N-(1-phenylcyclohexyl)piperidine [PCP] by Asch

Reaxys

PubChem

eMolecules

Reactions (40)

Substances (7)

Structure

Citations (453)

Structure/Compound Data Chemical Name: Phencyclidine Reaxys Registry Number: 1287039

CAS Registry Number: 77-10-1 Type of Substance: heterocyclic Molecular Formula: C17H25N Linear Structure Formula: C17H25N Molecular Weight: 243.392

InChI Key: JTJMJGYZQZDUJJ-UHFFFAOYSA-N

N° of preparations All Preps | All Reactions 11 prep out of 33 reactions.

Available Data

N° of ref.

Identification Physical Data (30) Spectra (40) Bioactivity (220) Use/Application (54)

381

Synthesize | Hide Details Find similar Chemical Names and Synonyms Phencyclidine, N-(1-phenylcyclohexyl)piperidine, phencyclidine, Sernyl.(R)., PCP, 1-[1-(phenylcyclohexyl)]piperidine, 1-(1-phenylcyclohexyl) piperidine Identification Substance Label (11) Label

Reference

PCP

Wessinger, William D.

European Journal of Pharmacology, 1995 , vol. 277, # 1 p. 107 - 112 Title/Abstract Full Text View citing articles Show Details

Haradahira, Terushi; Sasaki, Sigeki; Maeda, Minoru; Kobayashi, Kaoru; Inoue, Osamu; Tomita, Urara; Nishikawa, Toru; Suzuki, Kazutoshi

Journal of Labelled Compounds and Radiopharmaceuticals, 1998 , vol. 41, # 9 p. 843 - 858 Title/Abstract Full Text View citing articles Show Details

Nakahara; Takahashi; Kikura

Biological and Pharmaceutical Bulletin, 1995 , vol. 18, # 9 p. 1223 - 1227 Title/Abstract Full Text View citing articles Show Details

Maurel-Remy; Bervoets; Millan

European Journal of Pharmacology, 1995 , vol. 280, # 2 p. R9-R11 Title/Abstract Full Text View citing articles Show Details

Peruche; Klaassens; Krieglstein

Pharmacology, 1995 , vol. 50, # 4 p. 229 - 237 Title/Abstract Full Text View citing articles Show Details

Fryer, John D.; Lukas, Ronald J.

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 288, # 1 p. 88 - 92 Title/Abstract Full Text View citing articles Show Details

Palmer; Stagnitto; Garske; Napier; Harris; Kaiser; Griffith; Woodhead; White; Wolf; Swinyard

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 273, # 3 p. 1023 - 1031 Title/Abstract Full Text View citing articles Show Details

Silverthorn; Dersch; Baumann; Cadet; Partilla; Rice; Carroll; Becketts; Brockington; Rothman

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 273, # 1 p. 213 - 222 Title/Abstract Full Text View citing articles Show Details

Ali, S. F.; Newport, G. D.; Bracha, H. S.

Neurotoxicology and Teratology, 1994 , vol. 16, # 4 p. 335 - 342 Title/Abstract Full Text View citing articles Show Details

French

Neurotoxicology and Teratology, 1994 , vol. 16, # 4 p. 355 - 362 Title/Abstract Full Text View citing articles Show Details

Sircar, Ratna; Li, Chang-Sheng

Neurotoxicology and Teratology, 1994 , vol. 16, # 4 p. 369 - 376 Title/Abstract Full Text View citing articles Show Details

Sayre; Engelhart; Nadkarni; Babu; Klein; McCoy

Xenobiotica, 1995 , vol. 25, # 7 p. 769 - 775 Title/Abstract Full Text View citing articles Show Details

Okuyama, Shigeru; Chaki, Shigeyuki; Yae, Tetsuji; Nakazato, Atsuro; Muramatsu, Makoto

Life Sciences, 1995 , vol. 57, # 21 p. PL333-PL337 Title/Abstract Full Text View citing articles Show Details

Rothman; Silverthorn; Baumann; Goodman; Cadet; Matecka; Rice; Carroll; Wang; Uhl; Partilla; Dersch

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 274, # 1 p. 385 - 395 Title/Abstract Full Text View citing articles Show Details

Lurtz, Monica M.; Pedersen, Steen E.

Molecular Pharmacology, 1999 , vol. 55, # 1 p. 159 - 167 Title/Abstract Full Text View citing articles Show Details

Yonezawa; Kuroki; Tashiro; Hondo; Uchimura

European Journal of Pharmacology, 1995 , vol. 285, # 3 p. 305 - 308 Title/Abstract Full Text View citing articles Show Details

Noda, Yukihiro; Yamada, Kiyofumi; Komori, Yumiko; Sugihara, Hisayoshi; Furukawa, Hiroshi; Nabeshima, Toshitaka

British Journal of Pharmacology, 1996 , vol. 117, # 7 p. 1579 - 1585 Title/Abstract Full Text View citing articles Show Details

Ishii, Akira; Seno, Hiroshi; Watanabe-Suzuki, Kanako; Kumazawa, Takeshi; Matsushima, Hajime; Suzuki, Osamu; Katsumata, Yoshinao

Analytical Chemistry, 2000 , vol. 72, # 2 p. 404 - 407 Title/Abstract Full Text View citing articles Show Details

Anderson; Williams; Pauly; Raszkiewicz; Campbell; Rotert; Surber; Thomas; Wasicak; Arneric; Sullivan

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Jin, Jingji; Yamamoto, Tsuneyuki; Watanabe, Shigenori

European Journal of Pharmacology, 1997 , vol. 319, # 2-3 p. 147 - 152 Title/Abstract Full Text View citing articles Show Details

Etou; Kuroki; Tatebayashi; Tashiro; Hirano

Biochemical Pharmacology, 1996 , vol. 51, # 1 p. 83 - 86 Title/Abstract Full Text View citing articles Show Details

Kamei, Hiroyuki; Kameyama, Tsutomu; Nabeshima, Toshitaka

European Journal of Pharmacology, 1996 , vol. 299, # 1-3 p. 21 - 28 Title/Abstract Full Text View citing articles Show Details

Sagi, Naoki; Yamamoto, Hideko; Yamamoto, Toshifumi; Okuyama, Shigeru; Moroji, Takashi

European Journal of Pharmacology, 1996 , vol. 304, # 1-3 p. 185 - 190 Title/Abstract Full Text View citing articles Show Details

Boireau, Alain; Malgouris, Christiane; Burgevin, Marie-Claude; Peny, Colette; Durand, Gabrielle; Bordier, Francoise; Meunier, Mireille; Miquet, Jean Marie; Daniel, Marc; Chevet, Thierry; Jimonet, Patrick; Mignani, Serge; Blanchard, Jean-Charles; Doble, Adam

European Journal of Pharmacology, 1996 , vol. 300, # 3 p. 237 - 246 Title/Abstract Full Text View citing articles Show Details

Hutson, Peter H.; Hogg, Joanne E.

European Journal of Pharmacology, 1996 , vol. 295, # 1 p. 45 - 52 Title/Abstract Full Text View citing articles Show Details

Krebs-Thomson, Kirsten; Lehmann-Masten, Virginia; Naiem, Shahrouz; Paulus, Martin P.; Geyer, Mark A.

European Journal of Pharmacology, 1998 , vol. 343, # 2-3 p. 135 - 143 Title/Abstract Full Text View citing articles Show Details

Wu, Yan-Na; Johnson, Steven W.

Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 279, # 2 p. 457 - 463 Title/Abstract Full Text View citing articles Show Details

Hu, Ping-Sheng; Ross, Svante B.

Pharmacology and Toxicology, 1997 , vol. 80, # 2 p. 97 - 102 Title/Abstract Full Text View citing articles Show Details

Witkin, Jeffrey M.; Steele, Thomas D.; Sharpe, Lawrence G.

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 280, # 1 p. 46 - 52 Title/Abstract Full Text View citing articles Show Details

Chan, Susan L.F.; Pallett, Anna L.; Clews, John; Ramsden, Christopher A.; Morgan, Noel G.

European Journal of Pharmacology, 1997 , vol. 323, # 2-3 p. 241 - 244 Title/Abstract Full Text View citing articles Show Details

Hendrickson, Howard P.; Whaley, E. Cathrine; Owens, S. Michael

Journal of Mass Spectrometry, 2005 , vol. 40, # 1 p. 19 - 24 Title/Abstract Full Text View citing articles Show Details

Wang, Cheng; Kaufmann, Joel A.; Sanchez-Ross, Monica G.; Johnson, Kenneth M.

Journal of Pharmacology and Experimental Therapeutics, 2000 , vol. 294, # 1 p. 287 - 295 Title/Abstract Full Text View citing articles Show Details

Huerta-Fontela, Maria; Galceran, Maria Teresa; Ventura, Francesc

Environmental Science and Technology, 2008 , vol. 42, # 18 p. 6809 - 6816 Title/Abstract Full Text View citing articles Show Details

Hamouda, Ayman K.; Stewart, Deirdre S.; Chiara, David C.; Savechenkov, Pavel Y.; Bruzik, Karol S.; Cohen, Jonathan B.

Molecular Pharmacology, 2014 , vol. 85, # 5 p. 735 - 746 Title/Abstract Full Text View citing articles Show Details

Swedberg, Michael D.B.; Raboisson, Patrick

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Hamaguchi, Wataru; Masuda, Naoyuki; Miyamoto, Satoshi; Shiina, Yasuhiro; Kikuchi, Shigetoshi; Mihara, Takuma; Moriguchi, Hiroyuki; Fushiki, Hiroshi; Murakami, Yoshihiro; Amano, Yasushi; Honbou, Kazuya; Hattori, Kouji

Bioorg. Med. Chem., 2015 , vol. 23, # 2 p. 297 - 313 Title/Abstract Full Text View citing articles Show Details

Wallach, Jason; Kang, Heather; Colestock, Tristan; Morris, Hamilton; Bortolotto, Zuner A.; Collingridge, Graham L.; Lodge, David; Halberstadt, Adam L.; Brandt, Simon D.; Adejare, Adeboye

PLoS ONE, 2016 , vol. 11, # 6 art. no. E0157021 Title/Abstract Full Text View citing articles Show Details

Ahmadi, Abbas; Khalili, Mohsen; Barzin, Mahnaz; Pooladi, Mohsen; Bakhtiari, Fatemeh; Barjeste, Maede; Nahri-Niknafs, Babak

Monatshefte fur Chemie, 2016 , vol. 147, # 2 p. 457 - 464 Title/Abstract Full Text View citing articles Show Details

Grimm, Stefanie H.; Höfner, Georg; Wanner, Klaus T.

ChemMedChem, 2015 , vol. 10, # 6 p. 1027 - 1039 Title/Abstract Full Text View citing articles Show Details

phencyclidine

THE GENERAL HOSPITAL CORPORATION; PETERSON, Randall T.; RENNEKAMP, Andrew J.; KOKEL, David

Patent: WO2015/200674 A1, 2015 ; Title/Abstract Full Text Show Details

Prashad, Mahavir; Liu, Yugang; Har, Denis; Repic, Oljan; Blacklock, Thomas J.

Tetrahedron Letters, 2005 , vol. 46, # 33 p. 5455 - 5458 Title/Abstract Full Text View citing articles Show Details

Koehler, Jens; Bergander, Klaus; Fabian, Joerg; Schepmann, Dirk; Wuensch, Bernhard

Journal of Medicinal Chemistry, 2012 , vol. 55, # 20 p. 8953 - 8957 Title/Abstract Full Text View citing articles Show Details

Jozwiak, Krzysztof; Ravichandran, Sarangan; Collins, Jack R.; Moaddel, Ruin; Wainer, Irving W.

Journal of Medicinal Chemistry, 2007 , vol. 50, # 24 p. 6279 - 6283 Title/Abstract Full Text View citing articles Show Details

Phen

Campbell, Cory M.; Butelman, Eduardo R.; Woods, James H.

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 289, # 1 p. 521 - 527 Title/Abstract Full Text View citing articles Show Details

Merck 7364

Eshleman; Neve; Janowsky

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 274, # 1 p. 276 - 283 Title/Abstract Full Text View citing articles Show Details

Washburn, Mark S.; Dingledine, Raymond

Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 278, # 2 p. 669 - 678 Title/Abstract Full Text View citing articles Show Details

PCP (Merck 7364)

Roth, Jane E.; Murray, Thomas F.; Franklin, Paul H.

Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 277, # 3 p. 1823 - 1836 Title/Abstract Full Text View citing articles Show Details

Klarica, Marijan; Fage, Dominique; Carter, Chris

European Journal of Pharmacology, 1996 , vol. 308, # 2 p. 135 - 144 Title/Abstract Full Text View citing articles Show Details

M 7364

Souverbie; Mo; Liu; von Euler; Sundstr-om

European journal of pharmacology, 1996 , vol. 307, # 3 p. 347 - 353 Title/Abstract Full Text View citing articles Show Details

PCP, Merck 7364

Gandolfo, Gabriel; Lambeau, Gerard; Lazdunski, Michel; Gottesmann, Claude

Pharmacology and Toxicology, 1996 , vol. 78, # 5 p. 341 - 347 Title/Abstract Full Text View citing articles Show Details

Derivative (18) Comment (Derivative)

Reference

By formation of salt/complex with HCl. Additional data: 13C-NMR

Kamenka; Michaud; Geneste; et al.

European Journal of Medicinal Chemistry, 1985 , vol. 20, # 5 p. 419 - 424 Title/Abstract Full Text View citing articles Show Details

*HCl: F: 215-216grad (korr.); 1H-NMR; pK(a)

Geneste et al.

European Journal of Medicinal Chemistry, 1979 , vol. 14, p. 301,302 Full Text Show Details

Hydrochlorid: F:Konformation (Roentgenstrukturanalyse)

Bhattacharjee; Chacko

Current Science, 1979 , vol. 48, p. 969 Full Text Show Details

Methoiodid: F: 112-115grad unkorr.

Kalir et al.

European Journal of Medicinal Chemistry, 1978 , vol. 13, p. 17,18 Full Text Show Details

Hydrochlorid;: F: 232-233grad, Vert.koeff. Isooctan/H2O, UV, pK(a)

Kalir et al.

European Journal of Medicinal Chemistry, 1978 , vol. 13, p. 17,18 Full Text Show Details

Hydrobromid: F: 214-218grad

Sokolovsky; Hordeckai

Patent: DE2339342 , 1974 ; Chem.Abstr., vol. 80, # 132908 Full Text Show Details

Hydrochlorid: F: 243-244grad

Sokolovsky; Hordeckai

Patent: DE2339342 , 1974 ; Chem.Abstr., vol. 80, # 132908 Full Text Show Details

HBr-Salz: Kristallstruktur; Bindungslaengen; Bindungswinkel; D: 1.322 gcm-3

Argos et al.

Acta Crystallographica, Section B: Structural Crystallography and Crystal Chemistry, 1970 , vol. 26, p. 53 Full Text Show Details

HCl-Salz: Kristallstruktur; Bindungslaengen; Bindungswinkel; D: 1.110 gcm-3

Argos et al.

Acta Crystallographica, Section B: Structural Crystallography and Crystal Chemistry, 1970 , vol. 26, p. 53 Full Text Show Details

HBr: F: 225-226grad

Parke; Davis

Patent: US3192219 , 1965 ; Chem.Abstr., 1965 , vol. 63, # 9921f Full Text Show Details

HCl: F: 243-244grad

Parke; Davis

Patent: US3192219 , 1965 ; Chem.Abstr., 1965 , vol. 63, # 9921f Full Text Show Details

Hydrobromid, C17H25N*HBr, F: 225-226grad (unkorr.)

Maddox,V.H. et al.

J. Med. Chem., 1965 , vol. 8, p. 230 - 235 Title/Abstract Full Text View citing articles Show Details

Hydrochlorid, C17H25N*HCl, F: 234-234.5grad (unkorr.)

Maddox,V.H. et al.

J. Med. Chem., 1965 , vol. 8, p. 230 - 235 Title/Abstract Full Text View citing articles Show Details

Hydrochlorid, C17H25N*HCl, F: 233-233.5grad (aus Propan-2-ol, unkorr.), UV-Abs.

Maddox,V.H. et al.

J. Med. Chem., 1965 , vol. 8, p. 230 - 235 Title/Abstract Full Text View citing articles Show Details

Pikrat: F:183-184grad

Tanabe

Patent: JP1908767 , 1960 ; Chem.Abstr., 1968 , vol. 69, # 10195f Full Text Show Details

Hydrochlorid: F:228grad

Tanabe

Patent: JP1908767 , 1960 ; Chem.Abstr., 1968 , vol. 69, # 10195f Full Text Show Details

Hydrochlorid: F: 243-244grad (aus MeOH + Et2O)

Parke; Davis and Co.

Patent: US3097136 , 1960 ; Chem.Abstr., 1963 , vol. 59, # 13881 Full Text Show Details

Sernyl hydrochlorid, Kristallstruktur

Barr R. E.

Dissert. Abstr. (B), 27 <1966> 1079, zit. n. Molecular Structure and Dimensions, Vol. 1 <1970> 242 Full Text Show Details

Physical Data Melting Point (3) Melting Point

Solvent (Melting Point)

Reference

45 - 46 °C

ethanol

Johnson, Peter Y.; Pan, Robert; Wen, Jing Quan; Halfman, Clarke J.

Journal of Organic Chemistry, 1981 , vol. 46, # 10 p. 2049 - 2054 Title/Abstract Full Text View citing articles Show Details

44 - 45 °C

Mousseron et al.

Chimica Therapeutica, 1966 , vol. 1, p. 284,286 Full Text Show Details

Geneste et al.

European Journal of Medicinal Chemistry, 1979 , vol. 14, p. 301,302 Full Text Show Details

46 - 46.5 °C

Maddox,V.H. et al.

J. Med. Chem., 1965 , vol. 8, p. 230 - 235 Title/Abstract Full Text View citing articles Show Details

Parke; Davis and Co.

Patent: US3097136 , 1960 ; Chem.Abstr., 1963 , vol. 59, # 13881 Full Text Show Details

Sokolovsky; Hordeckai

Patent: DE2339342 , 1974 ; Chem.Abstr., vol. 80, # 132908 Full Text Show Details

Parke; Davis

Patent: US3192219 , 1965 ; Chem.Abstr., 1965 , vol. 63, # 9921f Full Text Show Details

Boiling Point (5) Boiling Point

Pressure (Boiling Point)

Reference Giannoukos, Stamatios; Brki, Boris; Taylor, Stephen; France, Neil

Journal of the American Society for Mass Spectrometry, 2015 , vol. 26, # 2 p. 231 - 239 Title/Abstract Full Text View citing articles Show Details

136 °C

122 - 127 °C

1 Torr

Mousseron et al.

Chimica Therapeutica, 1966 , vol. 1, p. 284,286 Full Text Show Details

135 - 137 °C

1 Torr

Parke; Davis and Co.

Patent: US3097136 , 1960 ; Chem.Abstr., 1963 , vol. 59, # 13881 Full Text Show Details

Parke; Davis

Patent: US3192219 , 1965 ; Chem.Abstr., 1965 , vol. 63, # 9921f Full Text Show Details

132 - 137 °C

1.5 Torr

Welvart

Comptes Rendus Hebdomadaires des Seances de l'Academie des Sciences, 1960 , vol. 250, p. 1870,1871 Full Text Show Details

118 °C

0.5 Torr

Tanabe

Patent: JP1908767 , 1960 ; Chem.Abstr., 1968 , vol. 69, # 10195f Full Text Show Details

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

Partner (Association (MCS))

Formation constant of a complex

membranes of HEK293 cells expressing α3β2 neuronal nicotinic acetylcholine receptor

Solvent (Association (MCS))

Temperature (Association (MCS))

Reference Jozwiak, Krzysztof; Ravichandran, Sarangan; Collins, Jack R.; Moaddel, Ruin; Wainer, Irving W.

Journal of Medicinal Chemistry, 2007 , vol. 50, # 24 p. 6279 - 6283 Title/Abstract Full Text View citing articles Show Details

Stability constant of the complex with ...

melanin

dimethylsulfoxide aq. phosphate buffer

Stability constant of the complex with ...

β-cyclodextrine

H2O

36 °C

Nakahara; Takahashi; Kikura

Biological and Pharmaceutical Bulletin, 1995 , vol. 18, # 9 p. 1223 - 1227 Title/Abstract Full Text View citing articles Show Details Soon M. Han; Purdie

Analytical Chemistry, 1984 , vol. 56, # 14 p. 2822 - 2825 Title/Abstract Full Text View citing articles Show Details

Circular Dichroism (2) Solvent (Circular Dichroism)

Comment (Circular Dichroism)

Reference

H2O

250 - 285 nm

Soon M. Han; Purdie

Analytical Chemistry, 1984 , vol. 56, # 14 p. 2822 - 2825 Title/Abstract Full Text View citing articles Show Details

H2O

220 - 280 nm

Bowen, John M.; Purdie, Neil

Analytical Chemistry, 1981 , vol. 53, # 14 p. 2239 - 2242 Analytical Chemistry, 1981 , vol. 53, # 14 p. 2239 - 2242 Title/Abstract Full Text View citing articles Show Details

Conformation (3) Object of Investigation

Reference

Conformation

Argos et al.

Acta Crystallographica, Section B: Structural Crystallography and Crystal Chemistry, 1970 , vol. 26, p. 53 Full Text Show Details

Manoharan; Eliel; Carrol; Kenam Jr.

Tetrahedron Letters, 1983 , vol. 24, # 18 p. 1855 - 1858 Title/Abstract Full Text View citing articles Show Details

Zenone; Kamenka

European Journal of Medicinal Chemistry, 1991 , vol. 26, # 7 p. 677 - 686 Title/Abstract Full Text View citing articles Show Details

Iorio; Molinari; Scotti de Carolis; Niglio

Farmaco, Edizione Scientifica, 1984 , vol. 39, # 7 p. 599 - 611 Title/Abstract Full Text View citing articles Show Details

Conformer equilibrium

Zenone; Kamenka

European Journal of Medicinal Chemistry, 1991 , vol. 26, # 7 p. 677 - 686 Title/Abstract Full Text View citing articles Show Details

Kamenka; Chicheportiche

European Journal of Medicinal Chemistry, 1987 , vol. 22, # 3 p. 193 - 197 Title/Abstract Full Text View citing articles Show Details

Energy difference between the conformers

Geneste et al.

European Journal of Medicinal Chemistry, 1979 , vol. 14, p. 301,302 Full Text Show Details

Kamenka; Chicheportiche

European Journal of Medicinal Chemistry, 1987 , vol. 22, # 3 p. 193 - 197 Title/Abstract Full Text View citing articles Show Details

Dissociation Exponent (2) Dissociation Exponent (pK)

Type (Dissociation Exponent)

8.7

a1/apparent

Huerta-Fontela, Maria; Galceran, Maria Teresa; Ventura, Francesc

Environmental Science and Technology, 2008 , vol. 42, # 18 p. 6809 - 6816 Title/Abstract Full Text View citing articles Show Details

a1/apparent

Earley; Kumar; Mallamo; Subramanyam; Dority Jr.; Miller; DeHaven-Hudkins; Aimone; Kelly; Ault

Journal of Medicinal Chemistry, 1995 , vol. 38, # 18 p. 3586 - 3592 Title/Abstract Full Text View citing articles Show Details

Reference

Electrochemical Behaviour (1) Description (Electrochemical Behaviour)

Reference

Electrolytic dissociation / protonation equilibrium

Earley; Kumar; Mallamo; Subramanyam; Dority Jr.; Miller; DeHaven-Hudkins; Aimone; Kelly; Ault

Journal of Medicinal Chemistry, 1995 , vol. 38, # 18 p. 3586 - 3592 Title/Abstract Full Text View citing articles Show Details

Further Information (5) Description (Further Information)

Reference

Further information

Bhattacharjee; Chacko

Current Science, 1979 , vol. 48, p. 969 Full Text Show Details

Further information

Lin et al.

Biomedical Mass Spectrometry, 1975 , vol. 2, p. 206,212,213 Full Text Show Details

Further information

Fales et al.

Archives of Mass Spectral Data, 1971 , vol. 2, p. 596 Full Text Show Details

Further information

Maddox,V.H. et al.

J. Med. Chem., 1965 , vol. 8, p. 230 - 235 Title/Abstract Full Text View citing articles Show Details

Further information

Barr R. E.

Dissert. Abstr. (B), 27 <1966> 1079, zit. n. Molecular Structure and Dimensions, Vol. 1 <1970> 242 Full Text Show Details

Liquid/Liquid Systems (MCS) (4) Description (Liquid/Liquid Systems (MCS))

Partner (Liquid/Liquid Systems (MCS))

Solvent (Liquid/Liquid Systems (MCS))

Reference

Distribution between solvent 1+2

octanol/buffer pH=7.4

Earley; Kumar; Mallamo; Subramanyam; Dority Jr.; Miller; DeHavenHudkins; Aimone; Kelly; Ault

Journal of Medicinal Chemistry, 1995 , vol. 38, # 18 p. 3586 - 3592 Title/Abstract Full Text View citing articles Show Details

Distribution between solvent 1+2

octanol : water

Hays, Sheryl J.; Novak, Perry M.; Ortwine, Daniel F.; Bigge, Christopher F.; Colbry, Norman L.; et al.

Journal of Medicinal Chemistry, 1993 , vol. 36, # 6 p. 654 - 670 Title/Abstract Full Text View citing articles Show Details

Distribution between solvent 1+2

pH = 7.4

Distribution between solvent 1+2

octanol; H2O

various solvent(s) H2O

Bigge; Malone; Hays; Johnson; Novak; Lescosky; Retz; Ortwine; Probert Jr.; Coughenour; Boxer; Robichaud; Brahce; Shillis

Journal of Medicinal Chemistry, 1993 , vol. 36, # 14 p. 1977 - 1995 Title/Abstract Full Text View citing articles Show Details

Hansch; Bjorkroth; Leo

Journal of Pharmaceutical Sciences, 1987 , vol. 76, # 9 p. 663 - 687 Title/Abstract Full Text View citing articles Show Details

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

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

Reference Huerta-Fontela, Maria; Galceran, Maria Teresa; Ventura, Francesc

Environmental Science and Technology, 2008 , vol. 42, # 18 p. 6809 - 6816 Title/Abstract Full Text View citing articles Show Details

1.9

1.69

Haradahira, Terushi; Sasaki, Sigeki; Maeda, Minoru; Kobayashi, Kaoru; Inoue, Osamu; Tomita, Urara; Nishikawa, Toru; Suzuki, Kazutoshi

Journal of Labelled Compounds and Radiopharmaceuticals, 1998 , vol. 41, # 9 p. 843 - 858 Title/Abstract Full Text View citing articles Show Details

23 °C

Spectra NMR Spectroscopy (30) Description (NMR Spectroscopy)

Nucleus (NMR Spectroscopy)

Solvents (NMR Spectroscopy)

Spectrum

13C

CDCl3

Temperature (NMR Spectroscopy)

Reference Iorio, Maria A.; Tomassini, Lamberto; Mattson, Mariena V.; George, Clifford; Jacobson, Arthur E.

