads us to the hypothesis that the low dose of the sodium valproate is having a beneficial effect on fixational and saccade activity during reading and non reading tasks. The magnitude of the change for many of these individuals was comparable to changes in behaviour that occurred during their first experience of stimulant therapy.Additionally, the self-reported improvement appeared to correlate closely to notable changes in the complex interpersonal interaction during the clinical consultation. Verbal interactions between the treating psychiatrist and patients appeared more spontaneous and fluid, and patients appeared to be able

Results

patients treated by sodium valproate (200 to 700 mg/day) and title compound (15 to 70 mg/day) reported a subjective improvement in ADHD symptoms also described an improvement in their reading and verbal comprehension abilities; the improvement occurred almost immediately on initiation of therapy

Location

Page/Page column 17-26

Reference

GOSFORTH CENTRE (HOLDINGS) PTY LTD

Patent: WO2008/95221 A1, 2008 ; Title/Abstract Full Text Show Details

140 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

nasal

Method (Pharmacological Data)

Example 15: Intranasal study of Amp. Lys-Amp and hArg-Amp[0187] Male Sprague-Dawley rats were fasted overnight and dosed by intranasal administration with either hArg-Amp, Lys-Amp or d-amphetamine. Doses were calculated at an equivalent 1.5mg/kg freebase equivalent of Jamphetamine. Plasma concentrations of d-amphetamine were measured using ELISA. Mean plasma concentration curves (n=5) of d- amphetamine released by hArg-Amp or Lys-Amp are shown in Figure 9. Pharmacokinetic parameters of this study are listed in Table 6. No significant release (<50percent) was observed in either hArg-Amp or Lys-Amp and less release was observed within the first hour of administration (<25percent). Observed levels from Lys-Amp are significantly higher than previously published data.Table 6. Intranasal Properties of d- Amp, hArg-Amp and Lys-Amp

Results

title compound showed 100percentAUC, 5m Tmax, 779ng/ml Cmax, 100percentTmax, 100percentCmax in the overnight-fasted rats; figure is given

Location

Page/Page column 8; 48; 5/5

Reference

KEMPHARM, INC.

Patent: WO2008/98151 A2, 2008 ; Title/Abstract Full Text Show Details

141 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intravenous

Method (Pharmacological Data)

Example 16: Intravenous study of d- Amp, hArg-Amp, Lys-Amp[0188] Male Sprague-Dawley rats were dosed by intravenous administration through the tail vein with hArg-Amp, Lys-Amp or d- amphetamine. Doses were calculated at an equivalent 1.5mg/kg freebase equivalent of J-amphetamine. Plasma concentrations of d-amphetamine were measured using ELISA. Mean plasma concentration curves (n=5) of d- amphetamine released by hArg-Amp or Lys-Amp are shown in Figure 10. Pharmacokinetic parameters of this study are listed in Table 7. No significant release (<15percent) was observed in either hArg-Amp or Lys-Amp though hArg-Amp was significantly less. Observed levels from Lys-Amp are significantly higher than previously published data. The initial spike in d- amphetamine released from hArg- Amp cleared quickly.Table 7. Intravenous Properties of d- Amp, hArg-Amp and Lys-Amp

Results

title compound showed 100percentAUC, 5m Tmax, 554ng/ml Cmax, 100percentTmax, 100percentCmax in the overnight-fasted rats; figure is given

Location

Page/Page column 9; 49; 5/5

Reference

KEMPHARM, INC.

Patent: WO2008/98151 A2, 2008 ; Title/Abstract Full Text Show Details

142 of 303

143 of 303

144 of 303

Effect (Pharmacological Data)

agonist

Species or TestSystem (Pharmacological Data)

RD-HGA16 cells expressing human TAAR 1 receptor

Method (Pharmacological Data)

hTAAR1 activation assay; title comp. incubated with test cells in presence of Calcium 3 dye as fluorescent substrate (HAM's F-12 medium, 10percent FBS, 5percent CO2/95percent air, 37 deg C, 1 h); title comp. effect on internal calcium mobilization assessed; fluorimetry

Further Details (Pharmacological Data)

hTAAR1: human trace amine receptor 1; Emax: maximal title comp. efficacy

Type (Pharmacological Data)

EC50

Value of Type (Pharmacological Data)

935 nmol/l

Results

title comp. exhibited Emax 74percent

Reference

Lewin, Anita H.; Navarro, Hernan A.; Wayne Mascarella

Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 15 p. 7415 - 7423 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neuroregulatoric

Species or TestSystem (Pharmacological Data)

129Sv mouse

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

1 - 8 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in methylcellulose 0.25percent

Method (Pharmacological Data)

title comp. administered; polygraphic records performed within 14 h and scored by 30-s epochs for W, SWS and PS; W, SWS and PS amount as well as latencies to SWS and PS determined

Further Details (Pharmacological Data)

further investigation using HDC knockout mice; W: wakefulness; SWS: slow wave sleep; PS: paradoxical sleep; HDC: histidine decarboxylase

Results

title comp. increased W and decreased SWS and PS; this effect did not depend on HDC

Reference

Parmentier; Anaclet; Guhennec; Brousseau; Bricout; Giboulot; Bozyczko-Coyne; Spiegel; Ohtsu; Williams; Lin

Biochemical Pharmacology, 2007 , vol. 73, # 8 p. 1157 - 1171 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

hypertensive

145 of 303

146 of 303

Species or TestSystem (Pharmacological Data)

hybrid 129/SvCPJ and C57BL/6J mouse

Sex

male

Route of Application

intravenous

Concentration (Pharmacological Data)

1 mg/kg

Kind of Dosing (Pharmacological Data)

dissolved in normal saline, injected at volume of 20 - 100 μl

Method (Pharmacological Data)

Dbh-/- and Dbh+/- littermates used; carotid artery catheterized for measurment of systemic arterial pressure before/after title comp. administration; magnitude, area under-the-curve of response analysed

Further Details (Pharmacological Data)

reference comp.: 100 μg/kg tyramine, 0.3 μg/kg noradrenaline, 100 μg/kg dopamine, 0.1 μg/kg angiotensin II, 10 μg/kg phenylephrine; Dbh -/-: dopamine β-hyroxylase knockout

Results

title comp.-induced pressor response was smaller in Dbh-/- then in Dbh+/- mice similar to that of tyramine suggesting that action depend on endogenous noradrenaline; pressor responses of other reference comp. were similar in Dbh-/- and Dbh+/- mice

Reference

Liles; Baber; Deng; Porter; Corll; Murthy; Thomas; Kadowitz

British Journal of Pharmacology, 2007 , vol. 150, # 1 p. 29 - 36 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

chronotropic pos.

Species or TestSystem (Pharmacological Data)

hybrid 129/SvCPJ and C57BL/6J mouse

Sex

male

Route of Application

intravenous

Concentration (Pharmacological Data)

1 mg/kg

Kind of Dosing (Pharmacological Data)

dissolved in normal saline, injected at volume of 20 - 100 μl

Method (Pharmacological Data)

Dbh-/- and Dbh+/- littermates used; carotid artery catheterized for measurment of systemic arterial pressure before/after title comp. administration; heart rate determined from arterial pressure pulses

Further Details (Pharmacological Data)

reference comp.: 100 μg/kg tyramine, 0.3 μg/kg noradrenaline, 100 μg/kg dopamine, 0.1 μg/kg angiotensin II, 10 μg/kg phenylephrine; Dbh -/-: dopamine β-hyroxylase knockout; heart rate

Results

title comp. increased HR in Dbh+/- but not in Dbh-/- mice similar to tyramine suggesting that action of these compounds depended on presence of endogenous noradrenaline; other reference comp. produced similar HR increase in Dbh-/- and Dbh+/- mice

Reference

Liles; Baber; Deng; Porter; Corll; Murthy; Thomas; Kadowitz

British Journal of Pharmacology, 2007 , vol. 150, # 1 p. 29 - 36 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein expression; inhibition of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

2 mg/kg

Method (Pharmacological Data)

1-4 h after title comp. injection, rats sacrificed; striatal tissue removed; striatal synaptosomes prepared; VMAT-2 immunoreactivity in P2, P3, S3 determined by Western blot analysis after GE; bands on blots as OD quantified by densitometry

147 of 303

148 of 303

Further Details (Pharmacological Data)

P2: whole synaptosomes; P3 and S3: synaptosomal membrane and cytoplasmic fractions, resp.; VMAT-2: vesicular monoamine transporter-2; OD: optical density; GE: gel electrophoresis; vehicle control

Results

title comp. decreased VMAT-2 immunoreactivity in S3, with maximum at 1 h and return to control level by 4 h, indicating decrease in accumulation of VMAT-2 protein in S3; title comp. had no effect in P2 or P3; fig.

Reference

Riddle, Evan L.; Hanson, Glen R.; Fleckenstein, Annette E.

European Journal of Pharmacology, 2007 , vol. 571, # 1 p. 25 - 28 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein expression; effect on

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

2 - 15 mg/kg

Method (Pharmacological Data)

1 h after title comp. dose, rats sacrificed; striatal tissue removed; synaptosomes prepared; VGLUT-1,-2, VAChT, VGAT protein immunoreactivity in P2 and S3 measured by Western blotting after gel electrophoresis; bands on blots measured by densitometry

Further Details (Pharmacological Data)

P2: whole synaptosomes; S3: cytoplasmic fraction; VGLUT, VAChT and VGAT: vesicular glutamate, acetylcholine and GABA transporters, resp.; vehicle control

Comment (Pharmacological Data)

No effect

Reference

Riddle, Evan L.; Hanson, Glen R.; Fleckenstein, Annette E.

European Journal of Pharmacology, 2007 , vol. 571, # 1 p. 25 - 28 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

locomotor behaviors; effect on

Species or TestSystem (Pharmacological Data)

DAT-KO mouse

Sex

male and female

Method (Pharmacological Data)

Experimental We report here that the pharmacologic inhibition of the rate-limiting enzyme of DA synthesis, TH, almost immediately depletes brain DA to undetectable levels in DAT-KO mice and induces a transient recapitulation of essentially all PD symptoms for up to 16 h. DA-deficient DAT-KO mice (DDD mice) thus represent an acute PD model that is useful for studying the efficacy of compounds that potentially can restore control of locomotion in the absence of any contribution of the dopaminergic system. By using this approach, we found that several amphetamine derivatives can counteract the behavioral manifestations of severe DA deficiency, suggesting that, in addition to well-known DA-mediated effects, amphetamine-like compounds can also affect motor functions in a DA- and DAT-independent manner. Materials and Methods Animals. DAT-KO mice were generated as previously described [11]. Animal care was in accordance with the Guide for Care and Use of Laboratory Animals (National Institutes of Health publication No.86523, Bethesda, Md., United States) with an approved protocol from the Duke University Institutional Animal Care and Use Committee. C57BL/6J3129Sv/J hybrid WT and DAT-KO mice, 3-5 mo old, of both sexes were used. None of animals used in these studies had the neurodegenerative phenotype sporadically observed in DAT-KO mice [60]. Drugs. Drugs or saline (0.9percent NaCl) were administered intraperitoneally (IP) or subcutaneously (SC) in a volume of 10 ml/kg. The drags were either from Sigma (St. Louis, Mo., United States) or supplied by the National Institute of Drug Abuse (NIDA). Drugs provided by the NIDA Drug Supply Program included: (+/-)-MDMA, (+)-MDMA, (+/-)-6-OH-MDA, (+/-)-MDA, (+/-)-MDE, (+)-MDE, (-)-MDE, and AFT (alpha-ethyl-tryptamine acetate). Neurochemical assessments. Striatal tissue contents of DA and frontal cortical tissue levels of NE were assessed using HPLC-EC (high performance liquid chromatography with electrochemical detection) as described [8]. In vivo microdialysis measurements of striatal extracellular DA levels in freely moving mice were performed at least 24 h after implantation of a microdialysis probe as described previously [50]. Dialysate samples were assayed for DA using HPLC-EC. Behavioral methods. Locomotor activity of littermate WT and DATKO mice was measured in an Omnitech CCDigiscan (Accuscan Instruments, Columbus, Ohio United States) activity monitor under bright illumination [83]. All behavioral experiments were performed between 10:00 AM and 5:00 PM. Activity was measured at 5-min intervals, To evaluate the effects of drugs on motor behaviors, mice were placed into activity monitor chambers (20.x.20 cm) for 30 min and then treated with αMT (250 mg/kg IP). A drug or combination of drugs were injected 1 h after αMT administration, and various parameters of locomotor activity were monitored for up to 3 h. In cumulative dosing experiments, animals were treated with increasing doses of drugs after a 1-h interval. For the akinesia test, the mouse is held by the tail so that it is standing on forelimbs only and moving on its own. The number of steps taken with both forelimbs was recorded during a 30-s trial [57]. The presence of catalepsy was determined and measured by placing the animal's forepaws on a horizontal wooden bar (0.7 cm in diameter), 4 cm above the tabletop. The time until the mouse removed both forepaws from the bar was recorded, with a maximum cut-off time of 3 min [53]. In the grasping test of muscular rigidity, the mouse is suspended by its forelimbs on a metal rod (diameter: 0.25 cm) positioned approximately 20 cm above the table. The time the animal remains on the rod (maximum 1 min) was noted [58]. To assess rigidity in a bracing task, the number of steps taken with each forelimb when the mouse is pushed sideways over a distance of 50 cm was recorded [57]. Tremor was scored visually in mice using the rating scale [54]: 0, no tremor; 1, occasional isolated twi

Results

Akinesia test: ~5-25 number of steps; at Catalepsy test: ~100-180sec; at Grasping test: ~9-28 seconds time spent on the rod of the title compound administered after 1h of αMT treatment; figure is given

Location

Page/Page column 3; 12-15; sheet 9

Reference

Caron, Marc G.; Sotnikova, Tatyana D.; Gainetdinov, Raul R.

Patent: US2007/27208 A1, 2007 ; Title/Abstract Full Text Show Details

149 of 303

Effect (Pharmacological Data)

prepulse inhibition

Species or TestSystem (Pharmacological Data)

Sprague-Dawley (SD) rat

Sex

male

Route of Application

subcutaneous

Method (Pharmacological Data)

METHODS AND MATERIALSPrepulse inhibition of the acoustic startle reflex (PPI) is an operational measure of sensorimotor gating that can be measured across many species. Deficits in PPI have been reported in patients with schizophrenia, leading to its use as a preclinical model of the disease. In rats, PPI is decreased in a manner homologous to that seen in schizophrenia following administration of certain psychotomimetic drugs (e.g. MK801 ; amphetamine). In our study we utilized MK801 , a non-competitive NMDA antagonist and d-Amphetamine, a non-selective dopamine agonist. MK801 (0.1 mg/kg sc, 10 min prior to test) and d-Amphetamine (4 mg.kg sc, 10 min prior to test) produced significant disruption across three prepulse intensities (5dB, 1OdB 15dB).Animals: Male Sprague-Dawley derived Rats (SD) weighing 200-250 g were group housed in standard bedding cages, allowed access to food and water ad libitum, and maintained on a 12-hour light dark cycle. All behavioral testing was performed during the light cycle. All studies were previously approved by the Institutional Animal Care and Use Committee, and performed in accordance to the Guide for the Care and Use of Laboratory Animals as adopted and promulgated by the National Institutes of Health.Test Compounds: The oxytocin agonist cpd A was dissolved in a 1percent Tween-80/1 percent DMSO/saline vehicle. MK801 (Sigma, St. Louis MO) was dissolved in 2percentTween- 80/saline. d-Amphetamine (Sigma, St. Louis MO) was dissolved in saline.Tesif EquipmentEach testing chamber (SR-LAB system, San Diego Instruments) consisted of aPlexiglas cylinder (8.8 cm in diameter) mounted on a frame and held in position by four metal pins to a base unit. Movement of the rat within the cylinder was detected by a piezoelectric accelerometer attached below the frame. A loudspeaker mounted 24 cm above the cylinder provided background white noise, acoustic noise bursts and acoustic prepulses. The entire apparatus was housed in a ventilated enclosure (39 x 38 x 56 cm). Presentation of acoustic pulse and prepulse stimuli were controlled by the SR-LAB software and interface system, which also digitized, rectified and recorded the responses from the accelerometer. Mean startle amplitude was determined by averaging 100, 1 ms readings taken from the beginning of the pulse stimulus onset. For calibration purposes, sound levels were measured with a Quest sound level meter, scale "A", with the microphone placed inside the Plexiglas cylinder.Test SessionsTest sessions began when the rats were placed in the startle chambers for a 5-min acclimation period with a 64 dB (A) background of white noise. After the acclimation period, rats were exposed to four types of stimuli. The startle-eliciting stimulus was a 20-ms broad band burst at a sound pressure level of 120 dB (A). Three different intensities of auditory prepulse stimuli were utilized. These consisted of a 69, 74 or 79 dB (A), 20-ms broad band burst which was presented 100-ms (onset to onset), prior to the startle pulse. These four trial types were presented against a constant 64 dB (A) background of white noise. A test session consisted of an initial pulse stimulus, followed by 15 sequences of the four stimulus types, presented in pseudorandom order, for a total of 61 trials. Inter-trial intervals averaged 15 s.Evaluation of ResultsStartle amplitude was defined as the mean value of pulse alone trials. To evaluate the effect of drug treatment on startle response, data from the pulse alone trials was analyzed using one-factor ANOVA with repeated measures (one-way randomized block design), followed by a least significant difference (LSD) post-hoc test (comparison was made to vehicle/disrupting agent control). Prepulse inhibition was defined as 100-[(startle amplitude on prepulse trials/startle amplitude on pulse alone trials) x 100]. Although data for gating at three different prepulse intensities was generated, an averaged gating score across all prepulse intensiti

Results

title compound shown perpulse inhibition effect (for more details see fig 5A)

Location

Page/Page column 31-33; 35

Reference

WYETH

Patent: WO2007/50353 A2, 2007 ; Title/Abstract Full Text Show Details

150 of 303

Effect (Pharmacological Data)

startle response; increasing of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley (SD) rat

Sex

male

Route of Application

subcutaneous

Method (Pharmacological Data)

METHODS AND MATERIALSPrepulse inhibition of the acoustic startle reflex (PPI) is an operational measure of sensorimotor gating that can be measured across many species. Deficits in PPI have been reported in patients with schizophrenia, leading to its use as a preclinical model of the disease. In rats, PPI is decreased in a manner homologous to that seen in schizophrenia following administration of certain psychotomimetic drugs (e.g. MK801 ; amphetamine). In our study we utilized MK801 , a non-competitive NMDA antagonist and d-Amphetamine, a non-selective dopamine agonist. MK801 (0.1 mg/kg sc, 10 min prior to test) and d-Amphetamine (4 mg.kg sc, 10 min prior to test) produced significant disruption across three prepulse intensities (5dB, 1OdB 15dB).Animals: Male Sprague-Dawley derived Rats (SD) weighing 200-250 g were group housed in standard bedding cages, allowed access to food and water ad libitum, and maintained on a 12-hour light dark cycle. All behavioral testing was performed during the light cycle. All studies were previously approved by the Institutional Animal Care and Use Committee, and performed in accordance to the Guide for the Care and Use of Laboratory Animals as adopted and promulgated by the National Institutes of Health.Test Compounds: The oxytocin agonist cpd A was dissolved in a 1percent Tween-80/1 percent DMSO/saline vehicle. MK801 (Sigma, St. Louis MO) was dissolved in 2percentTween- 80/saline. d-Amphetamine (Sigma, St. Louis MO) was dissolved in saline.Tesif EquipmentEach testing chamber (SR-LAB system, San Diego Instruments) consisted of aPlexiglas cylinder (8.8 cm in diameter) mounted on a frame and held in position by four metal pins to a base unit. Movement of the rat within the cylinder was detected by a piezoelectric accelerometer attached below the frame. A loudspeaker mounted 24 cm above the cylinder provided background white noise, acoustic noise bursts and acoustic prepulses. The entire apparatus was housed in a ventilated enclosure (39 x 38 x 56 cm). Presentation of acoustic pulse and prepulse stimuli were controlled by the SR-LAB software and interface system, which also digitized, rectified and recorded the responses from the accelerometer. Mean startle amplitude was determined by averaging 100, 1 ms readings taken from the beginning of the pulse stimulus onset. For calibration purposes, sound levels were measured with a Quest sound level meter, scale "A", with the microphone placed inside the Plexiglas cylinder.Test SessionsTest sessions began when the rats were placed in the startle chambers for a 5-min acclimation period with a 64 dB (A) background of white noise. After the acclimation period, rats were exposed to four types of stimuli. The startle-eliciting stimulus was a 20-ms broad band burst at a

sound pressure level of 120 dB (A). Three different intensities of auditory prepulse stimuli were utilized. These consisted of a 69, 74 or 79 dB (A), 20-ms broad band burst which was presented 100-ms (onset to onset), prior to the startle pulse. These four trial types were presented against a constant 64 dB (A) background of white noise. A test session consisted of an initial pulse stimulus, followed by 15 sequences of the four stimulus types, presented in pseudorandom order, for a total of 61 trials. Inter-trial intervals averaged 15 s.Evaluation of ResultsStartle amplitude was defined as the mean value of pulse alone trials. To evaluate the effect of drug treatment on startle response, data from the pulse alone trials was analyzed using one-factor ANOVA with repeated measures (one-way randomized block design), followed by a least significant difference (LSD) post-hoc test (comparison was made to vehicle/disrupting agent control). Prepulse inhibition was defined as 100-[(startle amplitude on prepulse trials/startle amplitude on pulse alone trials) x 100]. Although data for gating at three different prepulse intensities was generated, an averaged gating score across all prepulse intensiti Results

title compound administration increase of startle response in rats (for more details see fig 5B)

Location

Page/Page column 31-33; 35

Reference

WYETH

Patent: WO2007/50353 A2, 2007 ; Title/Abstract Full Text Show Details

151 of 303

152 of 303

153 of 303

Effect (Pharmacological Data)

monoamine transporter; interaction with

Species or TestSystem (Pharmacological Data)

rat caudate putamen crude vesicular fraction

Method (Pharmacological Data)

vesicular fraction incubated with title comp. and 2 nmol/l <3H>DHTBZ for 4 h at 25 deg C; rapid filtration; liquid scintillation counting

Further Details (Pharmacological Data)

DHTBZ: dihydrotetrabenazine; VMAT2: vesicular monoamine transporter type 2; IC50 for title comp. inhibition of <3H>DHTBZ binding

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

185 μmol/l

Reference

Partilla, John S.; Dempsey, Allison G.; Nagpal, Ameet S.; Blough, Bruce E.; Baumann, Michael H.; Rothman, Richard B.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 319, # 1 p. 237 - 246 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

monoamine transporter; interaction with

Species or TestSystem (Pharmacological Data)

rat caudate putamen crude vesicular fraction

Method (Pharmacological Data)

vesicular fraction incubated with title comp. and 60 nmol/l <3H>dopamine for 5 min at 25 deg C; rapid filtration; liquid scintillation counting

Further Details (Pharmacological Data)

DHTBZ: dihydrotetrabenazine; VMAT2: vesicular monoamine transporter type 2; IC50 for title comp. inhibition of <3H>dopamine uptake