Journal of Medicinal Chemistry, 1991 , vol. 34, # 8 p. 2615 - 2623 Title/Abstract Full Text View citing articles Show Details

Johnson, Peter Y.; Pan, Robert; Wen, Jing Quan; Halfman, Clarke J.

Journal of Organic Chemistry, 1981 , vol. 46, # 10 p. 2049 - 2054 Title/Abstract Full Text View citing articles Show Details

Iorio, Maria A.; Tomassini, Lamberto; Mattson, Mariena V.; George, Clifford; Jacobson, Arthur E.

Journal of Medicinal Chemistry, 1991 , vol. 34, # 8 p. 2615 - 2623 Title/Abstract Full Text View citing articles Show Details

Kamenka; Michaud; Geneste; et al.

European Journal of Medicinal Chemistry, 1985 , vol. 20, # 5 p. 419 424 Title/Abstract Full Text View citing articles Show Details

Katritzky, Alan R.; Najzarek, Zbigniew; Dega-Szafran, Zofia

Synthesis, 1989 , # 1 p. 66 - 69 Title/Abstract Full Text Show Details

Iorio; Molinari; Scotti de Carolis; Niglio

Farmaco, Edizione Scientifica, 1984 , vol. 39, # 7 p. 599 - 611 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

CDCl3

Chemical shifts

13C

dibutyl ether

28.9 °C

Zenone; Kamenka

European Journal of Medicinal Chemistry, 1991 , vol. 26, # 7 p. 677 686 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

diethyl ether

28.9 °C

Zenone; Kamenka

European Journal of Medicinal Chemistry, 1991 , vol. 26, # 7 p. 677 686 Title/Abstract Full Text View citing articles Show Details

Kamenka; Chicheportiche

European Journal of Medicinal Chemistry, 1987 , vol. 22, # 3 p. 193 197 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

various solvent(s)

28.9 °C

Zenone; Kamenka

European Journal of Medicinal Chemistry, 1991 , vol. 26, # 7 p. 677 686 Title/Abstract Full Text View citing articles Show Details

Kamenka; Chicheportiche

European Journal of Medicinal Chemistry, 1987 , vol. 22, # 3 p. 193 197 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

ethyl acetate

28.9 °C

Zenone; Kamenka

European Journal of Medicinal Chemistry, 1991 , vol. 26, # 7 p. 677 686 Title/Abstract Full Text View citing articles Show Details

Kamenka; Chicheportiche

European Journal of Medicinal Chemistry, 1987 , vol. 22, # 3 p. 193 197 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

pentan-1-ol

28.9 °C

Zenone; Kamenka

European Journal of Medicinal Chemistry, 1991 , vol. 26, # 7 p. 677 686 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

butan-1-ol

28.9 °C

Zenone; Kamenka

European Journal of Medicinal Chemistry, 1991 , vol. 26, # 7 p. 677 686 Title/Abstract Full Text View citing articles Show Details

Kamenka; Chicheportiche

European Journal of Medicinal Chemistry, 1987 , vol. 22, # 3 p. 193 197 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

butan-2-ol

28.9 °C

Zenone; Kamenka

European Journal of Medicinal Chemistry, 1991 , vol. 26, # 7 p. 677 686 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

acetone

28.9 °C

Zenone; Kamenka

European Journal of Medicinal Chemistry, 1991 , vol. 26, # 7 p. 677 686 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

acetonitrile

28.9 °C

Zenone; Kamenka

European Journal of Medicinal Chemistry, 1991 , vol. 26, # 7 p. 677 686 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

dibutyl ether H2O

28.9 °C

Zenone; Kamenka

European Journal of Medicinal Chemistry, 1991 , vol. 26, # 7 p. 677 686 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

diethyl ether H2O

28.9 °C

Zenone; Kamenka

European Journal of Medicinal Chemistry, 1991 , vol. 26, # 7 p. 677 686 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

various solvent(s) H2O

28.9 °C

Zenone; Kamenka

European Journal of Medicinal Chemistry, 1991 , vol. 26, # 7 p. 677 686 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

ethyl acetate H2O

28.9 °C

Zenone; Kamenka

European Journal of Medicinal Chemistry, 1991 , vol. 26, # 7 p. 677 686 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

pentan-1-ol H2O

28.9 °C

Zenone; Kamenka

European Journal of Medicinal Chemistry, 1991 , vol. 26, # 7 p. 677 686 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

butan-1-ol H2O

28.9 °C

Zenone; Kamenka

European Journal of Medicinal Chemistry, 1991 , vol. 26, # 7 p. 677 686 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

butan-2-ol H2O

28.9 °C

Zenone; Kamenka

European Journal of Medicinal Chemistry, 1991 , vol. 26, # 7 p. 677 686 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

acetone H2O

28.9 °C

Zenone; Kamenka

European Journal of Medicinal Chemistry, 1991 , vol. 26, # 7 p. 677 686 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

CDCl3

Johnson, Peter Y.; Pan, Robert; Wen, Jing Quan; Halfman, Clarke J.

Journal of Organic Chemistry, 1981 , vol. 46, # 10 p. 2049 - 2054 Title/Abstract Full Text View citing articles Show Details

Jones; Beaver; Schmoeger; et al.

Journal of Organic Chemistry, 1981 , vol. 46, # 16 p. 3330 - 3333 Title/Abstract Full Text View citing articles Show Details

Katritzky, Alan R.; Najzarek, Zbigniew; Dega-Szafran, Zofia

Synthesis, 1989 , # 1 p. 66 - 69 Title/Abstract Full Text Show Details

Description (NMR Spectroscopy)

Nucleus (NMR Spectroscopy)

Solvents (NMR Spectroscopy)

Temperature (NMR Spectroscopy)

Chemical shifts

13C

cyclohexane

28.9 °C

Kamenka; Chicheportiche

European Journal of Medicinal Chemistry, 1987 , vol. 22, # 3 p. 193 - 197 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

CCl4

28.9 °C

Kamenka; Chicheportiche

European Journal of Medicinal Chemistry, 1987 , vol. 22, # 3 p. 193 - 197 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

benzene

28.9 °C

Kamenka; Chicheportiche

European Journal of Medicinal Chemistry, 1987 , vol. 22, # 3 p. 193 - 197 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

CH2Cl2

28.9 °C

Kamenka; Chicheportiche

European Journal of Medicinal Chemistry, 1987 , vol. 22, # 3 p. 193 - 197 Title/Abstract Full Text View citing articles Show Details

Reference

Chemical shifts

13C

CD2Cl2

25 °C

Manoharan; Eliel; Carrol; Kenam Jr.

Tetrahedron Letters, 1983 , vol. 24, # 18 p. 1855 1858 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

CD2Cl2

-80 °C

Manoharan; Eliel; Carrol; Kenam Jr.

Tetrahedron Letters, 1983 , vol. 24, # 18 p. 1855 1858 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

acetone-d6 CD3CN

25 °C

Manoharan; Eliel; Carrol; Kenam Jr.

Tetrahedron Letters, 1983 , vol. 24, # 18 p. 1855 1858 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

acetone-d6 CD3CN

-70 °C

Manoharan; Eliel; Carrol; Kenam Jr.

Tetrahedron Letters, 1983 , vol. 24, # 18 p. 1855 1858 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

tetradeuteriomethanol CD2Cl2

25 °C

Manoharan; Eliel; Carrol; Kenam Jr.

Tetrahedron Letters, 1983 , vol. 24, # 18 p. 1855 1858 Title/Abstract Full Text View citing articles Show Details

Brine; Williams; Boldt; Carroll

Journal of Heterocyclic Chemistry, 1979 , vol. 16, # 7 p. 1425 - 1429 Title/Abstract Full Text View citing articles Show Details Geneste; Kamenka

Organic Magnetic Resonance, 1975 , vol. 7, p. 581 Full Text Show Details

Geneste et al.

European Journal of Medicinal Chemistry, 1979 , vol. 14, p. 301,302 Full Text Show Details

NMR

IR Spectroscopy (1) Solvent (IR Spectroscopy) CHCl3

Original Text (IR Spectroscopy)

Signals

Reference

IR (CHCl3) ν 3358, 3281, 3013, 2917, 2847, 1595, 1468, 1451, 1437, 747, 718 cm-1

3358 cm-1

University of Pittsburgh

Patent: US5132313 A1, 1992 ;

3281 cm-1 3013 cm-1 2917 cm-1 2847 cm-1 1595 cm-1 1468 cm-1 1451 cm-1 1437 cm-1 747 cm-1

718 cm-1

Mass Spectrometry (7) Description (Mass Spectrometry)

Reference

spectrum tandem mass spectrometry

Hendrickson, Howard P.; Whaley, E. Cathrine; Owens, S. Michael

Journal of Mass Spectrometry, 2005 , vol. 40, # 1 p. 19 - 24

Title/Abstract Full Text Show Details

Title/Abstract Full Text View citing articles Show Details

spectrum fragmentation pattern electron impact (EI)

Ishii, Akira; Seno, Hiroshi; Watanabe-Suzuki, Kanako; Kumazawa, Takeshi; Matsushima, Hajime; Suzuki, Osamu; Katsumata, Yoshinao

Analytical Chemistry, 2000 , vol. 72, # 2 p. 404 - 407 Title/Abstract Full Text View citing articles Show Details

spectrum electron impact (EI)

Jones; Beaver; Schmoeger; et al.

Journal of Organic Chemistry, 1981 , vol. 46, # 16 p. 3330 - 3333 Title/Abstract Full Text View citing articles Show Details

chemical ionization (CI) electron impact (EI) spectrum

Ghaderi, Sahba; Kulkarni, P.S.; Ledford, Edward B.; Wilkins, Charles L.; Gross, Michael L.

Analytical Chemistry, 1981 , vol. 53, # 3 p. 428 - 437 Title/Abstract Full Text View citing articles Show Details

spectrum chemical ionization (CI)

Carroll, F. Ivy; Brine, George A.; Boldt, Karl G.; Cone, Edward J.; Yousefnejad, David; et al.

Journal of Medicinal Chemistry, 1981 , vol. 24, # 9 p. 1047 - 1051 Title/Abstract Full Text View citing articles Show Details

spectrum electron impact (EI) chemical ionization (CI)

Addison, J. B.

Pharmaceutical Chemistry Journal, 1981 , vol. 15, # 3 p. 215 - 217 Khimiko-Farmatsevticheskii Zhurnal, 1981 , vol. 15, # 3 p. 110 - 113 Title/Abstract Full Text View citing articles Show Details

Fales et al.

Archives of Mass Spectral Data, 1971 , vol. 2, p. 596 Full Text Show Details

Lin et al.

Biomedical Mass Spectrometry, 1975 , vol. 2, p. 206,212,213 Full Text Show Details

Wilson; Domino

Biomedical Mass Spectrometry, 1978 , vol. 5, # 2 p. 112 - 116 Title/Abstract Full Text View citing articles Show Details

UV/VIS Spectroscopy (2) Description (UV/VIS Spectroscopy)

Solvent (UV/VIS Spectroscopy)

Comment (UV/VIS Spectroscopy)

Spectrum

H2O

220 - 280 nm

Reference Bowen, John M.; Purdie, Neil

Analytical Chemistry, 1981 , vol. 53, # 14 p. 2239 - 2242 Analytical Chemistry, 1981 , vol. 53, # 14 p. 2239 - 2242 Title/Abstract Full Text View citing articles Show Details

Maddox,V.H. et al.

J. Med. Chem., 1965 , vol. 8, p. 230 - 235 Title/Abstract Full Text View citing articles Show Details

Absorption maxima

Bioactivity Pharmacological Data (219) 1 of 219

Comment (Pharmacological Data)

Bioactivities present

Reference

Maddox,V.H. et al.

J. Med. Chem., 1965 , vol. 8, p. 230 - 235 Title/Abstract Full Text View citing articles Show Details

The United States of America as represented by the Department of Health and Human Services; Office of Technology Transfer; Research Triangle Institue

Patent: US5574060 A1, 1996 ; Title/Abstract Full Text Show Details

Washington University

Patent: US5958919 A1, 1999 ; Title/Abstract Full Text Show Details

SRI International

Patent: US5086054 A1, 1992 ; Title/Abstract Full Text Show Details

University of Pittsburgh

Patent: US5132313 A1, 1992 ; Title/Abstract Full Text Show Details

Brine; Williams; Boldt; Carroll

Journal of Heterocyclic Chemistry, 1979 , vol. 16, # 7 p. 1425 - 1429 Title/Abstract Full Text View citing articles Show Details

ORION CORPORATION

Patent: WO2003/82825 A1, 2003 ; Title/Abstract Full Text Show Details

Institut National de la Sante et de la Recherche Medicale (INSERM)

Patent: EP1462117 A1, 2004 ; Title/Abstract Full Text Show Details

MITSUBISHI PHARMA CORPORATION

Patent: WO2004/87124 A1, 2004 ; Title/Abstract Full Text Show Details

KIM, Dr. Hyoung-Chun; GREEN CROSS CORP.

Patent: US2005/256147 A1, 2005 ; Title/Abstract Full Text Show Details

Laboratorios Dr. Esteve S.A.

Patent: US2006/19968 A1, 2006 ; Title/Abstract Full Text Show Details

deCODE Genetics, Inc.

Patent: US2006/29546 A1, 2006 ; Title/Abstract Full Text Show Details

AZAYA THERAPEUTICS, INC.

Patent: WO2007/70779 A2, 2007 ; Title/Abstract Full Text Show Details

NEWRON PHARMACEUTICALS S.P.A.

Patent: WO2007/71311 A1, 2007 ; Title/Abstract Full Text Show Details

CORNELL RESEARCH FOUNDATION, INC.

Patent: WO2008/8884 A2, 2008 ; Title/Abstract Full Text Show Details

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ; Title/Abstract Full Text Show Details

Fales et al.

Archives of Mass Spectral Data, 1971 , vol. 2, p. 596 Full Text Show Details

Bhattacharjee; Chacko

Current Science, 1979 , vol. 48, p. 969 Full Text Show Details

Bailey; Chow; Downie; Pike

Journal of Pharmacy and Pharmacology, 1976 , vol. 28, # 9 p. 713 - 714 Title/Abstract Full Text View citing articles Show Details

Parke; Davis and Co.

Patent: US3097136 , 1960 ; Chem.Abstr., 1963 , vol. 59, # 13881 Full Text Show Details

2 of 219

Comment (Pharmacological Data)

Bioactivities present

Reference

Geneste; Kamenka

Organic Magnetic Resonance, 1975 , vol. 7, p. 581 Full Text Show Details

Mousseron et al.

Chimica Therapeutica, 1966 , vol. 1, p. 284,286 Full Text Show Details

Geneste et al.

European Journal of Medicinal Chemistry, 1979 , vol. 14, p. 301,302 Full Text Show Details

Sokolovsky; Hordeckai

Patent: DE2339342 , 1974 ; Chem.Abstr., vol. 80, # 132908 Full Text Show Details

Parke; Davis

Patent: US3192219 , 1965 ; Chem.Abstr., 1965 , vol. 63, # 9921f Full Text Show Details

Welvart

Comptes Rendus Hebdomadaires des Seances de l'Academie des Sciences, 1960 , vol. 250, p. 1870,1871 Full Text Show Details

Barr R. E.

Dissert. Abstr. (B), 27 <1966> 1079, zit. n. Molecular Structure and Dimensions, Vol. 1 <1970> 242 Full Text Show Details

Lin et al.

Biomedical Mass Spectrometry, 1975 , vol. 2, p. 206,212,213

Full Text Show Details

Kalir et al.

European Journal of Medicinal Chemistry, 1978 , vol. 13, p. 17,18 Full Text Show Details

Wilson; Domino

Biomedical Mass Spectrometry, 1978 , vol. 5, # 2 p. 112 - 116 Title/Abstract Full Text View citing articles Show Details

Tanabe

Patent: JP1908767 , 1960 ; Chem.Abstr., 1968 , vol. 69, # 10195f Full Text Show Details

Argos et al.

Acta Crystallographica, Section B: Structural Crystallography and Crystal Chemistry, 1970 , vol. 26, p. 53 Full Text Show Details

Ilagouma, A. T.; Dornand, J.; Liu, C. F.; Zenone, F.; Mani, J. C.; Kamenka, J. M.

European Journal of Medicinal Chemistry, 1990 , vol. 25, # 7 p. 609 - 615 Title/Abstract Full Text View citing articles Show Details

Manoharan; Eliel; Carrol; Kenam Jr.

Tetrahedron Letters, 1983 , vol. 24, # 18 p. 1855 - 1858 Title/Abstract Full Text View citing articles Show Details

Moriarty, Robert M.; Vaid, Radhe K.; Duncan, Michael P.; Ochiai, Masahito; Inenaga, Minako; Nagao, Yoshimitsu

Tetrahedron Letters, 1988 , vol. 29, # 52 p. 6913 - 6916 Title/Abstract Full Text View citing articles Show Details

Ghaderi, Sahba; Kulkarni, P.S.; Ledford, Edward B.; Wilkins, Charles L.; Gross, Michael L.

Analytical Chemistry, 1981 , vol. 53, # 3 p. 428 - 437 Title/Abstract Full Text View citing articles Show Details

Bowen, John M.; Purdie, Neil

Analytical Chemistry, 1981 , vol. 53, # 14 p. 2239 - 2242 Analytical Chemistry, 1981 , vol. 53, # 14 p. 2239 - 2242 Title/Abstract Full Text View citing articles Show Details

Johnson, Peter Y.; Pan, Robert; Wen, Jing Quan; Halfman, Clarke J.

Journal of Organic Chemistry, 1981 , vol. 46, # 10 p. 2049 - 2054 Title/Abstract Full Text View citing articles Show Details

Jones; Beaver; Schmoeger; et al.

Journal of Organic Chemistry, 1981 , vol. 46, # 16 p. 3330 - 3333 Title/Abstract Full Text View citing articles Show Details

Iorio, Maria A.; Tomassini, Lamberto; Mattson, Mariena V.; George, Clifford; Jacobson, Arthur E.

Journal of Medicinal Chemistry, 1991 , vol. 34, # 8 p. 2615 - 2623 Title/Abstract Full Text View citing articles Show Details

3 of 219

Comment (Pharmacological Data)

Bioactivities present

Reference

Zenone; Kamenka

European Journal of Medicinal Chemistry, 1991 , vol. 26, # 7 p. 677 - 686 Title/Abstract Full Text View citing articles Show Details

Tsukiyama; Hashimoto; Katayama; Nishikawa; Tobe; Maeda

Chemical and Pharmaceutical Bulletin, 1991 , vol. 39, # 6 p. 1581 - 1584 Title/Abstract Full Text View citing articles Show Details

Kamenka; Michaud; Geneste; et al.

European Journal of Medicinal Chemistry, 1985 , vol. 20, # 5 p. 419 - 424 Title/Abstract Full Text View citing articles Show Details

Itzhak, Yossef; Kalir, Asher; Weissman, Ben Avi; Cohen, Sasson

Journal of Medicinal Chemistry, 1981 , vol. 24, # 5 p. 496 - 499 Title/Abstract Full Text View citing articles Show Details

Carroll, F. Ivy; Brine, George A.; Boldt, Karl G.; Cone, Edward J.; Yousefnejad, David; et al.

Journal of Medicinal Chemistry, 1981 , vol. 24, # 9 p. 1047 - 1051 Title/Abstract Full Text View citing articles Show Details

Ward; Kalir; Trevor; Adams; Baillie; Castagnoli Jr.

Journal of Medicinal Chemistry, 1982 , vol. 25, # 5 p. 491 - 492 Title/Abstract Full Text View citing articles Show Details

Kamenka; Chiche; Goudal; Geneste; Vignon; Vincent; Lazdunski

Journal of Medicinal Chemistry, 1982 , vol. 25, # 4 p. 431 - 435 Title/Abstract Full Text View citing articles Show Details

Addison, J. B.

Pharmaceutical Chemistry Journal, 1981 , vol. 15, # 3 p. 215 - 217 Khimiko-Farmatsevticheskii Zhurnal, 1981 , vol. 15, # 3 p. 110 - 113 Title/Abstract Full Text View citing articles Show Details

Katritzky, Alan R.; Najzarek, Zbigniew; Dega-Szafran, Zofia

Synthesis, 1989 , # 1 p. 66 - 69 Title/Abstract Full Text Show Details

Thurkauf; Mattson; Richardson; Mirsadeghi; Ornstein; Harrison Jr.; Rice; Jacobson; Monn

Journal of Medicinal Chemistry, 1992 , vol. 35, # 8 p. 1323 - 1329 Title/Abstract Full Text View citing articles Show Details

Beaver, Rodney W.; Jones, Louis A.

Canadian Journal of Chemistry, 1984 , vol. 62, p. 1022 - 1027 Title/Abstract Full Text Show Details

Masumoto; Takeuchi; Ohta; Hirobe

Chemical and Pharmaceutical Bulletin, 1989 , vol. 37, # 7 p. 1788 - 1794 Title/Abstract Full Text View citing articles Show Details

Kamenka; Chicheportiche

European Journal of Medicinal Chemistry, 1987 , vol. 22, # 3 p. 193 - 197 Title/Abstract Full Text View citing articles Show Details

Soon M. Han; Purdie

Analytical Chemistry, 1984 , vol. 56, # 14 p. 2822 - 2825

Title/Abstract Full Text View citing articles Show Details

Canton; Doble; Miquet; Jimonet; Blanchard

Journal of Pharmacy and Pharmacology, 1992 , vol. 44, # 10 p. 812 - 816 Title/Abstract Full Text View citing articles Show Details

Costa, Brian R. de; Mattson, Mariena V.; George, Clifford; Linders, Joannes T. M.

Journal of Medicinal Chemistry, 1992 , vol. 35, # 25 p. 4704 - 4712 Title/Abstract Full Text View citing articles Show Details

Chen; Kozikowski; Wood; Reynolds; Ball; Pang

Journal of Medicinal Chemistry, 1992 , vol. 35, # 9 p. 1634 - 1638 Title/Abstract Full Text View citing articles Show Details

Jarv; Bartfai

1982 , vol. 36, # 7 B p. 487 - 490 Title/Abstract Full Text View citing articles Show Details

Hays, Sheryl J.; Novak, Perry M.; Ortwine, Daniel F.; Bigge, Christopher F.; Colbry, Norman L.; et al.

Journal of Medicinal Chemistry, 1993 , vol. 36, # 6 p. 654 - 670 Title/Abstract Full Text View citing articles Show Details

Sagratella; Longo

Arzneimittel-Forschung/Drug Research, 1985 , vol. 35, # 1 A p. 251 - 254 Title/Abstract Full Text View citing articles Show Details

4 of 219

Comment (Pharmacological Data)

Bioactivities present

Reference

Costa, Brian R. de; George, Clifford; Burke, Terrence R.; Rafferty, Michael F.; Contreras, Patricia C.; et al.

Journal of Medicinal Chemistry, 1988 , vol. 31, # 8 p. 1571 - 1575 Title/Abstract Full Text View citing articles Show Details

Thurkauf; Hillery; Mattson; Jacobsen; Rice

Journal of Medicinal Chemistry, 1988 , vol. 31, # 8 p. 1625 - 1628 Title/Abstract Full Text View citing articles Show Details

Kalir; Teomy; Amir; Fuchs; Lee; Holsztynska; Rocki; Domino

Journal of Medicinal Chemistry, 1984 , vol. 27, # 10 p. 1267 - 1271 Title/Abstract Full Text View citing articles Show Details

Eiden; Schmidt; Buchborn

Archiv der Pharmazie, 1987 , vol. 320, # 4 p. 348 - 361 Title/Abstract Full Text View citing articles Show Details

Cone; Vaupel; Yousefnejad

Journal of Pharmacy and Pharmacology, 1982 , vol. 34, # 3 p. 197 - 199 Title/Abstract Full Text View citing articles Show Details

Martin; Elgin Jr.; Mathiasen; Davis; Kesslick; Baldy; Shank; DiStefano; Fedde; Scott

Journal of Medicinal Chemistry, 1989 , vol. 32, # 5 p. 1052 - 1056 Title/Abstract Full Text View citing articles Show Details

Bigge; Malone; Hays; Johnson; Novak; Lescosky; Retz; Ortwine; Probert Jr.; Coughenour; Boxer; Robichaud; Brahce; Shillis

Journal of Medicinal Chemistry, 1993 , vol. 36, # 14 p. 1977 - 1995 Title/Abstract Full Text View citing articles Show Details

Gray, Nancy M.; Cheng, Brian K.; Mick, Stephen J.; Lair, Cecelia M.; Contreras, Patricia C.

Journal of Medicinal Chemistry, 1989 , vol. 32, # 6 p. 1242 - 1248 Title/Abstract Full Text View citing articles Show Details

Iorio; Molinari; Scotti de Carolis; Niglio

Farmaco, Edizione Scientifica, 1984 , vol. 39, # 7 p. 599 - 611 Title/Abstract Full Text View citing articles Show Details

Hansch; Bjorkroth; Leo

Journal of Pharmaceutical Sciences, 1987 , vol. 76, # 9 p. 663 - 687 Title/Abstract Full Text View citing articles Show Details

Eiden; Denk; Hofner

Archiv der Pharmazie, 1994 , vol. 327, # 7 p. 405 - 412 Title/Abstract Full Text View citing articles Show Details

Mallamo; Earley; Kumar; Subramanyam; Dority Jr.; Miller; Dehaven-Hudkins; Ault; Herrmann Jr.; Dung; McMullen; Jaeger; Kullnig; Magee

Journal of Medicinal Chemistry, 1994 , vol. 37, # 26 p. 4438 - 4448 Title/Abstract Full Text View citing articles Show Details

Subramanyam; Mallamo; Dority Jr.; Earley; Kumar; Aimone; Ault; Miller; Luttinger; DeHaven-Hudkins

Journal of Medicinal Chemistry, 1995 , vol. 38, # 1 p. 21 - 27 Title/Abstract Full Text View citing articles Show Details

Shafik; Rida; Eshba; Abdel-Kreem; El-Dardiry

Farmaco, 1995 , vol. 50, # 4 p. 273 - 279 Title/Abstract Full Text View citing articles Show Details

Earley; Kumar; Mallamo; Subramanyam; Dority Jr.; Miller; DeHaven-Hudkins; Aimone; Kelly; Ault

Journal of Medicinal Chemistry, 1995 , vol. 38, # 18 p. 3586 - 3592 Title/Abstract Full Text View citing articles Show Details

Shuto, Satoshi; Ono, Shizuka; Hase, Yukako; Ueno, Yoshihito; Noguchi, Tomohiro; Yoshii, Kiyonori; Matsuda, Akira

Journal of Medicinal Chemistry, 1996 , vol. 39, # 24 p. 4844 - 4852 Title/Abstract Full Text View citing articles Show Details

Hamon; Vignon; Kamenka

European Journal of Medicinal Chemistry, 1996 , vol. 31, # 6 p. 489 - 495 Title/Abstract Full Text View citing articles Show Details

Sakamoto; Endo; Nagasaki; Nakamura; Watanabe; Nakahara; Tanaka, Akira

Pharmazie, 1998 , vol. 53, # 5 p. 310 - 314 Title/Abstract Full Text View citing articles Show Details

Kroemer, Romano T.; Koutsilieri, Eleni; Hecht, Peter; Liedl, Klaus R.; Riederer, Peter; Kornhuber, Johannes

Journal of Medicinal Chemistry, 1998 , vol. 41, # 3 p. 393 - 400 Title/Abstract Full Text View citing articles Show Details

Moriarty, Robert M.; Enache, Livia A.; Zhao, Lei; Gilardi, Richard; Mattson, Mariena V.; Prakash, Om

Journal of Medicinal Chemistry, 1998 , vol. 41, # 4 p. 468 - 477 Title/Abstract Full Text View citing articles Show Details

5 of 219

6 of 219

Comment (Pharmacological Data)

Bioactivities present

Reference

Wanner, Klaus Th.; Beer, Herbert; Hoefner, Georg; Ludwig, Matthias

European Journal of Organic Chemistry, 1998 , # 9 p. 2019 - 2029 Title/Abstract Full Text View citing articles Show Details

Sasaki, Shigeki; Ishibashi, Nobuyasu; Kuwamura, Tshuneo; Sano, Hiromi; Matoba, Masaki; Nisikawa, Tohru; Maeda, Minora

Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 21 p. 2983 - 2986 Title/Abstract Full Text View citing articles Show Details

Wessinger, William D.

European Journal of Pharmacology, 1995 , vol. 277, # 1 p. 107 - 112 Title/Abstract Full Text View citing articles Show Details

Haradahira, Terushi; Sasaki, Sigeki; Maeda, Minoru; Kobayashi, Kaoru; Inoue, Osamu; Tomita, Urara; Nishikawa, Toru; Suzuki, Kazutoshi

Journal of Labelled Compounds and Radiopharmaceuticals, 1998 , vol. 41, # 9 p. 843 - 858 Title/Abstract Full Text View citing articles Show Details

Nakahara; Takahashi; Kikura

Biological and Pharmaceutical Bulletin, 1995 , vol. 18, # 9 p. 1223 - 1227 Title/Abstract Full Text View citing articles Show Details

Maurel-Remy; Bervoets; Millan

European Journal of Pharmacology, 1995 , vol. 280, # 2 p. R9-R11 Title/Abstract Full Text View citing articles Show Details

Peruche; Klaassens; Krieglstein

Pharmacology, 1995 , vol. 50, # 4 p. 229 - 237 Title/Abstract Full Text View citing articles Show Details

Hustveit; Maurset; Oye

Pharmacology and Toxicology, 1995 , vol. 77, # 6 p. 355 - 359 Title/Abstract Full Text View citing articles Show Details

Fryer, John D.; Lukas, Ronald J.

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 288, # 1 p. 88 - 92 Title/Abstract Full Text View citing articles Show Details

Palmer, Gene C.; Murray, Robert J.; Cramer, Carrie L.; Stagnitto, Mary L.; Knowles, Marilyn K.; Freedman, Lou R.; Eismann, Mark S.; Mahmood, Nik; Balestra, Mike; Borrelli, Alfonso R.; Hudzik, Thomas J.; McCarthy, Dennis J.

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 288, # 1 p. 121 - 132 Title/Abstract Full Text View citing articles Show Details

Palmer; Stagnitto; Garske; Napier; Harris; Kaiser; Griffith; Woodhead; White; Wolf; Swinyard

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 273, # 3 p. 1023 - 1031 Title/Abstract Full Text View citing articles Show Details

Yazdanian, Mehran; Glynn, Susan L.; Wright, James L.; Hawi, Amale

Pharmaceutical Research, 1998 , vol. 15, # 9 p. 1490 - 1494 Title/Abstract Full Text View citing articles Show Details

Silverthorn; Dersch; Baumann; Cadet; Partilla; Rice; Carroll; Becketts; Brockington; Rothman

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 273, # 1 p. 213 - 222 Title/Abstract Full Text View citing articles Show Details

Ali, S. F.; Newport, G. D.; Bracha, H. S.

Neurotoxicology and Teratology, 1994 , vol. 16, # 4 p. 335 - 342 Title/Abstract Full Text View citing articles Show Details

French

Neurotoxicology and Teratology, 1994 , vol. 16, # 4 p. 355 - 362 Title/Abstract Full Text View citing articles Show Details

Sircar, Ratna; Li, Chang-Sheng

Neurotoxicology and Teratology, 1994 , vol. 16, # 4 p. 369 - 376 Title/Abstract Full Text View citing articles Show Details

Sayre; Engelhart; Nadkarni; Babu; Klein; McCoy

Xenobiotica, 1995 , vol. 25, # 7 p. 769 - 775 Title/Abstract Full Text View citing articles Show Details

Roshol; Skrede; Aero; Wiik

European Journal of Pharmacology, 1995 , vol. 286, # 1 p. 9 - 17 Title/Abstract Full Text View citing articles Show Details

Okuyama, Shigeru; Chaki, Shigeyuki; Yae, Tetsuji; Nakazato, Atsuro; Muramatsu, Makoto

Life Sciences, 1995 , vol. 57, # 21 p. PL333-PL337 Title/Abstract Full Text View citing articles Show Details

Rothman; Silverthorn; Baumann; Goodman; Cadet; Matecka; Rice; Carroll; Wang; Uhl; Partilla; Dersch

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 274, # 1 p. 385 - 395 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

Bioactivities present

Reference

Lurtz, Monica M.; Pedersen, Steen E.

Molecular Pharmacology, 1999 , vol. 55, # 1 p. 159 - 167 Title/Abstract Full Text View citing articles Show Details

Yonezawa; Kuroki; Tashiro; Hondo; Uchimura

European Journal of Pharmacology, 1995 , vol. 285, # 3 p. 305 - 308 Title/Abstract Full Text View citing articles Show Details

Noda, Yukihiro; Yamada, Kiyofumi; Komori, Yumiko; Sugihara, Hisayoshi; Furukawa, Hiroshi; Nabeshima, Toshitaka

British Journal of Pharmacology, 1996 , vol. 117, # 7 p. 1579 - 1585 Title/Abstract Full Text View citing articles Show Details

Swedberg; Jacobsen; Honore

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 274, # 3 p. 1113 - 1121 Title/Abstract Full Text View citing articles Show Details

Wuensch, Bernhard; Bauschke, Gerd; Diekmann, Heike; Hoefner, Georg

Archiv der Pharmazie, 1999 , vol. 332, # 12 p. 413 - 421

Title/Abstract Full Text View citing articles Show Details

Tanaka; Shirasaki; Kaku; Muramatsu; Otomo

Naunyn-Schmiedeberg's Archives of Pharmacology, 1995 , vol. 351, # 3 p. 244 - 251 Title/Abstract Full Text View citing articles Show Details

Ishii, Akira; Seno, Hiroshi; Watanabe-Suzuki, Kanako; Kumazawa, Takeshi; Matsushima, Hajime; Suzuki, Osamu; Katsumata, Yoshinao

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Anderson; Williams; Pauly; Raszkiewicz; Campbell; Rotert; Surber; Thomas; Wasicak; Arneric; Sullivan

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Roth, Jane E.; Murray, Thomas F.; Franklin, Paul H.

Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 277, # 3 p. 1823 - 1836 Title/Abstract Full Text View citing articles Show Details

Jin, Jingji; Yamamoto, Tsuneyuki; Watanabe, Shigenori

European Journal of Pharmacology, 1997 , vol. 319, # 2-3 p. 147 - 152 Title/Abstract Full Text View citing articles Show Details

Etou; Kuroki; Tatebayashi; Tashiro; Hirano

Biochemical Pharmacology, 1996 , vol. 51, # 1 p. 83 - 86 Title/Abstract Full Text View citing articles Show Details

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Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 278, # 2 p. 669 - 678 Title/Abstract Full Text View citing articles Show Details

Kamei, Hiroyuki; Kameyama, Tsutomu; Nabeshima, Toshitaka

European Journal of Pharmacology, 1996 , vol. 299, # 1-3 p. 21 - 28 Title/Abstract Full Text View citing articles Show Details

Klarica, Marijan; Fage, Dominique; Carter, Chris

European Journal of Pharmacology, 1996 , vol. 308, # 2 p. 135 - 144 Title/Abstract Full Text View citing articles Show Details

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European journal of pharmacology, 1996 , vol. 307, # 3 p. 347 - 353 Title/Abstract Full Text View citing articles Show Details

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Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 277, # 1 p. 292 - 298 Title/Abstract Full Text View citing articles Show Details

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7 of 219

Comment (Pharmacological Data)

Bioactivities present

Reference

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European Journal of Pharmacology, 1996 , vol. 295, # 1 p. 45 - 52 Title/Abstract Full Text View citing articles Show Details

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European Journal of Pharmacology, 1998 , vol. 343, # 2-3 p. 135 - 143 Title/Abstract Full Text View citing articles Show Details

Wu, Yan-Na; Johnson, Steven W.

Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 279, # 2 p. 457 - 463 Title/Abstract Full Text View citing articles Show Details

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European Journal of Pharmacology, 1997 , vol. 323, # 2-3 p. 241 - 244 Title/Abstract Full Text View citing articles Show Details

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Journal of Medicinal Chemistry, 2004 , vol. 47, # 16 p. 4008 - 4021 Title/Abstract Full Text View citing articles Show Details

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Journal of Clinical Pharmacology, 2004 , vol. 44, # 1 p. 7 - 19 Title/Abstract Full Text View citing articles Show Details

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Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 283, # 2 p. 666 - 674 Title/Abstract Full Text View citing articles Show Details

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Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 2 p. 928 - 940 Title/Abstract Full Text View citing articles Show Details

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8 of 219

Comment (Pharmacological Data)

Bioactivities present

Reference

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European Journal of Pharmacology, 2002 , vol. 438, # 1-2 p. 75 - 78 Title/Abstract Full Text View citing articles Show Details

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Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 289, # 1 p. 521 - 527 Title/Abstract Full Text View citing articles Show Details

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Jordan, Shaun; Chen, Ruoyan; Fernalld, Raymond; Johnson, Janelle; Regardie, Karen; Kambayashi, Junichi; Tadori, Yoshihiro; Kitagawa, Hisashi; Kikuchi, Tetsuro

European Journal of Pharmacology, 2006 , vol. 540, # 1-3 p. 53 - 56 Title/Abstract Full Text View citing articles Show Details

Katsuta, Kiyotaka; Umemura, Kazuo; Ueyama, Noriko; Matsuoka, Nobuya

European Journal of Pharmacology, 2003 , vol. 467, # 1-3 p. 103 - 109 Title/Abstract Full Text View citing articles Show Details

Yang, Jiansong; Jamei, Masoud; Yeo, Karen Rowland; Tucker, Geoffrey T.; Rostami-Hodjegan, Amin

European Journal of Pharmaceutical Sciences, 2007 , vol. 31, # 3-4 p. 232 - 241 Title/Abstract Full Text View citing articles Show Details

Buyukbingol, Erdem; Sisman, Arzu; Akyildiz, Murat; Alparslan, Ferda Nur; Adejare, Adeboye

Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 12 p. 4265 - 4282 Title/Abstract Full Text View citing articles Show Details

Moda, Tiago L.; Montanari, Carlos A.; Andricopulo, Adriano D.

Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 24 p. 7738 - 7745 Title/Abstract Full Text View citing articles Show Details

Jozwiak, Krzysztof; Ravichandran, Sarangan; Collins, Jack R.; Moaddel, Ruin; Wainer, Irving W.

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Ikonomidou, Hrissanthi

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Union Carbide Chemicals and Plastics Technology Corporation

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DUKE UNIVERSITY

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Comment (Pharmacological Data)

Bioactivities present

Reference

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Zarantonello, Paola; Bettini, Ezio; Paio, Alfredo; Simoncelli, Chiara; Terreni, Silvia; Cardullo, Francesco

Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 7 p. 2059 - 2063 Title/Abstract Full Text View citing articles Show Details

Xia, Yan; Wang, Cheng Z.; Liu, Jie; Anastasio, Noelle C.; Johnson, Kenneth M.

Neuropharmacology, 2010 , vol. 58, # 2 p. 330 - 336 Title/Abstract Full Text View citing articles Show Details

Ahmadi, Abbas; Solati, Jalal; Hajikhani, Ramin; Onagh, Masoud; Javadi, Mojdeh

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Utech, Tina; Koehler, Jens; Wuensch, Bernhard

European Journal of Medicinal Chemistry, 2011 , vol. 46, # 6 p. 2157 - 2169 Title/Abstract Full Text View citing articles Show Details

Abdrakhmanova, Galya R.; Blough, Bruce E.; Nesloney, Carey; Navarro, Hernan A.; Damaj, M. Imad; Carroll, F. Ivy

Neuropharmacology, 2010 , vol. 59, # 6 p. 511 - 517 Title/Abstract Full Text View citing articles Show Details

Arias, Hugo R.; Feuerbach, Dominik; Targowska-Duda, Katarzyna M.; Jozwiak, Krzysztof

Neurochemistry International, 2010 , vol. 57, # 2 p. 153 - 161 Title/Abstract Full Text View citing articles Show Details

Ahmadi; Kermani; Naderi; Hajikhani; Rezaee; Javadi; Niknafs

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Ghanbari; Rowland-Yeo; Bloomer; Clarke; Lennard; Tucker; Rostami-Hodjegan

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Current Topics in Medicinal Chemistry, 2006 , vol. 6, # 8 p. 749 - 770 Title/Abstract Full Text View citing articles Show Details

10 of 219

11 of 219

Comment (Pharmacological Data)

Bioactivities present

Reference

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Neuropharmacology, 2006 , vol. 50, # 8 p. 941 - 952 Title/Abstract Full Text View citing articles Show Details

Jushchyshyn, Monica I.; Wahlstrom, Jan L.; Hollenberg, Paul F.; Wienkers, Larry C.

Drug Metabolism and Disposition, 2006 , vol. 34, # 9 p. 1523 - 1529 Title/Abstract Full Text View citing articles Show Details

Turpeinen, Miia; Raunio, Hannu; Pelkonen, Olavi

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Mitchell; Redfern

Current Pharmaceutical Design, 2005 , vol. 11, # 2 p. 171 - 203 Title/Abstract Full Text View citing articles Show Details

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Paixao, Paulo; Gouveia, Luis F.; Morais, Jose A.G.

European Journal of Pharmaceutical Sciences, 2009 , vol. 36, # 4-5 p. 544 - 554 Title/Abstract Full Text View citing articles Show Details

Seeman, Philip

Journal of psychiatry and neuroscience : JPN, 2009 , vol. 34, # 2 p. 143 - 149 Title/Abstract Full Text Show Details

Patterson, Stephen; Jones, Deuan C.; Shanks, Emma J.; Frearson, Julie A.; Gilbert, Ian H.; Wyatt, Paul G.; Fairlamb, Alan H.

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Wickenden; Maher; Chaplan

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Badolo, Lassina; Rasmussen, Louise Munk; Hansen, Helle Ruesz; Sveigaard, Christina

European Journal of Pharmaceutical Sciences, 2010 , vol. 40, # 4 p. 282 - 288 Title/Abstract Full Text View citing articles Show Details

Bettini, Ezio; Sava, Anna; Griffante, Cristiana; Carignani, Corrado; Buson, Alberto; Capelli, Anna Maria; Negri, Michele; Andreetta, Filippo; Senar-Sancho, Sergio A.; Guiral, Lorena; Cardullo, Francesca

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Large, Charles H.; Bison, Silvia; Sartori, Ilaria; Read, Kevin D.; Gozzi, Alessandro; Quarta, Davide; Antolini, Marinella; Hollands, Emma; Gill, Catherine H.; Gunthorpe, Martin J.; Idris, Nagi; Neill, Jo C.; Alvaro, Giuseppe S.

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Felipe; Bielanska; Comes; Vallejo; Roig; Ramon Y Cajal; E. Condom; Hernandez-Losa; Ferreres

Current Medicinal Chemistry, 2012 , vol. 19, # 5 p. 661 - 674 Title/Abstract Full Text View citing articles Show Details

Wiedemeyer, Kathrin; Wuensch, Bernhard

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Ruppa, Kamalesh B.; King, Dalton; Olson, Richard E.

Annual Reports in Medicinal Chemistry, 2012 , vol. 47, p. 89 - 103 Title/Abstract Full Text View citing articles Show Details

Banister, Samuel D.; Kassiou, Michael

Current Pharmaceutical Design, 2012 , vol. 18, # 7 p. 884 - 901 Title/Abstract Full Text View citing articles Show Details

Koehler, Jens; Bergander, Klaus; Fabian, Joerg; Schepmann, Dirk; Wuensch, Bernhard

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JAMA : the journal of the American Medical Association, 1977 , vol. 238, # 6 p. 515 - 516 Title/Abstract Full Text Show Details

Vincent; Cavey; Kamenka; Geneste; Lazdunski

Brain Research, 1978 , vol. 152, # 1 p. 176 - 182 Title/Abstract Full Text Show Details

Speth; Wastek; Johnson; Yamamura

Life Sciences, 1978 , vol. 22, # 10 p. 859 - 866 Title/Abstract Full Text Show Details

Comment (Pharmacological Data)

Bioactivities present

Reference

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Drug Metabolism and Disposition, 2003 , vol. 31, # 1 p. 46 - 52 Title/Abstract Full Text View citing articles Show Details

Wellendorph; Goodman; Burstein; Nash; Brann; Weiner

Neuropharmacology, 2002 , vol. 42, # 7 p. 929 - 940 Title/Abstract Full Text View citing articles Show Details

Pagan; Eterovic; Garcia; Vergne; Basilio; Rodriguez; Hann

Biochemistry, 2001 , vol. 40, # 37 p. 11121 - 11130 Title/Abstract Full Text View citing articles Show Details

De Vry, Jean; Horvath, Ervin; Schreiber, Rudy

European Journal of Pharmacology, 2001 , vol. 428, # 2 p. 203 - 214 Title/Abstract Full Text View citing articles Show Details

Karasawa; Takahashi; Horikomi

European journal of pharmacology, 2000 , vol. 400, # 1 p. 51 - 57 Title/Abstract Full Text Show Details

Arias, Hugo RubeI n

Archives of Biochemistry and Biophysics, 1999 , vol. 371, # 1 p. 89 - 97 Title/Abstract Full Text View citing articles Show Details

Booth, Raymond G.; Owens, Constance E.; Brown, Randall L.; Bucholtz, Ehren C.; Lawler, Cindy P.; Wyrick, Steven D.

Brain Research, 1999 , vol. 837, # 1-2 p. 95 - 105 Title/Abstract Full Text View citing articles Show Details

Hoefner; Wanner

Neuroscience letters, 1997 , vol. 226, # 2 p. 79 - 82 Title/Abstract Full Text Show Details

Hudkins; DeHaven-Hudkins

Life sciences, 1991 , vol. 49, # 17 p. 1229 - 1235 Title/Abstract Full Text Show Details

Ferrer-Montiel, Antonio V.; Merino, Jaime M.; Planells-Cases, Rosa; Sun, William; Montal, Mauricio

Neuropharmacology, 1998 , vol. 37, # 2 p. 139 - 147 Title/Abstract Full Text View citing articles Show Details

Shuto; Ono; Hase; Ueno; Noguchi; Yoshii; Matsuda

Journal of Medicinal Chemistry, 1996 , vol. 39, # 24 p. 4844 - 4852 Title/Abstract Full Text Show Details

Wu; Johnson

Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 279, # 2 p. 457 - 463 Title/Abstract Full Text View citing articles Show Details

Souverbie, Frederic; Mo, Li-Li; Liu, Yun; Von Euler, Gabriel; Sundstroem, Erik

European Journal of Pharmacology, 1996 , vol. 307, # 3 p. 347 - 353 Title/Abstract Full Text View citing articles Show Details

Kamei; Kameyama; Nabeshima

European Journal of Pharmacology, 1996 , vol. 299, # 1-3 p. 21 - 28 Title/Abstract Full Text Show Details

Lowe; Emre; Frey; Kelly; Malanowski; McAllister; Neijt; Ruedeberg; Urwyler; White; Herring

Neurochemistry International, 1994 , vol. 25, # 6 p. 583 - 600 Title/Abstract Full Text Show Details

Panetta; Patel

Life Sciences, 1995 , vol. 56, # 5 p. 333 - 342 Title/Abstract Full Text Show Details

Tanaka; Shirasaki; Kaku; Muramatsu; Otomo

Naunyn-Schmiedeberg's Archives of Pharmacology, 1995 , vol. 351, # 3 p. 244 - 251 Title/Abstract Full Text Show Details

Reuman; Mallamo; DeHaven-Hudkins

Bioorganic and Medicinal Chemistry Letters, 1995 , vol. 5, # 4 p. 371 - 376 Title/Abstract Full Text Show Details

Wessinger

European Journal of Pharmacology, 1995 , vol. 277, # 1 p. 107 - 112 Title/Abstract Full Text Show Details

Coderc; Cerruti; Vignon; Rouayrenc; Kamenka

European Journal of Medicinal Chemistry, 1995 , vol. 30, # 6 p. 463 - 470 Title/Abstract Full Text Show Details

12 of 219

Comment (Pharmacological Data)

Bioactivities present

Reference

Ali; Newport; Bracha

Neurotoxicology and Teratology, 1994 , vol. 16, # 4 p. 335 - 342 Title/Abstract Full Text Show Details

Sircar; Li

Neurotoxicology and Teratology, 1994 , vol. 16, # 4 p. 369 - 375 Title/Abstract Full Text Show Details

Nock; Giordano; Moore; Cicero

Journal of Pharmacology and Experimental Therapeutics, 1993 , vol. 264, # 1 p. 349 - 359 Title/Abstract Full Text View citing articles Show Details

De Vry; Benz; Schreiber; Traber

European Journal of Pharmacology, 1993 , vol. 249, # 3 p. 331 - 339 Title/Abstract Full Text Show Details

Kimes; Wilson; Scheffel; Campbell; London

Journal of Medicinal Chemistry, 1992 , vol. 35, # 25 p. 4683 - 4689 Title/Abstract Full Text View citing articles Show Details

De Costa; Mattson; George; Linders

Journal of Medicinal Chemistry, 1992 , vol. 35, # 25 p. 4704 - 4712 Title/Abstract Full Text Show Details

He; Raymon; Mattson; Eldefrawi; De Costa

Journal of Medicinal Chemistry, 1993 , vol. 36, # 9 p. 1188 - 1193 Title/Abstract Full Text Show Details

Hays; Novak; Ortwine; Bigge; Colbry; Johnson; Lescosky; Malone; Michael; Reily; Coughenour; Brahce; Shillis; Probert Jr.

Journal of Medicinal Chemistry, 1993 , vol. 36, # 6 p. 654 - 670 Title/Abstract Full Text Show Details

Sweetnam; Caldwell; Lancaster; Bauer Jnr.; McMillan; Kinnier; Price

Journal of Natural Products (Lloydia), 1993 , vol. 56, # 4 p. 441 - 455 Title/Abstract Full Text Show Details

DeHaven-Hudkins; Fleissner; Ford-Rice

European journal of pharmacology, 1992 , vol. 227, # 4 p. 371 - 378 Title/Abstract Full Text Show Details

Newman; Bevan; Bowery; Tortella

Journal of Medicinal Chemistry, 1992 , vol. 35, # 22 p. 4135 - 4142 Title/Abstract Full Text View citing articles Show Details

DeHaven-Hudkins; Fleissner

Life sciences, 1992 , vol. 50, # 9 p. PL65-70 Title/Abstract Full Text Show Details

Iorio; Tomassini; Mattson; George; Jacobson

Journal of Medicinal Chemistry, 1991 , vol. 34, # 8 p. 2615 - 2623 Title/Abstract Full Text Show Details

Holsztynska; Weber; Domino

Drug Metabolism and Disposition, 1991 , vol. 19, # 1 p. 48 - 53 Title/Abstract Full Text View citing articles Show Details

Lee; El-Fakahany

Journal of Pharmacology and Experimental Therapeutics, 1991 , vol. 256, # 2 p. 468 - 479 Title/Abstract Full Text View citing articles Show Details

Zaczek; Culp; Goldberg; Mccann; De Souza

The Journal of pharmacology and experimental therapeutics, 1991 , vol. 257, # 2 p. 820 - 829 Title/Abstract Full Text Show Details

Goodnow Jr.; Bukownik; Nakanishi; Usherwood; Eldefrawi; Anis

Journal of medicinal chemistry, 1991 , vol. 34, # 8 p. 2389 - 2394 Title/Abstract Full Text Show Details

Todd; Balster; Martin

Life Sciences, 1990 , vol. 46, # 12 p. 895 - 901 Title/Abstract Full Text Show Details

Thurkauf; De Costa; Mattson; France; Price; Olney; Woods; Jacobson; Rice

Journal of Medicinal Chemistry, 1990 , vol. 33, # 8 p. 2211 - 2215 Title/Abstract Full Text Show Details

Owens; McMillan; Hardwick; Wessinger

Pharmacology Biochemistry and Behavior, 1990 , vol. 35, # 4 p. 797 - 801 Title/Abstract Full Text Show Details

13 of 219

Comment (Pharmacological Data)

Bioactivities present

Reference

Ilagouma; Dornand; Liu; Zenone; Mani; Kamenka

European Journal of Medicinal Chemistry, 1990 , vol. 25, # 7 p. 609 - 615 Title/Abstract Full Text Show Details

Scheri; Jacobson; Lessor; Rice

Life Sciences, 1989 , vol. 45, # 18 p. 1689 - 1698 Title/Abstract Full Text Show Details

Bolanos; Schechter; Miquel; Emerit; Rumigny; Hamon; Gozlan

Biochemical pharmacology, 1990 , vol. 40, # 7 p. 1541 - 1550 Title/Abstract Full Text Show Details

Albuquerque; Tsai; Aronstam; Eldefrawi

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Potasiewicz, Agnieszka; Hołuj, Małgorzata; Kos, Tomasz; Popik, Piotr; Arias, Hugo R.; Nikiforuk, Agnieszka

Neuropharmacology, 2017 , vol. 113, p. 188 - 197 Title/Abstract Full Text Show Details

Shafi, Humera; Imran, Muhammad; Usman, Hafiz Faisal; Sarwar, Muhammad; Tahir, Muhammad Ashraf; Naveed, Rabia; Ashiq, Muhammad Zar; Tahir, Ammar M.