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

3.27 μmol/l

Reference

Partilla, John S.; Dempsey, Allison G.; Nagpal, Ameet S.; Blough, Bruce E.; Baumann, Michael H.; Rothman, Richard B.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 319, # 1 p. 237 - 246 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transmitter releasing

Species or TestSystem (Pharmacological Data)

rat caudate putamen crude vesicular fraction

Method (Pharmacological

vesicular fraction preloaded with 60 nmol/l <3H>tyramine for 20 min at 25 deg C, incubated with title comp. for 2 min at 25 deg C; rapid filtration; liquid scintillation counting; <3H>tyramine release evaluated

Data)

154 of 303

155 of 303

156 of 303

Further Details (Pharmacological Data)

EC50 and EMAX for title comp. inhibition of <3H>tyramine release

Type (Pharmacological Data)

EC50

Value of Type (Pharmacological Data)

18.0 μmol/l

Results

EMAX = 111 percent

Reference

Partilla, John S.; Dempsey, Allison G.; Nagpal, Ameet S.; Blough, Bruce E.; Baumann, Michael H.; Rothman, Richard B.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 319, # 1 p. 237 - 246 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transmitter releasing

Species or TestSystem (Pharmacological Data)

rat caudate putamen crude vesicular fraction

Concentration (Pharmacological Data)

Ca. 1E-07 - 0.0001 mol/l

Method (Pharmacological Data)

vesicular fraction preloaded with 60 nmol/l <3H>dopamine for 20 min at 25 deg C, incubated with title comp. for 10 min at 25 deg C; rapid filtration; liquid scintillation counting; <3H>dopamine release evaluated

Further Details (Pharmacological Data)

EC50 and EMAX for title comp. inhibition of <3H>dopamine release

Type (Pharmacological Data)

EC50

Value of Type (Pharmacological Data)

2.5 μmol/l

Results

EMAX = 63.1 percent

Reference

Partilla, John S.; Dempsey, Allison G.; Nagpal, Ameet S.; Blough, Bruce E.; Baumann, Michael H.; Rothman, Richard B.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 319, # 1 p. 237 - 246 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; inhib. of

Species or TestSystem (Pharmacological Data)

recombinant cytochrome P450 2B6

Concentration (Pharmacological Data)

30 μmol/l

Method (Pharmacological Data)

enzyme (1.8 pmol/ml) mixed with buffer, MgCl2, bupropion; warmed to 37 deg C; aliquots delivered to PCR plate wells (37 deg C); title comp. added; NADPH added; incub. (37 deg C, 10 min); HB detd. by HPLC/MS/MS; result expressed as percent of control activity

Further Details (Pharmacological Data)

HB: hydroxybupropion; control: mixture of water and CH3CN, or DMSO; positive control: 2-phenyl-2-(1-piperidinyl)propane; bupropion hydroxylase activity used as marker activity for CYP2B6 activity; enzyme expressed in Sf9 cells used

Results

title comp. inhibited the recombinant CYP2B6-catalyzed hydroxylation of bupropion; percent of control activity was 78.4 (for positive control: 13.1 μmol/l); table

Reference

Walsky, Robert L.; Astuccio, Angela V.; Obach, R. Scott

Journal of Clinical Pharmacology, 2006 , vol. 46, # 12 p. 1426 - 1438 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transmitter releasing

Species or Test-

Sprague-Dawley rat

System (Pharmacological Data)

157 of 303

158 of 303

Sex

male

Route of Application

intravenous

Concentration (Pharmacological Data)

0.3 - 1 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. sulfate was used, dissolved in saline and administered as bolus injection

Method (Pharmacological Data)

rats administered with title comp.; blood collected every 15 min pre-dosing and at 15-min intervals for 90 min post-dosing; dialyzed; dialysates assayed for 5-hydroxytryptamine and 5-hydroxyindoleacetic acid using HPLC with electrochemical detection

Further Details (Pharmacological Data)

control: saline; ref.: fluoxetine

Results

title comp. elevated 5-hydroxytryptamine 5-fold after 1.0 mg/kg; title comp. treatment did not affect plasma 5-hydroxyindoleacetic acid levels; diagram

Reference

Zolkowska, Dorota; Rothman, Richard B.; Baumann, Michael H.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 2 p. 604 - 610 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transmitter releasing

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat blood

Sex

male

Concentration (Pharmacological Data)

0.3 - 33 μmol/l

Kind of Dosing (Pharmacological Data)

title comp. sulfate was used, dissolved in saline

Method (Pharmacological Data)

title comp. added to blood samples; microdialysis probes placed into blood samples; dialysate efflux collected for 15 min; assayed for 5hydroxytryptamine levels

Further Details (Pharmacological Data)

control: saline; ref.: fluoxetine

Results

title comp. increased plasma 5-hydroxytryptamine levels, producing 4- and 44-fold elevations when administered at concentrations of 3 and 33 μmol/l, resp.; diagram

Reference

Zolkowska, Dorota; Rothman, Richard B.; Baumann, Michael H.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 2 p. 604 - 610 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

nasal

Method (Pharmacological Data)

Example 11. Decreased intranasal bioavailability of L-lysine-Table 20. Pharmacokinetic parameters of d-amphetamine vs. L-lysine- ^-amphetamine hydrochloride by IN administrationb. Intranasal bioavailability of L-lysine-d-amphetamine dimesylate[0202] The process of part a was repeated using Llysine-ef-amphetamine mesylate salt:Table 21. Pharmacokinetic parameters of ^-amphetamine vs. L-lysine-^-amphetamine mesylate salt by IN administration[0203] This example illustrates that when lysine is conjugated to the active agent ^-amphetamine, the bioavailability by the intranasal route is substantially decreased, thereby diminishing the ability to abuse the drug by this route.

Results

at 3 mg/kg title compound AUC at 0-1.5 h= 573-727 ng.H/ml; Cmax= 1114-1377 ng/ml; figure is given

Location

Page/Page column 3; 44-45; 17/70

Reference

NEW RIVER PHARMACEUTICALS INC.

Patent: WO2006/121552 A2, 2006 ;

Title/Abstract Full Text Show Details

159 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intravenous

Method (Pharmacological Data)

Example 12. Intravenous bioavailability of amphetamine vs. L-lysine-^-amphetamine dimesylate[0204] Male Sprague-Dawley rats were dosed by intravenous tail vein injection with 1.5 mg/kg of ^/-amphetamine or L-lysine- J-amphetamine containing the equivalent amount of amphetamine. As observed with IN dosing, the conjugate did not release a significant amount of J-amphetamine. Mean (n=4) plasma concentration curves of amphetamine vs. L- lysine-J-amphetamine are shown in FIG. 19. Pharmacokinetic parameters for IV administration of L-lysine-Table 22. Pharmacokinetic parameters of d-amphetamine vs. L-lysine-tZ-amphetamine by IV administration[0205] This example illustrates that when lysine is conjugated to the active agent amphetamine, the bioavailability of amphetamine by the intravenous route is substantially decreased, thereby diminishing the ability to abuse the drug by this route.

Results

at 1.5-3 mg/kg title compound AUC at 0-24 h = 546.7-1032 ng.H/ml; Cmax= 169-1962.9 ng/ml; Tmax= 0.083 h; figure is given

Location

Page/Page column 3; 45-46; 19/70

Reference

NEW RIVER PHARMACEUTICALS INC.

Patent: WO2006/121552 A2, 2006 ; Title/Abstract Full Text Show Details

160 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

rat

Route of Application

peroral

Method (Pharmacological Data)

Example 13. Oral bioavailability of L-lysine-J-amphetamine dimesylate compared to d- amphetamine at escalating doses[0206] The fraction of intact Llysine-e?-amphetamine absorbed following oral administration in rats increased non-linearly in proportion to escalating doses from 1.5 to 12 mg/kg (FIG. 21 - FIG. 25). The fraction absorbed at 1.5 mg/kg was only 2.6 percent whereas it increased to 24.6 percent by 12 mg/kg. The fraction absorbed fell to 9.3 percent at the high dose of 60 mg/kg. Tmax ranged from 0.25 to 3 hours, and peak concentrations occurred earlier for L- lysine-J-amphetamine than for J-amphetamine. L-lysine-J-amphetamine was cleared more rapidly than ^-amphetamine with nearly undetectable concentrations by 8 hours at the lowest dose.[0207] The bioavailability (AUC) of J-amphetamine from each drug administered was approximately equivalent at low doses. Tmax for rfamphetamine from L-lysine-d-amphetamine ranged from 1.5 to 5 hours as compared to 0.5 to 1.5 following administration of ^/-amphetamine sulfate. The difference in Tmaχ was greater at higher doses. Cmax of d-amphetamine from L-lysine-J-amphetamine was reduced by approximately half as compared to the Cmax of ^-amphetamine from ^-amphetamine sulfate administration at doses of 1.5 to 6 mg/kg, doses approximating therapeutic human equivalent doses (HEDs). Thus, at therapeutic doses, the pharmacokinetics of ^-amphetamine from L-lysine-[0208] HEDs are defined as the equivalent dose for a 60 kg person in accordance to the body surface area of the animal model. The adjustment factor for rats is 6.2. The HED for a rat dose of 1.5 mg/kg of cf-amphetamine, for example, is equivalent to 1.5/6.2 X OO =1 14.52 d- amphetamine base; which is equivalent to 14.52/.7284 = 19.9 mg ^/-amphetamine sulfate, when adjusted for the salt content.Table 23. Human Equivalent Doses (HEDs) of cf-amphetamine sulfate[0209] At suprapharmacological doses (12 and 60 mg/kg), Cmax was reduced by 73 and 84 percent, respectively, as compared to cf-amphetamine sulfate. For these high doses, the AUCs for d-amphetamine from L-lysine-nf reduced by 76percent at the highest dose (60 mg/kg). At 60 mg/kg, the levels of ^amphetamine from [0211] The results suggest that the capacity for clearance of J-amphetamine when delivered as the sulfate salt becomes saturated at the higher doses whereas the gradual hydrolysis of L- lysine-f-amphetamine precludes saturation of rf-amphetamine elimination at higher doses. The difference in proportionality of dose to bioavailability (Cmax and AUC) for d- amphetamine and L-lysine-^-amphetamine is illustrated in FIG. 26 - FIG. 28. The pharmacokinetic properties of L-lysine-d-amphetamine as compared to ^-amphetamine at the higher doses decrease

Results

at 1.5-60 mg/kg dose of title compound Cmax = 142.2-13735 ng/ml; Tmax=0.25-1.5 h; AUC at 0-8 h= 486-14281 ng.h/ml; figures are given

Location

Page/Page column 5; 46-55; 21/70-25/70; 31/70-34/70

Reference

NEW RIVER PHARMACEUTICALS INC.

Patent: WO2006/121552 A2, 2006 ; Title/Abstract Full Text Show Details

161 of 303

Effect (Pharmacological Data)

horizontal locomotor activity (HLA); effect on

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

peroral

Method (Pharmacological

Example 18. Pharmacodynamic (locomotor) response to amphetamine vs. L-lysine-fif-amphetamine diHCl by oral administration[0238] Male SpragueDawley rats were provided water ad libitum, fasted overnight, and dosed by oral gavage with 6 mg/kg of amphetamine or L-lysine-J-amphetamine

Data)

containing the equivalent amount of J-amphetamine. Horizontal locomotor activity (HLA) was recorded during the light cycle using photocell activity chambers (San Diego Instruments). Total counts were recorded every 12 minutes for the duration of the test. Rats were monitored in three separate experiments for 5, 8, and 12 hours, respectively. Time vs. HLA counts for d- amphetamine vs. L-lysine-d-amphetamine is shown in FIG. 45 and FIG. 46. In each EPO experiment the time until peak activity was delayed, and the pharmacodynamic effect was evident for an extended period of time for Llysine-^-amphetamine as compared to d- amphetamine. The total activity counts for HLA of Lys-Amp dosed rats were increased (11- 41percent) over those induced by ^/-amphetamine in all three experiments.Table 49. Locomotor activity of rats orally administered J-amphetamine vs. L-lysine- famphetamine (5 h)Table 50. Locomotor activity of rats orally administered ^-amphetamine vs. L-lysine- <f-amphetamine (12 h)

Results

total activity count = 515-6622 at 5-12 hours; total activity counts above baseline is 0-5686 at 5-12 hours; peak of activity (counts per 0.2 h) = 223291 at 5-12 hours; time of peak (counts per 0.2 h) = 0.6; time of last count above 200 per 0.2 h = 2.6-6.4 h; figures are given

Location

Page/Page column 6; 66-67; 45/70-46/70

Reference

NEW RIVER PHARMACEUTICALS INC.

Patent: WO2006/121552 A2, 2006 ; Title/Abstract Full Text Show Details

162 of 303

Effect (Pharmacological Data)

horizontal locomotor activity (HLA); effect on

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

nasal

Method (Pharmacological Data)

Example 18. Pharmacodynamic (locomotor) response to amphetamine vs. L-lysine-fif-amphetamine diHCl by oral administration[0238] Male SpragueDawley rats were provided water ad libitum, fasted overnight, and dosed by oral gavage with 6 mg/kg of amphetamine or L-lysine-J-amphetamine containing the equivalent amount of J-amphetamine. Horizontal locomotor activity (HLA) was recorded during the light cycle using photocell activity chambers (San Diego Instruments). Total counts were recorded every 12 minutes for the duration of the test. Rats were monitored in three separate experiments for 5, 8, and 12 hours, respectively. Time vs. HLA counts for d- amphetamine vs. L-lysine-d-amphetamine is shown in FIG. 45 and FIG. 46. In each EPO experiment the time until peak activity was delayed, and the pharmacodynamic effect was evident for an extended period of time for Llysine-^-amphetamine as compared to d- amphetamine. The total activity counts for HLA of Lys-Amp dosed rats were increased (11- 41percent) over those induced by ^/-amphetamine in all three experiments.Table 49. Locomotor activity of rats orally administered J-amphetamine vs. L-lysine- famphetamine (5 h)Table 50. Locomotor activity of rats orally administered ^-amphetamine vs. L-lysine- <f-amphetamine (12 h)

Results

total activity count = 858 at 5-12 hours; total activity counts above baseline is 686 at 5-12 hours; figures are given

Location

Page/Page column 6; 66-67; 47/70-48/70

Reference

NEW RIVER PHARMACEUTICALS INC.

Patent: WO2006/121552 A2, 2006 ; Title/Abstract Full Text Show Details

163 of 303

Effect (Pharmacological Data)

horizontal locomotor activity (HLA); effect on

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intravenous

Method (Pharmacological Data)

Example 20. Pharmacodynamic response to J-amphetamine vs. L-lysine-J-amphetamine diHCl by intravenous administration[0240] Male SpragueDawley rats were dosed by intravenous administration with J-amphetamine or L-lysine-J-amphetamine (1.0 mg/kg). The activity expressed as total activity counts over a three hour period of time is shown in FIG. 49. The activity induced by L-lysine- ^-amphetamine was substantially decreased, and time to peak activity was delayed. The increase in activity over baseline of L-lysine-Table 52. Total activity counts after intravenous administration of ^amphetamine vs. L-lysine-J-amphetamine

Results

total activity count = 1659 at 3 hours; total activity counts above baseline is 1355 at 3 hours; figures are given

Location

Page/Page column 6; 68-69; 49/70

Reference

NEW RIVER PHARMACEUTICALS INC.

Patent: WO2006/121552 A2, 2006 ; Title/Abstract Full Text Show Details

164 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

peroral

Method (Pharmacological Data)

Example 25. Bioavailability of various peptide amphetamine conjugates (HCl salts') administered by oral, intranasal, and intravenous routes[0262] Oral administration: Male Sprague-Dawley rats were provided water ad libitum, fasted overnight, and dosed by oral gavage with amphetamine or amino acidamphetamine conjugates containing the equivalent amount of amphetamine.[0263] Intranasal administration: Male Sprague-Dawley rats were dosed by intranasal administration with amphetamine or Iy sine-amphetamine (1.8 mg/kg).[0264] The relative in vivo performance of various amino acidamphetamine compounds is shown in FIG. 50 - FIG. 58 and summarized in Table 61. Intranasal bioavailability of amphetamine from Ser-Amp was decreased to some degree relative to free amphetamine.However, this compound was not bioequivalent with amphetamine by the oral route of administration. Phenylalanine was bioequivalent with amphetamine by the oral route of administration, however, little or no decrease in bioavailability by parenteral routes of administration was observed. Gly3-Amp had nearly equal bioavailability (90percent) by the oral EPO route accompanied by a decrease in Cmax (74percent). Additionally, Gly3-Amp showed a decrease in bioavailability relative to amphetamine by intranasal and intravenous routes.Table 61. Percent bioavailability of amino acid amphetamine compounds administered by oral, intranasal, or intravenous routes EPO [0265] Several single amino acid amphetamine conjugates had comparable oral bioavailability (80-100percent) to d-amphetamine. Lys, GIy, and Phe conjugates, for example, all demonstrated similar oral bioavailability to the parent drug. Dipeptide prodrugs generally showed lower bioavailability than the respective amino acid analogs, and tripeptide compounds displayed no discernable trend. Several amino acid amphetamine conjugates had decreased parenteral bioavailability. Preferred conjugates, such as Lys- Amp, exhibit both oral bioavailability comparable to c?-amphetamine and decreased parenteral bioavailability compared to ^/-amphetamine.[0266] Male Sprague-Dawley rats were provided water ad libitum, fasted overnight, and dosed by oral gavage with amphetamine conjugate or ^-amphetamine sulfate. All doses contained equivalent amounts of fif-amphetamine base. Plasma J-amphetamine concentrations were measured by ELISA (Amphetamine Ultra, 109319, Neogen, Corporation, Lexington, KY). The assay is specific for ?-amphetamine with only minimal reactivity (0.6percent) of the major Example 28. Decreased intravenous bioavailability (AUC and Crnm) of J-amphetamine conjugates[0268] Male Sprague-Dawley rats were provided water ad libitum, and doses were administered by intravenous tail vein injection of 0.1 ml of water containing amphetamine conjugate or of-amphetamine sulfate. All doses contained equivalent amounts of d- amphetamine base. Plasma (^-amphetamine concentrations were measured by ELISA (Amphetamine Ultra, 109319, Neogen, Corporation,

Results

percent AUC =100 percent; percentCmax = 100

Location

Page/Page column 7; 76-79; 50/70-58/70

Reference

NEW RIVER PHARMACEUTICALS INC.

Patent: WO2006/121552 A2, 2006 ; Title/Abstract Full Text Show Details

165 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

nasal

Method (Pharmacological Data)

Example 25. Bioavailability of various peptide amphetamine conjugates (HCl salts') administered by oral, intranasal, and intravenous routes[0262] Oral administration: Male Sprague-Dawley rats were provided water ad libitum, fasted overnight, and dosed by oral gavage with amphetamine or amino acidamphetamine conjugates containing the equivalent amount of amphetamine.[0263] Intranasal administration: Male Sprague-Dawley rats were dosed by intranasal administration with amphetamine or Iy sine-amphetamine (1.8 mg/kg).[0264] The relative in vivo performance of various amino acidamphetamine compounds is shown in FIG. 50 - FIG. 58 and summarized in Table 61. Intranasal bioavailability of amphetamine from Ser-Amp was decreased to some degree relative to free amphetamine.However, this compound was not bioequivalent with amphetamine by the oral route of administration. Phenylalanine was bioequivalent with amphetamine by the oral route of administration, however, little or no decrease in bioavailability by parenteral routes of administration was observed. Gly3-Amp had nearly equal bioavailability (90percent) by the oral EPO route accompanied by a decrease in Cmax (74percent). Additionally, Gly3-Amp showed a decrease in bioavailability relative to amphetamine by intranasal and intravenous routes.Table 61. Percent bioavailability of amino acid amphetamine compounds administered by oral, intranasal, or intravenous routes EPO [0265] Several single amino acid amphetamine conjugates had comparable oral bioavailability (80-100percent) to d-amphetamine. Lys, GIy, and Phe conjugates, for example, all demonstrated similar oral bioavailability to the parent drug. Dipeptide prodrugs generally showed lower bioavailability than the respective amino acid analogs, and tripeptide compounds displayed no discernable trend. Several amino acid amphetamine conjugates had decreased parenteral bioavailability. Preferred conjugates, such as Lys- Amp, exhibit both oral bioavailability comparable to c?-amphetamine and decreased parenteral bioavailability compared to ^/-amphetamine.[0266] Male Sprague-Dawley rats were provided water ad libitum, fasted overnight, and dosed by oral gavage with amphetamine conjugate or ^-amphetamine sulfate. All doses contained equivalent amounts of fif-amphetamine base. Plasma J-amphetamine concentrations were measured by ELISA (Amphetamine Ultra, 109319, Neogen, Corporation, Lexington, KY). The assay is specific for ?-amphetamine with only minimal reactivity (0.6percent) of the major Example 28. Decreased intravenous bioavailability (AUC and Crnm) of J-amphetamine conjugates[0268] Male Sprague-Dawley rats were provided water ad libitum, and doses were administered by intravenous tail vein injection of 0.1 ml of water containing amphetamine conjugate or of-amphetamine sulfate. All doses contained equivalent amounts of d- amphetamine base. Plasma (^-amphetamine concentrations were measured by ELISA (Amphetamine Ultra, 109319, Neogen, Corporation,

Results

percent AUC =100 percent; percentCmax = 100

Location

Page/Page column 7; 76-79; 50/70-58/70

Reference

NEW RIVER PHARMACEUTICALS INC.

Patent: WO2006/121552 A2, 2006 ; Title/Abstract Full Text Show Details

166 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intravenous

Method (Pharmacological Data)

Example 25. Bioavailability of various peptide amphetamine conjugates (HCl salts') administered by oral, intranasal, and intravenous routes[0262] Oral administration: Male Sprague-Dawley rats were provided water ad libitum, fasted overnight, and dosed by oral gavage with amphetamine or amino acidamphetamine conjugates containing the equivalent amount of amphetamine.[0263] Intranasal administration: Male Sprague-Dawley rats were dosed by intranasal administration with amphetamine or Iy sine-amphetamine (1.8 mg/kg).[0264] The relative in vivo performance of various amino acidamphetamine compounds is shown in FIG. 50 - FIG. 58 and summarized in Table 61. Intranasal bioavailability of amphetamine from Ser-Amp was decreased to some degree relative to free amphetamine.However, this compound was not bioequivalent with amphetamine by the oral route of administration. Phenylalanine was bioequivalent with amphetamine by the oral route of administration, however, little or no decrease in bioavailability by parenteral routes of administration was observed. Gly3-Amp had nearly equal bioavailability (90percent) by the oral EPO route accompanied by a decrease in Cmax (74percent). Additionally, Gly3-Amp showed a decrease in bioavailability relative to amphetamine by intranasal and intravenous routes.Table 61. Percent bioavailability of amino acid amphetamine compounds administered by oral, intranasal, or intravenous routes EPO [0265] Several single amino acid amphetamine conjugates had comparable oral bioavailability (80-100percent) to d-amphetamine. Lys, GIy, and Phe conjugates, for example, all demonstrated similar oral bioavailability to the parent drug. Dipeptide prodrugs generally showed lower bioavailability than the respective amino acid analogs, and tripeptide compounds displayed no discernable trend. Several amino acid amphetamine conjugates had decreased parenteral bioavailability. Preferred conjugates, such as Lys- Amp, exhibit both oral bioavailability comparable to c?-amphetamine and decreased parenteral bioavailability compared to ^/-amphetamine.[0266] Male Sprague-Dawley rats were provided water ad libitum, fasted overnight, and dosed by oral gavage with amphetamine conjugate or ^-amphetamine sulfate. All doses contained equivalent amounts of fif-amphetamine base. Plasma J-amphetamine concentrations were measured by ELISA (Amphetamine Ultra, 109319, Neogen, Corporation, Lexington, KY). The assay is specific for ?-amphetamine with only minimal reactivity (0.6percent) of the major Example 28. Decreased intravenous bioavailability (AUC and Crnm) of J-amphetamine conjugates[0268] Male Sprague-Dawley rats were provided water ad libitum, and doses were administered by intravenous tail vein injection of 0.1 ml of water containing amphetamine conjugate or of-amphetamine sulfate. All doses contained equivalent amounts of d- amphetamine base. Plasma (^-amphetamine concentrations were measured by ELISA (Amphetamine Ultra, 109319, Neogen, Corporation,

Results

percent AUC =100 percent; percentCmax = 100

Location

Page/Page column 7; 76-79; 50/70-58/70

Reference

NEW RIVER PHARMACEUTICALS INC.