Egyptian Journal of Forensic Sciences, 2016 , vol. 6, # 3 p. 280 - 283 Title/Abstract Full Text Show Details

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Comment (Pharmacological Data)

Bioactivities present

Reference

Kyzar, Evan J.; Kalueff, Allan V.

Zebrafish, 2016 , vol. 13, # 5 p. 379 - 390 Title/Abstract Full Text Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Bioorganic and Medicinal Chemistry, 2016 , vol. 24, # 2 p. 130 - 139 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Ahmadi, Abbas; Khalili, Mohsen; Barzin, Mahnaz; Pooladi, Mohsen; Bakhtiari, Fatemeh; Barjeste, Maede; Nahri-Niknafs, Babak

Monatshefte fur Chemie, 2016 , vol. 147, # 2 p. 457 - 464 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Yang, Xin; Atkinson, Karen; Di, Li

Drug Metabolism and Disposition, 2016 , vol. 44, # 3 p. 460 - 465 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Wallach, Jason; Kang, Heather; Colestock, Tristan; Morris, Hamilton; Bortolotto, Zuner A.; Collingridge, Graham L.; Lodge, David; Halberstadt, Adam L.; Brandt, Simon D.; Adejare, Adeboye

PLoS ONE, 2016 , vol. 11, # 6 art. no. E0157021 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Alkermes, Inc.; Deaver, Daniel; Eyerman, David; Wynn, Thomas Andrew

Patent: US2016/243112 A1, 2016 ; Title/Abstract Full Text Show Details

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Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Bioorg. Med. Chem., 2015 , vol. 23, # 2 p. 297 - 313 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Sun, Shengguo; Wallach, Jason; Adejare, Adeboye

Medicinal Chemistry, 2014 , vol. 10, # 8 p. 843 - 852 Title/Abstract Full Text View citing articles Show Details

Journal of Medicinal Chemistry, 2015 , vol. 58, # 21 p. 8601 - 8615 Title/Abstract Full Text View citing articles Show Details

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Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Grimm, Stefanie H.; Höfner, Georg; Wanner, Klaus T.

ChemMedChem, 2015 , vol. 10, # 6 p. 1027 - 1039 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

MedChemComm, 2015 , vol. 6, # 7 p. 1272 - 1277 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Heusler, Peter; Tourette, Amlie; Cussac, Didier

Naunyn-Schmiedeberg's Archives of Pharmacology, 2015 , vol. 388, # 5 art. no. 1085, p. 509 - 516 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Kazmi, Faraz; Barbara, Joanna E.; Yerino, Phyllis; Parkinson, Andrew

Drug Metabolism and Disposition, 2015 , vol. 43, # 4 p. 523 - 533 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Berger, Michael L.; Rebernik, Patrick

Bioorganic and Medicinal Chemistry Letters, 2015 , vol. 25, # 19 p. 4131 - 4135 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Hamouda, Ayman K.; Stewart, Deirdre S.; Chiara, David C.; Savechenkov, Pavel Y.; Bruzik, Karol S.; Cohen, Jonathan B.

Molecular Pharmacology, 2014 , vol. 85, # 5 p. 735 - 746 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Swedberg, Michael D.B.; Raboisson, Patrick

Journal of Pharmacology and Experimental Therapeutics, 2014 , vol. 350, # 2 p. 212 - 222 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Amin, Jahanshah; Bisht, Kirpal S.; Gali, Meghanath

Patent: US2014/221473 A1, 2014 ; Title/Abstract Full Text Show Details

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Comment (Pharmacological Data)

physiological behaviour discussed

Reference

ARIEL-UNIVERSITY RESEARCH AND DEVELOPMENT COMPANY, LTD.; NAPROMED BIOPHARMACEUTICALS GMBH; ANAVIGOFFER, Sharon; GERTSCH, Juerg

Patent: WO2013/140342 A1, 2013 ; Title/Abstract Full Text Show Details

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Effect (Pharmacological Data)

receptor binding affinity

Species or Test-

brain cortex membrane homogenates of pig

System (Pharmacological Data)

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Kind of Dosing (Pharmacological Data)

comparative comp. dissolved in DMSO

Method (Pharmacological Data)

labelled ligand: [3H]-(+)-MK-801 (2 nmol/l); name of assay/method: radioligand binding assay

Further Details (Pharmacological Data)

inhibition constant (Ki); Ki related to: NMDA receptor

Type (Pharmacological Data)

Value of Type (Pharmacological Data)

59 nmol/l

Location

supporting information

Reference

Koehler, Jens; Bergander, Klaus; Fabian, Joerg; Schepmann, Dirk; Wuensch, Bernhard

Journal of Medicinal Chemistry, 2012 , vol. 55, # 20 p. 8953 - 8957 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor binding affinity

Species or TestSystem (Pharmacological Data)

brain cortex membrane homogenates of pig

Kind of Dosing (Pharmacological Data)

comparative comp. dissolved in DMSO

Method (Pharmacological Data)

labelled ligand: [3H]-(+)-MK-801 (2 nmol/l); name of assay/method: radioligand binding assay

Results

molecular target: NMDA receptor; species of target: pig

Location

supporting information

Reference

Koehler, Jens; Bergander, Klaus; Fabian, Joerg; Schepmann, Dirk; Wuensch, Bernhard

Journal of Medicinal Chemistry, 2012 , vol. 55, # 20 p. 8953 - 8957 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor binding affinity

Species or TestSystem (Pharmacological Data)

not explicitly stated by authors

Method (Pharmacological Data)

labelled ligand: [3H]-(+)-MK-801; name of assay/method: radioligand binding assay

Further Details (Pharmacological Data)

Ki related to: NMDA receptor

Type (Pharmacological Data)

Value of Type (Pharmacological Data)

15 nmol/l

Reference

Wiedemeyer, Kathrin; Wuensch, Bernhard

Carbohydrate Research, 2012 , vol. 359, p. 24 - 29 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor binding affinity

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Species or TestSystem (Pharmacological Data)

not explicitly stated by authors

Method (Pharmacological Data)

labelled ligand: [3H]-(+)-MK-801; name of assay/method: radioligand binding assay

Results

molecular target: NMDA receptor

Reference

Wiedemeyer, Kathrin; Wuensch, Bernhard

Carbohydrate Research, 2012 , vol. 359, p. 24 - 29 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

antagonist

Species or TestSystem (Pharmacological Data)

U2-OS cells; genetically modified/infected with: human GluN1/N2A receptor

Further Details (Pharmacological Data)

FLIPR/Ca2+ assay; pIC50 related to: human GluN1/N2A receptor

Type (Pharmacological Data)

pIC50

Value of Type (Pharmacological Data)

5.9

Reference

Zarantonello, Paola; Bettini, Ezio; Paio, Alfredo; Simoncelli, Chiara; Terreni, Silvia; Cardullo, Francesco

Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 7 p. 2059 - 2063 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

antagonist

Species or TestSystem (Pharmacological Data)

U2-OS cells; genetically modified/infected with: human GluN1/N2A receptor

Further Details (Pharmacological Data)

FLIPR/Ca2+ assay

Results

molecular target: human GluN1/N2A receptor

Reference

Zarantonello, Paola; Bettini, Ezio; Paio, Alfredo; Simoncelli, Chiara; Terreni, Silvia; Cardullo, Francesco

Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 7 p. 2059 - 2063 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

antagonist

Species or TestSystem (Pharmacological Data)

U2-OS cells; genetically modified/infected with: human GluN1/N2B receptor

Further Details (Pharmacological Data)

FLIPR/Ca2+ assay; pIC50 related to: human GluN1/N2B receptor

Type (Pharmacological Data)

pIC50

Value of Type (Pharmacological Data)

6.4

Reference

Zarantonello, Paola; Bettini, Ezio; Paio, Alfredo; Simoncelli, Chiara; Terreni, Silvia; Cardullo, Francesco

Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 7 p. 2059 - 2063 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological

antagonist

Data)

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47 of 219

Species or TestSystem (Pharmacological Data)

U2-OS cells; genetically modified/infected with: human GluN1/N2B receptor

Further Details (Pharmacological Data)

FLIPR/Ca2+ assay

Results

molecular target: human GluN1/N2B receptor

Reference

Zarantonello, Paola; Bettini, Ezio; Paio, Alfredo; Simoncelli, Chiara; Terreni, Silvia; Cardullo, Francesco

Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 7 p. 2059 - 2063 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor binding affinity

Species or TestSystem (Pharmacological Data)

cortex membrane homogenate of pig

Further Details (Pharmacological Data)

radioligand binding assay; radioligand: 2 nM of [3H]-(+)-MK-801; NMDA: N-methyl-D-aspartate receptor; Ki related to: pig NMDA receptor; inhibition constant (Ki)

Type (Pharmacological Data)

Value of Type (Pharmacological Data)

28 nmol/l

Reference

Utech, Tina; Koehler, Jens; Wuensch, Bernhard

European Journal of Medicinal Chemistry, 2011 , vol. 46, # 6 p. 2157 - 2169 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor binding affinity

Species or TestSystem (Pharmacological Data)

cortex membrane homogenate of pig

Further Details (Pharmacological Data)

radioligand binding assay; radioligand: 2 nM of [3H]-(+)-MK-801; NMDA: N-methyl-D-aspartate receptor

Results

molecular target: pig NMDA receptor

Reference

Utech, Tina; Koehler, Jens; Wuensch, Bernhard

European Journal of Medicinal Chemistry, 2011 , vol. 46, # 6 p. 2157 - 2169 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

analgesic

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

female

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

6 mg/kg

Kind of Dosing (Pharmacological Data)

in saline; used as hydrochloride salt

Further Details (Pharmacological Data)

mass of species: 250 - 300 g

effective concentration in tail immersion test

Type (Pharmacological Data)

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Value of Type (Pharmacological Data)

6 mg/kg

Reference

Ahmadi, Abbas; Khalili, Mohsen; Mihandoust, Farnaz; Barghi, Leila

Arzneimittel-Forschung/Drug Research, 2010 , vol. 60, # 1 p. 30 - 35 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

analgesic

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

female

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

6 mg/kg

Kind of Dosing (Pharmacological Data)

in saline; used as hydrochloride salt

Further Details (Pharmacological Data)

mass of species: 250 - 300 g

Type (Pharmacological Data)

effective concentration in formalin test

Value of Type (Pharmacological Data)

6 mg/kg

Reference

Ahmadi, Abbas; Khalili, Mohsen; Mihandoust, Farnaz; Barghi, Leila

Arzneimittel-Forschung/Drug Research, 2010 , vol. 60, # 1 p. 30 - 35 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

[3H]TCP binding to NMDA receptor; inhibition of

Species or TestSystem (Pharmacological Data)

brain homogenate of Sprague-Dawley rat

Sex

male

Further Details (Pharmacological Data)

TCP: 1-[1-(2-thienyl)-1-cyclohexyl]piperidine; NMDA: N-methyl-D-aspartate; brain homogenate used without cerebellum; Ki related to: NMDA receptor; inhibition constant (Ki)

Type (Pharmacological Data)

Value of Type (Pharmacological Data)

53 nmol/l

Reference

Linders, Joannes T. M.; Furlano, David C.; Mattson, Mariena V.; Jacobson, Arthur E.; Rice, Kenner C.

Letters in Drug Design and Discovery, 2010 , vol. 7, # 2 p. 79 - 87 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

[3H]TCP binding to NMDA receptor; inhibition of

Species or TestSystem (Pharmacological Data)

brain homogenate of Sprague-Dawley rat

Sex

male

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Further Details (Pharmacological Data)

TCP: 1-[1-(2-thienyl)-1-cyclohexyl]piperidine; NMDA: N-methyl-D-aspartate; brain homogenate used without cerebellum

Results

molecular target: NMDA receptor

Reference

Linders, Joannes T. M.; Furlano, David C.; Mattson, Mariena V.; Jacobson, Arthur E.; Rice, Kenner C.

Letters in Drug Design and Discovery, 2010 , vol. 7, # 2 p. 79 - 87 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

apoptosis; induction of

Species or TestSystem (Pharmacological Data)

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corticostriatal slice cultures of Sprague-Dawley rat

Concentration (Pharmacological Data)

3 μmol/l

Further Details (Pharmacological Data)

caspase-3 assay and DNA fragmentation using TUNEL staining

Type (Pharmacological Data)

effective concentration

Value of Type (Pharmacological Data)

3 μmol/l

Reference

Xia, Yan; Wang, Cheng Z.; Liu, Jie; Anastasio, Noelle C.; Johnson, Kenneth M.

Neuropharmacology, 2010 , vol. 58, # 2 p. 330 - 336 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

analgesic

Species or TestSystem (Pharmacological Data)

NMRI mouse

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

1 - 10 mg/kg

Further Details (Pharmacological Data)

tail immersion (acute thermal pain) and formalin (acute and chronic chemical pain) tests; pain score at 0-15 min: 2.03 min, at 15-40 min: 1.86 min, at 40-60 min: 1.73 min; mass of species: 20 - 30 g

Type (Pharmacological Data)

increase in tail immersion latency at 5 mg/kg

Value of Type (Pharmacological Data)

Ca. 10 s

Reference

Ahmadi, Abbas; Solati, Jalal; Hajikhani, Ramin; Onagh, Masoud; Javadi, Mojdeh

Arzneimittel-Forschung/Drug Research, 2010 , vol. 60, # 8 p. 492 - 496 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

analgesic

Species or TestSystem (Pharmacological Data)

NMRI mouse

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

1 - 10 mg/kg

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Further Details (Pharmacological Data)

tail immersion (acute thermal pain) and formalin (acute and chronic chemical pain) tests; pain score at 0-15 min: 2.03 min, at 15-40 min: 1.86 min, at 40-60 min: 1.73 min; mass of species: 20 - 30 g

Type (Pharmacological Data)

increase in tail immersion latency at 10 mg/kg

Value of Type (Pharmacological Data)

Ca. 1 s

Reference

Ahmadi, Abbas; Solati, Jalal; Hajikhani, Ramin; Onagh, Masoud; Javadi, Mojdeh

Arzneimittel-Forschung/Drug Research, 2010 , vol. 60, # 8 p. 492 - 496 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

analgesic

Species or TestSystem (Pharmacological Data)

NMRI mouse

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

1 - 10 mg/kg

Further Details (Pharmacological Data)

tail immersion (acute thermal pain) and formalin (acute and chronic chemical pain) tests; pain score at 0-15 min: 2.03 min, at 15-40 min: 1.86 min, at 40-60 min: 1.73 min; mass of species: 20 - 30 g

Type (Pharmacological Data)

pain score at 0-15 min

Value of Type (Pharmacological Data)

1.82 - 2.14 min

Reference

Ahmadi, Abbas; Solati, Jalal; Hajikhani, Ramin; Onagh, Masoud; Javadi, Mojdeh

Arzneimittel-Forschung/Drug Research, 2010 , vol. 60, # 8 p. 492 - 496 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

analgesic

Species or TestSystem (Pharmacological Data)

NMRI mouse

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

1 - 10 mg/kg

Further Details (Pharmacological Data)

tail immersion (acute thermal pain) and formalin (acute and chronic chemical pain) tests; pain score at 0-15 min: 2.03 min, at 15-40 min: 1.86 min, at 40-60 min: 1.73 min; mass of species: 20 - 30 g

Type (Pharmacological Data)

pain score at 15-40 min

Value of Type (Pharmacological Data)

0.9 - 1.83 min

Reference

Ahmadi, Abbas; Solati, Jalal; Hajikhani, Ramin; Onagh, Masoud; Javadi, Mojdeh

Arzneimittel-Forschung/Drug Research, 2010 , vol. 60, # 8 p. 492 - 496 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

analgesic

Species or TestSystem (Pharmacological

NMRI mouse

Data)

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Route of Application

intraperitoneal

Concentration (Pharmacological Data)

1 - 10 mg/kg

Further Details (Pharmacological Data)

tail immersion (acute thermal pain) and formalin (acute and chronic chemical pain) tests; pain score at 0-15 min: 2.03 min, at 15-40 min: 1.86 min, at 40-60 min: 1.73 min; mass of species: 20 - 30 g

Type (Pharmacological Data)

pain score at 40-60 min

Value of Type (Pharmacological Data)

1.27 - 1.98 min

Reference

Ahmadi, Abbas; Solati, Jalal; Hajikhani, Ramin; Onagh, Masoud; Javadi, Mojdeh

Arzneimittel-Forschung/Drug Research, 2010 , vol. 60, # 8 p. 492 - 496 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

acetylcholine-evoked currents; inhibition of

Species or TestSystem (Pharmacological Data)

SH-EP1 cells; genetically modified/infected with: human neuronal nicotinic acetylcholine α4β2 receptor

Further Details (Pharmacological Data)

patch-clamp technique; nH related to: human neuronal nicotinic acetylcholine α4β2 receptor; Hill coefficient (nH)

Type (Pharmacological Data)

Value of Type (Pharmacological Data)

1.4

Reference

Abdrakhmanova, Galya R.; Blough, Bruce E.; Nesloney, Carey; Navarro, Hernan A.; Damaj, M. Imad; Carroll, F. Ivy

Neuropharmacology, 2010 , vol. 59, # 6 p. 511 - 517 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

acetylcholine-evoked currents; inhibition of

Species or TestSystem (Pharmacological Data)

SH-EP1 cells; genetically modified/infected with: human neuronal nicotinic acetylcholine α4β2 receptor

Further Details (Pharmacological Data)

patch-clamp technique; inhibitory concentration (IC)

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

28.97 μmol/l

Reference

Abdrakhmanova, Galya R.; Blough, Bruce E.; Nesloney, Carey; Navarro, Hernan A.; Damaj, M. Imad; Carroll, F. Ivy

Neuropharmacology, 2010 , vol. 59, # 6 p. 511 - 517 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

acetylcholine-evoked currents; inhibition of

Species or TestSystem (Pharmacological Data)

SH-EP1 cells; genetically modified/infected with: human neuronal nicotinic acetylcholine α4β2 receptor

Further Details (Pharmacological Data)

patch-clamp technique

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Results

molecular target: human neuronal nicotinic acetylcholine α4β2 receptor

Reference

Abdrakhmanova, Galya R.; Blough, Bruce E.; Nesloney, Carey; Navarro, Hernan A.; Damaj, M. Imad; Carroll, F. Ivy

Neuropharmacology, 2010 , vol. 59, # 6 p. 511 - 517 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

acetylcholine-evoked currents; inhibition of

Species or TestSystem (Pharmacological Data)

HEK 293 cells; genetically modified/infected with: rat neuronal nicotinic acetylcholine α3β4 receptor

Further Details (Pharmacological Data)

patch-clamp technique; nH related to: rat neuronal nicotinic acetylcholine α3β4 receptor; Hill coefficient (nH)

Type (Pharmacological Data)

Value of Type (Pharmacological Data)

0.65

Reference

Abdrakhmanova, Galya R.; Blough, Bruce E.; Nesloney, Carey; Navarro, Hernan A.; Damaj, M. Imad; Carroll, F. Ivy

Neuropharmacology, 2010 , vol. 59, # 6 p. 511 - 517 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

acetylcholine-evoked currents; inhibition of

Species or TestSystem (Pharmacological Data)

HEK 293 cells; genetically modified/infected with: rat neuronal nicotinic acetylcholine α3β4 receptor

Further Details (Pharmacological Data)

patch-clamp technique; inhibitory concentration (IC)

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

6.35 μmol/l

Reference

Abdrakhmanova, Galya R.; Blough, Bruce E.; Nesloney, Carey; Navarro, Hernan A.; Damaj, M. Imad; Carroll, F. Ivy

Neuropharmacology, 2010 , vol. 59, # 6 p. 511 - 517 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

acetylcholine-evoked currents; inhibition of

Species or TestSystem (Pharmacological Data)

HEK 293 cells; genetically modified/infected with: rat neuronal nicotinic acetylcholine α3β4 receptor

Further Details (Pharmacological Data)

patch-clamp technique

Results

molecular target: rat neuronal nicotinic acetylcholine α3β4 receptor

Reference

Abdrakhmanova, Galya R.; Blough, Bruce E.; Nesloney, Carey; Navarro, Hernan A.; Damaj, M. Imad; Carroll, F. Ivy

Neuropharmacology, 2010 , vol. 59, # 6 p. 511 - 517 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

acetylcholine-evoked currents; inhibition of

Species or TestSystem (Pharmacological Data)

HEK 293 cells; genetically modified/infected with: rat neuronal nicotinic acetylcholine α7 receptor

Further Details (Pharmacological

patch-clamp technique; 55percent inhibition by title comp. at 0.1 μmol/l; nH related to: rat neuronal nicotinic acetylcholine α7 receptor; Hill coefficient (nH)

Data)

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Type (Pharmacological Data)

Value of Type (Pharmacological Data)

0.97

Reference

Abdrakhmanova, Galya R.; Blough, Bruce E.; Nesloney, Carey; Navarro, Hernan A.; Damaj, M. Imad; Carroll, F. Ivy

Neuropharmacology, 2010 , vol. 59, # 6 p. 511 - 517 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

acetylcholine-evoked currents; inhibition of

Species or TestSystem (Pharmacological Data)

HEK 293 cells; genetically modified/infected with: rat neuronal nicotinic acetylcholine α7 receptor

Further Details (Pharmacological Data)

patch-clamp technique; 55percent inhibition by title comp. at 0.1 μmol/l; inhibitory concentration (IC)

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

1.25 μmol/l

Reference

Abdrakhmanova, Galya R.; Blough, Bruce E.; Nesloney, Carey; Navarro, Hernan A.; Damaj, M. Imad; Carroll, F. Ivy

Neuropharmacology, 2010 , vol. 59, # 6 p. 511 - 517 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

acetylcholine-evoked currents; inhibition of

Species or TestSystem (Pharmacological Data)

HEK 293 cells; genetically modified/infected with: rat neuronal nicotinic acetylcholine α7 receptor

Further Details (Pharmacological Data)

patch-clamp technique; 55percent inhibition by title comp. at 0.1 μmol/l

Results

molecular target: rat neuronal nicotinic acetylcholine α7 receptor

Reference

Abdrakhmanova, Galya R.; Blough, Bruce E.; Nesloney, Carey; Navarro, Hernan A.; Damaj, M. Imad; Carroll, F. Ivy

Neuropharmacology, 2010 , vol. 59, # 6 p. 511 - 517 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

nicotine-induced antinociception; inhibition of

Species or TestSystem (Pharmacological Data)

ICR mouse

Sex

male

Route of Application

subcutaneous

Further Details (Pharmacological Data)

tail-flick test; 20percent inhibition by title comp. at 10 mg/kg in hot-plate test; 20percent inhibition by comparative comp. at 5 mg/kg in hot-plate test; antinociceptive dose (AD)

Type (Pharmacological Data)

AD50

Value of Type (Pharmacological Data)

1.1 mg/kg

Reference

Abdrakhmanova, Galya R.; Blough, Bruce E.; Nesloney, Carey; Navarro, Hernan A.; Damaj, M. Imad; Carroll, F. Ivy

Neuropharmacology, 2010 , vol. 59, # 6 p. 511 - 517 Title/Abstract Full Text View citing articles Show Details

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Effect (Pharmacological Data)

nicotine-induced antinociception; inhibition of

Species or TestSystem (Pharmacological Data)

ICR mouse

Sex

male

Route of Application

subcutaneous

Further Details (Pharmacological Data)

tail-flick test; 20percent inhibition by title comp. at 10 mg/kg in hot-plate test; 20percent inhibition by comparative comp. at 5 mg/kg in hot-plate test

Results

molecular target: neuronal nicotinic acetylcholine receptor

Reference

Abdrakhmanova, Galya R.; Blough, Bruce E.; Nesloney, Carey; Navarro, Hernan A.; Damaj, M. Imad; Carroll, F. Ivy

Neuropharmacology, 2010 , vol. 59, # 6 p. 511 - 517 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

antinociceptive

Species or TestSystem (Pharmacological Data)

ICR mouse

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

5 mg/kg

Further Details (Pharmacological Data)

effect rate determined in tail-flick and hot-plate tests

Type (Pharmacological Data)

effect rate

Value of Type (Pharmacological Data)

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5 - 6 percent

Reference

Abdrakhmanova, Galya R.; Blough, Bruce E.; Nesloney, Carey; Navarro, Hernan A.; Damaj, M. Imad; Carroll, F. Ivy

Neuropharmacology, 2010 , vol. 59, # 6 p. 511 - 517 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

antinociceptive

Species or TestSystem (Pharmacological Data)

ICR mouse

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

5 mg/kg

Further Details (Pharmacological Data)

effect rate determined in tail-flick and hot-plate tests

Results

molecular target: neuronal nicotinic acetylcholine receptor

Reference

Abdrakhmanova, Galya R.; Blough, Bruce E.; Nesloney, Carey; Navarro, Hernan A.; Damaj, M. Imad; Carroll, F. Ivy

Neuropharmacology, 2010 , vol. 59, # 6 p. 511 - 517 Title/Abstract Full Text View citing articles Show Details

Effect

receptor binding affinity

(Pharmacological Data)

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Species or TestSystem (Pharmacological Data)

electric organ AChR native membranes of Torpedo californica

Kind of Dosing (Pharmacological Data)

title comp. used as hydrochloride

Further Details (Pharmacological Data)

AChR: nicotinic acetylcholine receptor; binding studied in AChR desensitized (carbamylcholine chloride-bound) conformational state; radioligand binding assay; radioligand: 15 nM [3H]ibogaine; inhibition constant (Ki); Ki related to: α1β1γδ AChR

Type (Pharmacological Data)

Value of Type (Pharmacological Data)

0.39 μmol/l

Reference

Arias, Hugo R.; Feuerbach, Dominik; Targowska-Duda, Katarzyna M.; Jozwiak, Krzysztof

Neurochemistry International, 2010 , vol. 57, # 2 p. 153 - 161 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor binding affinity

Species or TestSystem (Pharmacological Data)

electric organ AChR native membranes of Torpedo californica

Kind of Dosing (Pharmacological Data)

title comp. used as hydrochloride

Further Details (Pharmacological Data)

AChR: nicotinic acetylcholine receptor; binding studied in AChR desensitized (carbamylcholine chloride-bound) conformational state; radioligand binding assay; radioligand: 15 nM [3H]ibogaine

Results

molecular target: α1β1γδ AChR

Reference

Arias, Hugo R.; Feuerbach, Dominik; Targowska-Duda, Katarzyna M.; Jozwiak, Krzysztof

Neurochemistry International, 2010 , vol. 57, # 2 p. 153 - 161 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)

Value of Type (Pharmacological Data)

0.27 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

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

Data)

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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)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

CHO cells expressing human dopamine D2Long receptors

Concentration (Pharmacological Data)

0.01 - 10000 nmol/l

Method (Pharmacological Data)

cells incubated with buffer containing GDP and <35S>GTPγS for 40 min at 22 deg C; title comp. added with or without 1 μmol/l dopamine; filtered; radioactivity detected by liquid scintillation counting; <35S>GTPγS binding determined

Further Details (Pharmacological Data)

control: vehicle; references: (+)terguride and S(-)-3-(3-hydroxyphenyl)-N-n-propyl-piperidine; further, effect of title comp. in presence of 150 mmol/l NaCl observed; <35S>GTPγ: guanosine-5'-O-(3-<35S>thio)-triphosphate

Results

<35S>GTPγS binding was unaffected by title comp.; dopamine activity was unchanged in response to title comp.; title comp. was inactive under conditions of low sodium; fig.