Patent: WO2006/121552 A2, 2006 ; Title/Abstract Full Text Show Details

167 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

human

Route of Application

peroral

Method (Pharmacological Data)

Example 32. Clinical pharmacokinetic evaluation and oral bioavailability of L-lvsine-^-amphetamine dimesylate 70 mg capsules administered to healthy adults under fasting conditions for 7 days[0291] In this open-label, single-arm study, healthy adults between the ages of 18 to 55 years were administered 70 mg of L-lysine-d-amphetamine dimesylate with 8 ounces of water once daily (7 am) for 7 consecutive days. Patients fasted for at least 10 hours before and 4 hours after final dosing. Venous blood samples (7 mL) were drawn into EDTA vacutainers both before medication dosing on days 0, 1, 6, and 7 (in the morning) and at 16 time points (hours 0.5, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 10, 12, 16, 24, 48, and 72) after final dosing on day 7. Immediately after sample collection, vacutainer tubes were centrifuged at 3000 rpm at 40C for 10 minutes; within 1 hour of collection, they were stored at -20°C. Plasma samples were analyzed for L-lysine-d-amphetamine and d-amphetamine using a validated LC/MS/MS method.[0292] By dose 5, ^amphetamine reached steady state. After dose 7, mean AUC0-24 was 1113 ng.h/mL, mean AUCo-.infin. was 1453 ng.h/mL, mean Cmax was 90.1 ng.h/mL, and mean Tmax was 3.68 hours. See Table 63 and FIG. 60. In comparison, extended-release amphetamine salts exhibit a Tmax of 5.8 hours and AUCo-.infin. 853 ng.h/mL after an overnight fast. J.F. Auiler et al., "Effect of food on early drug exposure from extended-release stimulants: results from the Concerta, Adderall XR Food Evaluation (CAFE) study," Curr Med Res Opin 18 : 311 -316 at 313 (2002).[0293] Intact L-lysine-J-amphetamine was rapidly converted to ^/-amphetamine. After dose 7, mean AUCo-24 was 60.66 ng.h/mL, and mean AUCo-.infin.was 61.06 ng.h/mL. See Table 63 and FIG. 60. In addition, mean Cmax was 47.9 ng.h/mL, and mean Tmax was 1.14 hours for intact L-lysine-J-amρhetamine. L-lysine-rf-amphetamine was completely eliminated within approximately 6 hours.[0294] There were no gender differences in systemic exposure to ^-amphetamine, though Cmax was 12percent higher in men after normalization by body weight.[0295] The multidose pharmacokinetic profile of J-amphetamine released from the prodrug L-lysine-d'-amphetamine is consistent with extended-release properties. The adverse events that occurred in this setting are consistent with other stimulants and suggest that suggest that L-lysine-Table 63. Steady-state pharmacokinetics parameters (n=l 1)

Results

Cmax=90.1 ng/ml; Cmin=18.2 ng/ml; Tmax=3.68 h; T1/2=10.08 h; AUCat 0-24 h=1113 ng.H/ml; AUC 0-infinity=1453 ng.H/ml; AUC 0-T=1371 ng.H/ml; FI = 163.55percent

Location

Page/Page column 82-83

Reference

NEW RIVER PHARMACEUTICALS INC.

Patent: WO2006/121552 A2, 2006 ; Title/Abstract Full Text Show Details

168 of 303

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

human

Route of Application

peroral Example 34. Clinical pharmacokinetic evaluation and oral bioavailability of L-lysine-cj- amphetamine dimesylate[0299] In pediatric patients (6-12 yrs)

Method (Pharmacological Data)

with ADHD, the Tmax of ^-amphetamine was approximately 3.5 hours following single-dose oral administration of L-lysine-^-amphetamine dimesylate either 30 mg, 50 mg, or 70 mg after a 8-hour overnight fast. See FIG. 65. The Tmax of L-lysine-d-amphetamine dimesylate was approximately 1 hour. Linear pharmacokinetics of ^-amphetamine after single-dose oral administration of L- lysine-dr-amphetamine dimesylate was established over the dose range of 30 mg to 70 mg in children.Table 72. Pharmacokinetic parameters of ^/-amphetamine and L-lysine-max by approximately 1 hour (from 3.78 hrs at fasted state to 4.72 hrs after a high fat meal). After an 8-hour fast, the extent of absorption of J-amphetamine following oral administration of Llysine-J-amphetamine dimesylate in solution and as intact capsules was equivalent. EPO [0302] There were no apparent differences between males and females in exposure as measured by dose-normalized Cmax and AUC although the range of values in children was higher than that in adults. This is a consequence of the significant correlation between dose- normalized Cmax and AUC and body weight and thus the differences are due to the higher doses in mg/kg administered to children. There were no apparent differences in \\a between male and female subjects nor were there any apparent relationships between \\\\n and either age or body weight.[0303] Exemplary results of clinical pharmacokinetic evaluation are presented in FIG. 66 (AUC), FIG. 67 (Cmax), and FIG. 68 (Tmax).

Results

at 30-70 mg Cmax = 53.2 -134 ng/ml; Tmax = 3.41 to 3.58 h; AUC = 845-2457 ng.H/ml; T1/2 = 8.61 -8.90 h; figures are given

Location

Page/Page column 8; 99-100; 65/70

Reference

NEW RIVER PHARMACEUTICALS INC.

Patent: WO2006/121552 A2, 2006 ; Title/Abstract Full Text Show Details

169 of 303

170 of 303

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

COS-7 cells

Concentration (Pharmacological Data)

Ca. 1E-09 - 0.001 mol/l

Method (Pharmacological Data)

ability of title comp. to inhibit <3H>CFT binding to DAT studied; cells incubated with title comp. and <3H>CFT (2 nmol/l) for 2 h at 4 deg C in KRH buffer, pH 7.4; radioactivity measured by liquid scintillation counting

Further Details (Pharmacological Data)

cells expressing wild-type dopamine transporter; KRH: Krebs-Ringer-Henseleit; CFT: carboxyfluorotropane; DAT: dopamine transporter; IC50 value of low affinity site

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

66006 nmol/l

Reference

Dar, Dalit E.; Mayo, Cheryl; Uhl, George R.

Biochemical Pharmacology, 2005 , vol. 70, # 3 p. 461 - 469 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

COS-7 cells

Concentration (Pharmacological Data)

Ca. 1E-09 - 0.001 mol/l

Method (Pharmacological Data)

ability of title comp. to inhibit <3H>CFT binding to DAT studied; cells incubated with title comp. and <3H>CFT (2 nmol/l) for 2 h at 4 deg C in KRH buffer, pH 7.4; radioactivity measured by liquid scintillation counting

Further Details (Pharmacological Data)

cells expressing wild-type dopamine transporter; KRH: Krebs-Ringer-Henseleit; CFT: carboxyfluorotropane; DAT: dopamine transporter; Ki value of high affinity site

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

442 nmol/l

Reference

Dar, Dalit E.; Mayo, Cheryl; Uhl, George R.

Biochemical Pharmacology, 2005 , vol. 70, # 3 p. 461 - 469 Title/Abstract Full Text View citing articles Show Details

171 of 303

172 of 303

173 of 303

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

COS-7 cells

Concentration (Pharmacological Data)

Ca. 1E-09 - 0.001 mol/l

Method (Pharmacological Data)

ability of title comp. to inhibit <3H>CFT binding to DAT studied; cells incubated with title comp. and <3H>CFT (2 nmol/l) for 2 h at 4 deg C in KRH buffer, pH 7.4; radioactivity measured by liquid scintillation counting

Further Details (Pharmacological Data)

cells expressing D79A mutant type dopamine transporter (aspartic acid 79 mutated to alanine); KRH: Krebs-Ringer-Henseleit; CFT: carboxyfluorotropane; DAT: dopamine transporter

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

70523 nmol/l

Reference

Dar, Dalit E.; Mayo, Cheryl; Uhl, George R.

Biochemical Pharmacology, 2005 , vol. 70, # 3 p. 461 - 469 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

COS-7 cells

Concentration (Pharmacological Data)

Ca. 1E-09 - 0.001 mol/l

Method (Pharmacological Data)

ability of title comp. to inhibit <3H>CFT binding to DAT studied; cells incubated with title comp. and <3H>CFT (2 nmol/l) for 2 h at 4 deg C in KRH buffer, pH 7.4; radioactivity measured by liquid scintillation counting

Further Details (Pharmacological Data)

cells expressing Y251A mutant type dopamine transporter (tyrosine 251 mutated to alanine); KRH: Krebs-Ringer-Henseleit; CFT: carboxyfluorotropane; DAT: dopamine transporter

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

47517 nmol/l

Reference

Dar, Dalit E.; Mayo, Cheryl; Uhl, George R.

Biochemical Pharmacology, 2005 , vol. 70, # 3 p. 461 - 469 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

COS-7 cells

Concentration (Pharmacological Data)

Ca. 1E-09 - 0.001 mol/l

Method (Pharmacological Data)

ability of title comp. to inhibit <3H>CFT binding to DAT studied; cells incubated with title comp. and <3H>CFT (2 nmol/l) for 2 h at 4 deg C in KRH buffer, pH 7.4; radioactivity measured by liquid scintillation counting

Further Details (Pharmacological Data)

cells expressing Y273A mutant type dopamine transporter (tyrosine 273 mutated to alanine); KRH: Krebs-Ringer-Henseleit; CFT: carboxyfluorotropane; DAT: dopamine transporter

Type

IC50

(Pharmacological Data)

174 of 303

175 of 303

176 of 303

Value of Type (Pharmacological Data)

62430 nmol/l

Reference

Dar, Dalit E.; Mayo, Cheryl; Uhl, George R.

Biochemical Pharmacology, 2005 , vol. 70, # 3 p. 461 - 469 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

COS-7 cells

Concentration (Pharmacological Data)

Ca. 1E-09 - 0.001 mol/l

Method (Pharmacological Data)

ability of title comp. to inhibit <3H>CFT binding to DAT studied; cells incubated with title comp. and <3H>CFT (2 nmol/l) for 2 h at 4 deg C in KRH buffer, pH 7.4; radioactivity measured by liquid scintillation counting

Further Details (Pharmacological Data)

cells expressing S356,359A mutant type dopamine transporter (serines 356 and 359 mutated to alanine); KRH: Krebs-Ringer-Henseleit; CFT: carboxyfluorotropane; DAT: dopamine transporter

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

20663 nmol/l

Reference

Dar, Dalit E.; Mayo, Cheryl; Uhl, George R.

Biochemical Pharmacology, 2005 , vol. 70, # 3 p. 461 - 469 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transport; inhibition of

Species or TestSystem (Pharmacological Data)

COS-7 cells

Concentration (Pharmacological Data)

Ca. 1E-08 - 0.0001 mol/l

Method (Pharmacological Data)

ability of title comp. to inhibit <3H>dopamine uptake studied; cells incubated with title comp. and <3H>dopamine for 5 min at 37 deg C in KRH buffer, pH 7.4; radioactivity measured by liquid scintillation counting

Further Details (Pharmacological Data)

cells expressing wild-type dopamine transporter; KRH: Krebs-Ringer-Henseleit

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

424.9 nmol/l

Results

dose-dependent inhibition (figure)

Reference

Dar, Dalit E.; Mayo, Cheryl; Uhl, George R.

Biochemical Pharmacology, 2005 , vol. 70, # 3 p. 461 - 469 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transport; inhibition of

Species or TestSystem (Pharmacological Data)

COS-7 cells

177 of 303

178 of 303

Concentration (Pharmacological Data)

Ca. 1E-08 - 0.0001 mol/l

Method (Pharmacological Data)

ability of title comp. to inhibit <3H>dopamine uptake studied; cells incubated with title comp. and <3H>dopamine for 5 min at 37 deg C in KRH buffer, pH 7.4; radioactivity measured by liquid scintillation counting

Further Details (Pharmacological Data)

cells expressing Y251A mutant type dopamine transporter (tyrosine 251 mutated to alanine); KRH: Krebs-Ringer-Henseleit

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

402.9 nmol/l

Results

dose-dependent inhibition (figure)

Reference

Dar, Dalit E.; Mayo, Cheryl; Uhl, George R.

Biochemical Pharmacology, 2005 , vol. 70, # 3 p. 461 - 469 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transport; inhibition of

Species or TestSystem (Pharmacological Data)

COS-7 cells

Concentration (Pharmacological Data)

Ca. 1E-08 - 0.0001 mol/l

Method (Pharmacological Data)

ability of title comp. to inhibit <3H>dopamine uptake studied; cells incubated with title comp. and <3H>dopamine for 5 min at 37 deg C in KRH buffer, pH 7.4; radioactivity measured by liquid scintillation counting

Further Details (Pharmacological Data)

cells expressing Y273A mutant type dopamine transporter (tyrosine 273 mutated to alanine); KRH: Krebs-Ringer-Henseleit

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

703.7 nmol/l

Results

dose-dependent inhibition (figure)

Reference

Dar, Dalit E.; Mayo, Cheryl; Uhl, George R.

Biochemical Pharmacology, 2005 , vol. 70, # 3 p. 461 - 469 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transport; inhibition of

Species or TestSystem (Pharmacological Data)

COS-7 cells

Concentration (Pharmacological Data)

Ca. 1E-08 - 0.0001 mol/l

Method (Pharmacological Data)

ability of title comp. to inhibit <3H>dopamine uptake studied; cells incubated with title comp. and <3H>dopamine for 5 min at 37 deg C in KRH buffer, pH 7.4; radioactivity measured by liquid scintillation counting

Further Details (Pharmacological Data)

cells expressing S356,359A mutant type dopamine transporter (serines 356 and 359 mutated to alanine); KRH: Krebs-Ringer-Henseleit

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological

1638.95 nmol/l

Data)

179 of 303

180 of 303

181 of 303

Results

dose-dependent inhibition (figure)

Reference

Dar, Dalit E.; Mayo, Cheryl; Uhl, George R.

Biochemical Pharmacology, 2005 , vol. 70, # 3 p. 461 - 469 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein phosphorylation; induction of

Species or TestSystem (Pharmacological Data)

C57BL/6J mouse

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

5 - 10 mg/kg

Kind of Dosing (Pharmacological Data)

used as sulfate; dissolved in 0.9 percent (w/v) NaCl

Method (Pharmacological Data)

mice treated with title comp.; after 10 - 30 min mice decapitated; heads frosen and sliced; microdisks (1.4 mm diameter) punched out bilaterally from median prefrontal cortex and homogenized; phosphorylated/total GluR1 and ERK1/2 determined by WBA

Further Details (Pharmacological Data)

GluR1: GluR1 subunit of AMPA receptor; ERK: extracellular signal-regulated kinase; WBA: Western blot analysis; AMPA: α-amino-3-hydroxy-5-methyl-4isoxazolepropionic acid

Results

title comp. produced dose- and time-dependent increase in phosphorylation of GluR1 on Ser845 and ERK on Thr183 and Tyr185 without affecting total GluR1 and ERK levels; ERK2 phosphorylation was much more pronounced than phosphorylation of ERK1

Reference

Pascoli, Vincent; Valjent, Emmanuel; Corbille, Anne-Gaelle; Corvol, Jean-Christophe; Tassin, Jean-Pol; Girault, Jean-Antoine; Herve, Denis

Molecular Pharmacology, 2005 , vol. 68, # 2 p. 421 - 429 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein phosphorylation; induction of

Species or TestSystem (Pharmacological Data)

C57BL/6J mouse

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

10 mg/kg

Kind of Dosing (Pharmacological Data)

used as sulfate; dissolved in 0.9 percent (w/v) NaCl

Method (Pharmacological Data)

mice pretreated or not with various antagonists and then treated with title comp. for 15 min; heads frosen and sliced; microdisks punched out bilaterally from median prefrontal cortex and homogenized; phosphorylated GluR1 determined by WBA

Further Details (Pharmacological Data)

antagonists used: haloperidol (Hal), SCH23390, propranolol (Pro), betaxolol (Bet), prazosin (Pra), ICI-118,551, yohimbine (Yoh), 4-chlorophenylalanine (p-CPA), ritanserin (Rit), SDZ 205,557 and dizocilpine maleate (MK801); WBA: Western blot analysis

Results

title comp.-induced phosphorylation of GluR1 inhibited in presence of Pro and Bet, slightly but significantly enhanced in presence of Pra and did not significantly change in presence of Hal, SCH23390, ICI-118,551, Yoh, p-CPA, Rit, SDZ 205,557, and MK801

Reference

Pascoli, Vincent; Valjent, Emmanuel; Corbille, Anne-Gaelle; Corvol, Jean-Christophe; Tassin, Jean-Pol; Girault, Jean-Antoine; Herve, Denis

Molecular Pharmacology, 2005 , vol. 68, # 2 p. 421 - 429 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein phosphorylation; induction of

Species or TestSystem

C57BL/6J mouse

(Pharmacological Data)

182 of 303

183 of 303

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

10 mg/kg

Kind of Dosing (Pharmacological Data)

used as sulfate; dissolved in 0.9 percent (w/v) NaCl

Method (Pharmacological Data)

mice pretreated or not with antagonists and then treated with title comp. for 15 min; heads frosen and sliced; microdisks punched out bilaterally from median prefrontal cortex and homogenized; phosphorylated ERK2 determined by Western blot analysis

Further Details (Pharmacological Data)

antagonists: haloperidol (Hal), SCH23390, propranolol (Pro), betaxolol (Bet), prazosin (Pra), ICI-118,551, yohimbine (Yoh), 4-chlorophenylalanine (pCPA), ritanserin (Rit), SDZ 205,557, and dizocilpine acetate; ERK: extracellular signal-regulated kinase

Results

title comp.-induced phosphorylation of ERK2 significantly reduced in presence of Pro, Bet, Pra, p-CPA, dizocilpine acetate, slightly reduced in presence of Yoh, did not significantly change in presence of Hal, SCH23390, ICI-118,551, Rit, and SDZ 205,557

Reference

Pascoli, Vincent; Valjent, Emmanuel; Corbille, Anne-Gaelle; Corvol, Jean-Christophe; Tassin, Jean-Pol; Girault, Jean-Antoine; Herve, Denis

Molecular Pharmacology, 2005 , vol. 68, # 2 p. 421 - 429 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

C57BL/6J mouse

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

2 mg/kg

Kind of Dosing (Pharmacological Data)

used as sulfate; dissolved in 0.9 percent (w/v) NaCl

Method (Pharmacological Data)

title comp. administered; locomotor activity determined at 5-min intervals during 60 min using circular corridor

Further Details (Pharmacological Data)

further investigations with propranolol (Pro), betaxolol (Bet) and β2-adrenergic receptor selective antagonist ICI-118,551

Results

title comp. increased locomotor activity; effect of title comp. was significantly enhanced in presence of Pro or Bet and did not change in presence of ICI-118,551

Reference

Pascoli, Vincent; Valjent, Emmanuel; Corbille, Anne-Gaelle; Corvol, Jean-Christophe; Tassin, Jean-Pol; Girault, Jean-Antoine; Herve, Denis

Molecular Pharmacology, 2005 , vol. 68, # 2 p. 421 - 429 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; inhib. of

Species or TestSystem (Pharmacological Data)

Pichia pastoris expressing human liver MAO A

Method (Pharmacological Data)

kynuramine used as substrate

Further Details (Pharmacological Data)

MAO: monoamine oxidase; Ki: competitive inhibition constant

Type (Pharmacological Data)

Ki

184 of 303

185 of 303

Value of Type (Pharmacological Data)

14.4 μmol/l

Reference

Vintem, Ana Paula B.; Price, Nigel T.; Silverman, Richard B.; Ramsay, Rona R.

Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 10 p. 3487 - 3495 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; inhib. of

Species or TestSystem (Pharmacological Data)

Pichia pastoris expressing human liver MAO A Cys374Ala

Method (Pharmacological Data)

kynuramine used as substrate

Further Details (Pharmacological Data)

MAO: monoamine oxidase; Ki: competitive inhibition constant

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

11.5 μmol/l

Reference

Vintem, Ana Paula B.; Price, Nigel T.; Silverman, Richard B.; Ramsay, Rona R.

Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 10 p. 3487 - 3495 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

Nestlet shredding; influence on

Species or TestSystem (Pharmacological Data)

NIH Swiss mice

Method (Pharmacological Data)

Nestlet Shredding Mice naturally will construct nests of material available in their living environment. Since this behavior is obsessive in nature, it has been used to model OCD (Xia Li, Denise Morrow and Jeffrey M. Witkin, "Decreases in nestlet shredding of mice by serotonin uptake inhibitors: comparison with marble burying", Psychopharmacology, submitted July 14,2003). House experimentally-naive male, NIH Swiss mice (Harlan SpragueDawley, Indianapolis, IN) weighing between 28-35 g in groups of 12 for at least three days prior to testing in a vivarium with a 12 hr. LIGHT/DARK cycle. Conduct experiments during the light cycle in an experimental room with normal overhead fluorescent lighting. Dose mice with vehicle or test compound and after a specified pretreatment interval (generally 30 min. ), place the mice individually in a 17 x 28 x 12 cm high plastic tub with about 5 mm sawdust shavings on the floor along with a pre-weighed multi-ply gauze pad (51 mm square). After 30 min. , weigh the remainder of the gauze pad not removed by the mouse. Determine the weight of the gauze used for nestlet construction by subtraction. Compare the results for test compound treated mice to the results for vehicle control treated mice with Dunnett's test. Clinically effective OCD treatment standard compounds suppress nestlet shredding at doses that are devoid of motor-impairing effects as measured by the rotorod test. The in vivo efficacy of 5HT2C compounds at the 5HT2C receptor was confirmed by the prevention of effects of the 5HT2C agonists on nestlet shredding by co-administration of the 5HT2C receptor antagonist, 6-chloro-5-methyl-N- (2- (2-methylpyridin-3-yl- oxy) pyridin-5-yl) aminocarbonyl) -2, 3-dihydroindole. The compound of the present invention (Example 2) was assayed essentially as described above and surprisingly found to suppress nestlet shredding at doses that were devoid of motor-impairing effects as measured by the rotorod test. In contrast to the compound of the present invention, the anxiolytic chlordiazepoxide and the psychomotor stimulant damphetamine decrease nestlet shredding only at doses that produce motoric side effects (depression or stimulation, respectively).

Results

Decrease of nestlet shredding only at doses that produce motoric side effects

Location

Page/Page column 24-25

Reference

ELI LILLY AND COMPANY

Patent: WO2005/19180 A1, 2005 ; Title/Abstract Full Text Show Details

186 of 303

Effect (Pharmacological Data)

Schedule-lnduced polydipsia; influence on

Species or TestSystem (Pharmacological Data)

Wistar rats

Method (Pharmacological Data)

Schedule-Induced POLYDIPSIA Food-deprived rats exposed to intermittent presentations of food will drink amounts of water that are far in excess of their normal daily intake and in excess of their intake when given all of their food at one time (Falk JL."Production of polydipsia in normal rats by an intermittent food schedule", Science 133: 195-196, (1961) ). This excessive behavior is persistent and has been used to model OCD. Maintain Wistar rats on a food restricted diet (to maintain 85percent free feeding weight), but with free access to water. Train the rats in a behavioral testing chamber to press a lever to receive a food pellet under a fixed interval schedule, such that the rats are rewarded with a 45 mg food pellet the first time they press a lever after a 120 second interval has elapsed. The fixed interval is then reset to 120 seconds and the process repeated. Thus, during a 90 min. test session, the rats can earn a maximum of 45 pellets. The behavioral chamber is also equipped with a water bottle that is weighed before and after the

session to determine the amount of water consumed. Administer test compounds on Tuesdays and Fridays. Determine control day performances on Thursdays. Administer compounds either orally at 60 min. before the beginning of a test session, or subcutaneously at 20 min. before the beginning of a test session. Compare the rates of lever pressing and water consumption for each animal's performance during sessions after test compound treatment with that animal's performance during control sessions, expressed as a percent of the control rate. Average the individual percent of control rates for each dose and calculate the standard error'of the mean. Clinically effective OCD treatment standard compounds (e. g. chlomipramine, fluoxetine) suppress schedule-induced polydipsia without producing notable changes in motor patterns, food intake, or behavior the following day. The in vivo efficacy of 5HT2C compounds at the 5HT2C receptor was confirmed by the prevention of effects of the 5HT2C agonists on excessive drinking by coadministration of the 5HT2C receptor antagonist, 6-CHLORO-5-METHYL-N-(2-(2-METHYLPYRIDIN-3-YL-OXY) PYRIDIN-5 yl) aminocarbonyl) -2, 3dihydroindole. The compound of the present invention (Example 2) was assayed in the schedule- induced polydipsia assay essentially as described above and surprisingly found to suppress schedule-induced polydipsia without producing notable changes in motor patterns, food intake, or behavior the following day. The behavior suppression was blocked by co-administration of the 5-HT2C antagonist. In contrast to the comopund of the present invention, the psychomotor stimulant d- amphetamine decreases excessive drinking only at behaviorally stimulating doses and these effects are not prevented by the 5HT2C receptor antagonist. Results

Decrease of excessive drinking only at behaviorally stimulating doses

Location

Page/Page column 25-26

Reference

ELI LILLY AND COMPANY

Patent: WO2005/19180 A1, 2005 ; Title/Abstract Full Text Show Details

187 of 303

Effect (Pharmacological Data)

time spent; effect on

Species or TestSystem (Pharmacological Data)

BKW (Bradford bred) mouse

Sex

male

Route of Application

subcutaneous

Method (Pharmacological Data)

CPP Study CPP was assessed in a 3-chambered apparatus (76 x 30 x 30 cm) constructed from Plexiglass. The outer two chambers measured 30 x 30 x 30 cm, one with a striped wood floor/metal walls and the other with a textured glass floor/striped wood walls. This combination of textures and visual clues has been chosen since it ensures that the two chambers are distinct. Mice are allocated to the initially preferred and non-preferred chamber using a counterbalanced design. The smaller central chamber (16 x 30 x 30 cm) consists of a permanently black painted floor with clear walls. All three chambers are connected by guillotine doors, which are staggered to prevent visual communication between the chambers. The experimental session was divided into three separate phases.Pre-conditioning: Naive mice were placed in the central chamber, with the guillotine doors raised, and allowed free access to all three sections of the apparatus for 15 min on three consecutive days. The position of the mouse in the apparatus was monitored automatically using a system of photocell beams and the time spent (s) in each of the two outer chambers was recorded, from which the preconditioning preference was determined (mean +/- sem of the 3 days). The time spent in the central chamber reflects the number of transitions between the two outer chambers.Conditioning: This consisted of a period of 8 days in which the guillotine doors were lowered and the mice (groups n = 7-12) were injected with drug or saline and placed immediately into one of the two outer chambers for 30 min. On alternate days the mice received the other treatment and were placed into the opposing chamber. Each mouse thus received 4 drug and 4 saline pairings. Drug pairing was counterbalanced through the groups to both preferred and non-preferred sides as was the first day of administration of the drug. Saline/saline controls were included in the experimental design.Post-conditioning: The guillotine doors were raised and the mice again placed into the central chambers and allowed free access to all three sections for 15 min. The position of each mouse was monitored and the time spent in each outer chamber was measured in s. Seven groups were incorporated into the design: [] Group 1saline/saline controls (n = 10)Group 2d-amphetamine sulphate (1.25 mg/kg, s.c.; n = 7)Group 3d,l-MPH (10 mg/kg, s.c.; n = 10)Group 4d-MPH (5 mg/kg, s.c.; n = 8)Groups 5-7/-MPH (6.25 mg/kg s.c., 12.5 mg/kg s.c. or 25 mg/kg s.c.; n = 12, 9 and 10)Antagonism Study Groups of mice (n = 9-10/group) received saline or /-MPH (25 mg/kg, s.c.) followed 20 min later by saline, d-MPH (2.5 mg/kg, s.c.) or d,l-MPH (5 mg/kg, s.c.). Locomotor activity was measured in individual photocell boxes during the subsequent 60 min period as described in detail previously. Five groups (n = 9-10/treatment group) were used: [] Group 1saline + saline controls: (n = 10)Group 2saline + d-MPH (2.5 mg/kg, s.c.); n = 10Group 3saline + d,l-MPH (5 mg/kg, s.c.); n = 10Group 4/-MPH (25 mg/kg, s.c.) + d-MPH (2.5 mg/kg, s.c.); n = 10Group 5/-MPH (25 mg/kg s.c.) + d,l-MPH (5 mg/kg s.c.); n = 9Statistical AnalysisPreliminary Study: The total number of counts/time period was recorded and the data analysed by one-way analysis of variance with post-hoc t-test.CPP Study: The time spent (s) by individual mice in the outer chambers pre- and post-conditioning were compared. Data were analysed by two-way analysis within subject analysis of variance followed by post-hoc t-test analysis.Antagonism Study: The total number of counts/time period was recorded and the data analysed by one-way analysis of variance with Dunnett's t-test for multiple comparison against a single control. From any analysis, p<0.05 was taken to be significant.CPP Study ResultsPre-Conditioning: Individual mice were exposed to the apparatus on each of three pre-conditioning test days. The initial preference for each mouse was calc

Results

test compound (1.25 mg/kg, s.c.) significantly increased the time spent in the drug-paired chamber (250.8 +/- 7.9 s to 401.4 +/- 35.3 s), consistent with a preference response.

Location

Page/Page column 3-6

Reference

Celltech Pharma Europe Limited

Patent: EP1185268 B1, 2005 ; Title/Abstract Full Text Show Details

188 of 303

Effect (Pharmacological Data)

locomotor activity; stimulation of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Method

EXAMPLE Evaluation of the neuroprotective potential of argon gas, administered alone or as a mixture with nitrous oxide, on the development and

(Pharmacological Data)

expression of sensitization to D-amphetamine. The aim of the study is to evaluate the neuroprotective potential, on sensitization to D-amphetamine, of argon, for which the mechanisms of action, that are still poorly understood, could involve an agonist action with respect to GABAA receptors, in particular with respect to the benzodiazepine site, the argon being administered alone or as a mixture; Abraini et al., Anesth Analg, 2003, vol. 96, p. 746-749, 2003. To do this, adult male Sprague-Dawley rats that weighed approximately 220 g when they arrived in the laboratory were used. Throughout the study, the animals were placed under standard animalhouse conditions, in groups of 8, so as to avoid the appearance of a stress reaction subsequent to isolation. They had water and food ad libitum. The D-amphetamine sensitization protocol followed and the trials for treatment by administration of gas used were as follows: For 3 consecutive days (from D1 to D3), 8 groups of animals (8 rats per group) were administered intraperitoneally (i.p.) either Damphetamine (amph: 1 mg/ml/kg), or a saline solution (saline: 1 ml/kg) for the control animals. After each injection of D-amphetamine, the rats were immediately placed, for 3 hours, in a closed chamber having a volume of 100 litres, that was swept under dynamic conditions, namely: with air (group 1: saline; group 2: amph); with a mixture of argon at 37.5 vol percent and of nitrous oxide at 37.5 vol percent (group 3: saline; group 4: amph), the remainder being oxygen; with a mixture of argon at 50 vol percent and of nitrous oxide at 25 vol percent (group 5: saline; group 6: amph), the remainder being oxygen; with argon at 75 vol percent (group 7: saline; group 8: amph), the remainder being oxygen. The gases used in this study were administered under dynamic conditions at an initial rate of 10 l.min-1 for 30 minutes, and then at a constant rate of 1 l.min-1 for 2 h 30 min. By proceeding in this way, the effective concentration after treatment for 30 minutes is equal to 95percent of the desired final concentration (corresponding to the mixture used) and the cumulative dose x time value is more than 25percent greater than the dose.x.time value obtained using, as previously, a constant rate of introduction of gases of 5 l.min-1; see the document Abraini and David, for Air Liquide Sante International "etude du potentiel neuroprotecteur du xenon et du protoxyde d'azote" [study of the neuroprotective potential of xenon and of nitrous oxide], May 2001-October 2003), which makes it possible to optimize the treatment in its initial phase; the total cumulative dose.x.time values are substantially equal; see Table 1 below; Table 1 indicates the cumulative doses (dose.x.time; cumulative D*T) as a function of the dynamic sweep conditions used (corresponding to the rate of introduction of the gases or mixtures of gases) to saturate a chamber having a volume of 100 litres. It is noted that, after 30 minutes, the cumulative dose obtained using an initial rate of 10 l.min-1 (followed by a constant rate of 1 l.min-1 for 2 h 30 min) is approximately 25percent greater than the cumulative dose obtained using a constant rate of 5 l.min-1. The locomotor activity and the righting activity of the animals were evaluated at D6, after an i.p. injection of a saline solution (1 ml/kg) in order to determine the actual effects of the treatments administered with the various gases and mixtures of gas, and on D7 after an i.p. administration of D-amphetamine (1 mg/ml/kg) in order to evaluate the effects of the gases and mixtures of gas on sensitization to D-amphetamine. The locomotor activity and the stereotypic righting activity of the animals in response to these injections were registered by means of a photoelectric

Results

title compound at 1 mg/kg increased locomotor activity (figure)

Location

Page/Page column 2-5; figure 1

Reference

Lemaire, Marc; Abraini, Jacques

Patent: US2005/152988 A1, 2005 ; Title/Abstract Full Text Show Details

189 of 303

Effect (Pharmacological Data)

stereotypic movements; stimulation of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Method (Pharmacological Data)

EXAMPLE Evaluation of the neuroprotective potential of argon gas, administered alone or as a mixture with nitrous oxide, on the development and expression of sensitization to D-amphetamine. The aim of the study is to evaluate the neuroprotective potential, on sensitization to D-amphetamine, of argon, for which the mechanisms of action, that are still poorly understood, could involve an agonist action with respect to GABAA receptors, in particular with respect to the benzodiazepine site, the argon being administered alone or as a mixture; Abraini et al., Anesth Analg, 2003, vol. 96, p. 746-749, 2003. To do this, adult male Sprague-Dawley rats that weighed approximately 220 g when they arrived in the laboratory were used. Throughout the study, the animals were placed under standard animalhouse conditions, in groups of 8, so as to avoid the appearance of a stress reaction subsequent to isolation. They had water and food ad libitum. The D-amphetamine sensitization protocol followed and the trials for treatment by administration of gas used were as follows: For 3 consecutive days (from D1 to D3), 8 groups of animals (8 rats per group) were administered intraperitoneally (i.p.) either Damphetamine (amph: 1 mg/ml/kg), or a saline solution (saline: 1 ml/kg) for the control animals. After each injection of D-amphetamine, the rats were immediately placed, for 3 hours, in a closed chamber having a volume of 100 litres, that was swept under dynamic conditions, namely: with air (group 1: saline; group 2: amph); with a mixture of argon at 37.5 vol percent and of nitrous oxide at 37.5 vol percent (group 3: saline; group 4: amph), the remainder being oxygen; with a mixture of argon at 50 vol percent and of nitrous oxide at 25 vol percent (group 5: saline; group 6: amph), the remainder being oxygen; with argon at 75 vol percent (group 7: saline; group 8: amph), the remainder being oxygen. The gases used in this study were administered under dynamic conditions at an initial rate of 10 l.min-1 for 30 minutes, and then at a constant rate of 1 l.min-1 for 2 h 30 min. By proceeding in this way, the effective concentration after treatment for 30 minutes is equal to 95percent of the desired final concentration (corresponding to the mixture used) and the cumulative dose x time value is more than 25percent greater than the dose.x.time value obtained using, as previously, a constant rate of introduction of gases of 5 l.min-1; see the document Abraini and David, for Air Liquide Sante International "etude du potentiel neuroprotecteur du xenon et du protoxyde d'azote" [study of the neuroprotective potential of xenon and of nitrous oxide], May 2001-October 2003), which makes it possible to optimize the treatment in its initial phase; the total cumulative dose.x.time values are substantially equal; see Table 1 below; Table 1 indicates the cumulative doses (dose.x.time; cumulative D*T) as a function of the dynamic sweep conditions used (corresponding to the rate of introduction of the gases or mixtures of gases) to saturate a chamber having a volume of 100 litres. It is noted that, after 30 minutes, the cumulative dose obtained using an initial rate of 10 l.min-1 (followed by a constant rate of 1 l.min-1 for 2 h 30 min) is approximately 25percent greater than the cumulative dose obtained using a constant rate of 5 l.min-1. The locomotor activity and the righting activity of the animals were evaluated at D6, after an i.p. injection of a saline solution (1 ml/kg) in order to determine the actual effects of the treatments administered with the various gases and mixtures of gas, and on D7 after an i.p. administration of D-amphetamine (1 mg/ml/kg) in order to evaluate the effects of the gases and mixtures of gas on sensitization to D-amphetamine. The locomotor activity and the stereotypic righting activity of the animals in response to these injections were registered by means of a photoelectric

Results

title compound at 1 mg/kg increased stereotypic movements (figure)

Location

Page/Page column 2-5; figure 2

Reference

Lemaire, Marc; Abraini, Jacques

Patent: US2005/152988 A1, 2005 ; Title/Abstract Full Text Show Details

190 of 303

191 of 303

192 of 303

Effect (Pharmacological Data)

mRNA expression; inhibition of

Species or TestSystem (Pharmacological Data)

human astrocytoma cells U373 MG

Concentration (Pharmacological Data)

1 - 100 μmol/l

Kind of Dosing (Pharmacological Data)

treatment with title comp. renewed every 24 h; title comp. admin. as sulfate

Method (Pharmacological Data)

cells treated with increasing conc. of title comp. for 24-48 h; mRNA expression of nuclear receptors, GR, CAR and PXR determined; total RNA isolated; RT-PCR; electrophoresis; UV analysis

Further Details (Pharmacological Data)

GR: glucocorticoid receptor; CAR: constitutive androstane receptor; PXR: pregnane X receptor; nuclear receptors mRNA normalized to GADPH and expressed as percentage of untreated control

Comment (Pharmacological Data)

No effect

Reference

Malaplate-Armand; Ferrari; Masson; Visvikis-Siest; Lambert; Batt

Toxicology Letters, 2005 , vol. 159, # 3 p. 203 - 211 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein expression; inhibition of

Species or TestSystem (Pharmacological Data)

human astrocytoma cells U373 MG

Concentration (Pharmacological Data)

1 - 100 μmol/l

Kind of Dosing (Pharmacological Data)

treatment with title comp. renewed every 24 h; title comp. admin. as sulfate

Method (Pharmacological Data)

cells treated with increasing conc. of title comp. for 72 h; microsomal fraction from MG cells prepared 72 h after treatment; protein levels of CYP2C8 and CYP2C9 determined; western-blotting analysis; Lowry method used

Further Details (Pharmacological Data)

GR: glucocorticoid receptor; CAR: constitutive androstane receptor; PXR: pregnane X receptor; nuclear receptors mRNA normalized to GADPH and expressed as percentage of untreated control

Comment (Pharmacological Data)

No effect

Reference

Malaplate-Armand; Ferrari; Masson; Visvikis-Siest; Lambert; Batt

Toxicology Letters, 2005 , vol. 159, # 3 p. 203 - 211 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

cytotoxicity

Species or TestSystem (Pharmacological Data)

human astrocytoma cells U373 MG

Concentration (Pharmacological Data)

1 - 100 μmol/l

Kind of Dosing (Pharmacological Data)

treatment with title comp. renewed every 24 h; title comp. admin as sulfate

Method (Pharmacological Data)

cells treated with increasing conc. of title comp. for 24-72 h; cytotoxicity examined by measuring mitochondrial dehydrogenase activity; spectrophotometric method using MTT

Comment

No effect

(Pharmacological Data)

193 of 303

194 of 303

195 of 303

Reference

Malaplate-Armand; Ferrari; Masson; Visvikis-Siest; Lambert; Batt

Toxicology Letters, 2005 , vol. 159, # 3 p. 203 - 211 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

mRNA expression; inhibition of

Species or TestSystem (Pharmacological Data)

human astrocytoma cells U373 MG

Concentration (Pharmacological Data)

1 - 100 μmol/l

Kind of Dosing (Pharmacological Data)

treatment with title comp. renewed every 24 h; title comp. admin. as sulfate

Method (Pharmacological Data)

cells treated with increasing conc. of title comp. for 48 h; mRNA expression of CYP2C8 and CYP2C9 isoforms determined; total RNA isolated; RT-PCR; electrophoresis; UV analysis

Further Details (Pharmacological Data)

CYP: cytochromes P450; CYP mRNA normalized to GADPH and expressed as percentage of control

Comment (Pharmacological Data)

No effect

Reference

Malaplate-Armand; Ferrari; Masson; Visvikis-Siest; Lambert; Batt

Toxicology Letters, 2005 , vol. 159, # 3 p. 203 - 211 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)

2 mg/kg

Method (Pharmacological Data)

pretreatment with saline or title comp. for 7 d; 10-d abstinence period; challenge injection of title comp. (0.5 mg/kg, i.p.); distance traveled was measured during 120 min; activity monitoring chamber

Further Details (Pharmacological Data)

saline control

Results

pretreatment with title comp. resulted in sensitized locomotor response (figure)

Reference

Armstrong, Victoria; Reichel, Carmela M.; Doti, Jonathan F.; Crawford, Cynthia A.; McDougall, Sanders A.

European Journal of Pharmacology, 2004 , vol. 488, # 1-3 p. 111 - 115 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neuroregulatoric

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

2 mg/kg

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197 of 303

198 of 303

Method (Pharmacological Data)

pretreatment with saline or title comp. for 7 d; 10-d abstinence period; challenge injection of title comp. (0.5 mg/kg, i.p.); coronal sections of brain; analysis of GFAP, DAT, and GLT-1 immunoreactivities

Further Details (Pharmacological Data)

saline control; GFAP: glial fibrillary acidic protein; DAT: dopamine transporter; GLT-1: glutamate transporter-1

Results

title comp. increased number of GFAP-positive cells in dorsal and ventral caudate-putamen; DAT and GLT-1 immunoreactivities were unaffected (table)

Reference

Armstrong, Victoria; Reichel, Carmela M.; Doti, Jonathan F.; Crawford, Cynthia A.; McDougall, Sanders A.

European Journal of Pharmacology, 2004 , vol. 488, # 1-3 p. 111 - 115 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

HEK-293 cell membranes

Kind of Dosing (Pharmacological Data)

stock solution in water

Method (Pharmacological Data)

cells expressing human DAT; 30 - 50 μg of membrane preparation incubated with 3.4 nmol/l <3H>WIN 35,428, 0.3 - 100 μmol/l DA and title comp. for 15 min at 21 deg C; binding to DAT was assessed by shifting of DA inhibition curve

Further Details (Pharmacological Data)

assay buffer (mmol/l): 122 NaCl, 5 KCl, 1 MgSO4, 10 glucose, 1 CaCl2, 0.1 tropolone, 30 sodium phosphate, pH 7.4; DAT: dopamine transporter; WIN 35,428: 2β-carbomethoxy-3β-(4-fluorophenyl)tropane; DA: dopamine; vehicle control

Results

title comp. showed ca. 60 percent of pure competitive interaction with DA (table, figure)

Reference

Appell, Michael; Berfield, Janet L.; Wang, Lijuan C.; Dunn III, William J.; Chen, Nianhang; Reith, Maarten E.A.

Biochemical Pharmacology, 2004 , vol. 67, # 2 p. 293 - 302 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

HEK-293 cell membranes

Kind of Dosing (Pharmacological Data)

stock solution in water

Method (Pharmacological Data)

cells expressing human DAT; 30 - 50 μg of membrane preparation incubated with 3.4 nmol/l <3H>WIN 35,428 and title comp. for 15 min at 21 deg C; binding to DAT was assessed

Further Details (Pharmacological Data)

assay buffer (mmol/l): 122 NaCl, 5 KCl, 1 MgSO4, 10 glucose, 1 CaCl2, 0.1 tropolone, 30 sodium phosphate, pH 7.4; DAT: dopamine transporter; WIN 35,428: 2β-carbomethoxy-3β-(4-fluorophenyl)tropane; vehicle control

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

6.33 μmol/l

Reference

Appell, Michael; Berfield, Janet L.; Wang, Lijuan C.; Dunn III, William J.; Chen, Nianhang; Reith, Maarten E.A.