Reference

Jordan, Shaun; Chen, Ruoyan; Fernalld, Raymond; Johnson, Janelle; Regardie, Karen; Kambayashi, Junichi; Tadori, Yoshihiro; Kitagawa, Hisashi; Kikuchi, Tetsuro

European Journal of Pharmacology, 2006 , vol. 540, # 1-3 p. 53 - 56 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

CHO cells expressing human dopamine D2Long receptors

Concentration (Pharmacological Data)

10 μmol/l

Method (Pharmacological Data)

cells incubated with Fluo-3AM and pluronic F-127 for 75 min; washed; title comp. added with or without 1 μmol/l dopamine; densitometric image analysis done; effect of title comp. on dopamine-induced intracellular Ca(2+) mobilization determined

Further Details (Pharmacological Data)

control: vehicle; references: (+)terguride and S(-)-3-(3-hydroxyphenyl)-N-n-propyl-piperidine

Results

Ca(2+) mobilization was unaffected by title comp.; dopamine activity was not affected by title comp.; fig.

Reference

Jordan, Shaun; Chen, Ruoyan; Fernalld, Raymond; Johnson, Janelle; Regardie, Karen; Kambayashi, Junichi; Tadori, Yoshihiro; Kitagawa, Hisashi; Kikuchi, Tetsuro

European Journal of Pharmacology, 2006 , vol. 540, # 1-3 p. 53 - 56 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

rat dorsal striatal membranes

Concentration (Pharmacological Data)

0.01 - 10000 nmol/l

Method (Pharmacological Data)

test system incubated with <35S>GTPγS for 60 min at 30 deg C; title comp. added with or without 1 μmol/l dopamine; filtered; radioactivity detected by liquid scintillation counting; <35S>GTPγS binding determined

Further Details (Pharmacological Data)

control: vehicle; references: (+)terguride and S(-)-3-(3-hydroxyphenyl)-N-n-propyl-piperidine; <35S>GTPγ: guanosine-5'-O-(3<35S>thio)-triphosphate

Results

title comp. was inactive in <35S>GTPγS binding to test system; dopamine activity was unchanged in response to title comp.

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Reference

Jordan, Shaun; Chen, Ruoyan; Fernalld, Raymond; Johnson, Janelle; Regardie, Karen; Kambayashi, Junichi; Tadori, Yoshihiro; Kitagawa, Hisashi; Kikuchi, Tetsuro

European Journal of Pharmacology, 2006 , vol. 540, # 1-3 p. 53 - 56 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 - 4 mg/kg

Method (Pharmacological Data)

operant behaviour test; rats on a fixed-interval 90 seconds schedule of water reinforcement received title comp. 20 min prior to session; number of reinforcers per session and quarter-life values detected

Further Details (Pharmacological Data)

further investigations after bilateral intraventricular injection of 6-hydroxytriptamine or kainic acid (neurotoxic lesion of striatum)

Results

title comp. dose-dependently decreased number of reinforcers and quarter-life values; 6-hydroxytriptamine treatment resulted in tolerance to schedule-disruptive effect of title comp., whereas kainic acid treatment increased sensitivity to title comp.

Reference

Carlson, Kirsten M.; Wagner, George C.

Life Sciences, 2005 , vol. 77, # 4 p. 372 - 385 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 - 4 mg/kg

Method (Pharmacological Data)

operant behaviour test; rats on a fixed-interval 90 seconds schedule of water reinforcement received title comp. 20 min prior to session; response rate per min detected

Further Details (Pharmacological Data)

further investigations with bilateral intraventricular injection of 6-hydroxytriptamine or kainic acid (neurotoxic lesion of striatum)

Type (Pharmacological Data)

ED50

Value of Type (Pharmacological Data)

Ca. 3.6 mg/kg

Results

title comp. increased response rate up to conc. of 1 mg/kg and than decreased it; 6-hydroxytriptamine treatment resulted in tolerance to schedule-disruptive effect of title comp., whereas kainic acid treatment increased sensitivity to title comp.

Reference

Carlson, Kirsten M.; Wagner, George C.

Life Sciences, 2005 , vol. 77, # 4 p. 372 - 385 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

apoptosis induction

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat corticostriatal slices

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Concentration (Pharmacological Data)

3 μmol/l

Kind of Dosing (Pharmacological Data)

dissolved in Dulbecco's modified Eagle's medium

Method (Pharmacological Data)

brain tissues cultured with title comp. for 48 h followed by 24 h washout; nuclei containing fragmented DNA determined by TUNEL assay; 0.1 μg/ml Hoechst 33258 staining; light microscopy with epifluorescence equipment (excitation at 365 nm)

Further Details (Pharmacological Data)

brain slices from 7-days-old neonatal rats

Results

title comp. increased DNA fragmentation in frontal cortex, but not in striatum (figures)

Reference

Wang, Cheng; Fridley, Jared; Johnson, Kenneth M.

Biochemical Pharmacology, 2005 , vol. 69, # 9 p. 1373 - 1383 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

apoptosis induction

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat corticostriatal slices

Concentration (Pharmacological Data)

3 μmol/l

Kind of Dosing (Pharmacological Data)

dissolved in Dulbecco`s modified Eagle`s medium

Method (Pharmacological Data)

brain tissues cultured with title comp. for 2-48 h followed by 2-24 h washout; apoptosis assessed by measuring nucleosomal DNA fragmentation using two-site ELISA assay with chromogen as substrate; optical density measured at 405 nm

Further Details (Pharmacological Data)

slices from 7-d-old neonatal rats; chromogen: 2,2'-azinobis(3-ethylbinzthiazoline) sulfonic acid; further investigation with antisense or sense ODN for NR1, antisense ODN for NR2A and NR2B; ODN: oligodeoxy-nucleotide; NR: N-methyl-D-aspartate receptor

Results

title comp. induced DNA fragmentation after treatment for 24 or 48 h followed by at least 8 h washout (figures); induction of cortical apoptosis by title comp. treatment prevented by co-incubation with NR1 and NR2A but not NR2B antisense ODN (figures)

Reference

Wang, Cheng; Fridley, Jared; Johnson, Kenneth M.

Biochemical Pharmacology, 2005 , vol. 69, # 9 p. 1373 - 1383 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein expression; induction of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat corticostriatal slices

Concentration (Pharmacological Data)

3 μmol/l

Kind of Dosing (Pharmacological Data)

dissolved in Dulbecco's modified Eagle's medium

Method (Pharmacological Data)

brain tissues from 7-days-old rats cultured with title comp. for 48 h followed by 24 h washout; total protein extracted; Bax, Bcl-xL, NR1, NR2A and NR2B protein levels determined by Western blotting

Further Details (Pharmacological Data)

further investigations with 2 μmol/l antisense or sense ODN for NR1, antisense ODN for NR2A and NR2B; ODN: oligodeoxy-nucleotide; NR: N-methyl-D-aspartate receptor

Results

title comp. increased expression of Bax and NR2A only in cortex and NR1 in cortex and striatum; this effect prevented by co-incubation with NR1 and NR2A but not NR2B antisense ODN (figures); no effect on Bcl-xL and NR2B proteins

Reference

Wang, Cheng; Fridley, Jared; Johnson, Kenneth M.

Biochemical Pharmacology, 2005 , vol. 69, # 9 p. 1373 - 1383 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological

locomotor activity; effect on

Data) Species or TestSystem (Pharmacological Data)

C57BL/6 mouse

Sex

male

Route of Application

intraperitoneal

Method (Pharmacological Data)

Experimental Example 1.8 Changes in Locomotor Activity Following Repeated Administration of Morphinans or Phencyclidine (PCP) The behavioral data are summarized in FIGS. 2-4. Saline-injected animals showed basal locomotor activity. Repeated administration of DX or DM (20 or 40 mg/kg) significantly increased locomotor activity. This effect appeared to be more pronounced in the animals treated with DX than in those treated with DM. The behavioural profile induced by DX is comparable to that of PCP. Although treatment with AM appeared to increase locomotor activity slightly, the locomotor activity following treatment with HM, CM or DF was comparable to that with saline (FIG. 2A). DX induced a significant increase in marginal activity (circling behaviour) in a dose-related manner (DX 20 or 40 mg/kg vs. saline, p<0.01). The behavioral effect induced by DX was similar to that of PCP (PCP 2.5 vs. 5.0 mg/kg, p<0.05). In contrast, DM also induced a significant increase in marginal activity (DM 20 or 40 mg/kg vs. saline, p<0.05). However, HM, AM, CM, and DF did not significantly affect marginal activity versus the saline group (FIG. 2B). PCP produced much stronger stereotypies (i.e. circling behaviorsmarginal activities) than seen in any other group (FIGS. 2A and B). Saline-treated animals did not show any significant locomotor pattern. The locomotor patterns were significantly altered after treatment with PCP, DM, and DX. PCP, DM, and DX produced marginal activity (circling behaviour). By contrast, HM, AM, CM and DF did not produce significant marginal activity in any locomotor pattern (FIG. 3).

Results

treatment with title compound significantly increased locomotor activity at 2.5 or 5 mg/kg concentrations; figure is given

Location

Page/Page column 2; 52-53; Sheet 2

Reference

KIM, Dr. Hyoung-Chun; GREEN CROSS CORP.

Patent: US2005/256147 A1, 2005 ; Title/Abstract Full Text Show Details

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Effect (Pharmacological Data)

marginal activity; induction of

Species or TestSystem (Pharmacological Data)

C57BL/6 mouse

Sex

male

Route of Application

intraperitoneal

Method (Pharmacological Data)

Results

title compound treatment indiced a significant increase in marginal activity in a dose-dependent manner; figure is given

Location

Page/Page column 2; 52-53; Sheet 2

Reference

KIM, Dr. Hyoung-Chun; GREEN CROSS CORP.

Patent: US2005/256147 A1, 2005 ; Title/Abstract Full Text Show Details

84 of 219

Effect (Pharmacological Data)

locomotor patterns; effect on

Species or TestSystem (Pharmacological Data)

C57BL/6 mouse

Sex

male

Route of Application

intraperitoneal

Method (Pharmacological Data)

to increase locomotor activity slightly, the locomotor activity following treatment with HM, CM or DF was comparable to that with saline (FIG. 2A). DX induced a significant increase in marginal activity (circling behaviour) in a dose-related manner (DX 20 or 40 mg/kg vs. saline, p<0.01). The behavioral effect induced by DX was similar to that of PCP (PCP 2.5 vs. 5.0 mg/kg, p<0.05). In contrast, DM also induced a significant increase in marginal activity (DM 20 or 40 mg/kg vs. saline, p<0.05). However, HM, AM, CM, and DF did not significantly affect marginal activity versus the saline group (FIG. 2B). PCP produced much stronger stereotypies (i.e. circling behaviorsmarginal activities) than seen in any other group (FIGS. 2A and B). Saline-treated animals did not show any significant locomotor pattern. The locomotor patterns were significantly altered after treatment with PCP, DM, and DX. PCP, DM, and DX produced marginal activity (circling behaviour). By contrast, HM, AM, CM and DF did not produce significant marginal activity in any locomotor pattern (FIG. 3). Results

locomotor patterns were significantly altered after treatment with 2.5 or 5.0 mg/kg title compound; title compound treatment produced marginal activity in any locomotor pattern; figure is given

Location

Page/Page column 2; 52-53; Sheet 3

Reference

KIM, Dr. Hyoung-Chun; GREEN CROSS CORP.

Patent: US2005/256147 A1, 2005 ; Title/Abstract Full Text Show Details

85 of 219

Effect (Pharmacological Data)

conditioned place preference (CPP); effect on

Species or TestSystem (Pharmacological Data)

C57BL/6 mouse

Sex

male

Route of Application

intraperitoneal

Method (Pharmacological Data)

Experimental Example 1.9 Changes of Conditioned Place Preference (CPP) Profile Following Repeated Administration of Morphinans or Phencyclidine (PCP) The saline-treated animals did not show any CPP effects. DX-treated animals produced CPP in a dose-dependent manner (DX 20 or 40 mg/kg vs. saline, p<0.01; DX 20 vs. 40 mg/kg, p<0.05). As with DX, treatment with DM also produced CPP (DM 20 mg/kg vs. saline, p<0.05; DM 40 mg/kg vs. saline, p<0.01). The most significant CPP followed PCP (PCP 5 mg/kg vs. saline, p<0.001; PCP 2.5 vs. 5.0 mg/kg, p<0.05). By contrast, HM, CM, AM and DF-treated animals showed almost no CPP effects compared with saline-treated animals (FIG. 4).

Results

title compound treatment produced changes of conditioned place preference (CPP) in a dose-dependent manner; figure is given

Location

Page/Page column 2; 52-53; Sheet 4

Reference

KIM, Dr. Hyoung-Chun; GREEN CROSS CORP.

Patent: US2005/256147 A1, 2005 ; Title/Abstract Full Text Show Details

86 of 219

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

KXα3β4R2 cells expressing α3β4 nAChR

Concentration (Pharmacological Data)

10 μmol/l

Method (Pharmacological Data)

chromatographic system; cells used to create the column on immobilized artificial membrane stationary phase; chromatograms detected with MS chromatographic parameters determined

Further Details (Pharmacological Data)

chromatographic parameters: k': thermodynamic capacity factor; kon: association rate constant; koff: dissociation rate constant; K: equilibrium constant for complex formation

Results

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k': 24.1; kon: 23.2 (μmol/l)-1*s-1; koff: 2.69 s-1; K: 8.6 (μmol/l)-1

Reference

Jozwiak, Krzysztof; Ravichandran, Sarangan; Collins, Jack R.; Wainer, Irving W.

Journal of Medicinal Chemistry, 2004 , vol. 47, # 16 p. 4008 - 4021 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; examination of

Species or TestSystem (Pharmacological Data)

human liver cytosol

Concentration (Pharmacological Data)

50 μmol/l

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Kind of Dosing (Pharmacological Data)

DMSO stock; final solvent conc. 1 percent (v/v)

Method (Pharmacological Data)

aldehyde oxidase study; phthalazine (2 μmol/l) preincubated with title comp. at 37 deg C; reaction mixture containing cytosol, EDTA and potassium phosphate buffer (pH 7.4) added; 2.5 min incubation; 1-phthalazinone in filtrate analysed by HPLC-MS

Further Details (Pharmacological Data)

EDTA: ethylenediaminetetraacetic acid

Comment (Pharmacological Data)

No effect

Reference

Obach, R. Scott; Huynh, Phuong; Allen, Mary C.; Beedham, Christine

Journal of Clinical Pharmacology, 2004 , vol. 44, # 1 p. 7 - 19 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

anti-schizophrenic

Species or TestSystem (Pharmacological Data)

hooded Long Evans of rat

Sex

male

Route of Application

intraperitoneal

Method (Pharmacological Data)

In vivo activity: To test the hypothesis that a serominic compound would show efficacy in the treatment of schizophrenia, we exploited our recent discovery of an animal model of schizophrenia that mimics the neurochemical and metabolic dysfunction in the brains of patients with schizophrenia (Cochran et al. , 2003). Schizophrenic patients show reduced metabolic activity in the prefrontal cortex, auditory system and hippocampus, along with reduced levels of expression of parvalbumin within inhibitory interneurones of the prefrontal cortex. The hypometabolism in the prefrontal cortex is not restored to normal by typical APDs, or by atypical APDs such as clozapine, although the hypometabolism in the auditory system is thought to be improved by both typical and atypical APDs (Schroeder et al. , 1994; Andreasen et al. , 1992 and Potkin et al., 1994). We have previously reported (Cochran et al., 2003) that these deficits observed in schizophrenic patients are reproduced in rats treated chronically with phencyclidine (PCP) -a drug known to cause schizophrenic symptoms when administered chronically in humans. We have also observed that, in parallel with the clinical observations, the prefrontal cortex hypometabolism in PCPtreated rats is not attenuated by the representative atypical and typical antipsychotic drugs clozapine or haloperidol (Cochran et al. , 2003), whereas the hypometabolism in the auditory system is restored towards normal levels by both haloperidol and clozapine. Thus evidence that a serominic compound could restore the prefrontal cortex hypometabolism in PCP-treated rats towards normal levels would indicate that a serominic compound would be more effective than currently available antipsychotic drugs for the treatment of schizophrenia. (5R, 6R) 6- (3-PROPYLTHIO-1, 2, 5-THIADIAZOL-4-YL)-1- azabicyclo (3.2. 1) octane. When the M4 muscarinic partial agonist (PTAC) (Calbiochem Biochemicals) was administered chronically in combination with the 5-HT7 antagonist SB258741, the drug combination was found to attenuate the hypometabolism in the prefrontal cortex, and thus demonstrate efficacy superior not only to haloperidol, but also to clozapine. A similar effect was observed in the reticular thalamus, which is a brain region functionally connected with the prefrontal cortex and involved in the regulation of its activity. In addition, the hypometabolism in the auditory system was also restored to normal by the M4 AGONIST/5-HT7 antagonist combination. Thus, the combination of M4 AGONIST/5-HT7 antagonist appears to exert profound antipsychotic activity, as assessed by these markers, in the absence of any Dz affinity. Experimental procedure Male hooded Long Evans rats (180-220g) were randomly allocated to one of the following treatment groups: vehicle/vehicle, PCP/vehicle, and PCP/SB258741+PTAC. The first drug (PCP or vehicle) was administered by i. p injection and the second drug combination (SB258741 + PTAC) was delivered via osmotic minipump which was implanted under halothane anaesthetic on day 8 of the YRING PCP model. See W001/75440. The doses of drug used were 2.58mg/kg PCP, vehicle (sterile saline), O. lmg/kg/day PTAC together with SB258741 20mg/kg/day. The full treatment paradigm of the chronic PCP model is shown in Figure 1. On the day of the 2-DG procedure, the animals were prepared according to the method of Crane and Porrino, (1989). The brains were sectioned and exposed to X-ray film and LCGU measurements were calculated using the MCID 5 densitometry system. The results were analysed using a one way ANOVA followed by LSD post hoc test where appropriate for each discrete brain region. Statistical significance was defined as P<0. 05. The rats treated chronically with the M4 agonist/5- HT7 antagonist combination did not show any overt evidence of side-effects. LCGU within cortical regions The effect of PTAC and SB258741 (the serominic combination) on LCGU within cortical brain regions is shown in table 1.1. Th

Results

PCP shows significant decrease in LCGU (local glucose utilisation) following chronic PCP compared to controls in layer 1 (19percent) and layers II and III (25percent). Layers VVI was just outside statistical significance. When SB258741+PTAC were administered in conjunction with PCP they reversed the PCP-induced hypofunction back to control levels; synergistic effect between PCP and PTAC/SB; figure 1

Location

Page/Page column 26-29

Reference

MITSUBISHI PHARMA CORPORATION

Patent: WO2004/87124 A1, 2004 ; Title/Abstract Full Text Show Details

89 of 219

Effect (Pharmacological Data)

anti-schizophrenic

Species or TestSystem (Pharmacological Data)

hooded Long Evans of rat

Sex

male

Route of Application

intraperitoneal

Method (Pharmacological Data)

LCGU within auditory structures Table 1.2 shows the effect of the serominic combination given in combination with the YRING PCP Model on LCGU in auditory brain structures. PCP treatment induced a metabolic hypofunction within a few structures of the auditory system. Within the ventral lateral lemniscus, the ventral cochlear nucleus and the primary auditory cortex chronic PCP treatment significantly reduced LCGU (26percent, 21percent and 25percent respectively). In all these three auditory structures the serominic combination reversed the PCP-induced hypofunction

Results

PCP treatment induced a metabolic hypofunction within a few structures of the auditory system. Within the ventral lateral lemniscus, the ventral cochlear nucleus and the primary auditory cortex chronic PCP treatment significantly reduced LCGU (local glucose utilisation) (26percent, 21percent and 25percent respectively). In all these three auditory structures the serominic combination PTAC/SB reversed the PCP-induced hypofunction back to control levels; synergistic effect between PCP and PTAC/SB; figure 1

Location

Page/Page column 29

Reference

MITSUBISHI PHARMA CORPORATION

Patent: WO2004/87124 A1, 2004 ; Title/Abstract Full Text Show Details

90 of 219

Effect (Pharmacological Data)

anti-schizophrenic

Species or TestSystem (Pharmacological Data)

hooded Long Evans of rat

Sex

male

Route of Application

intraperitoneal

Method (Pharmacological Data)

LCGU within thalamic nuclei The effect of the serominic given in combination with the YRING PCP Model on LCGU within thalamic brain regions is shown in table 1.3. The only thalamic nuclei which displayed a metabolic hypofunction with PCP was the reticular thalamus. Within the dorsal region of the reticular thalamus LCGU was significantly decreased by 25percent and in the ventral reticular thalamus the PCP-induced decrease was 21percent. In both regions of the reticular thalamus the serominic combination completely reversed the PCPinduced hypofunction.

Results

PCP treatment induced a metabolic hypofunction within thalamic brain. Within the dorsal region of the reticular thalamus LCGU was significantly decreased by 25percent and in the ventral reticular thalamus the PCP-induced decrease was 21percent. In both regions of the reticular thalamus the serominic combination PTAC/SB completely reversed the PCP-induced hypofunction; synergistic effect between PCP and PTAC/SB; figure 1

Location

Page/Page column 30

Reference

MITSUBISHI PHARMA CORPORATION

Patent: WO2004/87124 A1, 2004 ; Title/Abstract Full Text Show Details

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Effect (Pharmacological Data)

neuroregulatoric

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat prefrontal cortex

Sex

male

Concentration (Pharmacological Data)

1 - 10 μmol/l

Kind of Dosing (Pharmacological Data)

solution of title comp. applied either using negative currents <= 50 nA (micro-iontophoresis), or pressure ejection (5 - 40 psi for 10 - 20 ms at 15 - 40 pulses/s)

Method (Pharmacological Data)

280 - 300-μm coronal slices; medium at room temp. saturated with 95 percent O2/5 percent CO2; whole-cell recordings from pyramidal cells; Glu (100 mmol/l, pH 8.5) application on apical dendrites in presence of title comp.; voltage and current signals were analysed

Further Details (Pharmacological Data)

reference comp.: ketamine and CGP37849; further investigation in presence of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) blocker NBQX; selective activation of NMDA receptors was also performed; ISI: interspike interval; Glu: glutamate

Results

title comp. decreased number of Glu-induced bursts; at 1-5 μmol/l decreased spikes per burst and increased ISI; at 10 μmol/l increased spikes per burst and decreased ISI; effect was secondary to the increased AMPA receptor contribution to Glu response

Reference

Shi, Wei-Xing; Zhang, Xue-Xiang

Journal of Pharmacology and Experimental Therapeutics, 2003 , vol. 305, # 2 p. 680 - 687 Title/Abstract Full Text View citing articles Show Details

Effect

neuroprotective

(Pharmacological Data)

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94 of 219

Species or TestSystem (Pharmacological Data)

Meriones unguiculatus, Mongolian gerbil

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

3.2 - 32 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. was dissolved in physiological saline and administered in a volume of 1 ml/100 g body weight

Method (Pharmacological Data)

gerbils admin. with title comp.; after 30 min, induced with transient global cerebral ischemia by bilateral occlusion of common carotid arteries for 5 min; locomotor activity of gerbils measured for 30 min, 24 h after reperfusion

Further Details (Pharmacological Data)

controls: sham-operated and vehicle-treated gerbils

Type (Pharmacological Data)

ED50

Value of Type (Pharmacological Data)

4.64 mg/kg

Results

title comp. treatment significantly ameliorated locomotor hyperactivity; table

Reference

Katsuta, Kiyotaka; Umemura, Kazuo; Ueyama, Noriko; Matsuoka, Nobuya

European Journal of Pharmacology, 2003 , vol. 467, # 1-3 p. 103 - 109 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neuroprotective

Species or TestSystem (Pharmacological Data)

Meriones unguiculatus, Mongolian gerbil

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

3.2 - 32 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. was dissolved in physiological saline and administered in a volume of 1 ml/100 g body weight

Method (Pharmacological Data)

gerbils admin. with title comp.; after 30 min, transient global cerebral ischemia induced by bilateral occlusion of common carotid arteries for 5 min; after 4 days, brain removed; coronal blocks stained; intact neurons in hippocampal CA1 counted

Further Details (Pharmacological Data)

controls: sham-operated and vehicle-treated gerbils

Type (Pharmacological Data)

ED50

Value of Type (Pharmacological Data)

7.60 mg/kg

Results

title comp. treatment significantly ameliorated hippocampal delayed neuronal death; title comp. showed almost complete blockade of delayed neuronal death at highest doses; table

Reference

Katsuta, Kiyotaka; Umemura, Kazuo; Ueyama, Noriko; Matsuoka, Nobuya

European Journal of Pharmacology, 2003 , vol. 467, # 1-3 p. 103 - 109 Title/Abstract Full Text View citing articles Show Details

Effect

prepulse inhibition (PPI) disruption; inducing

(Pharmacological Data) Species or TestSystem (Pharmacological Data)

rat

Method (Pharmacological Data)

In order to study the effect of alpha2-antagonists on startle reflex and its prepulse- inhibition, groups of rats (n =10/group) were pretreated with the alpha2C-antagonist or vehicle 20 min before measurement of the acoustic startle reactivity and PPI in a test system designed for startle studies (SR-LAB, San Diego Instruments, CA, USA). In a subsequent experiment the effects of the alpha2-adrenoceptor subtype selective alpha2C-antagonist and or the subtype non-selective antagonist atipamezole (Haapalinna, A. et al., NaunynSchmiedeberg's Arch. Pharmacol. 356 (1997) 570- 582) on PCP-induced PPI-disruption was studied. The antagonists were given 20 min, and PCP or vehicle 10 min before start of the startle measurements. The method otherwise corresponds to the procedure described in Sallinen, J. et al., J. Neurosci. 18 (1998) 3035-42. It was found that the receptor subtype selective alpha2C-antagonist acridin-9-yl- [4- (4methylpiperazin-1-yl)-phenyl] amine (JP-1302) did not affect the startle reflex per se, but it increased PPI dose-dependently and effectively (Figures 1A and 1B). The effect of the alpha2C-antagonist was especially clearly seen in the presence of PCP (Figures 2A and 2B). In the Figures 2A and 2B it is also shown that the specific and potent alpha2-antagonist atipamezole, that has no alpha2-adrenoceptor subtype selectivity, increased significantly the startle reactivity per se, but it had no effect on the PPI phenomenon; this points to the significance of the alpha2C-adrenoceptor subtype selective antagonism. ; Figures 1A and 1B show the effect of the selective alpha2C-antagonist acridin-9yl- [4- (4-methylpiperazin-1-yl)-phenyl] amine (JP-1302) (WO 01/64645) on the startle reflex and its prepulse inhibition in rats. The selective alpha2C-antagonist enhanced sensorimotor gating (prepulse inhibition percent) without significantly affecting the startle reactivity to intense pulses without prepulses. Asterisk refers to significant difference between vehicle and treatment group p<0.05 ; 1-way ANOVA and LSD post hoc test.