Biochemical Pharmacology, 2004 , vol. 67, # 2 p. 293 - 302 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

male

Route of Application

intraperitoneal

199 of 303

200 of 303

Concentration (Pharmacological Data)

1 mg/kg

Kind of Dosing (Pharmacological Data)

as 1 mg/ml (calculated for free base) in isotonic saline

Method (Pharmacological Data)

225-250 g rats with free access to food and water; acute administration of title comp. in rats pretreated or not with 0.1 mg/kg of (+)-MK-801; locomotor activity measured for 60 min after treatment

Further Details (Pharmacological Data)

control: saline injection

Results

title comp. significantly increased locomotor activity; the effect not affected significantly by (+)-MK-801 (diagram)

Reference

Groenig; Atalla; Kuschinsky

Naunyn-Schmiedeberg's Archives of Pharmacology, 2004 , vol. 369, # 2 p. 228 - 231 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

1 mg/kg

Kind of Dosing (Pharmacological Data)

as 1 mg/ml (calculated for free base) in isotonic saline; acutely or in CS rats on day 17

Method (Pharmacological Data)

225-250 g rats with free access to food and water; title comp. injected and locomotor activity measured for 60 min after treatment

Further Details (Pharmacological Data)

control: saline injection; associative sensitized (CS) rats received title comp. on days 1, 3, 5 and 7 and saline on days 2, 4 and 6, during title comp. treatment rats exposed to conditioned stimuli

Results

title comp. led to significantly higher locomotor activity on day 17 then after acute administration (diagram)

Reference

Groenig; Atalla; Kuschinsky

Naunyn-Schmiedeberg's Archives of Pharmacology, 2004 , vol. 369, # 2 p. 228 - 231 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

1 mg/kg

Kind of Dosing (Pharmacological Data)

as 1 mg/ml (calculated for free base) in isotonic saline; on day 17, 20 min after (+)-MK-801 pretreatment

Method (Pharmacological Data)

225-250 g rats with free access to food and water; title comp. injected in CS and PS rats, pretreated or not with 0.1 mg/kg of (+)-MK-801; locomotor activity measured for 60 min after injection

Further Details (Pharmacological Data)

associative sensitized (CS) rats received title comp. on days 1, 3, 5 and 7 and saline on days 2, 4 and 6, during title comp. treatment rats exposed to conditioned stimuli; non-associatively sensitized (PS) exposed to stimuli during saline treatment

Results

title comp. increased locomotor activity; the effect reduced by (+)-MK-801 pretreatment in CS, but not in PS rats (diagram)

Reference

Groenig; Atalla; Kuschinsky

Naunyn-Schmiedeberg's Archives of Pharmacology, 2004 , vol. 369, # 2 p. 228 - 231 Title/Abstract Full Text View citing articles Show Details

201 of 303

202 of 303

Effect (Pharmacological Data)

metabolic

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

1 mg/kg

Kind of Dosing (Pharmacological Data)

as 1 mg/ml (calculated for free base) in isotonic saline; on day 17, 20 min after (+)-MK-801 pretreatment

Method (Pharmacological Data)

225-250 g rats with free access to food and water; title comp. injected in CS and PS rats, pretreated or not with 0.1 mg/kg of (+)-MK-801; in 20 min extracellular fraction of nucleus accumbens collected by in vivo microdialysis for HPLC of dopamine

Further Details (Pharmacological Data)

associative sensitized (CS) rats received title comp. on days 1, 3, 5 and 7 and saline on days 2, 4 and 6, during title comp. treatment rats exposed to conditioned stimuli; non-associatively sensitized (PS) exposed to stimuli during saline treatment

Results

title comp. increased dopamine level; the effect reduced by (+)-MK-801 pretreatment in CS, but enhanced in PS rats (diagram)

Reference

Groenig; Atalla; Kuschinsky

Naunyn-Schmiedeberg's Archives of Pharmacology, 2004 , vol. 369, # 2 p. 228 - 231 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

hyperlocomotor activity

Species or TestSystem (Pharmacological Data)

Coloboma mice

Sex

male and female

Route of Application

intraperitoneal

Method (Pharmacological Data)

Hyperlocomotor activity assesment

Results

significantly decreased locomotor activity

Location

Page 99-102

Reference

PREDIX PHARMACEUTICALS HOLDINGS, INC.

Patent: WO2004/69794 A2, 2004 ; Title/Abstract Full Text Show Details

203 of 303

Effect (Pharmacological Data)

secretion inhibition

Species or TestSystem (Pharmacological Data)

bovine adrenal chromaffin cells

Concentration (Pharmacological Data)

Ca. 1 - 1000 μmol/l

Kind of Dosing (Pharmacological Data)

used as sulfate

Method (Pharmacological Data)

cells loaded with fura-2 acetoxymethyl ester (30 min, 37 deg C); effect of title comp. on cytosolic Ca2+ ((Ca2+)c)-rise induced by DMPP, K+ (50 mmol/l KCl), epibatidine (0.5 μmol/l), choline (3 mmol/l) or veratridine studied by fluorescence method

Further Details (Pharmacological Data)

DMPP = 1,1-dimethyl-4-phenyl-piperazinium iodide, 10 μmol/l; IC50 refers to inhibition of DMPP-induced (Ca2+)c rise; further investigation on mechanism of action by using specific nicotine antagonists and Ca2+ channel blocker

204 of 303

205 of 303

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

30 μmol/l

Results

title comp. dose-dependently suppressed DMPP- (ca. 1-1000 μmol/l title comp.), epibatidine- or choline (100-300 μmol/l)-induced (Ca2+)c rise, but no effect in case of K+ or veratridine

Reference

Liu, Pei-Shan; Liaw, Chwen-Tzy; Lin, Meng-Kai; Shin, Song-Huah; Kao, Lung-Sen; Lin, Lih-Fang

European journal of pharmacology, 2003 , vol. 460, # 1 p. 9 - 17 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

secretion inhibition

Species or TestSystem (Pharmacological Data)

bovine adrenal chromaffin cells

Concentration (Pharmacological Data)

Ca. 1 - 1000 μmol/l

Kind of Dosing (Pharmacological Data)

used as sulfate

Method (Pharmacological Data)

cells incubated with (3H)norepinephrine (NE, 1 h, 37 deg C); effect of title comp. on NE, DO and EP release induced by DMPP (10 μmol/l), K+ (56 mmol/l) or veratridine (0.3 mmol/l) studied by measuring radioactivity

Further Details (Pharmacological Data)

DMPP = 1,1-dimethyl-4-phenyl-piperazinium iodide; IC50 refers to inhibition of DMPP-induced NE-release; EP = epinephrine; DO = dopamine

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

200 μmol/l

Results

title comp. dose-dependently suppressed DMPP-induced NE release and suppressed DMPP-induced EP and DO release at 500 μmol/l, but no effect in case of K+ or veratridine

Reference

Liu, Pei-Shan; Liaw, Chwen-Tzy; Lin, Meng-Kai; Shin, Song-Huah; Kao, Lung-Sen; Lin, Lih-Fang

European journal of pharmacology, 2003 , vol. 460, # 1 p. 9 - 17 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

bovine adrenal chromaffin cells

Concentration (Pharmacological Data)

Ca. 0.1 - 2000 μmol/l

Kind of Dosing (Pharmacological Data)

used as sulfate

Method (Pharmacological Data)

cells incubated with (3H)nicotine (40 nmol/l) in presence of title comp. for 90 min, then radioactivity measured by scintillation counting

Further Details (Pharmacological Data)

nonspecific binding determined by preincubation with 1 mmol/l nicotine for 30 min

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

50 μmol/l

206 of 303

207 of 303

208 of 303

Results

title comp. dose-dependently replaced (3H)nicotine and bound with nicotinic receptors

Reference

Liu, Pei-Shan; Liaw, Chwen-Tzy; Lin, Meng-Kai; Shin, Song-Huah; Kao, Lung-Sen; Lin, Lih-Fang

European journal of pharmacology, 2003 , vol. 460, # 1 p. 9 - 17 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

secretion stimulant

Species or TestSystem (Pharmacological Data)

bovine adrenal chromaffin cells

Concentration (Pharmacological Data)

Ca. 0.01 - 1000 μmol/l

Kind of Dosing (Pharmacological Data)

used as sulfate

Method (Pharmacological Data)

cells incubated with (3H)norepinephrine (NE, 1 h, 37 deg C) or loaded with fura-2 acetoxymethyl ester (30 min, 37 deg C); NE release assayed by measuring radioactivity or cytosolic Ca2+ ((Ca2+)c) concentration by fluorescence method

Results

dose- and extracellular Ca2+-dependent increase in NE release and (Ca2+)c concentration; NE release almost twice basal release above 100 μmol/l of title comp.; (Ca2+)c: bell curve, transient rise and decay of (Ca2+)c decreased above 100 μmol/l

Reference

Liu, Pei-Shan; Liaw, Chwen-Tzy; Lin, Meng-Kai; Shin, Song-Huah; Kao, Lung-Sen; Lin, Lih-Fang

European journal of pharmacology, 2003 , vol. 460, # 1 p. 9 - 17 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transport

Species or TestSystem (Pharmacological Data)

human embryonic kidney 293 cell membranes

Method (Pharmacological Data)

competition for <3H>CFT binding studied at pH 7.0 in presence of 2-300 mmol/l Na+ with different anions (Br-, NO3-, SO42-)

Further Details (Pharmacological Data)

CFT: 2β-carbomethoxy-3β-(4-fluorophenyl)tropane; cells expressing human dopamine transporter

Results

title comp. showed dramatic increases in binding on raising Na+ concentration with any anions

Reference

Chen, Nianhang; Reith, Maarten E.A.

European Journal of Pharmacology, 2003 , vol. 479, # 1-3 p. 213 - 221 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

releasing hormones

Species or TestSystem (Pharmacological Data)

MA-10 mouse Leydig tumor cells

Concentration (Pharmacological Data)

1e-06 mol/l

Kind of Dosing (Pharmacological Data)

sulphate salt of title comp. in Waymouth medium without serum used

Method (Pharmacological Data)

cells treated with title comp. in the absence or presence of hCG (50 ng/ml) for 0-360 min; media collected; progesterone production assayed by radioimmunoassay

Further Details (Pharmacological Data)

control: hCG alone; hCG: human chorionic gonadotropin

Results

title comp. alone did not stimulate progesterone production; title comp. + hCG produced a statistically significant difference with 49 percent increase in progesterone production compared to hCG alone at 3 h; fig.

Reference

Chen, Liang-Yu; Huang, Yuan-Li; Liu, Ming-Yie; Leu, Sew-Fen; Huang, Bu-Miin

Life Sciences, 2003 , vol. 72, # 17 p. 1983 - 1995 Title/Abstract Full Text View citing articles Show Details

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Effect (Pharmacological Data)

releasing hormones

Species or TestSystem (Pharmacological Data)

MA-10 mouse Leydig tumor cells

Concentration (Pharmacological Data)

1e-10 mol/l

Kind of Dosing (Pharmacological Data)

sulphate salt of title comp. in Waymouth medium without serum used

Method (Pharmacological Data)

cells treated with title comp. in the absence or presence of hCG (50 ng/ml) for 0-360 min; media collected; progesterone production assayed by radioimmunoassay

Further Details (Pharmacological Data)

control: hCG alone; hCG: human chorionic gonadotropin

Results

title comp. alone did not stimulate progesterone production; title comp. + hCG produced a statistically significant difference with 37 percent increase in progesterone production compared to hCG alone at 3 h; fig.

Reference

Chen, Liang-Yu; Huang, Yuan-Li; Liu, Ming-Yie; Leu, Sew-Fen; Huang, Bu-Miin

Life Sciences, 2003 , vol. 72, # 17 p. 1983 - 1995 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

releasing hormones

Species or TestSystem (Pharmacological Data)

MA-10 mouse Leydig tumor cells

Concentration (Pharmacological Data)

1E-12 - 1E-05 mol/l

Kind of Dosing (Pharmacological Data)

sulphate salt of title comp. in Waymouth medium without serum used

Method (Pharmacological Data)

cells treated with title comp. in the absence or presence of hCG (50 ng/ml) for 180 min; media collected; progesterone production assayed by radioimmunoassay

Further Details (Pharmacological Data)

control: hCG alone; hCG: human chorionic gonadotropin

Results

title comp. at 1E-11, 1E-10 mol/l in the presence of hCG significantly induced 87 percent more progesterone production compared to hCG alone; at 1E12, 1E-9, 1E-8, 1E-7, 1E-6 mol/l, 30-50 percent increase of progesterone production induced in presence of hCG; fig.

Reference

Chen, Liang-Yu; Huang, Yuan-Li; Liu, Ming-Yie; Leu, Sew-Fen; Huang, Bu-Miin

Life Sciences, 2003 , vol. 72, # 17 p. 1983 - 1995 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein expression; induction of

Species or TestSystem (Pharmacological Data)

MA-10 mouse Leydig tumor cells

Concentration (Pharmacological Data)

1E-12 - 1E-05 mol/l

Kind of Dosing (Pharmacological Data)

sulphate salt of title comp. in Waymouth medium without serum used

Method (Pharmacological Data)

cells treated with title comp. in the presence and absence of hCG for 180 min; washed, homogenized, centrifuged; mitochondria isolated; expression of 30 KDa StAR protein determined by Western blot

Further Details (Pharmacological

control: hCG alone; hCG: human chorionic gonadotropin

Data)

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Results

title comp. (1E-12 to 1E-6 mol/l) did not induce more expression of StAR protein in the presence of hCG; fig.

Reference

Chen, Liang-Yu; Huang, Yuan-Li; Liu, Ming-Yie; Leu, Sew-Fen; Huang, Bu-Miin

Life Sciences, 2003 , vol. 72, # 17 p. 1983 - 1995 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; induction of

Species or TestSystem (Pharmacological Data)

MA-10 mouse Leydig tumor cells

Concentration (Pharmacological Data)

1E-12 - 1E-05 mol/l

Kind of Dosing (Pharmacological Data)

sulphate salt of title comp. in Waymouth medium without serum used

Method (Pharmacological Data)

cells treated with title comp. in the presence and absence of hCG for 180 min; washed, homogenized, centrifuged; mitochondria isolated; expression of P450scc enzyme expression determined by Western blot

Further Details (Pharmacological Data)

control: hCG alone; hCG: human chorionic gonadotropin; P450scc: P450 side-chain cleavage enzyme

Results

title comp. (1E-12 to 1E-6 mol/l) did not induce more expression of P450scc enzyme in the presence of hCG; fig.

Reference

Chen, Liang-Yu; Huang, Yuan-Li; Liu, Ming-Yie; Leu, Sew-Fen; Huang, Bu-Miin

Life Sciences, 2003 , vol. 72, # 17 p. 1983 - 1995 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; induction of

Species or TestSystem (Pharmacological Data)

MA-10 mouse Leydig tumor cells

Concentration (Pharmacological Data)

1e-10 mol/l

Kind of Dosing (Pharmacological Data)

sulphate salt of title comp. in Waymouth medium without serum used

Method (Pharmacological Data)

cells treated with 22R-hydroxycholesterol (22R-chol, 50 μmol/l) in the presence of title comp. for 180 min; media collected; progesterone production determined by radioimmunoassay

Further Details (Pharmacological Data)

22R-chol is a precursor of P450scc enzyme; P450scc: P450 side-chain cleavage enzyme

Results

title comp. significantly induced more progesterone production with 78 percent increase in the presence of 22R-chol at 50 μmol/l suggesting that title comp. could increase activity of P450scc to induce progesterone production; fig.

Reference

Chen, Liang-Yu; Huang, Yuan-Li; Liu, Ming-Yie; Leu, Sew-Fen; Huang, Bu-Miin

Life Sciences, 2003 , vol. 72, # 17 p. 1983 - 1995 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; induction of

Species or TestSystem (Pharmacological Data)

MA-10 mouse Leydig tumor cells

Concentration (Pharmacological Data)

1e-10 mol/l

Kind of Dosing (Pharmacological Data)

sulphate salt of title comp. in Waymouth medium without serum used

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Method (Pharmacological Data)

cells treated with pregnenolone (Preg, 7.95 μmol/l) in the presence of title comp. for 180 min; media collected; progesterone production determined by radioimmunoassay

Further Details (Pharmacological Data)

pregnenolone is a precursor of 3β-HSD enzyme

Results

title comp. did not induce more progesterone production with 78 percent increase in the presence of Preg at 7.95 μmol/l suggesting that title comp. did not increase activity of 3β-HSD to induce more progesterone production; fig.

Reference

Chen, Liang-Yu; Huang, Yuan-Li; Liu, Ming-Yie; Leu, Sew-Fen; Huang, Bu-Miin

Life Sciences, 2003 , vol. 72, # 17 p. 1983 - 1995 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

rat

Route of Application

parenteral

Method (Pharmacological Data)

inhibitory avoidance task study 30 min or different time after title comp. administration; second retention test one week after the first retention test

Results

when administered 30 min before training 0.25, about 0.50 and about 1.0 mg/kg had no effect; about 2.0 mg/kg significantly improved retention of the task; ; 2.0 mg/kg was effective when administered to the rats between 0 and 2 hours prior to training; rats received title comp. the previous week performed significantly better than rats that had received control injections of vehicle solution

Location

Page 37

Reference

Sention, Inc.

Patent: US2003/232890 A1, 2003 ; Title/Abstract Full Text Show Details

216 of 303

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

rat

Route of Application

parenteral

Method (Pharmacological Data)

amnesic rats (lesions of the fornix); inhibitory avoidance task study 1 h after title comp. administration;

Results

title comp. improved the performance of the fornix lesion rats

Location

Page 38

Reference

Sention, Inc.

Patent: US2003/232890 A1, 2003 ; Title/Abstract Full Text Show Details

217 of 303

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

rat

Route of Application

parenteral

Method (Pharmacological Data)

effects on stimulation of memory consolidation and motor stimulation determined in inhibitory avoidance test; title comp. administered 1 h before training

Results

2.0 mg/kg enhanced performance

Location

Page 38

Reference

Sention, Inc.

Patent: US2003/232890 A1, 2003 ; Title/Abstract Full Text Show Details

218 of 303

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

rat

Route of Application

parenteral

Method (Pharmacological Data)

effects on activity determined in motor stimulation test; title comp. administered prior to testing

Results

title comp. (2 mg/kg) produced a clear and significant enhancement in locomotor activity for the entire 10 minute session

Location

Page 39

Reference

Sention, Inc.

Patent: US2003/232890 A1, 2003 ; Title/Abstract Full Text Show Details

219 of 303

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

Long-Evans rat

Sex

male

Route of Application

intraperitoneal

Method (Pharmacological Data)

passive avoidance test; title comp. administered immediately after training; retention test 24 h later

Results

2.0 mg/kg of title comp.significantly improved task performance

Location

Page 43

Reference

Sention, Inc.

Patent: US2003/232890 A1, 2003 ; Title/Abstract Full Text Show Details

220 of 303

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

Long-Evans rat

Sex

male

Route of Application

intraperitoneal

Method (Pharmacological Data)

locomotor activity levels measured by an automated motion detector for 3 h after title comp. administration

Results

increases in activity at 0.25 mg/kg

Location

Page 44

Reference

Sention, Inc.

Patent: US2003/232890 A1, 2003 ; Title/Abstract Full Text Show Details

Show next 20

221 of 303

Hide facts Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

Macaca mulatta, rhesus monkey

Sex

male and female

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Route of Application

subcutaneous

Concentration (Pharmacological Data)

0.32 - 1.78 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. (sulfate) dissolved in sterile water, heated and/or sonicated; 0.1-1.0 ml admin. every 2nd or 3rd day as long as behavior was under adequate stimulus control

Method (Pharmacological Data)

monkeys trained to respond under FR placed in operant chambers with response levers; 1.0 mg/kg LAAM admin.; 7 h after 1st daily injection of LAAM, title comp. admin.; increasing doses of naltrexone admin.; discriminative effects of naltrexone detd.

Further Details (Pharmacological Data)

control: naltrexone alone; FR: fixed ratio schedules (stimulus shock termination); LAAM: L-α-acetylmethadol

Results

pretreatment with title comp. attenuated the discriminative effects of naltrexone, although there was variation in sensitivity among monkeys; diagram, table

Reference

Sell, Stacy L.; France, Charles P.

Journal of Pharmacology and Experimental Therapeutics, 2002 , vol. 301, # 3 p. 1103 - 1110 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein expression; effect on

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

5 mg/kg

Method (Pharmacological Data)

rats treated with title comp.; decapitated 4, 8, or 16 h post injection; striatum and nucleus accumbens dissected; homogenized; separated by SDSPAGE; CRP40 expression measured by Western immunoblotting assay

Further Details (Pharmacological Data)

control: 0.9 percent saline; SDS-PAGE: sodium dodecyl sulfate polyacrylamide gel electrophoresis; CRP40: 40-kDa catecholamine-regulated protein

Comment (Pharmacological Data)

No effect

Reference

Gabriele, Joseph; Rajaram, Mahesh; Zhang, Bingjun; Sharma, Sunjay; Mishra, Ram K

European Journal of Pharmacology, 2002 , vol. 453, # 1 p. 13 - 19 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein expression; induction of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

2.5 mg/kg

Kind of Dosing (Pharmacological Data)

administered at same time each day for 5 d

Method (Pharmacological Data)

rats treated with title comp.; decapitated next day post injection; striatum and nucleus accumbens (NA) dissected; homogenized; separated by SDSPAGE; CRP40 expression measured by Western immunoblotting assay

Further Details (Pharmacological Data)

control: 0.9 percent saline; SDS-PAGE: sodium dodecyl sulfate polyacrylamide gel electrophoresis; CRP40: 40-kDa catecholamine-regulated protein

Results

title comp. significantly increased CRP40 levels in striatum and NA next day post injection (37.64 percent and 27.86 percent, resp.) (figure)

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Reference

Gabriele, Joseph; Rajaram, Mahesh; Zhang, Bingjun; Sharma, Sunjay; Mishra, Ram K

European Journal of Pharmacology, 2002 , vol. 453, # 1 p. 13 - 19 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein expression; effect on

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

2.5 mg/kg

Kind of Dosing (Pharmacological Data)

administered at same time each day for 5 d

Method (Pharmacological Data)

rats treated with title comp.; decapitated next day post injection; striatum and nucleus accumbens (NA) dissected; homogenized; separated by SDSPAGE; Hsp-70 expression measured by Western immunoblotting assay

Further Details (Pharmacological Data)

control: 0.9 percent saline; SDS-PAGE: sodium dodecyl sulfate polyacrylamide gel electrophoresis; Hsp-70: 70-kDa heat shock protein

Comment (Pharmacological Data)

No effect

Reference

Gabriele, Joseph; Rajaram, Mahesh; Zhang, Bingjun; Sharma, Sunjay; Mishra, Ram K

European Journal of Pharmacology, 2002 , vol. 453, # 1 p. 13 - 19 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein expression; effect on

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

2.5 mg/kg

Kind of Dosing (Pharmacological Data)

administered at same time each day for 5 d

Method (Pharmacological Data)

rats treated with title comp.; decapitated 14 d post injection; striatum and nucleus accumbens (NA) dissected; homogenized; separated by SDS-PAGE; CRP40 expression measured by Western immunoblotting assay

Further Details (Pharmacological Data)

control: 0.9 percent saline; SDS-PAGE: sodium dodecyl sulfate polyacrylamide gel electrophoresis; CRP40: 40-kDa catecholamine-regulated protein

Comment (Pharmacological Data)

No effect

Reference

Gabriele, Joseph; Rajaram, Mahesh; Zhang, Bingjun; Sharma, Sunjay; Mishra, Ram K

European Journal of Pharmacology, 2002 , vol. 453, # 1 p. 13 - 19 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein expression; effect on

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

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Sex

male

Route of Application

intraperitoneal

Kind of Dosing (Pharmacological Data)

rats injected with 2.5 mg/kg title comp. for 5 d; 14 d after last injection challenged once with 0.5 mg/kg title comp.

Method (Pharmacological Data)

rats treated with title comp.; decapitated 4 h post last injection; striatum and nucleus accumbens (NA) dissected; homogenized; separated by SDSPAGE; CRP40 expression measured by Western immunoblotting assay

Further Details (Pharmacological Data)

control: 0.9 percent saline; SDS-PAGE: sodium dodecyl sulfate polyacrylamide gel electrophoresis; CRP40: 40-kDa catecholamine-regulated protein

Comment (Pharmacological Data)

No effect

Reference

Gabriele, Joseph; Rajaram, Mahesh; Zhang, Bingjun; Sharma, Sunjay; Mishra, Ram K

European Journal of Pharmacology, 2002 , vol. 453, # 1 p. 13 - 19 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein expression; induction of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Kind of Dosing (Pharmacological Data)

rats injected with 2.5 mg/kg title comp. for 5 d; 14 d after last injection challenged once with 0.5 mg/kg title comp.

Method (Pharmacological Data)

rats treated with title comp.; decapitated 8 h post last injection; striatum and nucleus accumbens (NA) dissected; homogenized; separated by SDSPAGE; CRP40 expression measured by Western immunoblotting assay

Further Details (Pharmacological Data)

control: 0.9 percent saline; SDS-PAGE: sodium dodecyl sulfate polyacrylamide gel electrophoresis; CRP40: 40-kDa catecholamine-regulated protein

Results

title comp. sign. increased CRP40 levels in NA only (40.49 percent) (figure)

Reference

Gabriele, Joseph; Rajaram, Mahesh; Zhang, Bingjun; Sharma, Sunjay; Mishra, Ram K

European Journal of Pharmacology, 2002 , vol. 453, # 1 p. 13 - 19 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

uptake; inhibition of

Species or TestSystem (Pharmacological Data)

COS cells expressing wild-type dopamine transporter

Concentration (Pharmacological Data)

<= 1 mmol/l

Method (Pharmacological Data)

cells incubated with 20 nmol/l <3H>dopamine and title comp. at 37 deg C for 5 min; radioactivity assessed using scintillation fluid

Further Details (Pharmacological Data)

inhibition of dopamine uptake studied

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

0.28 μmol/l

Reference

Lin, Zhicheng; Uhl, George R.

Molecular Pharmacology, 2002 , vol. 61, # 4 p. 885 - 891 Title/Abstract Full Text View citing articles Show Details

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Effect (Pharmacological Data)

uptake; inhibition of

Species or TestSystem (Pharmacological Data)

COS cells expressing dopamine transporter F154A mutant

Concentration (Pharmacological Data)

<= 1 mmol/l

Method (Pharmacological Data)

cells incubated with 20 nmol/l <3H>dopamine and title comp. at 37 deg C for 5 min; radioactivity assessed using scintillation fluid

Further Details (Pharmacological Data)

inhibition of dopamine uptake studied

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

0.32 μmol/l

Reference

Lin, Zhicheng; Uhl, George R.

Molecular Pharmacology, 2002 , vol. 61, # 4 p. 885 - 891 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neurotoxicity

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

5 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in normal saline; admin. in 4 doses at 23 deg C with 2 h separating each dose

Method (Pharmacological Data)

4-5-month-old rats with or without microdialysis; rectal temperature taken; hyperthermic effects recorded; brains histologically exam. 3-4 d after treatm.; TH immunoreactivity and degenerating axons and terminals in CPu anal.

Further Details (Pharmacological Data)

TH = tyrosine hydroxylase; CPu = caudate/putamen

Results

thermogenic effects observed; neurodegeneration in forebrain depending on degree of hyperthermia; extensive nerodegeneration in parietal cortex, intralaminar, ventromedial and ventrolateral thalamic nuclei; depletion in TH immunoreactivity

Reference

Bowyer, John F; Hopkins, Keri J; Jakab, Robert; Ferguson, Sherry A

Toxicology Letters, 2001 , vol. 125, # 1-3 p. 151 - 166 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

antagonist

Species or TestSystem (Pharmacological Data)

Madine-Darby canine kidney cells

Method (Pharmacological Data)

cells transiently transfected with the Drosophila melanogaster dopamine transporter incub. with title comp.+<3H>dopamine in Krebs-Ringer's-HEPES buffer (pH 7.4; 6 min); radioligand uptake determined by liquid scintillation

Further Details (Pharmacological Data)

IC50 calculated from nonlinear regression

Type (Pharmacological

IC50

Data)

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Value of Type (Pharmacological Data)

6600 μmol/l

Reference

Poerzgen, Peter; Park, Sang Ki; Hirsh, Jay; Sonders, Mark S.; Amara, Susan G.

Molecular Pharmacology, 2001 , vol. 59, # 1 p. 83 - 95 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

anorectic

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

1 - 4 mg/kg

Method (Pharmacological Data)

rats 200-300 g; daily food intake (DFI), body weight change with respect to previous day checked daily; hypothalamic neuropeptide Y level (NPY) (from sonicated hypothalamus) detd. by radioimmunoassay on day 1 or on the day when DFI returned normal

Further Details (Pharmacological Data)

role of hypothalamic NPY on feeding behavior studied using intracerebroventricular inj. of antisense (to rat NPY mRNA sequence) or missense 18-mer oligodeoxynucleotide inj., 10 μg/day, 1 h before title comp. inj.

Results

dose-dependent anorectic effect on day 1, DFI and BWC gradually returned to normal value (tolerance); hypothalamic NPY changed in parallel manner; tolerance to title comp. was abolished by antisense pretreatment suggesting role of NPY; diagrams

Reference

Kuo, Dong-Yih; Hsu, Chao-Tien; Cheng, Juei-Tang

Life Sciences, 2001 , vol. 70, # 3 p. 243 - 251 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

agonist

Species or TestSystem (Pharmacological Data)

HEK293 cells expressing rTAR1

Concentration (Pharmacological Data)

Ca. 1E-09 - 1E-05 mol/l

Method (Pharmacological Data)

cells incubated in KRH with 100 μmol/l 3-isobutyl-1-methylxanthine and title comp. for 1 h at 37 deg C; cAMP content measured using competitive binding of <3H>cAMP to a cAMP-binding protein

Further Details (Pharmacological Data)

HEK: human embryonic kidney; rTAR1: rat trace amine receptor 1; reference comp.: forskolin; KRH: Krebs-Ringer-HEPES buffer

Type (Pharmacological Data)

EC50

Value of Type (Pharmacological Data)

440 nmol/l

Results

title comp. induced cAMP production acting as agonist (diagram)

Reference

Bunzow; Sonders; Arttamangkul; Harrison; Zhang; Quigley; Darland; Suchland; Pasumamula; Kennedy; Olson; Magenis; Amara; Grandy

Molecular Pharmacology, 2001 , vol. 60, # 6 p. 1181 - 1188 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; inhib. of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat lung homogenate

Sex

male

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Concentration (Pharmacological Data)

1E-06 - 0.001 mol/l

Method (Pharmacological Data)

homogenates preincubated with title comp. (20 min, 37 deg C); reaction started by <14C>serotonin; incubated (5 or 10 min); reaction stopped by 3 N HCl; serotonin deaminated metabolites extracted; radioactivity measured with LSS; MAO-A activity detd.

Further Details (Pharmacological Data)

LSS: liquid scintillation spectrometry; MAO-A: monoamine oxidase-A

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

6.1 μmol/l

Results

title comp. inhibited the ability of MAO-A to deaminate serotonin and the inhibition was concentration-dependent; table, figure

Reference

Ulus, Ismail H.; Maher, Timothy J.; Wurtman, Richard J.

Biochemical Pharmacology, 2000 , vol. 59, # 12 p. 1611 - 1621 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; inhib. of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat liver homogenate

Sex

male

Concentration (Pharmacological Data)

1E-06 - 0.001 mol/l

Method (Pharmacological Data)

homogenates preincubated with title comp. (20 min, 37 deg C); reaction started by <14C>serotonin; incubated (5 or 10 min); reaction stopped by 3 N HCl; serotonin deaminated metabolites extracted; radioactivity measured with LSS; MAO-A activity detd.

Further Details (Pharmacological Data)

LSS: liquid scintillation spectrometry; MAO-A: monoamine oxidase-A; further study: reversibility of inhibition of MAO-A by title comp. was studied

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

6.5 μmol/l

Results

title comp. inhibited the ability of MAO-A to deaminate serotonin and the inhibition was concentration-dependent; inhibitory effects of title comp. was reversible; table, figures

Reference

Ulus, Ismail H.; Maher, Timothy J.; Wurtman, Richard J.

Biochemical Pharmacology, 2000 , vol. 59, # 12 p. 1611 - 1621 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; inhib. of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat brain homogenate

Sex

male

Concentration (Pharmacological Data)

1E-06 - 0.001 mol/l

Method (Pharmacological Data)

homogenates preincubated with title comp. (20 min, 37 deg C); reaction started by <14C>serotonin; incubated (5 or 10 min); reaction stopped by 3 N HCl; serotonin deaminated metabolites extracted; radioactivity measured with LSS; MAO-A activity detd.

Further Details (Pharmacological Data)

LSS: liquid scintillation spectrometry; MAO-A: monoamine oxidase-A

Type

Ki

(Pharmacological Data)

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Value of Type (Pharmacological Data)

4.9 μmol/l

Results

title comp. inhibited the ability of MAO-A to deaminate serotonin and the inhibition was concentration-dependent; table, figure

Reference

Ulus, Ismail H.; Maher, Timothy J.; Wurtman, Richard J.

Biochemical Pharmacology, 2000 , vol. 59, # 12 p. 1611 - 1621 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; inhib. of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat lung homogenate

Sex

male

Concentration (Pharmacological Data)

1E-06 - 0.01 mol/l

Method (Pharmacological Data)

homogenates preincubated with title comp. (20 min, 37 deg C); reaction started by <14C>β-phenylethylamine; incubated (2 min); reaction stopped by 3 N HCl; deaminated metabolites extracted; radioactivity measured with LSS; MAO-B activity detd.

Further Details (Pharmacological Data)

LSS: liquid scintillation spectrometry; MAO-B: monoamine oxidase-B

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

106 μmol/l

Results

title comp. inhibited ability of MAO-B to deaminate β-phenylethylamine and the inhibition was concentration-dependent; table, fig.

Reference

Ulus, Ismail H.; Maher, Timothy J.; Wurtman, Richard J.

Biochemical Pharmacology, 2000 , vol. 59, # 12 p. 1611 - 1621 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; inhib. of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat liver homogenate

Sex

male

Concentration (Pharmacological Data)

1E-06 - 0.01 mol/l

Method (Pharmacological Data)

homogenates preincubated with title comp. (20 min, 37 deg C); reaction started by <14C>β-phenylethylamine; incubated (2 min); reaction stopped by 3 N HCl; deaminated metabolites extracted; radioactivity measured with LSS; MAO-B activity detd.

Further Details (Pharmacological Data)

LSS: liquid scintillation spectrometry; MAO-B: monoamine oxidase-B; further study: reversibility of MAO-B inhibition by title comp. was studied

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

119 μmol/l

Results

title comp. inhibited ability of MAO-B to deaminate β-phenylethylamine and the inhibition was concentration-dependent; inhibitory effect of title comp. was reversible; table, fig.

Reference

Ulus, Ismail H.; Maher, Timothy J.; Wurtman, Richard J.

Biochemical Pharmacology, 2000 , vol. 59, # 12 p. 1611 - 1621 Title/Abstract Full Text View citing articles Show Details

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Effect (Pharmacological Data)

enzyme; inhib. of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat brain homogenate

Sex

male

Concentration (Pharmacological Data)

1E-05 - 0.01 mol/l

Method (Pharmacological Data)

homogenates preincubated with title comp. (20 min, 37 deg C); reaction started by <14C>β-phenylethylamine; incubated (2 min); reaction stopped by 3 N HCl; deaminated metabolites extracted; radioactivity measured with LSS; MAO-B activity detd.

Further Details (Pharmacological Data)

LSS: liquid scintillation spectrometry; MAO-B: monoamine oxidase-B

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

118 μmol/l

Results

title comp. inhibited ability of MAO-B to deaminate β-phenylethylamine and the inhibition was concentration-dependent; table, fig.

Reference

Ulus, Ismail H.; Maher, Timothy J.; Wurtman, Richard J.

Biochemical Pharmacology, 2000 , vol. 59, # 12 p. 1611 - 1621 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

K(1+) current; decrease of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat ventricular myocytes

Concentration (Pharmacological Data)

100 μmol/l

Kind of Dosing (Pharmacological Data)

title comp. sulfate was used

Method (Pharmacological Data)

cells treated with title comp.; trace currents elicited by 500-ms pulses to +50 mV from holding potential of -120 mV with 30-ms prepulse to -40 mV in presence of title comp. were recorded using whole-cell variation of patch-clamp technique

Further Details (Pharmacological Data)

control: untreated cells

Results

title comp. reduced amplitude of peak current, but did not affect steady state; title comp. had no effect either on amplitude of inward rectifier K(1+) current; in presence of title comp., recovery from inactivation was similar to that of control; fig.

Reference

Casis, Oscar; Espina, Laura; Gallego, Monica

Journal of Cardiovascular Pharmacology, 2000 , vol. 36, # 3 p. 390 - 395 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

K(1+) current; decrease of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat ventricular myocytes

Concentration (Pharmacological Data)

1 - 1000 μmol/l

Kind of Dosing (Pharmacological Data)

title comp. sulfate was used

Method (Pharmacological

cells treated with title comp.; trace currents elicited by +50 mV from holding potential of -60 mV in presence of TEA were recorded using whole-cell variation of patch-clamp technique

Data)

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Further Details (Pharmacological Data)

control: untreated cells

Results

title comp. at 100 μmol/l reduced amplitude of transient outward K(1+) current and acceleration of inactivation process; title comp. (1-1000 μmol/l) reduced amplitude of outward K(1+) current concn.-dependently, effect disappeared on washout; fig.

Reference

Casis, Oscar; Espina, Laura; Gallego, Monica

Journal of Cardiovascular Pharmacology, 2000 , vol. 36, # 3 p. 390 - 395 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

K(1+) current; decrease of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat ventricular myocytes

Concentration (Pharmacological Data)

0.1 - 1 mmol/l

Kind of Dosing (Pharmacological Data)

title comp. sulfate was used

Method (Pharmacological Data)

cells treated with title comp.; suspended in internal solution contg. potassium aspartate, KH2PO4, MgSO4, KCl, HEPES-K, ATP-Na2 and EGTA-K, pH 7,4; current-voltage relations detd. by recorded traces using whole-cell variation of patch-clamp technique

Further Details (Pharmacological Data)

control: untreated cells; OS: open state; DP: depolarization

Results

in presence of title comp., K(1+) current block increased from -30 to +10 mV, suggesting that title comp. bound to OS of channel; title comp. increased block in exponential fashion during DP; at 1 mmol/l, blocked 54 percent of channels in resting state; fig.

Reference

Casis, Oscar; Espina, Laura; Gallego, Monica

Journal of Cardiovascular Pharmacology, 2000 , vol. 36, # 3 p. 390 - 395 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

Ca(2+) inward current; decrease of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat ventricular myocytes

Concentration (Pharmacological Data)

100 μmol/l

Kind of Dosing (Pharmacological Data)

title comp. sulfate was used

Method (Pharmacological Data)

cells treated with title comp.; trace currents elicited at 0 mV from holding potential of -70 mV with 30-ms prepulse to -40 mV in presence of title comp. were recorded using whole-cell variation of patch-clamp technique

Further Details (Pharmacological Data)

control: untreated cells

Comment (Pharmacological Data)

No effect

Reference

Casis, Oscar; Espina, Laura; Gallego, Monica

Journal of Cardiovascular Pharmacology, 2000 , vol. 36, # 3 p. 390 - 395 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

biotransformation

Species or TestSystem (Pharmacological Data)

human flavin-containing monooxygenase 3 Lys-158

Method

title comp. was incubated with FMO3-MBP for 0 - 20 min; potassium phosphate buffer, pH 8.4; organic phase was extracted and analysed by HPLC

(Pharmacological Data)

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Further Details (Pharmacological Data)

reference comp.: phenethylamine and tyramine; flavin-containing monooxygenase 3 was cloned and expressed as maltose binding fusion protein (FMO3-MBP) in E.coli

Results

formation of metabolite was active enzyme-dependent and time-dependent; Kmapp = 18.1 mmol/l, Vmax = 4.5 nmol/min/mg protein

Metabolite (Pharmacological Data)

N-hydroxy-1-phenyl-2-propylamine [Reaxys RN: 2208236]

Reference

Cashman, John R.; Xiong, Yeng N.; Lifen, Xu; Janowsky, Aaron

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 288, # 3 p. 1251 - 1260 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

biotransformation

Species or TestSystem (Pharmacological Data)

human flavin-containing monooxygenase 3 Glu-158

Method (Pharmacological Data)

title comp. was incubated with FMO3-MBP for 0 - 20 min; potassium phosphate buffer, pH 8.4; organic phase was extracted and analysed by HPLC

Further Details (Pharmacological Data)

reference comp.: phenethylamine and tyramine; flavin-containing monooxygenase 3 was cloned and expressed as maltose binding fusion protein (FMO3-MBP) in E.coli

Results

formation of metabolite was active enzyme-dependent and time-dependent; Kmapp = 11.0 mmol/l, Vmax = 1.1 nmol/min/mg protein

Metabolite (Pharmacological Data)

N-hydroxy-1-phenyl-2-propylamine [Reaxys RN: 2208236]

Reference

Cashman, John R.; Xiong, Yeng N.; Lifen, Xu; Janowsky, Aaron

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 288, # 3 p. 1251 - 1260 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transmitter releasing

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

1 - 10 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. used as sulfate

Method (Pharmacological Data)

anaesthetized rats administered with dopamine; reproducible baseline dopamine signals obtained in medial dorsal striata; title comp. administered; changes in DA clearance rate recorded at 5-min intervals for 1 h postinjection

Further Details (Pharmacological Data)

control: saline

Results

title comp. produced decreases of 30-70 percent in the dopamine clearance rate; table, diagram

Reference

Zahniser, Nancy R.; Larson, Gaynor A.; Gerhardt, Greg A.

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 289, # 1 p. 266 - 277 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transmitter releasing

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

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Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

1 - 10 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. used as sulfate

Method (Pharmacological Data)

anaesthetized rats administered with dopamine; reproducible baseline dopamine signals obtained in medial dorsal striata; title comp. administered; changes in signal time course (T80) recorded at 5-min intervals for 1 h postinjection

Further Details (Pharmacological Data)

control: saline

Results

title comp. produced a significant increase of 50-250 percent in T80 values in a dose-related manner; effect of title comp. (5-10 mg/kg) was significantly different from saline; table, diagram

Reference

Zahniser, Nancy R.; Larson, Gaynor A.; Gerhardt, Greg A.

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 289, # 1 p. 266 - 277 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transmitter releasing

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

1 - 10 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. used as sulfate

Method (Pharmacological Data)

anaesthetized rats administered with dopamine; reproducible baseline dopamine signals obtained in medial dorsal striata; title comp. administered; changes in dopamine signal amplitude recorded at 5-min intervals for 1 h postinjection

Further Details (Pharmacological Data)

control: saline

Results

title comp. (10 mg/kg) increased dopamine signal amplitude (25 percent) while 5 mg/kg produced a significant decrease in amplitude relative to baseline; change in amplitude by 10 mg/kg title comp. differed significantly from that of saline; table, diagram

Reference

Zahniser, Nancy R.; Larson, Gaynor A.; Gerhardt, Greg A.

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 289, # 1 p. 266 - 277 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

in vivo (male Sprague-Dawley rats) ability to discriminate serotonin-releasing agents and hallucinogens from saline: ED50=1.06 μmol/kg

Reference

Parker, Matthew A.; Marona-Lewicka, Danuta; Kurrasch, Deborah; Shulgin, Alexander T.; Nichols, David E.

Journal of Medicinal Chemistry, 1998 , vol. 41, # 6 p. 1001 - 1005 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

dopamine release

Species or TestSystem (Pharmacological Data)

substantia nigra of Sprague-Dawley rats

Concentration (Pharmacological Data)

2 mmol/l

Method (Pharmacological Data)

rats decapitated, brains chilled, cut slices incubated (oxygenated aftificial cerebrospinal fluid, 22 deg C, 1 h); title compd. locally applied; high-speed chronoamperometric monitoring (sw pulses 0 - 0.55 V vs. Ag/AgCl, 100 ms, 5 Hz)

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Further Details (Pharmacological Data)

T80 - time for the signal to rise and decay by 80 percent from peak amplitude; Tc - clearance rate

Results

peak amplitude 0.18 μM, T80 = 314 s, Tc = 0.0010 μM/s

Reference

Hoffman, Alexander F.; Lupica, Carl R.; Gerhardt, Greg A.

Journal of Pharmacology and Experimental Therapeutics, 1998 , vol. 287, # 2 p. 487 - 496 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

dopamine release

Species or TestSystem (Pharmacological Data)

striatum of Sprague-Dawley rats

Concentration (Pharmacological Data)

2 mmol/l

Method (Pharmacological Data)

rats decapitated, brains chilled, cut slices incubated (oxygenated aftificial cerebrospinal fluid, 22 deg C, 1 h); title compd. locally applied; high-speed chronoamperometric monitoring (sw pulses 0 - 0.55 V vs. Ag/AgCl, 100 ms, 5 Hz)

Further Details (Pharmacological Data)

T80 - time for the signal to rise and decay by 80 percent from peak amplitude; Tc - clearance rate

Results

peak amplitude 1.14 μM, T80 = 487 s, Tc = 0.0050 μM/s

Reference

Hoffman, Alexander F.; Lupica, Carl R.; Gerhardt, Greg A.

Journal of Pharmacology and Experimental Therapeutics, 1998 , vol. 287, # 2 p. 487 - 496 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

teratogenic

Species or TestSystem (Pharmacological Data)

Wistar rat embryos

Concentration (Pharmacological Data)

0.1 - 1.6 mmol/l

Kind of Dosing (Pharmacological Data)

0.1 (14 μg of title comp./ml culture medium), 0.4, 0.8, 1.2, and 1.6 mM

Exposure Period (Pharmacological Data)

28 h

Method (Pharmacological Data)

in vitro; embryos with 9 or 10 somites prepared by removing maternal tissue, parietal yolk sac and Reichert's membrane on day 10 of gestation; incubation with title comp. at 38 deg C; stereomicroscopy; estimation of embryonal development

Further Details (Pharmacological Data)

embryos from 12-weeks-old (270-300 g) pregnant rats; test comp. in distilled water; yolk sac diameter and circulation, crown-rump length of embryos and the number of somites recorded; calculation of developmental score

Results

no effect on embryonal viability; but at >1.2 mM, significant decrease in yolk sac diameter, crown-rump length, somite number, and protein content level in embryos; dose-dependent malformations in embryos

Reference

Yamamoto, Yoshiko; Yamamoto, Keiichi; Hayase, Tamaki; Fukui, Yuko; Shiota, Kohei

Reproductive Toxicology, 1998 , vol. 12, # 2 p. 133 - 137 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

secretion stimulant

Species or TestSystem (Pharmacological Data)

corpus striatal tissue from Sprague-Dawley rats

Sex

male

Concentration (Pharmacological Data)

10 μmol/l

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Method (Pharmacological Data)

adult rats (300-350 g) sacrificed by rapid decapitation, corpus striatum dissected

Further Details (Pharmacological Data)

effect on dopamine and 3,4-dihydroxyphenylacetic acid (DOPAC); high performance liquid chromatography with electrochemical detection

Results

maximum dopamine/DOPAC release rate (pg/mg/min): ca. 95/20

Reference

Dluzen, Dean E.; Anderson, Linda I.