Results

title compound induced prepulse inhibition (PPI) disruption; see Fig. 2A, 2B

Location

Page/Page column 3-5

Reference

ORION CORPORATION

Patent: WO2003/82825 A1, 2003 ; Title/Abstract Full Text Show Details

95 of 219

Effect (Pharmacological Data)

starle magnitude; effect on

Species or TestSystem (Pharmacological Data)

rat

Method (Pharmacological Data)

Figures 2A and 2B show the effect of the alpha2C-antagonist acridin-9-yl- [4- (4- methylpiperazin-l-yl)-phenyl] amine (JP-1302) and the alpha2-adrenoceptor subtype non-selective alpha2-antagonist atipamezole on the startle reflex and its prepulse inhibition in rats pretreated with the psychostimulant phencyclidine (PCP). PCP clearly disrupted the PPI and this was effectively counteracted by the subtype selective alpha2C-antagonist, but not by the receptor subtype non-selective alpha2- antagonist atipamezole. Asterisks refer to significant difference in statistical comparisons between the vehicle (veh) + PCP and other treatment groups. * p < 0.05, ** p < 0.01, *** p < 0.001 ; 1-way ANOVA and LSD post hoc test. ; In order to study the effect of alpha2-antagonists on startle reflex and its prepulse- inhibition, groups of rats (n =10/group) were pre-treated with the alpha2C-antagonist or vehicle 20 min before measurement of the acoustic startle reactivity and PPI in a test system designed for startle studies (SR-LAB, San Diego Instruments, CA, USA). In a subsequent experiment the effects of the alpha2-adrenoceptor subtype selective alpha2C-antagonist and or the subtype non-selective antagonist atipamezole (Haapalinna, A. et al., Naunyn-Schmiedeberg's Arch. Pharmacol. 356 (1997) 570- 582) on PCP-induced PPI-disruption was studied. The antagonists were given 20 min, and PCP or vehicle 10 min before start of the startle measurements. The method otherwise corresponds to the procedure described in Sallinen, J. et al., J. Neurosci. 18 (1998) 3035-42. It was found that the receptor subtype selective alpha2C-antagonist acridin9-yl- [4- (4-methylpiperazin-1-yl)-phenyl] amine (JP-1302) did not affect the startle reflex per se, but it increased PPI dose-dependently and effectively (Figures 1A and 1B). The effect of the alpha2C-antagonist was especially clearly seen in the presence of PCP (Figures 2A and 2B). In the Figures 2A and 2B it is also shown that the specific and potent alpha2-antagonist atipamezole, that has no alpha2-adrenoceptor subtype selectivity, increased significantly the startle reactivity per se, but it had no effect on the PPI phenomenon; this points to the significance of the alpha2C-adrenoceptor subtype selective antagonism.

Location

Page/Page column 3-5

Comment (Pharmacological Data)

No effect

Reference

ORION CORPORATION

Patent: WO2003/82825 A1, 2003 ; Title/Abstract Full Text Show Details

96 of 219

Effect (Pharmacological Data)

uptake; induction of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological

1 - 15 mg/kg

Data)

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Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline

Method (Pharmacological Data)

rats treated with title comp. and decapitated 1, 3 or 6 h later; striatum dissected; synaptosomal membranes prepared; vesicular <3H>dopamine uptake determined for 3 min at 30 deg C; liquid scintillation counting

Further Details (Pharmacological Data)

further investigation with eticlopride; control: saline; reference comp.: dizocilpine 0.01 - 1.0 mg/kg

Results

title comp. significantly increased vesicular dopamine uptake at doses 5 and 15 mg/kg 1 h after treatment, dopamine D2 receptors involved; reference comp. had no effect (figures)

Reference

Crosby, Michael J.; Hanson, Jarom E.; Fleckenstein, Annette E.; Hanson, Glen R.

European Journal of Pharmacology, 2002 , vol. 438, # 1-2 p. 75 - 78 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

binding; induction of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

15 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline

Method (Pharmacological Data)

rats treated with title comp.; decapitated 1 h later; striatum dissected; VMAT-2 radioligand binding assay; synaptosomal membranes incubated with <3H>dihydrotetrabenazine 2 nmol/l for 10 min at 25 deg C; filtered; liquid scintillation counting

Further Details (Pharmacological Data)

nonspecific binding determined with tetrabenazine; VMAT-2: vesicular monoamine transporter-2; control: saline

Results

title comp. significantly increased dihydrotetrabenazine binding by 30 percent 1 h after treatment

Reference

Crosby, Michael J.; Hanson, Jarom E.; Fleckenstein, Annette E.; Hanson, Glen R.

European Journal of Pharmacology, 2002 , vol. 438, # 1-2 p. 75 - 78 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transport

Species or TestSystem (Pharmacological Data)

Caco-2 cells

Concentration (Pharmacological Data)

0.01 - 0.1 mmol/l

Kind of Dosing (Pharmacological Data)

title comp. dissolved in HBSS

Method (Pharmacological Data)

in vitro; accelerated permeability model; cells grown under acceler. growth conditions; <3H>-label. title comp. add.; title comp. solution placed on apical side of cells; samples taken from basolateral side; HPLC or liquid scintil. count. analysis

Further Details (Pharmacological Data)

permeability coefficient from apical to basolateral direction; all permeability coefficient experiments performed between d 3 and 7; HBSS=Hank's balanced salt solution

Results

permeability coefficient P=50.6E-6 cm/s

Reference

Liang, Earvin; Chessic, Kelli; Yazdanian, Mehran

Journal of Pharmaceutical Sciences, 2000 , vol. 89, # 3 p. 336 - 345 Title/Abstract Full Text View citing articles Show Details

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Effect (Pharmacological Data)

cytotoxicity

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat forebrain neurons

Concentration (Pharmacological Data)

3 μmol/l

Kind of Dosing (Pharmacological Data)

solution in DMEM

Method (Pharmacological Data)

treatment with title comp. for 48 h at 37 deg C in DMEM; washing; treatment with 0, 30, or 100 μmol/l NMDA in DMEM with supplements and at physiological Mg(2+) concentration for 20 h; cells were fixed and fragmented DNA was visualized by TUNEL assay

Further Details (Pharmacological Data)

DMEM: Dulbecco's modified Eagle's medium; NMDA: N-methyl-D-aspartate; TUNEL: terminal dUTP nick-end labeling

Results

title comp. sensitized cells to NMDA toxicity and enhanced NMDA-induced increase of percentage of TUNEL-positive cells; title comp. alone had no effect on TUNEL staining

Reference

Wang, Cheng; Kaufmann, Joel A.; Sanchez-Ross, Monica G.; Johnson, Kenneth M.

Journal of Pharmacology and Experimental Therapeutics, 2000 , vol. 294, # 1 p. 287 - 295 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

cytotoxicity

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat forebrain neurons

Concentration (Pharmacological Data)

3 μmol/l

Kind of Dosing (Pharmacological Data)

solution in DMEM

Method (Pharmacological Data)

treatment with title comp. for 48 h at 37 deg C in DMEM; washing; treatment with 0 - 100 μmol/l NMDA in DMEM with supplements and at physiological Mg(2+) concentration for 20 h; cell death was evaluated as release of cellular LDH into culture medium

Further Details (Pharmacological Data)

DMEM: Dulbecco's modified Eagle's medium; NMDA: N-methyl-D-aspartate; LDH: lactate dehydrogenase; further investigations using superoxide dismutase (SOD) and catalase

Results

title comp. sensitized cells to NMDA toxicity and enhanced NMDA-induced increase in LDH release, but this effect was prevented by SOD and catalase; title comp. alone had no marked effect on LDH release

Reference

Wang, Cheng; Kaufmann, Joel A.; Sanchez-Ross, Monica G.; Johnson, Kenneth M.

Journal of Pharmacology and Experimental Therapeutics, 2000 , vol. 294, # 1 p. 287 - 295 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

cytotoxicity

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat forebrain neurons

Concentration (Pharmacological Data)

3 μmol/l

Kind of Dosing (Pharmacological Data)

solution in DMEM

Method (Pharmacological Data)

treatment with title comp. for 48 h at 37 deg C in DMEM; washing; treatment with 0, 30, or 100 μmol/l NMDA in DMEM with supplements and at physiological Mg(2+) concentration for 20 h; cell viability was evaluated by MTT dye reduction assay

Further Details (Pharmacological Data)

DMEM: Dulbecco's modified Eagle's medium; NMDA: N-methyl-D-aspartate; MTT: 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide; further investigations using superoxide dismutase (SOD) and catalase

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Results

title comp. sensitized cells to NMDA toxicity and enhanced NMDA-induced reduction of MTT dye uptake, but this effect was prevented by SOD and catalase; title comp. alone had no effect on MTT uptake

Reference

Wang, Cheng; Kaufmann, Joel A.; Sanchez-Ross, Monica G.; Johnson, Kenneth M.

Journal of Pharmacology and Experimental Therapeutics, 2000 , vol. 294, # 1 p. 287 - 295 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

cytotoxicity

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat forebrain neurons

Concentration (Pharmacological Data)

3 μmol/l

Kind of Dosing (Pharmacological Data)

solution in DMEM

Method (Pharmacological Data)

treatment with title comp. for 48 h at 37 deg C in DMEM; washing; treatment with 0 or 30 μmol/l NMDA in DMEM with supplements and at physiological Mg(2+) concentration for 20 h; fragmented histone-associated DNA was detected using specific 2-site ELISA

Further Details (Pharmacological Data)

DMEM: Dulbecco's modified Eagle's medium; NMDA: N-methyl-D-aspartate; ELISA: enzyme-linked immunosorbent assay

Results

title comp. sensitized cells to NMDA toxicity; treatment with title comp. and NMDA produced significant increase of amount of histoneassociated DNA fragments, compared to no effect of NMDA alone; title comp. alone had no effect on DNA fragmentation

Reference

Wang, Cheng; Kaufmann, Joel A.; Sanchez-Ross, Monica G.; Johnson, Kenneth M.

Journal of Pharmacology and Experimental Therapeutics, 2000 , vol. 294, # 1 p. 287 - 295 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein expression; increase of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat forebrain neurons

Concentration (Pharmacological Data)

3 μmol/l

Kind of Dosing (Pharmacological Data)

solution in DMEM

Method (Pharmacological Data)

treatment with title comp. for 48 h at 37 deg C in DMEM; washing; treatment with 0, 30, or 100 μmol/l NMDA in DMEM with supplements and at physiological Mg(2+) concentration for 20 h; Bax protein expression was determined by Western blot analysis

Further Details (Pharmacological Data)

DMEM: Dulbecco's modified Eagle's medium; NMDA: N-methyl-D-aspartate; further investigations with superoxide dismutase (SOD) and catalase

Results

title comp. alone increased Bax protein expression; title comp. pretreatment enhanced NMDA-induced increase of Bax expression, but this effect was prevented by SOD and catalase

Reference

Wang, Cheng; Kaufmann, Joel A.; Sanchez-Ross, Monica G.; Johnson, Kenneth M.

Journal of Pharmacology and Experimental Therapeutics, 2000 , vol. 294, # 1 p. 287 - 295 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

protein expression; reduction of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat forebrain neurons

Concentration (Pharmacological Data)

3 μmol/l

Kind of Dosing (Pharmacological Data)

solution in DMEM

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Method (Pharmacological Data)

treatment with title comp. for 48 h at 37 deg C in DMEM; washing; treatment with 0, 30, or 100 μmol/l NMDA in DMEM with supplements and at physiological Mg(2+) concentration for 20 h; Bcl-XL protein expression was determined by Western blot analysis

Further Details (Pharmacological Data)

DMEM: Dulbecco's modified Eagle's medium; NMDA: N-methyl-D-aspartate; further investigations with superoxide dismutase (SOD) and catalase

Results

title comp. alone reduced Bcl-XL protein expression; title comp. pretreatment enhanced NMDA-induced reduction of Bcl-XL expression, but this effect was prevented by SOD and catalase

Reference

Wang, Cheng; Kaufmann, Joel A.; Sanchez-Ross, Monica G.; Johnson, Kenneth M.

Journal of Pharmacology and Experimental Therapeutics, 2000 , vol. 294, # 1 p. 287 - 295 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

mRNA expression; increase of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat forebrain neurons

Concentration (Pharmacological Data)

3 μmol/l

Kind of Dosing (Pharmacological Data)

solution in DMEM

Method (Pharmacological Data)

treatment with title comp. for 48 h at 37 deg C in DMEM; mRNA level of NMDA receptor NR1 subunit was determined by in situ hybridization with 35S-labeled sequence-specific oligonucleotide

Further Details (Pharmacological Data)

DMEM: Dulbecco's modified Eagle's medium; NMDA: N-methyl-D-aspartate

Results

title comp. treatment caused a 47 percent increase in NR1 mRNA

Reference

Wang, Cheng; Kaufmann, Joel A.; Sanchez-Ross, Monica G.; Johnson, Kenneth M.

Journal of Pharmacology and Experimental Therapeutics, 2000 , vol. 294, # 1 p. 287 - 295 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

inhibition of carbamylcholine-induced receptor blockade

Species or TestSystem (Pharmacological Data)

TE671/RD cell line

Concentration (Pharmacological Data)

1E-09 - 0.001 mol/l

Exposure Period (Pharmacological Data)

5 min

Method (Pharmacological Data)

cells cultured; 86Rb(1+)-efflux assay in presence of title compd. and 1 mM carbamylcholine performed (Cerenkov counting)

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

4.76 -log M

Results

concn.-dependent inhibition of noncompetitive functional block of muscle-type nicotinic acetylcholine receptor α1β1γδ (evaluated as inhibition of carbamylcholine-stimulated 86Rb(1+) efflux) given (diagram)

Reference

Fryer, John D.; Lukas, Ronald J.

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 288, # 1 p. 88 - 92 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

inhibition of carbamylcholine-induced receptor blockade

Species or Test-

SH-SY5Y cell line

System (Pharmacological Data)

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Concentration (Pharmacological Data)

1E-09 - 0.001 mol/l

Exposure Period (Pharmacological Data)

5 min

Method (Pharmacological Data)

cells cultured; 86Rb(1+)-efflux assay in presence of title compd. and 1 mM carbamylcholine performed (Cerenkov counting)

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

5.28 -log M

Results

concn.-dependent inhibition of noncompetitive functional block of ganglionic nicotinic acetylcholine receptor α3β4 (evaluated as inhibition of carbamylcholine-stimulated 86Rb(1+) efflux) given (diagram)

Reference

Fryer, John D.; Lukas, Ronald J.

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 288, # 1 p. 88 - 92 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

prevention of N-methyl-DL-aspartic acid lethality

Endpoint of Effect (Pharmacological Data)

mortality

Species or TestSystem (Pharmacological Data)

CF1 mice

Sex

male

Route of Application

intraperitoneal

Exposure Period (Pharmacological Data)

60 min

Method (Pharmacological Data)

rats (ca. 70 g) treated with title compd., 1 h later N-methyl-DL-aspartic acid (150 mg/kg, i.v.) applied

Type (Pharmacological Data)

ED50

Value of Type (Pharmacological Data)

2.8 mg/kg

Reference

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 288, # 1 p. 121 - 132 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

anticonvulsant

Species or TestSystem (Pharmacological Data)

CF1 mice

Sex

male

Route of Application

intraperitoneal

Exposure Period (Pharmacological Data)

1 h

Method

mice (20-30 g) treated with title compd., 30 min later chemically induced seizures (N-methyl-DL-aspartic acid, 150 mg/kg, i.v.) testing

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(Pharmacological Data)

(30 min)

Type (Pharmacological Data)

ED50

Value of Type (Pharmacological Data)

6.3 mg/kg

Reference

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 288, # 1 p. 121 - 132 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

antagonist

Species or TestSystem (Pharmacological Data)

Torpedo californica electric organ membrane

Concentration (Pharmacological Data)

Ca. 0.3 - 300 μmol/l

Method (Pharmacological Data)

nicotinic acetylcholine receptor (AChR)-rich (90 nM AChR) membranes loaded with 22Na in HEPES-Torpedo phys. saline buffer; incubation with title comp., 10 min; 22Na efflux initiated by phenyltrimethylammonium (PTMA), 20 s

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

19.6 μmol/l

Results

inhibition of PTMA-stimulated 22Na efflux, effect lost above 100 μM

Reference

Lurtz, Monica M.; Pedersen, Steen E.

Molecular Pharmacology, 1999 , vol. 55, # 1 p. 159 - 167 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

antagonist

Species or TestSystem (Pharmacological Data)

Torpedo californica electric organ membrane

Concentration (Pharmacological Data)

0.01 - 10000 μmol/l

Method (Pharmacological Data)

nicotinic acetylcholine receptor (AChR)-rich membranes (20 nM AChR) incubated in HEPES-Torpedo phys. saline buffer, with 25-400 nM crystal violet (CrV) and 0.1 mM carbamylcholine; fluorescence assay

Results

inhibition of CrV fluorescence; CrV and title comp. binds to same site on AChR; graphical representation of Kapp (inhibition constant) values as function of CrV concentrations

Reference

Lurtz, Monica M.; Pedersen, Steen E.

Molecular Pharmacology, 1999 , vol. 55, # 1 p. 159 - 167 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

biotransformation

Species or TestSystem (Pharmacological Data)

rat liver microsomes

Sex

male and female

Concentration (Pharmacological Data)

1 μmol/l

Method

microsomes incubated for 20 min at 2 mg/ml microsomal protein with title comp., tracer dose of <3H>title comp., and NADPH-

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(Pharmacological Data)

generating system; microsomal proteins precipitated, filtered; metabolite formation analyzed by scintillation counting and HPLC

Further Details (Pharmacological Data)

adult SD rats, Dark Agouti rats, and Fischer 344 rats of both sexes were used

Results

rate of formation of all title comp. metabolites and amount of title comp. metabolized were sign. less in females; all rats showed stereoselective preference for formation of t-PPC than c-PPC; males formed sign. more irreversibly bound metabolites

Metabolite (Pharmacological Data)

cis-1-(1-phenyl-4-hydroxycyclohexyl)piperidine [Reaxys RN: 10712545] ; trans-1-(1-phenyl-4-hydroxy-cyclohexyl)piperidine [Reaxys RN: 10712546] ; 1-(1-phenylcyclohexyl)-4-hydroxypiperidine [Reaxys RN: 1472179]

Comment (Pharmacological Data)

Further metabolite(s)

Reference

Shelnutt, Susan R.; Gunnell, Melinda; Owens, S. Michael

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 290, # 3 p. 1292 - 1298 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

biotransformation

Species or TestSystem (Pharmacological Data)

SD rat

Sex

male and female

Concentration (Pharmacological Data)

1 mg/kg

Method (Pharmacological Data)

rats injected with title comp. and tracer dose of ca. 250 μCi <3H>title comp.; blood collected up to 30 h; urine collected; serum and urine samples analyzed for <3H>title comp. and <3H>metabolites by scintillation counting and HPLC

Results

systemic and nonrenal clearance of title comp. was much lower in female rats; females had longer terminal elimination half-life; elimination of unchanged title comp. in urine was complete at 30 h; females excreted higher amounts of unchanged title comp.

Metabolite (Pharmacological Data)

Comment (Pharmacological Data)

Further metabolite(s)

Reference

Shelnutt, Susan R.; Gunnell, Melinda; Owens, S. Michael

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 290, # 3 p. 1292 - 1298 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

determination in hair roots of male Dark Agouti pigmented rats already 5 min after i.p. adminstration of 80-120 mg/kg, dose-dependent conc. time course up to 48 h

Reference

Sakamoto; Endo; Nagasaki; Nakamura; Watanabe; Nakahara; Tanaka, Akira

Pharmazie, 1998 , vol. 53, # 5 p. 310 - 314 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

death of 2 male Dark Agouti pigmented rats after application of 120 mg/kg, the increase of the conc. of phencyclidine and its metabolite in hair roots stopped soon afterwards, the reached plateaus persist

Reference

Sakamoto; Endo; Nagasaki; Nakamura; Watanabe; Nakahara; Tanaka, Akira

Pharmazie, 1998 , vol. 53, # 5 p. 310 - 314 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

determination of the metabolites t-1-phenyl-1-(4-hydroxypiperidino)-4-cyclohexanol and 1-(1-phenylcyclohexyl)-4-hydroxypiperidine in hair roots of male Dark Agouti pigmented rats already 5/15 min after i.p. application of 80-120 mg/kg, conc. time course

Reference

Sakamoto; Endo; Nagasaki; Nakamura; Watanabe; Nakahara; Tanaka, Akira

Pharmazie, 1998 , vol. 53, # 5 p. 310 - 314 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

binding affinity to TCP site of NMDA receptors in rat brain homogenates (IC50 = 47 nM)

Reference

Sasaki, Shigeki; Ishibashi, Nobuyasu; Kuwamura, Tshuneo; Sano, Hiromi; Matoba, Masaki; Nisikawa, Tohru; Maeda, Minora

Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 21 p. 2983 - 2986 Title/Abstract Full Text View citing articles Show Details

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Comment (Pharmacological Data)

binding affinities for NMDA receptor (rat brain membrane) and σ receptor (guinea pig brain membrane) by radioreceptor assay (Ki=0.109 and 2.01 μM, respectively)

Reference

Wanner, Klaus Th.; Beer, Herbert; Hoefner, Georg; Ludwig, Matthias

European Journal of Organic Chemistry, 1998 , # 9 p. 2019 - 2029 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transport

Species or TestSystem (Pharmacological Data)

Caco-2 cells

Concentration (Pharmacological Data)

0.01 - 0.1 mmol/l

Kind of Dosing (Pharmacological Data)

title comp. in Hank's Balanced Salt Solution

Method (Pharmacological Data)

Transwell cell culture inserts; 80000 cells/cm2; title comp. + radiolabeled title comp.(final radioactive concn. of ca. 0.15 μCi/ml); incubator (37 deg C, 5 percent CO2); samples from the basolateral side; liquid scintillation counter

Type (Pharmacological Data)

permeability coefficient

Value of Type (Pharmacological Data)

24.7E6 cm/sec

Reference

Yazdanian, Mehran; Glynn, Susan L.; Wright, James L.; Hawi, Amale

Pharmaceutical Research, 1998 , vol. 15, # 9 p. 1490 - 1494 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

psychostimulant

Species or TestSystem (Pharmacological Data)

White Carneaux pigeon

Route of Application

intramuscular

Concentration (Pharmacological Data)

0.1 - 10 mg/kg

Method (Pharmacological Data)

Pigeons in operant chambers were trained to discriminate 5.6 mg/kg BMY 14802 from saline for food reinforcement using two-key operant procedure; then multiple-trial testing method (substitution test) used to assess title comp. stimulus effects

Further Details (Pharmacological Data)

Title comp. administered at the start of each trial (minimum 4 trials): the cumulative dosing; several months later retesting performed; appropriate responses and response rate measured

Results

Title comp. failed to substitute for the training stimulus (table); maximum BMY 14802 responding: 28.7 percent; substitution n/N: 1/6; response rate at maximum dose: 0 responses/s; second study of title comp. yielded substitution in one subject at 0.32 mg/kg

Reference

Vanecek, Susan A.; Essman, William D.; Taylor, Duncan P.; Woods, James H.