European Journal of Pharmacology, 1998 , vol. 341, # 1 p. 23 - 32 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics; modulation of

Species or TestSystem (Pharmacological Data)

human

Sex

male

Route of Application

peroral

Concentration (Pharmacological Data)

10 mg

Method (Pharmacological Data)

title comp. given in combination with modafinil (200 mg); blood samples collected up to 48 h; plasma modafinil and its metabolites conc. measured by HPLC, pharmacokinetic parameters calculated

Further Details (Pharmacological Data)

control: modafinil alone

Comment (Pharmacological Data)

No effect

Reference

Wong, Y. Nancy; Wang, Lixia; Hartman, Linda; Simcoe, Donna; Chen, Yusong; Laughton, Watson; Eldon, Richard; Markland, Colin; Grebow, Peter

Journal of Clinical Pharmacology, 1998 , vol. 38, # 10 p. 971 - 978 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)

10 mg

Method (Pharmacological Data)

title comp. administered, blood samples collected up to 48 h; plasma title comp. conc. measured by LC/MS/MS, pharmacokinetic parameters calculated

Further Details (Pharmacological Data)

AUC: area under serum conc.-time curve; Cmax: maximum serum conc.; tmax: time to Cmax; Cl/F: apparent oral clearance

Half-life Time (Pharmacological Data)

12.1 h

Results

Cmax = 24.7 ng/ml; tmax = 2.6 h; AUC = 431 ng*h/ml; Cl/F = 5.39 ml/min/kg (table)

Reference

Wong, Y. Nancy; Wang, Lixia; Hartman, Linda; Simcoe, Donna; Chen, Yusong; Laughton, Watson; Eldon, Richard; Markland, Colin; Grebow, Peter

Journal of Clinical Pharmacology, 1998 , vol. 38, # 10 p. 971 - 978 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

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Species or TestSystem (Pharmacological Data)

human

Route of Application

skinabsorption

Kind of Dosing (Pharmacological Data)

ca. 4 - 5 ml of > 95 percent title comp. solution poured on shirt and trousers and contacted for several min

Method (Pharmacological Data)

a case of accidental application of title comp. to skin (abdomen and thigh regions); plasma title comp. measured from 2.5 up to 24 h by mass spectrometry following chromatographic separation; amount of title comp. absorbed calculated

Half-life Time (Pharmacological Data)

Ca. 10 h

Results

plasma title comp. concentration at 2.5 h after application was 0.52 μg/ml and declined to ca. 0.17 μg/ml at 24 h (figure); absorbed amount of title comp. estimated to be 200 - 400 mg (10 - 20 percent of exposed one)

Reference

Hartvig

European Journal of Clinical Pharmacology, 1998 , vol. 54, # 9-10 p. 805 - 807 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

toxicity

Species or TestSystem (Pharmacological Data)

human

Route of Application

skinabsorption

Kind of Dosing (Pharmacological Data)

ca. 4 - 5 ml of > 95 percent title comp. solution poured on shirt and trousers and contacted for several min

Method (Pharmacological Data)

a case of accidental application of title comp. to skin (abdomen and thigh regions); adverse events recorded

Results

title comp. caused dizziness in 30 min, burn wound, elevated blood pressure (230/115 mm Hg), tachycardia, diaphoresis, headache, talkativeness, inability to empty the bladder, low intestinal mobility, insomnia, loss of appetite after 2 h up to ca. 40 h

Reference

Hartvig

European Journal of Clinical Pharmacology, 1998 , vol. 54, # 9-10 p. 805 - 807 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neuroregulatoric

Species or TestSystem (Pharmacological Data)

CD rat

Sex

male

Route of Application

peroral

Concentration (Pharmacological Data)

10 mg/kg

Kind of Dosing (Pharmacological Data)

dissolved in distilled water, 5 ml/kg; once daily for 14 days; used as sulphate

Method (Pharmacological Data)

24 h after last title comp. dose, frontal cortices removed, 5-HT2A receptors measured by <3H>ketanserin binding (15 min, 37 deg C, liquid scintillation counting)

Further Details (Pharmacological Data)

5-HT: 5-hydroxytryptamine; control: distilled water, 5 ml

Comment (Pharmacological Data)

No effect

Reference

Heal; Cheetham; Prow; Martin; Buckett

British Journal of Pharmacology, 1998 , vol. 125, # 2 p. 301 - 308 Title/Abstract Full Text View citing articles Show Details

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Effect (Pharmacological Data)

neuroregulatoric

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

4 mg/kg

Kind of Dosing (Pharmacological Data)

dissolved in 0.9percent (w/v) saline (2 ml/kg); used as sulphate

Method (Pharmacological Data)

microdialysis probe implanted into anterior hypothalamus; title comp. given, 20 min samples collected for 3 h, 5-HT measured by HPLC with electrochemical detection

Further Details (Pharmacological Data)

5-HT: 5-hydroxytryptamine; control: saline

Results

title comp. time-dependently increased 5-HT content with max. effect of 544percent at 25 min

Reference

Heal; Cheetham; Prow; Martin; Buckett

British Journal of Pharmacology, 1998 , vol. 125, # 2 p. 301 - 308 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neuroregulatoric

Species or TestSystem (Pharmacological Data)

CD rat

Sex

male

Route of Application

peroral

Concentration (Pharmacological Data)

0.3 - 10 mg/kg

Kind of Dosing (Pharmacological Data)

dissolved in distilled water, 5 ml/kg; used as sulphate

Method (Pharmacological Data)

rats received title comp., then 30 min later NSD-1015; 30 min later frontal cortex and hypothalamus removed, 5-HTP measured by HPLC with electrochemical detection

Further Details (Pharmacological Data)

5-HTP: 5-hydroxytryptophan; control: distilled water, 5 ml

Results

3-10 mg/kg title comp. inhibited 5-HTP formation in hypothalamus

Reference

Heal; Cheetham; Prow; Martin; Buckett

British Journal of Pharmacology, 1998 , vol. 125, # 2 p. 301 - 308 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transmitter releasing

Species or TestSystem (Pharmacological Data)

CD rat frontal cortices

Sex

male

Concentration (Pharmacological Data)

1E-07 - 0.0001 mol/l

Kind of Dosing (Pharmacological Data)

used as sulphate

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Method (Pharmacological Data)

slices incubated with <3H>5-HT, then superfused with title comp. for 8 min; radioactivity determined by liquid scintillation counter

Further Details (Pharmacological Data)

5-HT: 5-hydroxytryptamine

Results

1E-5-1E-4 M title comp. dose-dependently increased 5-HT release

Reference

Heal; Cheetham; Prow; Martin; Buckett

British Journal of Pharmacology, 1998 , vol. 125, # 2 p. 301 - 308 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

monoamine uptake; inhibition of

Species or TestSystem (Pharmacological Data)

CD rat striatal synaptosomes

Sex

male

Kind of Dosing (Pharmacological Data)

used as sulphate

Method (Pharmacological Data)

inhibition of <3H>dopamine uptake measured

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

132 nmol/l

Reference

Heal; Cheetham; Prow; Martin; Buckett

British Journal of Pharmacology, 1998 , vol. 125, # 2 p. 301 - 308 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

monoamine uptake; inhibition of

Species or TestSystem (Pharmacological Data)

CD rat frontal cortex synaptosomes

Sex

male

Kind of Dosing (Pharmacological Data)

used as sulphate

Method (Pharmacological Data)

inhibition of <3H>NA uptake measured

Further Details (Pharmacological Data)

NA: noradrenaline

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

45 nmol/l

Reference

Heal; Cheetham; Prow; Martin; Buckett

British Journal of Pharmacology, 1998 , vol. 125, # 2 p. 301 - 308 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

monoamine uptake; inhibition of

Species or TestSystem (Pharmacological

CD rat frontal cortex synaptosomes

Data)

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Sex

male

Kind of Dosing (Pharmacological Data)

used as sulphate

Method (Pharmacological Data)

inhibition of <3H>5-HT uptake measured

Further Details (Pharmacological Data)

5-HT: 5-hydroxytryptamine

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

1441 nmol/l

Reference

Heal; Cheetham; Prow; Martin; Buckett

British Journal of Pharmacology, 1998 , vol. 125, # 2 p. 301 - 308 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

0.5 mg/kg

Kind of Dosing (Pharmacological Data)

as sulphate

Method (Pharmacological Data)

in vivo; 405- to 567-g rats individually housed in Makrolon cages (12-h light/dark cycle); appetitive discrimination procedure; conditioning box; response latencies during pre-conditioned and conditioned reinforced and non-reinforced states

Results

only rats that had been food reinforced in title compound state displayed shorter magazine-response latencies in their previously reinforced than nonreinforced state, both prior to and during stimulation

Reference

Maes, J.H. Roald; Vossen, Jo M.H.

European Journal of Pharmacology, 1997 , vol. 319, # 1 p. 5 - 11 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

drug dependence

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

3 mg/kg

Kind of Dosing (Pharmacological Data)

dissolved in 0.9 percent saline and administered in a volume of 1 ml/kg

Method (Pharmacological Data)

title comp. injected to rats with MFB-implanted electrode and trained to respond in ICSS autotitration procedure; 4 h later, RDE of NTX (opioid antagonist-precipitated withdrawal test) studied; degree of sensitization assessed by ED25 for RDE of NTX

Further Details (Pharmacological Data)

ICSS: intracranial self-stimulation; MFB: medial forebrain bundle; RDE: rate-decreasing effect; NTX: naltrexone (opioid antagonist, cumulative doses 0.001 - 30 mg/kg); vehicle (saline) control

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Comment (Pharmacological Data)

No effect

Reference

Easterling, Keith W.; Holtzman, Stephen G.

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 1 p. 188 - 199 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

releasing hormones

Species or TestSystem (Pharmacological Data)

ventral midbrain culture

Concentration (Pharmacological Data)

10 μmol/l

Method (Pharmacological Data)

sister cultures (8 d in vitro) incubated with/without 1 μM reserpine; medium replaced with Ca2+-free/pargyline medium for 40 min incubation with/without reserpine and with/without title comp.

Further Details (Pharmacological Data)

extra- and intracellular dopamine (DA) measured

Results

reserpine inhibited DA release induced by title comp.

Reference

Sulzer, David; Remy, Carl St.; Rayport, Stephen

Molecular Pharmacology, 1996 , vol. 49, # 2 p. 338 - 342 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

hepatotoxic

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

male

Concentration (Pharmacological Data)

0.08 - 2 mmol/l

Method (Pharmacological Data)

adult rats (weight 200 - 250 g); hepatocytes isolated; 1E6 cells preincubated for 10 min with iprindole (10 μmol/l); incubated with title comp. in KrebsHenseleit buffer with Hepes(shaked) at 37 deg C for 3 h; samples taken at 60 min intervals

Further Details (Pharmacological Data)

glutathione (GSH) status evaluated; GSSG: disulfid form of glutathione; iprindole as P450 2D inhibitor

Results

title comp. caused depletion of total cellular GSH and GSSG was prevented by preincubation with iprindole (table)

Reference

Carvalho, Felix; Remiao, Fernando; Amado, Francisco; Domingues, Pedro; Ferrer Correia; Bastos, Maria Lourdes

Chemical Research in Toxicology, 1996 , vol. 9, # 6 p. 1031 - 1036 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

hepatotoxic

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

male

Concentration (Pharmacological Data)

0.08 - 2 mmol/l

Method (Pharmacological Data)

adult rats (weight 200 - 250 g); hepatocytes isolated; 1E6 cells preincubated for 10 min with metyrapone (1 mmol/l); incubated with title comp. in Krebs-Henseleit buffer with Hepes (shaked) at 37 deg C for 3 h; samples taken at 60 min intervals

Further Details (Pharmacological Data)

glutathione (GSH) status evaluated; GSSG: disulfid form of glutathione; metyrapone as P450 inhibitor

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Results

title comp. caused depletion of total cellular GSH and GSSG was prevented by preincubation with metyrapone (table)

Reference

Carvalho, Felix; Remiao, Fernando; Amado, Francisco; Domingues, Pedro; Ferrer Correia; Bastos, Maria Lourdes

Chemical Research in Toxicology, 1996 , vol. 9, # 6 p. 1031 - 1036 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

hepatotoxic

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

male

Concentration (Pharmacological Data)

0.08 - 2 mmol/l

Kind of Dosing (Pharmacological Data)

title comp. was incubated as sulfate

Method (Pharmacological Data)

adult animals weighing 200 - 250 g; hepatocytes isolated; 1E6 cells incubated with title comp. in Krebs-Henseleit buffer supplemented with Hepes in shaking water bath at 37 deg C for 3 h; samples taken at 60 min intervals

Further Details (Pharmacological Data)

cell viability, lipid peroxidation and glutathione (GSH) status evaluated; after 180 min glutathione adducts detected and characterized by MS; GSSG: disulfide form of glutathione

Results

title comp. did not affect cell viability and lipid peroxidation; title comp. decreased cellular GSH in dose-dependent manner (diagram) to 85 - 47 percent after 3 h; presence of (glutathion-S-yl)-p-hydroxyamphetamine and slight increase of GSSG was detected

Reference

Carvalho, Felix; Remiao, Fernando; Amado, Francisco; Domingues, Pedro; Ferrer Correia; Bastos, Maria Lourdes

Chemical Research in Toxicology, 1996 , vol. 9, # 6 p. 1031 - 1036 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

Macaca fasicularis, cynomolgus monkey

Sex

female

Route of Application

intramuscular

Concentration (Pharmacological Data)

0.01 - 0.16 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in water, given in a volume of 1 ml/10 kg; doses refer to the free base, title comp. used as hydrochloride

Method (Pharmacological Data)

animals (4.9-6.4 kg); number of eye blinks and the duration of time that the eyes were visible observed up to 62.5 min after title comp. administration, 5 observations (2.5 min) at 12.5 min intervals; saline and vehicle controls

Further Details (Pharmacological Data)

comparison with other indirect dopamine receptor agonists; effect of the title comp. on the spontaneous eye blink rate investigated

Results

no significant effect on eye blink rate at first two observation periods (diagram); at the highest dose significant increase of observation time (diagram)

Reference

Kleven, Mark S.; Koek, Wouter

Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 279, # 3 p. 1211 - 1219 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transmitter synthesis; inhibition of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

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Concentration (Pharmacological Data)

1.5 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in distilled water and admin. every 12 h for 14 d in a volume of 0.3 ml/100 g body weight; title comp. used as sulphate

Method (Pharmacological Data)

rats treated with title comp. or saline; NSD 1015 (100 mg/kg i.p.) admin.; after 1 h, rats killed; ventral striatum removed; homogenized; centrifuged; dopamine synthesis measured by quantifying accumulation of L-DOPA using HPLC

Further Details (Pharmacological Data)

NSD 1015: α-hydrazino-m-cresol; L-DOPA: L-dihydroxyphenylalanine; L-DOPA levels measured in 1 d and 1 week withdrawn rats; dopamine synthesis measured as L-DOPA accumulation after inhibition of dihydroxyphenylalanine decarboxylase with NSD 1015

Results

title comp. reduced L-DOPA formation by about 60 percent at 2 h, 24 h and 7 days after last dose; diagram

Reference

Imperato, Assunta; Obinu, M. Carmen; Carta, Giovanna; Mascia, M. Stefania; Casu, M. Antonietta; Gessa, Gian Luigi

European Journal of Pharmacology, 1996 , vol. 317, # 2-3 p. 231 - 237 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transmitter releasing

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

1.5 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in distilled water and admin. every 12 h for 14 d in volume of 0.3 ml/100 g body weight; title comp. used as sulphate

Method (Pharmacological Data)

rats implanted with dialysis tube at level of ventral striata; after 48 h, title comp. or saline admin.; ringer solution pumped; samples collected every 20 min; baseline extracellular dopamine conc. measured using HPLC

Further Details (Pharmacological Data)

baseline dopamine conc. defined as mean value for the samples collected during 2 h preceding the morning treatment; extracellular dopamine conc. in ventral striatum measured during the treatment and during 1 week of withdrawal

Results

title comp. raised dopamine conc. (DC) from 0.43 pmol/40 μl on d 1 to 0.59 pmol/40 μl on d 3; lowered DC rapidly to 0.16 pmol/40 μl on d 5; maintained DC at 0.11 pmol/40 μl on d 7, rest of treatment period and over 7 days of withdrawal; diagrams

Reference

Imperato, Assunta; Obinu, M. Carmen; Carta, Giovanna; Mascia, M. Stefania; Casu, M. Antonietta; Gessa, Gian Luigi

European Journal of Pharmacology, 1996 , vol. 317, # 2-3 p. 231 - 237 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transmitter releasing

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

1.5 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in distilled water and admin. every 12 h for 10 d in volume of 0.3 ml/100 g body weight; title comp. used as sulphate

Method (Pharmacological Data)

rats treated with title comp. and then challenged with 1.5 mg/kg title comp.; ringer solution pumped; samples collected every 20 min; baseline extracellular dopamine conc. measured using HPLC

Further Details (Pharmacological Data)

baseline dopamine conc. defined as mean value for the samples collected during 2 h preceding the morning treatment

Results

challenge dose of title comp. increased baseline dopamine release by 90 percent in title comp. treated rats

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Reference

Imperato, Assunta; Obinu, M. Carmen; Carta, Giovanna; Mascia, M. Stefania; Casu, M. Antonietta; Gessa, Gian Luigi

European Journal of Pharmacology, 1996 , vol. 317, # 2-3 p. 231 - 237 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transmitter releasing

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

1.5 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in distilled water and admin. every 12 h for 2 weeks in volume of 0.3 ml/100 g body weight; title comp. used as sulphate

Method (Pharmacological Data)

rats treated with title comp. and then challenged with 1.5 mg/kg title comp.; ringer solution pumped; samples collected every 20 min; baseline extracellular dopamine conc. measured using HPLC

Further Details (Pharmacological Data)

baseline dopamine conc. defined as mean value for the samples collected during 2 h preceding the morning treatment; extracellular dopamine conc. in ventral striatum measured during the treatment and during 1 week of withdrawal

Results

challenge dose of title comp. increased baseline dopamine release by 50 percent in title comp. treated rats

Reference

Imperato, Assunta; Obinu, M. Carmen; Carta, Giovanna; Mascia, M. Stefania; Casu, M. Antonietta; Gessa, Gian Luigi

European Journal of Pharmacology, 1996 , vol. 317, # 2-3 p. 231 - 237 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)

1.5 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in distilled water and admin. every 12 h for 14 d in volume of 0.3 ml/100 g body weight; title comp. used as sulphate

Method (Pharmacological Data)

rats implanted with dialysis tube at level of ventral striata; after 48 h, title comp. or saline admin.; behavioral response (locomotion, rearing, stereotypy: confined sniffing and licking) measured

Further Details (Pharmacological Data)

behavioral response evaluated by summing the percent of time spent by rats in the performance of behavioral items in 20-min period during 2 h after treatment; behavioral response measured during the treatment and during 1 week of withdrawal

Results

title comp. induced motor activity decreased gradually during treatment; title comp. induced stereotypy increased gradually; diagram

Reference

Imperato, Assunta; Obinu, M. Carmen; Carta, Giovanna; Mascia, M. Stefania; Casu, M. Antonietta; Gessa, Gian Luigi

European Journal of Pharmacology, 1996 , vol. 317, # 2-3 p. 231 - 237 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

drug interaction

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration

0.1 - 6.4 mg/kg

(Pharmacological Data)

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Kind of Dosing (Pharmacological Data)

5.0 mg/kg s.c. naloxone inj. 8.5 h after initiation of dialysis probe perfusion; cumulative doses of title comp. (0, 0.1, 0.4, 1.6, 6.4 mg/kg) follow at 30 min intervals

Exposure Period (Pharmacological Data)

260 min

Method (Pharmacological Data)

in vivo; microdialysis probes inserted into nucleus accumbens resp. striatum, perfused with artificial cerebrospinal fluid; dialysate samples analyzed for dopamine by HPLC; locomotor activity monitored

Further Details (Pharmacological Data)

adult rats 300-350 g; neurochemical and behavioral interactions between naloxone and title compound

Results

dose-dependent increase in extracellular dopamine content in nucleus accumbens and striatum and in locomotor activity, all signicantly attenuated by naloxone

Reference

Schad, Christina A.; Justice, Joseph B.; Holtzmann, Stephen G.

European Journal of Pharmacology, 1995 , vol. 275, # 1 p. 9 - 16 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

dopaminergic

Species or TestSystem (Pharmacological Data)

Sprague-Dawley albino rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

1 mg/kg

Exposure Period (Pharmacological Data)

180 min

Method (Pharmacological Data)

rat weight 200-300 g; dialysis probes implanted into striatum and nucleus accumbens in same rat; modified Dulbecco's phosphate buffer saline solution infusion (1.2 M Ca2+, pH 7.4, 0.8 μl/min); dialysates analyzed

Further Details (Pharmacological Data)

R(+)-8-OH-DPAT (0-1000 μg/kg, s.c.) added 30 min before title compound; measurement of extracellular dopamine levels by HPLC analysis; in vivo investigation of modulation of dopaminergic activity by 5-HT1A receptors

Results

title compound alone induced marked increase of extracellular dopamine in both areas; R(+)-8-OH-DPAT (8-hydroxy-2-(di-n-propylamino)tetralin) (25100 μg/kg) sign. inhibited it in both areas, but 1000 μg/kg had no sign. effect

Reference

Ichikawa; Kurok; Kitchen; Meltzer

European Journal of Pharmacology, 1995 , vol. 287, # 2 p. 179 - 184 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

dopaminergic

Species or TestSystem (Pharmacological Data)

Sprague-Dawley albino rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

1 mg/kg

Exposure Period (Pharmacological Data)

180 min

Method (Pharmacological Data)

rat weight 200-300 g; dialysis probes implanted into striatum and nucleus accumbens in same rat; modified Dulbecco's phosphate buffer saline solution infusion (1.2 M Ca2+, pH 7.4, 0.5 μl/min); dialysates analyzed

Further Details (Pharmacological

R(+)-8-OH-DPAT (50 μg/kg, s.c.) added 25 min, WAY 100,635 (100 μg/kg, s.c.) 30 min before title compound; measurement of extracellular dopamine levels by HPLC analysis; in vivo investigation of modulation of dopaminergic activity by 5-HT1A receptors

Data)

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Results

pretreatment abolished inhibitory effect of R(+)-8-OH-DPAT (8-hydroxy-2-(di-n-propylamino)tetralin) on title compound-induced dopamine level increase in both areas; WAY 100,635 alone did not

Reference

Ichikawa; Kurok; Kitchen; Meltzer

European Journal of Pharmacology, 1995 , vol. 287, # 2 p. 179 - 184 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neuroregulatoric

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Concentration (Pharmacological Data)

5 μmol/l

Method (Pharmacological Data)

in vitro; incubation of <7-3H>dopamine with synaptosomal suspension from rat (weighing ca. 200 g) striatum for 30 min; during the 80-100 min title comp. admin. with the perfusion buffer and <3H>dopamine measured

Further Details (Pharmacological Data)

Krebs-Ringer buffer; 37 deg C; pH 7.4

Results

increased release of dopamine

Reference

Pettersson

European Journal of Pharmacology, 1995 , vol. 282, # 1-3 p. 131 - 135 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neuroregulatoric

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Concentration (Pharmacological Data)

5 μmol/l

Method (Pharmacological Data)

in vitro; incubation of 5-<1,2-3H>serotonin creatinine sulphate with synaptosomal suspension from rat (weighing ca. 200 g) frontal cortex for 30 min; during the 80-100 min title comp. admin. with the perfusion buffer and <3H>serotonin measured

Further Details (Pharmacological Data)

Krebs-Ringer buffer; 37 deg C; pH 7.4

Results

increased release of serotonin

Reference

Pettersson

European Journal of Pharmacology, 1995 , vol. 282, # 1-3 p. 131 - 135 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neuroregulatoric

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Method (Pharmacological Data)

in vitro; effect of title comp. on uptake of L-<7-3H>noradrenaline in synaptosomal suspension from rat (weighing 200-300 g) cortex; incubation: 37 deg C, 10 min

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological

0.076 μmol/l

Data)

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Reference

Pettersson

European Journal of Pharmacology, 1995 , vol. 282, # 1-3 p. 131 - 135 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neuroregulatoric

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Method (Pharmacological Data)

in vitro; effect of title comp. on uptake of <7-3H>dopamine in synaptosomal suspension from rat (weighing 200-300 g) striatum; incubation: 37 deg C, 5 min

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

0.18 μmol/l

Reference

Pettersson

European Journal of Pharmacology, 1995 , vol. 282, # 1-3 p. 131 - 135 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neuroregulatoric

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Method (Pharmacological Data)

in vitro; effect of title comp. on uptake of <3H>serotonin in synaptosomal suspension from rat (weighing 200-300 g) frontal cortex; incubation: 37 deg C, 5 min

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

4.9 μmol/l

Reference

Pettersson

European Journal of Pharmacology, 1995 , vol. 282, # 1-3 p. 131 - 135 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Endpoint of Effect (Pharmacological Data)

gnawing in 50 percent of mice

Species or TestSystem (Pharmacological Data)

C57BL/6J mouse

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

0 - 40 mg/kg

Kind of Dosing (Pharmacological Data)

as sulfonate

Method (Pharmacological

in vivo; 21-to 32-g mice housed in groups of 4 in dimly illuminated and quiet testing room with free access to food and water; gnawing upon corrugated packing paper was behavioral measure (8 mice per dose, 75 min after drug administration)

Data)

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Type (Pharmacological Data)

ED50

Value of Type (Pharmacological Data)

6.6 mg/kg

Results

graded and quantal dose-response curves; produced dose-dependent increase in gnawing (max. effect at 7.5 mg/kg)

Reference

Tirelli; Witkin

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 273, # 1 p. 7 - 16 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

Saimiri sciureus, squirrel monkey

Sex

male

Route of Application

intramuscular

Concentration (Pharmacological Data)

0.03 - 1 mg/kg

Kind of Dosing (Pharmacological Data)

as sulfate

Method (Pharmacological Data)

4 adult animals (921-992 g) housed individually in temp- and humidity-controlled room with 12-h light/dark cycle and unrestricted access to food and water; behaviour of monkeys was observed and recorded at determined times

Results

dose-response curve; produced dose-related decreases in scratching

Reference

Pellon; Flores; Alling; Witkin; Katz

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 273, # 1 p. 138 - 145 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

agonist

Species or TestSystem (Pharmacological Data)

Sprague-Dawley albino rat

Sex

male

Route of Application

intravenous

Concentration (Pharmacological Data)

2 - 4 mg/kg

Method (Pharmacological Data)

chloral hydrate-anesthetized rats weighing 100 to 350 g; single unit recording technique; experiments with or without p-chlorophenylalanine (PCPA) methyl ester (1350 mg/kg, i.p.)-pretreatment

Further Details (Pharmacological Data)

firing rate histogram

Results

inhibition of substantia nigra dopamine neurons; no effect of PCPA-pretreatment

Reference

Shi Wei-Xing; Nathaniel; Bunney

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 274, # 2 p. 735 - 740 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neuroregulatoric

Species or TestSystem (Pharmacological Data)

rat forebrain synaptosomes

Concentration

100 - 500 μmol/l

(Pharmacological Data)

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Kind of Dosing (Pharmacological Data)

as sulphate

Method (Pharmacological Data)

in vitro release of 5HT, DA or NA from synaptosomes; forebrains removed from male Sprague-Dawley rats; Krebs buffer containing 10 μM pargyline and 1 μM diclofensine; 37 deg C; incubation time 15 min; endogenous amines conc. in synaptosomes determined

Further Details (Pharmacological Data)

HPLC

Results

was effective in reduction endogenous 5HT, DA, and NA content

Reference

Bondiolotti; Galva; Villa; Sciaba; Picotti

Biochemical Pharmacology, 1995 , vol. 50, # 1 p. 97 - 102 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neuroregulatoric

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

5 mg/kg

Kind of Dosing (Pharmacological Data)

once daily for 5 days; as sulfate salt

Method (Pharmacological Data)

200- to 225 g rats; in vivo single cell recording to determine efficacy of iontophoretically administered glutamate in altering the firing of ventral segmental area (VTA) DA neurons

Further Details (Pharmacological Data)

nucleus accumbens/NAc neurons assayed on 3rd day after last injection

Results

current-response curves and histograms; significantly enhanced responsiveness of VTA DA neurons to glutamate; NAc neurons were significantly less sensitive to rate-enhancing effects of glutamate

Reference

White; Hu; Zhang; Wolf

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 273, # 1 p. 445 - 454 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

psychostimulant

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

3.25 - 30 μmol/kg

Kind of Dosing (Pharmacological Data)

as sulfate

Method (Pharmacological Data)

in vivo; adult rats (240-270g), individually housed in clear plastic cages; 12 h light/dark cycle, with food and water ad lib.; observed and behaviorally rated before and after injection; sacrificed 3 h after dose

Further Details (Pharmacological Data)

brains were removed and sectioned for in situ hybridization histochemistry

Results

clear dose-related responsiveness of zif/268 and preprodynorphin gene expression in cortical and/or striatal neurons positively correlated with dosedependent motor-stimulating effect of title comp.

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Reference

Wang; McGinty

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 273, # 2 p. 909 - 917 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

subcutaneous

Concentration (Pharmacological Data)

0.5 - 5 mg/kg

Kind of Dosing (Pharmacological Data)

in saline in a volume of 1 ml/kg body weight

Method (Pharmacological Data)

rats (280-300 g) were cannulated; pretreatment with reserpine (2.5 mg/kg, i.p.), behavioral measures of locomotion were recorded automatically; saline control

Further Details (Pharmacological Data)

determination of locomotor activity

Results

title comp. induced locomotor activation was significantly and dose dependent decreased by reserpin-pretreatment

Reference

Florin; Kuczenski; Segal

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 274, # 1 p. 231 - 241 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

releasing hormones

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

0.5 - 5 mg/kg

Kind of Dosing (Pharmacological Data)

in saline in a volume of 1 ml/kg body weight

Method (Pharmacological Data)

rats (280-300 g) were cannulated; pretreatment with reserpine (RES, 2.5 mg/kg, i.p.), collected dialysis probes; add. of clorgyline (CLOR, 3.0 mg/kg, i.p.) before administration of title comp.; HPLC

Further Details (Pharmacological Data)

determination of norepinephrine (NE) in hippocampus or dopamine (DA) in caudate-putament levels vs. min and doses; determination of DA metabolites 3,4-dihydroxyphenylacetic acid (DOPAC), homovanillic acid (HVA) and 5-hydroxyindoleacetic acid (5-HIAA)

Results

title comp. dose dependently increased extracellular NE and DA; RES-pretreatment prevented NE response and at dose 0.5 or 5.0 attenuated DA increase (at dose 1.25 no change); HVA increased, DOPAC decreased and RES-pretreatment increased these effects

Reference

Florin; Kuczenski; Segal

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 274, # 1 p. 231 - 241 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

Wistar rats

Sex

female

Route of Application

intraperitoneal

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Concentration (Pharmacological Data)

0.56 mg/kg

Method (Pharmacological Data)

animals pretreated with title comp.; 20 min later after title comp treatment, PD 128907 administered (0.001-0.1 mg/kg/s.c.) immediately before a 30 min locomotor activity measurement (LMA)

Results

title comp.-induced increase in rat LMA was dose-dependent inhibited by PD 128907

Reference

Pugsley; Davis; Akunne; Mackenzie; Shih; Damsma; Wikstrom; Whetzel; Georgic; Cooke; Demattos; Corbin; Glase; Wise; Dijkstra; Heffner

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 275, # 3 p. 1355 - 1366 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

sensitization

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

0.5 mg/kg

Kind of Dosing (Pharmacological Data)

once daily for 5 days; as sulphate

Method (Pharmacological Data)

225- to 275-g rats; 3 days after the end of title comp. administrations place conditioning in response to cocaine was conducted

Results

treated rats showed significantly enhanced sensitivity to development of cocaine-induced place preferences

Reference

Shippenberg; Heidbreder

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 273, # 2 p. 808 - 815 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)

0.032 - 3.2 mg/kg

Kind of Dosing (Pharmacological Data)

as sulfate; administered cumulatively (0.032-3.2 mg/kg) within discrimination session

Method (Pharmacological Data)

in vivo; 8-12 rats (mean 330g) trained to discriminate two doses of midazolam 0.32 and 3.2 mg/kg s.c., from no-drug under three-lever multiple-trials procedure (15 min time out, 5 min fixed-ratio-10 schedule of food reinforcement)

Further Details (Pharmacological Data)

generalization gradient for title comp. generated for cumulative treatment

Results

produced a group mean 85 percent to 100 percent no-drug lever responding

Reference

Sannerud; Ator

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 272, # 1 p. 100 - 111 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

drug substitution: ED50 = 1.69 μmol/kg

Reference

Johnson; Frescas; Oberlender; Nichols

Journal of Medicinal Chemistry, 1991 , vol. 34, # 5 p. 1662 - 1668 Title/Abstract Full Text View citing articles Show Details

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Comment (Pharmacological Data)

effect on sleep architecture, sleep and awakening quality in elderlies

Reference

Saletu; Frey; Krupka; Anderer; Grunberger; Barbanoj

Arzneimittel-Forschung/Drug Research, 1989 , vol. 39, # 10 p. 1268 - 1273 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

reversible inhibition of bovine liver monoamine oxidase B, chirality influence

Reference

Smith, Roger A.; White, Robert L.; Krantz, Allen

Journal of Medicinal Chemistry, 1988 , vol. 31, # 8 p. 1558 - 1566 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

activity as inhibitor of PMNT (Ki): 422 μM

Reference

Grunewald; Ye

Journal of Medicinal Chemistry, 1988 , vol. 31, # 10 p. 1984 - 1986 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

reverses the tetrabenazine induced inhibition of the conditioned reflex, ED 50: ca. 0.15 mg/kg ( i.p., rats); enhancement of the tryptamine effects, ED 50: 2.1 mg/kg (i.p., rats)

Reference

Jahn; Adrian; Ismail; Michos

Arzneimittel-Forschung/Drug Research, 1983 , vol. 33, # 5 p. 726 - 730 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

inhibition of norepinephrine N-methyltransferase (NMT)

Reference

Grunewald, Gary L.; Monn, James A.; Rafferty, Michael F,; Borchardt, Ronald T.; Krass, Polina

Journal of Medicinal Chemistry, 1982 , vol. 25, # 10 p. 1248 - 1250 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

norepinephrine N-methyltransferase (NMT) inhibition constant

Reference

Rafferty, Michael F.; Wilson, David S.; Monn, James A.; Krass, Polina; Borchardt, Ronald T.; Grunewald, Gary L.

Journal of Medicinal Chemistry, 1982 , vol. 25, # 10 p. 1198 - 1204 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

affinity for the serotonin receptor (rat stomach fundus preparation)

Reference

Glennon; Liebowitz; Anderson III

Journal of Medicinal Chemistry, 1980 , vol. 23, # 3 p. 294 - 299 Title/Abstract Full Text View citing articles Show Details

Other Data Use (178) Use Pattern

Location

Reference

Pharmaceuticals

Page/Page column title page; 26

CONCERT PHARMACEUTICALS, INC.; TUNG, Roger D.; GRAHAM, Philip B.

Patent: WO2017/20016 A1, 2017 ;

Page/Page column title page; 26

CONCERT PHARMACEUTICALS, INC.; TUNG, Roger D.; GRAHAM, Philip B.

Patent: WO2017/20016 A1, 2017 ;

Page/Page column title page; 26

CONCERT PHARMACEUTICALS, INC.; TUNG, Roger D.; GRAHAM, Philip B.

Patent: WO2017/20016 A1, 2017 ;

Page/Page column 32

GOSFORTH CENTRE (HOLDINGS) PTY LTD.; BIRD, Philip

Patent: US2016/815 A1, 2016 ;

attention deficit hyperactive disorder (ADHD)

treatment of attention deficit disorder (ADD)

Alzheimer's disease

Title/Abstract Full Text Show Details

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Pharmaceuticals

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GOSFORTH CENTRE (HOLDINGS) PTY LTD.; BIRD, Philip

Patent: US2016/815 A1, 2016 ; Title/Abstract Full Text Show Details

dementia

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GOSFORTH CENTRE (HOLDINGS) PTY LTD.; BIRD, Philip

Patent: US2016/815 A1, 2016 ; Title/Abstract Full Text Show Details

mild cognitive impairment

Page/Page column 32

GOSFORTH CENTRE (HOLDINGS) PTY LTD.; BIRD, Philip

Patent: US2016/815 A1, 2016 ; Title/Abstract Full Text Show Details

treating a psychiatric disorder in combination with antiepileptic agent

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Anti-obesity agent

Page/Page column 55

GOSFORTH CENTRE (HOLDINGS) PTY LTD.; BIRD, Philip

Patent: US2016/815 A1, 2016 ; Title/Abstract Full Text Show Details

AUSPEX PHARMACEUTICAL, INC.; GANT, Thomas, G.; SHAHBAZ, Manoucherhr

Patent: WO2010/48358 A2, 2010 ; Title/Abstract Full Text Show Details

Appetite-regulating agent

Page/Page column 55

AUSPEX PHARMACEUTICAL, INC.; GANT, Thomas, G.; SHAHBAZ, Manoucherhr

Patent: WO2010/48358 A2, 2010 ; Title/Abstract Full Text Show Details

Obesity

Page/Page column 55

AUSPEX PHARMACEUTICAL, INC.; GANT, Thomas, G.; SHAHBAZ, Manoucherhr

Patent: WO2010/48358 A2, 2010 ; Title/Abstract Full Text Show Details

anti-obesity agent

Washburn, William; Meng, Wei

Patent: US2006/63722 A1, 2006 ; Title/Abstract Full Text Show Details

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

bulimia

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

disorder associated with excessive food intake

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

obesity related disorders

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

overeating

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

hypertension

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ;

Title/Abstract Full Text Show Details

diabetes

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

elevated plasma insulin concentrations

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

insulin resistance

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

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dyslipidemias

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

hyperlipidemia

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

endometrial cancer

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

breast cancer

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

prostate cancer

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

colon cancer

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

osteoarthritis

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

obstructive sleep apnea

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

gallstones

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

abnormal heart rhythms

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

heart arrythmias

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

myocardial infarction

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

congestive heart failure

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

coronary heart disease

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

sudden death

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

stroke

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

polycystic ovarian disease

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

craniopharyngioma

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

the Prader-Willi Syndrome

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

Frohlich's syndrome

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

GH-deficient subjects

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

normal variant short stature

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

Turner's syndrome

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.;

MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ;

Title/Abstract Full Text Show Details

metabolic syndrome

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

maintaining weight loss

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

obesity

Amatruda, John M.; Daruwala, Paul; Erondu, Ngozi E.; MacNeil, Douglas J.; Moller, David E.; Qian, Su

Patent: US2008/64632 A1, 2008 ; Title/Abstract Full Text Show Details

Central nervous system stimulants

INTRA-CELLULAR THERAPIES, INC.

Patent: WO2008/63505 A1, 2008 ; Title/Abstract Full Text Show Details

in combination with dapagliflozin or its propylene glycol hydrate

Bristol-Myers Squibb

Patent: US2008/234366 A1, 2008 ; Title/Abstract Full Text Show Details

anorectic agent

Bristol-Myers Squibb

Patent: US2008/234366 A1, 2008 ; Title/Abstract Full Text Show Details

antiobesity agent

NOVO NORDISK A/S

Patent: WO2006/40329 A1, 2006 ; Title/Abstract Full Text Show Details

Bristol-Myers Squibb

Patent: US2008/234366 A1, 2008 ; Title/Abstract Full Text Show Details

pyschostimulant

GOSFORTH CENTRE (HOLDINGS) PTY LTD

Patent: WO2008/95221 A1, 2008 ; Title/Abstract Full Text Show Details

attention-deficit hyperactivity disorder (ADHD)

GOSFORTH CENTRE (HOLDINGS) PTY LTD

Patent: WO2008/95221 A1, 2008 ; Title/Abstract Full Text Show Details

sympathomimetic agent

Hellstrom, Harold Richard

Patent: US2007/37797 A1, 2007 ; Title/Abstract Full Text Show Details

Therapeutic agent for an orally-dissolvable, edible film

Maibach, Todd

Patent: US2007/59346 A1, 2007 ; Title/Abstract Full Text Show Details

Attention deficit hyperactivity disorder

Maibach, Todd

Patent: US2007/59346 A1, 2007 ; Title/Abstract Full Text Show Details

Appetite regulating agent

IRM LLC

Patent: WO2007/89557 A2, 2007 ; Title/Abstract Full Text Show Details

IRM LLC

Patent: WO2007/89667 A1, 2007 ;

Title/Abstract Full Text Show Details

adrenoceptor agonist

BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG

Patent: WO2007/93624 A2, 2007 ; Title/Abstract Full Text Show Details

Attention Deficit Hyperactivity Disorder (ADHD)

BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG

Patent: WO2007/93624 A2, 2007 ; Title/Abstract Full Text Show Details

Attention Deficit Hyperactivity Disorder (ADHD) predominantly impulsivity type

BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG

Patent: WO2007/93624 A2, 2007 ; Title/Abstract Full Text Show Details

Attention Deficit Hyperactivity Disorder (ADHD) predominantly inattentive type

BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG

Patent: WO2007/93624 A2, 2007 ; Title/Abstract Full Text Show Details

Attention Deficit Hyperactivity Disorder (ADHD) predominantly hyperactive-impulsive type

BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG

Patent: WO2007/93624 A2, 2007 ; Title/Abstract Full Text Show Details

Attention Deficit Hyperactivity Disorder (ADHD) predominantly not otherwise specified

BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG

Patent: WO2007/93624 A2, 2007 ; Title/Abstract Full Text Show Details

Attention Deficit Disorder (ADD)

BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG

Patent: WO2007/93624 A2, 2007 ; Title/Abstract Full Text Show Details

Anti-obesity agent

NOVARTIS AG; NOVARTIS PHARMA GmbH

Patent: WO2007/41366 A1, 2007 ; Title/Abstract Full Text Show Details

Bristol-Myers Squibb Company

Patent: US2007/99913 A1, 2007 ; Title/Abstract Full Text Show Details

IRM LLC

Patent: WO2007/89557 A2, 2007 ; Title/Abstract Full Text Show Details

IRM LLC

Patent: WO2007/89667 A1, 2007 ; Title/Abstract Full Text Show Details

Sher, Philip; Wu, Gang; Stouch, Terry; Ellsworth, Bruce

Patent: US2004/2495 A1, 2004 ; Title/Abstract Full Text Show Details

eating disorders

CNS Response

Patent: US2005/96311 A1, 2005 ; Title/Abstract Full Text Show Details

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

Anorectic agent

Washburn, William; Meng, Wei

Patent: US2006/63722 A1, 2006 ; Title/Abstract Full Text Show Details

cause release of norepinephrine

Davis, Michael; Ressler, Kerry J.; Chhatwal, Jasmeer P.;

McDevitt, Jason P.

Patent: US2006/84659 A1, 2006 ;

Title/Abstract Full Text Show Details

pharmacologic agent increases the level of norepinephrine in the brain

Davis, Michael; Ressler, Kerry J.; Chhatwal, Jasmeer P.; McDevitt, Jason P.

Patent: US2006/84659 A1, 2006 ; Title/Abstract Full Text Show Details

Anti-obezity agent

Meng, Wei; Hamann, Lawrence G.; Brigance, Robert

Patent: US2006/142576 A1, 2006 ; Title/Abstract Full Text Show Details

Dopamine releasing compound co-administered in compositions containing mirtazapine to reduce side effects of mirtazapine, such as excessive daytime sleepness, sedation and weight gain

CNS disorders

CYPRESS BIOSCIENCE, INC.

Patent: WO2006/55854 A2, 2006 ; Title/Abstract Full Text Show Details

KETOCYTONYX INC.

Patent: WO2006/34361 A2, 2006 ; Title/Abstract Full Text Show Details

Parkinson's disease

KETOCYTONYX INC.

Patent: WO2006/34361 A2, 2006 ; Title/Abstract Full Text Show Details

autism

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

compulsivity

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

impulsivity

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

Asperger's syndrome

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

attention deficit disorder

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

attention deficit hyperactivity disorder

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

obsessive-compulsive disorder

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

Tourette's syndrome

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

body dismorphic disorder

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

hypochondriasis

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ;

Title/Abstract Full Text Show Details

impulse control disorders

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

paraphilias sexual addictions

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

nonparaphilic sexual addictions

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

Sydeham's chorea

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

torticollis

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

intermittent explosive disorder

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

kleptomania

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

pathological gambling

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

pyromania

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

compulsive shopping

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

compulsive buying

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

repetitive self-mutilation

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

onychophagia

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

psychogenic excoriation

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

trichotillomania

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ;

Title/Abstract Full Text Show Details

anorexia nervosa

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

binge eating

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

sexual compulsion

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

alcohol and substance use disorders

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

neurological disorders with disinhibition or frontal lobe deficits

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

bipolar disorder

MOUNT SINAI SCHOOL OF MEDICINE

Patent: WO2006/34187 A2, 2006 ; Title/Abstract Full Text Show Details

childhood onset bipolar disorder