Journal of Pharmacology and Experimental Therapeutics, 1998 , vol. 284, # 1 p. 1 - 9 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

psychostimulant

Species or TestSystem (Pharmacological Data)

White Carneaux pigeon

Route of Application

intramuscular

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Concentration (Pharmacological Data)

0.1 - 10 mg/kg

Method (Pharmacological Data)

Further Details (Pharmacological Data)

Title comp. administered at the start of each trial (minimum 4 trials): the cumulative dosing; appropriate responses and response rate measured

Results

Title comp. failed to substitute for the training stimulus (table); maximum BMY 14802 responding: 12.1 percent; substitution n/N: 0/6; response rate at max. dose: 0 responses/s; title comp. did not substitute for BMY 14802 training stimulus in any of pigeons

Reference

Vanecek, Susan A.; Essman, William D.; Taylor, Duncan P.; Woods, James H.

Journal of Pharmacology and Experimental Therapeutics, 1998 , vol. 284, # 1 p. 1 - 9 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

antagonist

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

0.75 - 10.125 mg/kg

Kind of Dosing (Pharmacological Data)

single dose in 1 ml/kg saline

Method (Pharmacological Data)

250-350 g rats (12 h light/dark cycle); after title comp.+0.75-10.125 mg/kg s.c. 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) tested in Behavioral Pattern Monitor for 120 min

Further Details (Pharmacological Data)

locomotor activity assessed by photocells; complexity of spatial motion (Sd) analyzed based on fractal geometry; title comp. effect on LA, Sd alone or with DOI studied

Results

increase of LA in second 30 min only; biphasic effect on Sd: increase of Sd in all doses, persisting in 2. 30 min only at 6.75-10.125 mg/kg; </= 2.25 mg/kg decrease of Sd in second 30 min; with DOI: LA increased; Sd decreased (diagram)

Reference

Krebs-Thomson, Kirsten; Lehmann-Masten, Virginia; Naiem, Shahrouz; Paulus, Martin P.; Geyer, Mark A.

European Journal of Pharmacology, 1998 , vol. 343, # 2-3 p. 135 - 143 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

psychotomimetic

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

1 - 3.2 mg/kg

Kind of Dosing (Pharmacological Data)

administered 30 min before test session

Method (Pharmacological Data)

in vivo; effect on attentional performance in 3-choice serial reaction time task examined; 7-to 9-week-old rats trained to obtain food pellets by pressing lever; choice reaction time (CRT), choice accuracy, correct and total responses determined

Further Details (Pharmacological Data)

control: saline treated rats

Results

at lower dose had no effect; at 3,2 mg/kg produced significant delay in CRT and significant decreases in choice accuracy and in correct lever-pressing without affecting total number of lever pressing

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Reference

Jin, Jingji; Yamamoto, Tsuneyuki; Watanabe, Shigenori

European Journal of Pharmacology, 1997 , vol. 319, # 2-3 p. 147 - 152 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

Method (Pharmacological Data)

changes in gross behaviour of rats (190-210 g) were observed for 90 min after injection of title comp.

Results

title comp. caused head weaves and body rolls were observed

Reference

Hu, Ping-Sheng; Ross, Svante B.

Pharmacology and Toxicology, 1997 , vol. 80, # 2 p. 97 - 102 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

metabolic

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

5 mg/kg

Method (Pharmacological Data)

rats were treated with 4-aminopyridine (5 mg/kg s.c.); homogenate of cerebellum in ice cold acetate buffer (pH 5.8); influence of title comp. (applied 15 min before 4-aminopyridine) on 4-aminopyridine-induced cGMP production was measured with EIA system

Further Details (Pharmacological Data)

animals were killed 10 min after 4-aminopyridine; cGMP: cyclic guanosine monophosphate; EIA: enzyme immunoassay; control: saline

Results

title comp. significantly inhibited 4-aminopyridine-induced cGMP formation (figure)

Reference

Hu, Ping-Sheng; Ross, Svante B.

Pharmacology and Toxicology, 1997 , vol. 80, # 2 p. 97 - 102 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)

Ca. 0.3 - 3 mg/kg

Kind of Dosing (Pharmacological Data)

dissolved in distilled water, administered as hydrochloride

Method (Pharmacological Data)

rats (ca. 350 g) trained to discriminate title comp.: experiments conducted in operant-conditioning test chambers, after drug administration responses on only one lever produced food, after saline administration responses on opposite lever produced food

Further Details (Pharmacological

depression of lever with a force exceeding 35 g recorded as a response; title comp. is an uncompetitive N-methyl-D-aspartate antagonist

Data)

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Type (Pharmacological Data)

ED50

Value of Type (Pharmacological Data)

1.00 mg/kg

Results

dose-related increases in responding on title comp.-associated lever

Reference

Witkin, Jeffrey M.; Steele, Thomas D.; Sharpe, Lawrence G.

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 280, # 1 p. 46 - 52 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)

Ca. 1 - 6 mg/kg

Kind of Dosing (Pharmacological Data)

dissolved in distilled water, administered as hydrochloride

Method (Pharmacological Data)

rats (ca. 350 g) trained to discriminate dizocilpine: experiments conducted in operant-conditioning test chambers, after drug administration responses on only one lever produced food, after saline administration responses on opposite lever produced food

Further Details (Pharmacological Data)

depression of lever with a force exceeding 35 g recorded as a response; title comp. is an uncompetitive N-methyl-D-aspartate antagonist

Type (Pharmacological Data)

ED50

Value of Type (Pharmacological Data)

1.50 mg/kg

Results

dose-related increases in responding on dizocilpine-associated lever

Reference

Witkin, Jeffrey M.; Steele, Thomas D.; Sharpe, Lawrence G.

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 280, # 1 p. 46 - 52 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

insulin secretion; induction of

Species or TestSystem (Pharmacological Data)

Wistar rat islets of Langerhans

Concentration (Pharmacological Data)

100 μmol/l

Method (Pharmacological Data)

islets incubated at 37 deg C for 1 h with title comp. in the absence or presence of 200 μmol/l diazoxide in the medium containing 4 or 20 mmol/l glucose; insulin levels measured by radioimmunoassay

Further Details (Pharmacological Data)

reference compound: efaroxan

Comment (Pharmacological Data)

No effect

Reference

Chan, Susan L.F.; Pallett, Anna L.; Clews, John; Ramsden, Christopher A.; Morgan, Noel G.

European Journal of Pharmacology, 1997 , vol. 323, # 2-3 p. 241 - 244 Title/Abstract Full Text View citing articles Show Details

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Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

New Zealand white rabbit

Sex

female

Route of Application

intramuscular

Concentration (Pharmacological Data)

0.1 - 1 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. in 0.9 percent saline admin. daily within 5 min before the training sessions

Method (Pharmacological Data)

rabbits (1.5-2 kg, 3-4 months old) treated with title comp. and trace-conditioned in pairs in a SAC for 80-trial sessions until the performance reached 80 percent CR or until a total of 2000 TT were received; AQ of TC studied

Further Details (Pharmacological Data)

EC: eyeblink conditioning; CR: conditioned responses; before the study, rabbits fitted with restraining headbolts; TT: training trials; SAC: sound-attenuated chamber; TC: trace-conditioning; AQ: acquisition; control: saline; UR: unconditioned response

Results

title comp. significantly impaired acquisition of EC in a dose- and task-dependent manner; TC was dose-dependently impaired by title comp.; 1.0 mg/kg completely blocked TC; no effect on UR; diagram

Reference

Thompson, Lucien T.; Disterhoft, John F.

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 2 p. 928 - 940 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

New Zealand white rabbit

Sex

female

Route of Application

intramuscular

Concentration (Pharmacological Data)

2.5 - 10 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. in 0.9 percent saline admin. daily within 5 min before the training sessions

Method (Pharmacological Data)

Further Details (Pharmacological Data)

Results

title comp. blocked AQ of trace-conditioning

Reference

Thompson, Lucien T.; Disterhoft, John F.

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 2 p. 928 - 940 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

New Zealand white rabbit

Sex

female

Route of Application

intramuscular

Concentration

0.1 - 10 mg/kg

(Pharmacological Data)

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Kind of Dosing (Pharmacological Data)

title comp. in 0.9 percent saline admin. daily within 5 min before the training sessions

Method (Pharmacological Data)

rabbits (1.5-2 kg, 3-4 months old) treated with title comp. and delay-conditioned in pairs in a SAC for 80-trial sessions until the performance reached 80 percent CR or until a total of 2000 TT were received; AQ of DC studied

Further Details (Pharmacological Data)

EC: eyeblink conditioning; CR: conditioned responses; rabbits fitted with restraining headbolts; TT: training trials; SAC: sound-attenuated chamber; AQ: acquisition; DC: delay-conditioning; control: saline; UR: unconditioned response; URF: UR frequency

Results

title comp. significantly impaired DC in a dose- and task-dependent manner; in DC, AQ was significantly slowed by 1.0 mg/kg or more doses of title comp. but was not completely blocked; diagram

Reference

Thompson, Lucien T.; Disterhoft, John F.

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 2 p. 928 - 940 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

New Zealand white rabbit

Sex

female

Route of Application

intramuscular

Concentration (Pharmacological Data)

1 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. in 0.9 percent saline admin. daily within 5 min before the training sessions

Method (Pharmacological Data)

rabbits (1.5-2 kg, 3-4 months old) pseudoconditioned; treated with title comp. and trained in pair with saline control for 10 daily TS of 160 trials each; response number, amplitude, latency assessed; NAE of title comp. studied

Further Details (Pharmacological Data)

EC: eyeblink conditioning; CR: conditioned responses; before the study, rabbits were fitted with restraining headbolts; TS: training sessions; NAE: non-associative effects

Comment (Pharmacological Data)

No effect

Reference

Thompson, Lucien T.; Disterhoft, John F.

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 2 p. 928 - 940 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

New Zealand white rabbit

Sex

female

Route of Application

intramuscular

Concentration (Pharmacological Data)

1 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. in saline administered daily within 5 min before extinction test training sessions for 3 d

Method (Pharmacological Data)

saline-treated rabbits (1.5-2 kg, 3-4 months old) trace- or delay-conditioned; after reaching criterion, treated with title comp./saline; trained for 3 additional daily sessions using unpaired CS; extinction of learned responses in TCER and DCER studied

Further Details (Pharmacological Data)

TCER: trace-conditioned eyeblink responses; DCER: delay-conditioned eyeblink responses; CS: conditioned stimulus

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Results

title comp. impaired extinction of learned responses in TCER and DCER; diagram

Reference

Thompson, Lucien T.; Disterhoft, John F.

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 2 p. 928 - 940 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

New Zealand white rabbit

Sex

female

Route of Application

intramuscular

Concentration (Pharmacological Data)

1 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. in saline administered daily within 5 min before extinction test training sessions for 3 d

Method (Pharmacological Data)

saline-treated rabbits (1.5-2 kg, 3-4 months old) trace- or delay-conditioned; 3 d after reaching criterion, trained for 3 additional daily sessions using paired CS-US; paired with saline; title comp. admin.; retention of previously learned ER studied

Further Details (Pharmacological Data)

ER: eyeblink response; control: saline; CS: conditioned stimulus; US: unconditioned stimulus

Comment (Pharmacological Data)

No effect

Reference

Thompson, Lucien T.; Disterhoft, John F.

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 2 p. 928 - 940 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

New Zealand white rabbit

Sex

female

Route of Application

intramuscular

Concentration (Pharmacological Data)

1 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in 0.9 percent saline administered daily within 5 min before conditioning

Method (Pharmacological Data)

rabbits (1.5-2 kg, 3-4 months old) treated with title comp. and trace- or delay-conditioned; conditioned response timings in acquisition studied

Results

title comp. severely altered conditioned response timings in trace- but not in delay-conditioning; diagrams

Reference

Thompson, Lucien T.; Disterhoft, John F.

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 2 p. 928 - 940 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

New Zealand white rabbit

Sex

female

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Route of Application

intramuscular

Concentration (Pharmacological Data)

0.1 - 1 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in 0.9 percent saline administered daily within 5 min before conditioning

Method (Pharmacological Data)

rabbits (1.5-2 kg, 3-4 months old) treated with title comp. and trace-conditioned; conditioned response onset latencies studied

Further Details (Pharmacological Data)

controls treated with saline

Results

title comp. even at 0.1 mg/kg strongly shifted conditioned response latency distributions; at 1.0 mg/kg showed many fewer conditioned responses but similar short-latency timing distribution; diagram

Reference

Thompson, Lucien T.; Disterhoft, John F.

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 2 p. 928 - 940 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)

0.3 - 3 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline and admin. as salt in a volume of 1 ml/kg; doses refer to the salt

Method (Pharmacological Data)

rats trained under the DRL 1-1.3 sec schedule for 6 months; title comp. admin.; after 10 min, effect on accuracy, mean interresponse time and response rate studied

Further Details (Pharmacological Data)

control: vehicle; DRL: differential reinforcement of low rate schedules; IRTs: interresponse times

Results

title comp. signif. increased the mean IRT and decreased accuracy at the highest dose; at low doses produced slight increase in response rates; table

Reference

Mcclure; Mcmillan

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 3 p. 1368 - 1380 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)

0.3 - 3 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline and admin. as salt in a volume of 1 ml/kg; doses refer to the salt

Method (Pharmacological Data)

rats trained under the DRL 4-5.2 sec schedule for 3-3.5 months; title comp. admin.; after 10 min, effect on accuracy, mean interresponse time and response rate studied

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Further Details (Pharmacological Data)

control: vehicle; DRL: differential reinforcement of low rate schedules; IRTs: interresponse times

Results

title comp. decreased accuracy across a range of doses; signif. increased the mean IRT at the highest dose; at low doses slight increases in response rates; at 3.0 mg/kg statistically significant response rate decrease; table

Reference

Mcclure; Mcmillan

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 3 p. 1368 - 1380 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)

0.3 - 3 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline and admin. as salt in a volume of 1 ml/kg; doses refer to the salt

Method (Pharmacological Data)

rats trained under the DRL 10-13 sec schedule for 3-3.5 months; title comp. admin.; after 10 min, effect on accuracy, mean interresponse time and response rate studied

Further Details (Pharmacological Data)

control: vehicle; DRL: differential reinforcement of low rate schedules; IRTs: interresponse times

Results

title comp. decreased accuracy across range of doses; signif. decreased the mean IRT with all doses; at low doses slight increase in response rates; rate increases signif. at 1 mg/kg and higher; table

Reference

Mcclure; Mcmillan

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 3 p. 1368 - 1380 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)

0.3 - 3 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline and admin. as salt in a volume of 1 ml/kg; doses refer to the salt

Method (Pharmacological Data)

rats trained under the differential reinforcement of low rate (DRL) 1-1.3 sec schedule for 6 months; title comp. admin.; after 10 min, effect on number of responses emitted and IRTs collected as performance indicators during every session

Further Details (Pharmacological Data)

control: vehicle; IRTs: interresponse times; CC: cumulative curve; LP: linear portion; RF: relative frequency

Results

title comp. had slight effect on RF distributions; at low doses, small shift of CC up, to left; at 1.7 and 3.0 curve shifted down, to right; large increased responses in bin 24 of RF distributions; at 1.0-3.0 mg/kg LP showed signif. difference; diagram

Reference

Mcclure; Mcmillan

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 3 p. 1368 - 1380 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

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Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

0.3 - 3 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline and admin. as salt in a volume of 1 ml/kg; doses refer to the salt

Method (Pharmacological Data)

rats trained under the differential reinforcement of low rate (DRL) 4-5.2 sec schedule for 3-3.5 months; title comp. admin.; after 10 min, number of responses emitted, IRTs (interresponse times) collected as performance indicators during every session

Further Details (Pharmacological Data)

illumination of house light, stimulus light above the right lever and onset of Sonalert tone signaled; CFC: cumulative frequency curve; LP: linear portion; RFD: relative frequency distributions; CD: cumulative distribution; FD: frequency distribution

Results

title comp. showed 2 distinct CFC effects; (0.3-1.7 mg/kg) increased early peak of RFD, increased short IRTs, IRT CD shifted to left; at 3.0 mg/kg, slope altered with early portion to relatively even FD; LP signif. different (all doses); diagram

Reference

Mcclure; Mcmillan

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 3 p. 1368 - 1380 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)

0.3 - 3 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline and admin. as salt in a volume of 1 ml/kg; doses refer to the salt

Method (Pharmacological Data)

rats trained under the differential reinforcement of low rate (DRL) 10-13 sec schedule for 3-3.5 months; title comp. admin.; after 10 min, number of responses emitted and IRTs collected as performance indicators during every session

Further Details (Pharmacological Data)

control: vehicle; IRTs: interresponse times; RF: relative frequency

Results

title comp. at all doses shifted the cumulative frequency response curves to left because increased RF of shorter IRTs; at 3.0 mg/kg, peak of the IRT distribution decreased to 6-7 sec; linear portion signif. different from control for all doses; diagram

Reference

Mcclure; Mcmillan

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 3 p. 1368 - 1380 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

noncompetitive NMDA antagonist in vitro; binding affinity for the NMDA receptors - IC50=0.0098 μM, cerebral cortical synaptic membrane of rats using <3H>MK-801

Reference

Shuto, Satoshi; Ono, Shizuka; Hase, Yukako; Ueno, Yoshihito; Noguchi, Tomohiro; Yoshii, Kiyonori; Matsuda, Akira

Journal of Medicinal Chemistry, 1996 , vol. 39, # 24 p. 4844 - 4852 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

in vitro inhibition constant of rat brain PCP receptor labelled with <3H>TCP, IC50 = 36.9 nM, and rat striatum dopamine transporter labelled with <3H>BTCP, IC50 = 760 nM

Reference

Hamon; Vignon; Kamenka

European Journal of Medicinal Chemistry, 1996 , vol. 31, # 6 p. 489 - 495 Title/Abstract Full Text View citing articles Show Details

Effect

behavioural effects

(Pharmacological Data)

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Species or TestSystem (Pharmacological Data)

mouse

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

1 - 10 mg/kg

Kind of Dosing (Pharmacological Data)

once a day for 13 days saline or title comp.; on 14th day, saline-treated with saline (control) or title comp. (acute-treat.); title comp.treated with title comp. (repeated-treat.)

Method (Pharmacological Data)

in vivo, mice (27-32 g) ddY strain, food and water ad lib., 12/12 h light-dark cycle; saline or title comp. in two groups; in transparent cage observ. 30 min later the degree of sniffing, head movement, ataxia

Further Details (Pharmacological Data)

placed on horizontal bar, each mouse clung to it (cut of time)

Results

behavioural changes in saline-, acute PCP- and repeated PCP-treated animals; (figure given)

Reference

Noda, Yukihiro; Yamada, Kiyofumi; Komori, Yumiko; Sugihara, Hisayoshi; Furukawa, Hiroshi; Nabeshima, Toshitaka

British Journal of Pharmacology, 1996 , vol. 117, # 7 p. 1579 - 1585 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

NO synthase activity

Species or TestSystem (Pharmacological Data)

mouse

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

1 - 10 mg/kg

Method (Pharmacological Data)

ddY mice (27-32 g), food and water ad lib., 12/12 h light-dark cycle; measured the effect in 3 groups (control, acute- or repeated treatment); after the behavioural study, animals killed, brain removed, dissected 4 regions

Further Details (Pharmacological Data)

brain regions (cerebral cortex, striatum, hippocampus, cerebellum) NO-synthase activity measured by monitoring the conversion of <3H>-arginine to <3H>-citrulline (liquid scintillation spectrometer)

Results

NO synthase act. in cerebral cortex and cerebellum decreased, but not in striatum and hippocampus; changes in activity reversed by repeated-treatment (table given)

Reference

Noda, Yukihiro; Yamada, Kiyofumi; Komori, Yumiko; Sugihara, Hisayoshi; Furukawa, Hiroshi; Nabeshima, Toshitaka

British Journal of Pharmacology, 1996 , vol. 117, # 7 p. 1579 - 1585 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

antagonist

Species or TestSystem (Pharmacological Data)

rat brain

Method (Pharmacological Data)

slide-mounted sections from 250-350 g male Sprague-Dawley rats incub. in HEPES/EDTA buffer with title comp.+40 nM <3H>dextrorphan (DEX; 20 deg C; 4 h); compet. binding determ. using densitometry; IC50 determ. from binding curves by nonlinear regression

Further Details (Pharmacological Data)

inhibition of DEX binding in granule cell layer (GC) or molecular layer (ML) of cerebellum studied; Ki (potency of binding)=IC50/(1+ <L>/KD); <L>: conc., KD: dissociation constant of radioligand

Results

conc.-dependent inhibition of DEX binding (graph); Ki, nM: 1.0 <GC>; >200 <ML> (table)

Reference

Roth, Jane E.; Murray, Thomas F.; Franklin, Paul H.

Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 277, # 3 p. 1823 - 1836

Title/Abstract Full Text View citing articles Show Details

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Effect (Pharmacological Data)

antagonist

Species or TestSystem (Pharmacological Data)

rat brain

Concentration (Pharmacological Data)

Ca. 1E-09 - 0.0001 nmol/l

Method (Pharmacological Data)

slide-mounted sections from 250-350 g male Sprague-Dawley rats incub. in HEPES/EDTA buffer with title comp.+40 nM <3H>dextrorphan (DEX; 20 deg C; 4 h); competition binding determined using densitometry; distribution of binding sites by autoradiography

Further Details (Pharmacological Data)

inhibition of DEX binding to striatum radiatum of CA1 (SR), outer cortex (OC) studied; IC50 determined from binding curves by non-linear regression; Ki (potency of binding)=IC50/(1+<L>/KD); <L>: conc., KD: dissociation constant of radioligand

Results

conc.-dependent inhibition of DEX binding (graph); Ki, nM: 43.3 <SR>; 60.1 <OC> (table)

Reference

Roth, Jane E.; Murray, Thomas F.; Franklin, Paul H.

Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 277, # 3 p. 1823 - 1836 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; induction of

Species or TestSystem (Pharmacological Data)

Wistar Kyoto rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

5 mg/kg

Kind of Dosing (Pharmacological Data)

as hydrochloride

Method (Pharmacological Data)

in vivo; effect on neurotransmitter metabolism assayed; 8-week-old rats weighed 240-300 g; sacrificed 1 h after title comp. injection; brain removed; regional brain tissue dissected

Further Details (Pharmacological Data)

DA, 5-HT, DOPAC, HVA and 5-HIAA determined simultaneously using HPLC-ECD; DA: dopamine; 5-HT: serotonin; DOPAC: 3,4dihydroxyphenylacetic acid; HVA: homovanillic acid; 5-HIAA: 5-hydroxyindoleacetic acid

Results

increased DOPAC and HVA in prefrontal cortex/amygdala by 82/46 percent and 34/46 percent respectively; increased DOPAC in nucleus caudatus putamen by 43 percent; had no effect on DA, 5-HT and 5-HIAA levels in any brain regions examined; graphical representation

Reference

Etou; Kuroki; Tatebayashi; Tashiro; Hirano

Biochemical Pharmacology, 1996 , vol. 51, # 1 p. 83 - 86 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor blocking agent

Species or TestSystem (Pharmacological Data)

AMPA GluR3 receptor, recombinant, in Xenopus oocytes

Concentration (Pharmacological Data)

300 μmol/l

Method (Pharmacological Data)

cells injected with GluR3 mRNA, perfused at room temp.; two-electrode voltage-clamp recordings to kainate (300 μM) evoked currents from -70 mV holding potential; title comp. applied to perfusion solution for ca. 2 min

Comment (Pharmacological Data)

No effect

Reference

Washburn, Mark S.; Dingledine, Raymond

Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 278, # 2 p. 669 - 678 Title/Abstract Full Text View citing articles Show Details

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Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

ddY mouse

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

1 mg/kg

Kind of Dosing (Pharmacological Data)

single dose 15 min before trial; phenytoin (10 mg/kg i.p.) was administered 30 min before trial

Method (Pharmacological Data)

10-13 animal groups; aged 7 weeks; animals received electric shocks during 6 min in test perspex cage with wire floor; after 24 h placed in the same cage without shocks; motility of animals monitored for 6 min with automatic activity counter

Further Details (Pharmacological Data)

automatic activity counter consisted from photosensors that surrounded the test cage and recording apparatus;controls did not recieve the shocks during the first stay in the test cage

Comment (Pharmacological Data)

No effect

Reference

Kamei, Hiroyuki; Kameyama, Tsutomu; Nabeshima, Toshitaka

European Journal of Pharmacology, 1996 , vol. 299, # 1-3 p. 21 - 28 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

ddY mouse

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

0.5 - 2 mg/kg

Kind of Dosing (Pharmacological Data)

single dose 15 min before trial

Method (Pharmacological Data)

11-14 animal groups; aged 7 weeks; animals received electric shocks durin 6 min in test perspex cage with wire floor; after 24 h placed in the same cage without shocks; motility of animals monitored for 6 min with automatic activity counter

Further Details (Pharmacological Data)

automatic activity counter consisted from photosensors that surrounded the test cage and recording apparatus;controls did not recieve the shocks during the first stay in the test cage

Results

title comp. caused significant increase in motility in both shocked and non-shocked animals at dose 2 mg/kg; the effect was higher in shocked animals

Reference

Kamei, Hiroyuki; Kameyama, Tsutomu; Nabeshima, Toshitaka

European Journal of Pharmacology, 1996 , vol. 299, # 1-3 p. 21 - 28 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neuroregulatoric

Species or TestSystem (Pharmacological Data)

rat spinal cord

Concentration

0.01 - 10 μmol/l

(Pharmacological Data)

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Method (Pharmacological Data)

3 cm dorsal and ventral slices from the cervical region of spinal cords incub. in Krebs buffer with <3H>noradrenaline (NA) (15 min; 37 deg C)

Further Details (Pharmacological Data)

after 48 min, perfused with title comp. in Mg-free Krebs buffer (14 min; +N-methyl-D-aspartate for the last 2 min); radioactivity in perfusate and in solubilized tissue counted by liquid scint.; title comp. effect on NMDA-induced NA-release studied

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

0.04 μmol/l

Results

total inhibition of induced NA-release (graph)

Reference

Klarica, Marijan; Fage, Dominique; Carter, Chris

European Journal of Pharmacology, 1996 , vol. 308, # 2 p. 135 - 144 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat cerebral cortex membrane

Sex

male

Concentration (Pharmacological Data)

Ca. 1E-08 - 1E-05 mol/l

Method (Pharmacological Data)

membranes from rats weighing 200-250 g; effect on binding of 2.5 nM <3H>MK-801 to membranes in presence of 10 μM glutamate and 30 μM glycine

Type (Pharmacological Data)

Value of Type (Pharmacological Data)

12.2 nmol/l

Results

monophasic inhibition of <3H>MK-801 binding

Reference

Souverbie; Mo; Liu; von Euler; Sundstr-om

European journal of pharmacology, 1996 , vol. 307, # 3 p. 347 - 353 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat spinal cord membrane

Sex

male

Concentration (Pharmacological Data)

Ca. 1E-09 - 1E-05 mol/l

Method (Pharmacological Data)

membranes from rats weighing 200-250 g; effect on binding of 2.5 nM <3H>MK-801 to membranes in presence of 10 μM glutamate and 30 μM glycine

Type (Pharmacological Data)

Value of Type (Pharmacological Data)

15.9 nmol/l

Results

monophasic inhibition of <3H>MK-801 binding

Reference

Souverbie; Mo; Liu; von Euler; Sundstr-om

European journal of pharmacology, 1996 , vol. 307, # 3 p. 347 - 353

Title/Abstract Full Text View citing articles Show Details

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Effect (Pharmacological Data)

metabolic

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat liver microsomes

Sex

male and female

Method (Pharmacological Data)

male rats were castrated or infused with 12 μg/day estradiol for 14 days; female rats were ovarectomized or administered 14.8 mg/kg/day testosterone via s.c. implanted osmotic pump for 2 weeks; at the end of 2-week infusion, microsomal were prepared

Further Details (Pharmacological Data)

microsomal proteins were incubated with 1 μM title compound and <3H>title compound for 20 min at 37 deg C; metabolites irreversible binding was determinated by liquid scintillation

Results

castration decreased metabolite binding to 57 percent of sham-operated male levels; administration of testosterone to ovarectomized rats increased metabolite binding to 41 percent of normal male levels; no metabolite adducts were in estradiol-treated male rats

Reference

Shelnutt; Badger; Owens

Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 277, # 1 p. 292 - 298 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; examination of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat liver microsomes

Sex

male and female

Method (Pharmacological Data)

Further Details (Pharmacological Data)

CYP2C11 function was assessed by formation of 2α-OH-testosterone (with thin layer chromatography); CYP2C11 expression was assessed by Western blot analysis

Results

CYP2C11 function in castrated and ovarectomized (testosterone-treated) rats were 65 and 28 percent of sham-operated control males; CYP2C11 amount in ovarectomized (testosterone-treated) rats was 41 percent, in castrated rats was 90 percent of sham-operated male level

Reference

Shelnutt; Badger; Owens

Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 277, # 1 p. 292 - 298 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

antagonist

Species or TestSystem (Pharmacological Data)

rat pheochromocytoma (PC12) cell

Kind of Dosing (Pharmacological Data)

dissolved in distilled water

Method (Pharmacological Data)

the differentiated cells were incubated for 30 min with 45Ca (300-400 kdpm/well) or (-)-nicotine (100 μmol/l), Ca2+ uptake was determined by liquid scintillation spectrometry

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

1.2 μmol/l

Reference

Sagi, Naoki; Yamamoto, Hideko; Yamamoto, Toshifumi; Okuyama, Shigeru; Moroji, Takashi

European Journal of Pharmacology, 1996 , vol. 304, # 1-3 p. 185 - 190 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

antagonist

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Species or TestSystem (Pharmacological Data)

rat cerebral cortex membranes

Sex

not specified

Method (Pharmacological Data)

membranes suspended in Hepes buffer (10 mM, pH 7.5, 0.2 mg protein/ml); 45 min incubation at 25 deg C with <3H>TCP (2.5 nm), glycine (1 mM), NMDA (100 μM) and title comp.; filtration; radioactivity on filters measured by liquid scintillometry

Further Details (Pharmacological Data)

<3H>N-(1-(2-thienyl)cyclohexyl)-3,4-piperidine (<3H>TCP); N-methyl-D-aspartate (NMDA)

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

56 nmol/l

Results

(table)

Reference

European Journal of Pharmacology, 1996 , vol. 300, # 3 p. 237 - 246 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

antagonist

Species or TestSystem (Pharmacological Data)

rat cerebral cortex membranes

Sex

not specified

Method (Pharmacological Data)

membranes suspended in Hepes buffer (10 mM, pH 7.5, 0.2 mg protein/ml); 45 min incubation at 25 deg C with <3H>TCP (2.5 nm), Nmethyl-D-aspartate (100 μM) and title comp.; filtration; radioactivity on filters measured by liquid scintillometry

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

54 nmol/l

Results

(table)

Reference

European Journal of Pharmacology, 1996 , vol. 300, # 3 p. 237 - 246 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

antagonist

Species or TestSystem (Pharmacological Data)

rat cerebral cortex membranes

Sex

not specified

Method (Pharmacological Data)

membranes suspended in Hepes buffer (10 mM, pH 7.5, 0.2 mg protein/ml); 45 min incubation at 25 deg C with <3H>TCP (2.5 nm), glycine (1 mM) and title comp.; filtration; radioactivity on filters measured by liquid scintillometry

Further Details (Pharmacological Data)

<3H>N-(1-(2-thienyl)cyclohexyl)-3,4-piperidine (<3H>TCP)

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

67 nmol/l

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Results

(table)

Reference

European Journal of Pharmacology, 1996 , vol. 300, # 3 p. 237 - 246 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

metabolic

Species or TestSystem (Pharmacological Data)

Spraque-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

5 - 10 mg/kg

Kind of Dosing (Pharmacological Data)

dissolved in 0.9 percent NaCl; administeredin a volume of 1 ml/kg

Exposure Period (Pharmacological Data)

<= 180 min

Method (Pharmacological Data)

animal weight: 250-350 g; isofluraneanesthesia; concentric dialysis probe; 5 mm membrane in the hippocampusor striatum; samples collected at 20 min intervals; administration of the drugs; controls: administration of vehicle

Further Details (Pharmacological Data)

effect on hippocamal acetylcholine efflux

Results

markedly increased hippocampal acetylcholine efflux; at lower dose (5 mg/kg): maximal at 40 min, return to basal at 120 min; at higher dose (10 mg/kg): maximal at 40 min, return tobasal at 180 min

Reference

Hutson, Peter H.; Hogg, Joanne E.

European Journal of Pharmacology, 1996 , vol. 295, # 1 p. 45 - 52 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

metabolic

Species or TestSystem (Pharmacological Data)

Spraque-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

10 mg/kg

Kind of Dosing (Pharmacological Data)

dissolved in 0.9 percent NaCl; administered in a volume of 1 ml/kg

Exposure Period (Pharmacological Data)

<= 180 min

Method (Pharmacological Data)

animal weight: 250-350 g; isoflurane anesthesia; concentric dialysis probe; 5 mm membrane in the hippocampus or striatum; samples collected at 20 min intervals; administration of the drugs; controls: administration of vehicle

Further Details (Pharmacological Data)

effect on striatal acetylcholine efflux

Comment (Pharmacological Data)

No effect

Reference

Hutson, Peter H.; Hogg, Joanne E.

European Journal of Pharmacology, 1996 , vol. 295, # 1 p. 45 - 52 Title/Abstract Full Text View citing articles Show Details

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Effect (Pharmacological Data)

neuroprotective

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

male

Route of Application

intracerebroventricular

Concentration (Pharmacological Data)

50 nmol

Method (Pharmacological Data)

300 pmol OS2 or 500 pmol phospholipase A2 from bee venom; behavioural and EEG study

Further Details (Pharmacological Data)

effects on neurotoxic effects of phospholipase A2 from snake Oxyuranus scutellatus scutellatus (OS2) venom or from bee venom

Comment (Pharmacological Data)

No effect

Reference

Gandolfo, Gabriel; Lambeau, Gerard; Lazdunski, Michel; Gottesmann, Claude

Pharmacology and Toxicology, 1996 , vol. 78, # 5 p. 341 - 347 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

channel blocker

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat midbrain

Sex

male

Concentration (Pharmacological Data)

0.01 - 10 μmol/l

Method (Pharmacological Data)

horizontal slice (thickness 300 μm) of brain tissue containing the VTA and SNC was perfused with title comp. and N-methyl-D-aspartate; whole-cell currents from neurons in the VTA and SNC were recorded

Further Details (Pharmacological Data)

VTA: ventral tegmental area; SNC: substantia nigra zona compacta

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

130 nmol/l

Results

title comp. completely blocked N-methyl-D-aspartate induced current

Reference

Wu, Yan-Na; Johnson, Steven W.

Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 279, # 2 p. 457 - 463 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

IC50 = 0.27 μM (open) and IC50 = 13.9 μM (closed channel) binding in mouse cortical neuronal cultures

Reference

Subramanyam; Mallamo; Dority Jr.; Earley; Kumar; Aimone; Ault; Miller; Luttinger; DeHaven-Hudkins

Journal of Medicinal Chemistry, 1995 , vol. 38, # 1 p. 21 - 27 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

in vivo effect on brain monoamine oxidase activity <using male Swiss Albino rats (70-80g), dose 0.14 mg/kg/day for 7 days, i.p.>; percent change in respect of control: 37.7

Reference

Shafik; Rida; Eshba; Abdel-Kreem; El-Dardiry

Farmaco, 1995 , vol. 50, # 4 p. 273 - 279 Title/Abstract Full Text View citing articles Show Details

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Comment (Pharmacological Data)

in vivo effect on brain dopamine and norepinephrine activity <using male Swiss Albino rats (70-80g), dose 0.14 mg/kg/day for 7 days, i.p.>; percent change in respect of control: 49.0 and 50.1, respectively

Reference

Shafik; Rida; Eshba; Abdel-Kreem; El-Dardiry

Farmaco, 1995 , vol. 50, # 4 p. 273 - 279 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

the ability to block open N-methyl-D-aspartic acid (NMDA) channel IC50=0.27 μM and closed NMDA channel IC50=0.45 μM in frog oocytes

Reference

Earley; Kumar; Mallamo; Subramanyam; Dority Jr.; Miller; DeHaven-Hudkins; Aimone; Kelly; Ault

Journal of Medicinal Chemistry, 1995 , vol. 38, # 18 p. 3586 - 3592 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male and female

Route of Application

subcutaneous

Concentration (Pharmacological Data)

10 mg/kg*d

Kind of Dosing (Pharmacological Data)

in sterile saline

Exposure Period (Pharmacological Data)

10 d

Method (Pharmacological Data)

rats (7 male and 8 female) were implanted with a osmotic minipump after 7 d were trained to respond under a FR30 schedule of food reimforcement four 30- trials occurring every 6 h; after 10 d pump was removed and behavior was recorded additional 10 d

Further Details (Pharmacological Data)

determination of session response rate (responses/s) versus days

Results

In females, responses were suppressed to 30-71 percent of control rates during the first 7 d of infusion of title comp.,in contrast, response in males never fell below 70 percent; stopping add. of title comp. behaviour dependence had developed similar in both sex

Reference

Wessinger, William D.

European Journal of Pharmacology, 1995 , vol. 277, # 1 p. 107 - 112 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat brain membranes

Sex

male and female

Concentration (Pharmacological Data)

100 μmol/l

Kind of Dosing (Pharmacological Data)

in sterile saline

Method (Pharmacological Data)

rats (5 male and 5 female) were decapitated and brain rapid removed, brain tissues homogenized, centrifuged; add. of <3H>dizolcipine (0.3-60 nM, 22.5 Ci/mmol), L-glutamate and glycine (10-10 μM); after 4 h incubation with title comp. filtered

Further Details (Pharmacological Data)

liquid scintillation spectrometry; determination of Eadie-Hofstee plot: bound (pmol/mg protein versus bound/free (pmol/mg protein nM)

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Results

title comp. caused no significant differences in Kd (7.6 and 7.1 for males and females, respectively) or Bmax (4.1 and 4.0 pmol/mg protein for males and females, respectively)

Reference

Wessinger, William D.

European Journal of Pharmacology, 1995 , vol. 277, # 1 p. 107 - 112 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

AUC

Species or TestSystem (Pharmacological Data)

dark-agouti rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

0.5 mg/kg

Kind of Dosing (Pharmacological Data)

drug administered once a day for 10 successive days

Exposure Period (Pharmacological Data)

10 d

Method (Pharmacological Data)

rats 5 weeks old; back hair shaved before experiment; blood samples collected 5, 15, 30, 60, 120, 360 min after drug administration; newly grown hair samples collected 4 weeks after first drug administration

Further Details (Pharmacological Data)

drug level in plasma and hair determination; GC/MS; HPLC

Type (Pharmacological Data)

AUC

Value of Type (Pharmacological Data)

1.5 μg*min/ml

Results

concentration in hair <H> = 3.34 ng/mg; drug incorporation rate ICR (<H>/AUC) = 2.3

Reference

Nakahara; Takahashi; Kikura

Biological and Pharmaceutical Bulletin, 1995 , vol. 18, # 9 p. 1223 - 1227 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

hyperlocomotion inducer

Species or TestSystem (Pharmacological Data)

Wistar rats

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

0.63 - 20 mg/kg

Method (Pharmacological Data)

rats placed into cages, movement recorded for 60 min by infrared beams

Further Details (Pharmacological Data)

effect of dopamine D2 and 5-HT2A receptor antagonists on hyperlocomotion caused by title compound

Results

title compound dose dependently elicited hyperlocomotion; this effect blocked by 5-HT2A receptor antagonists (r = 0.97) more effectively than by dopamine D2 antagonists (r = 0.57)

Reference

Maurel-Remy; Bervoets; Millan

European Journal of Pharmacology, 1995 , vol. 280, # 2 p. R9-R11 Title/Abstract Full Text View citing articles Show Details

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Effect (Pharmacological Data)

neuroprotective

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

male

Route of Application

intravenous

Concentration (Pharmacological Data)

5 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in physiological saline

Method (Pharmacological Data)

electrodes implanted in brain, electrocorticogram (ECoG) recorded by telemetry before as well as 1 h, 1 d and 7 days after ishemia; title comp. administered 15 min prior to ischemia

Further Details (Pharmacological Data)

10 min cerebral ischemia induced by clamping both common arteries and lowering systemic blood pressure to 40 mmHg by exsanguination

Results

decreased ECoG power of ψ, β, α bands 1 h after ischemia not influenced by title comp.; sign. elevated ECoG power with title comp. vs. saline after 1 d; sign. higher ECoG power after 7 d; graphical representations

Reference

Peruche; Klaassens; Krieglstein

Pharmacology, 1995 , vol. 50, # 4 p. 229 - 237 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

guinea pig brain homogenate

Sex

male

Concentration (Pharmacological Data)

100 μmol/l

Method (Pharmacological Data)

Dunkin-Hartley animals (250-300); killed, brain minus cerebellum and medulla oblongata removed; frosen in liquid air, pulverized, homogenized

Further Details (Pharmacological Data)

binding for phencyclidine site, 2 nM <3H>PCP used, plus 10 μM haloperidol, non-specific binding with title compound; incubated at 25 deg C for 30 min; measured with scintillation spectrophotofluorimeter

Type (Pharmacological Data)

Value of Type (Pharmacological Data)

45 nmol/l

Results

Ki = 1.1-3.2 μM (S and R ketamine)

Reference

Hustveit; Maurset; Oye

Pharmacology and Toxicology, 1995 , vol. 77, # 6 p. 355 - 359 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

anticonvulsant

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rats

Sex

male

Route of Application

peroral

Exposure Period

60 min

(Pharmacological Data) Method (Pharmacological Data)

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title compd. applied to rats (100-150 g), 60 min later maximal electroshock tested (bicorneal electrodes applied to eyes, 50 mA, 0.2 s)

Type (Pharmacological Data)

ED50

Value of Type (Pharmacological Data)

1.2 mg/kg

Reference

Palmer; Stagnitto; Garske; Napier; Harris; Kaiser; Griffith; Woodhead; White; Wolf; Swinyard

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 273, # 3 p. 1023 - 1031 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor blocking agent

Species or TestSystem (Pharmacological Data)

rat whole brain minus caudate membranes

Method (Pharmacological Data)

in vitro ligand binding assay; brains from male Sprague-Dawley rats (200-300 g); 0.01 nM <125I>RTI-55-labeled 5-HT transporter binding sites (DA transporter sites blocked with 1000 nM LR1111); 4 deg C; incubation time 18-24 h

Type (Pharmacological Data)

Value of Type (Pharmacological Data)

4119 nmol/l

Reference

Silverthorn; Dersch; Baumann; Cadet; Partilla; Rice; Carroll; Becketts; Brockington; Rothman

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 273, # 1 p. 213 - 222 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; inhib. of

Species or TestSystem (Pharmacological Data)

New Zealand white rabbit

Sex

male

Concentration (Pharmacological Data)

1 mmol/l

Exposure Period (Pharmacological Data)

30 min

Method (Pharmacological Data)

microsomes from the livers of phenobarbital-induced animals; with glucose-6-phosphate dehydrogenase (G6PD) as an NADPH-generating system; benzphetamine N-demethylase activity determined

Further Details (Pharmacological Data)

incubations at 37 deg C, pH 7.4

Results

benzphetamine N-demethylase activity ( percent): 58 (direct assay), 57 (after pelleting/resuspension)

Reference

Sayre; Engelhart; Nadkarni; Babu; Klein; McCoy

Xenobiotica, 1995 , vol. 25, # 7 p. 769 - 775 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

Hartley guinea pigs

Sex

male

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Method (Pharmacological Data)

pigs decapitated, brains removed, sectioned in the coronal plane (10 μm thick), sections thaw-mounted onto slides and incubated with 1 nM <3H>NE-100 in 50 mM Tris-HCl buffer at 25 deg C for 30 min; 30 min incubation with title compound

Further Details (Pharmacological Data)

competition study by radioactivity determination; sigma 1 receptor

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

5110 nmol/l

Reference

Okuyama, Shigeru; Chaki, Shigeyuki; Yae, Tetsuji; Nakazato, Atsuro; Muramatsu, Makoto

Life Sciences, 1995 , vol. 57, # 21 p. PL333-PL337 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

DAT in Sprague-Dawley rat whole brain minus caudate membrane

Sex

male

Method (Pharmacological Data)

rat weight 200-300 g; decapitation; membrane prep.; SERT blocked with 50 nM paroxetine; binding assay with 0.01-0.11 nM <125I>RTI55 alone or with 5 nM RTI-55+70 nM RTI-113+25 nM RTI-122 for 18 to 24 h at 4 deg C; radiometry by gamma counter

Further Details (Pharmacological Data)

selectivity=Ki (site 2)/Ki (site 1); SERT=serotonin transporter; DAT=dopamine transporter

Results

two binding sites: Ki (nM)=2077 (site 1) and 639 (site 2); selectivity=0.308

Reference

Rothman; Silverthorn; Baumann; Goodman; Cadet; Matecka; Rice; Carroll; Wang; Uhl; Partilla; Dersch

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 274, # 1 p. 385 - 395 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

dopamine release

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

male

Kind of Dosing (Pharmacological Data)

1-500 μM

Method (Pharmacological Data)

weight 250-350 g; anesthetized; dialysis probe implanted into the left striatum; 20 h recovery period; perfused with artificial cerebrospinal fluid and with title comp. for 20 min; dopamine levels assayed by HPLC with electrochemical detection

Results

local pefusion of the striatum increased extracellular dopamine levels in dose-dependent manner (AUC 323.4 pg/160 min), maximal increases observed 20 min after perfusion, returned to the basal level within ca. 40 min

Reference

Yonezawa; Kuroki; Tashiro; Hondo; Uchimura

European Journal of Pharmacology, 1995 , vol. 285, # 3 p. 305 - 308 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

Hartley guinea-pig brain membranes

Sex

male

Concentration (Pharmacological Data)

1E-10 - 3E-06 mol/l

Method (Pharmacological

brain membranes from 350-400 g guinea-pig incubated with increasing concentration of title comp. in presence 0.8-1.2 nM <3H>NE-100 at 25 deg C for 30 min; nonspecific binding determined in presence of 10 μM haloperidol

Data)

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Further Details (Pharmacological Data)

displacement of <3H>NE-100 specific binding to sigma-receptor by title comp.; Ki value determined from IC50 value derived from inhibition data and Kd value for NE-100 (1.2 nM)

Results

<3H>NE-100 specific binding inhibited by title comp. with Ki value 7133.0

Reference

Tanaka; Shirasaki; Kaku; Muramatsu; Otomo

Naunyn-Schmiedeberg's Archives of Pharmacology, 1995 , vol. 351, # 3 p. 244 - 251 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor blocking agent

Species or TestSystem (Pharmacological Data)

rat C6 glicoma cells

Method (Pharmacological Data)

in vitro; cells were transfected with pcDNA1-hDAT; pretreatment with title comp. for 10 min before add. of <3H>dopamine (20 nM, 35.1 Ci/mmol); radioligand binding assay

Further Details (Pharmacological Data)

title comp. was tested by use at least six concentration for determination of Ki value

Type (Pharmacological Data)

Value of Type (Pharmacological Data)

734 nmol/l

Reference

Eshleman; Neve; Janowsky

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 274, # 1 p. 276 - 283 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

COS-7 cells

Method (Pharmacological Data)

in vitro; cells were transfected with pcDNA1-hDAT; pretreatment with title comp. for 10 min before add. of <3H>-2β-carbomethoxy-3β(4-fluorophenyl)tropane (<3H>CFT, 85.9 Ci/mmol) diluted with unlabeled comp.(1 pM to 10 μM); radioligand binding assay

Further Details (Pharmacological Data)

title comp. was tested by use at least nine concentration for determination of Ki value

Type (Pharmacological Data)

Value of Type (Pharmacological Data)

155 nmol/l

Reference

Eshleman; Neve; Janowsky

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 274, # 1 p. 276 - 283 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

COS-7 cells

Method (Pharmacological Data)

in vitro; cells were transfected with pcDNA1-hDAT; pretreatment with title comp. for 10 min before add. of <3H>GBR-12935; radioligand binding assay

Further Details (Pharmacological Data)

title comp. was tested by use at least nine concentration for determination of Ki value

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Value of Type (Pharmacological Data)

1497 nmol/l

Reference

Eshleman; Neve; Janowsky

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 274, # 1 p. 276 - 283 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

whole brain membranes of Sprague-Dawley rats

Sex

male

Method (Pharmacological Data)

membrane-enriched fractions prepn. from rat (250-350 g) whole brains; incubation (60 min, 4 deg C) with title compd. (various concns.) and 3H-labeled ABT-418 (7.5 nM); liq. scintillation spectrometry

Further Details (Pharmacological Data)

nonspecific binding determined in presence of 10 μM (-)-nicotine

Results

binding const. K(i) > 10000 nM

Reference

Anderson; Williams; Pauly; Raszkiewicz; Campbell; Rotert; Surber; Thomas; Wasicak; Arneric; Sullivan

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 273, # 3 p. 1434 - 1441 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

whole brain membranes of Sprague-Dawley rats

Sex

male

Method (Pharmacological Data)

membrane-enriched fractions prepn. from rat (250-350 g) whole brains; incubation (75 min, 4 deg C) with title compd. (various concns.) and 3H-labeled (-)-cytisine (0.35 nM); liq. scintillation spectrometry

Further Details (Pharmacological Data)

nonspecific binding determined in presence of 10 μM (-)-nicotine

Results

binding const. K(i) > 10000 nM

Reference

Anderson; Williams; Pauly; Raszkiewicz; Campbell; Rotert; Surber; Thomas; Wasicak; Arneric; Sullivan

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 273, # 3 p. 1434 - 1441 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

affinity to phencyclidine binding site in NMDA-receptor complex: Ki 0.12 μM

Reference

Eiden; Denk; Hofner

Archiv der Pharmazie, 1994 , vol. 327, # 7 p. 405 - 412 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

affinity to "thienylcyclidine" binding sites on N-methyl-D-aspartate receptor-ionophore complex in rat brain tissue in vitro

Reference

Mallamo; Earley; Kumar; Subramanyam; Dority Jr.; Miller; Dehaven-Hudkins; Ault; Herrmann Jr.; Dung; McMullen; Jaeger; Kullnig; Magee

Journal of Medicinal Chemistry, 1994 , vol. 37, # 26 p. 4438 - 4448 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

dopaminergic

Species or TestSystem (Pharmacological

Sprague-Dawley rat

Data)

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Sex

female

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

10 mg/kg

Exposure Period (Pharmacological Data)

1 h

Method (Pharmacological Data)

single injection; rats 10-12 weeks old, ca. 300 g weight; neurochemical study

Results

increased of HVA (dopamine metabolite) in whole striatum; increased of dopamine, DOPAC and HVA in globus pallidus only on the left side; no effect on dopamine, DOPAC and HVA in medioventral and dorsolateral caudate

Reference

Ali, S. F.; Newport, G. D.; Bracha, H. S.

Neurotoxicology and Teratology, 1994 , vol. 16, # 4 p. 335 - 342 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neurological toxicity

Endpoint of Effect (Pharmacological Data)

circling preference

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

female

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

5 - 20 mg/kg

Exposure Period (Pharmacological Data)

2 h

Method (Pharmacological Data)

single injection; rats 10-12 weeks old, ca. 300 g weight; cylindrical glass enclosure: 16" diameter, 10" height

Results

max. effect at dose 10 mg/kg; preference to turn to the left (65 percent); highest 1 h after title comp. administration

Reference

Ali, S. F.; Newport, G. D.; Bracha, H. S.

Neurotoxicology and Teratology, 1994 , vol. 16, # 4 p. 335 - 342 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neurological toxicity

Endpoint of Effect (Pharmacological Data)

reinforcing strength

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intravenous

Concentration (Pharmacological Data)

0.33 mg/kg

Method (Pharmacological Data)

in vivo; self-administration study; chloral hydrate anesthetized rats; permanent catheter of Silastic tubing in the right jugular vein

Further Details

responses refer to total active lever presses made by rats

(Pharmacological Data)

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Results

active lever pressing behavior on a progresive-ratio (PR) and fixed-ratio (FR-1) schedule of reinforcement; PR: breaking point after 7 injections, ca. 25 responses (equivalent dose of cocaine: 18 injections, ca. 900 responses); diagram

Reference

French

Neurotoxicology and Teratology, 1994 , vol. 16, # 4 p. 355 - 362 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

antagonist

Endpoint of Effect (Pharmacological Data)

firing rate

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat ventral tegmental A10 neurons

Sex

male

Concentration (Pharmacological Data)

10 μmol/l

Method (Pharmacological Data)

in vitro electrophysiology; coronal slices of the rat midbrain through the ventral tegmental A10 neurons (VTA); artificial cerebrospinal fluid (ACSF); recording chamber perfused at a rate 2 ml/min; effect on excitations induced by NMDA, kainate and AMPA

Further Details (Pharmacological Data)

35 deg C

Results

selective antagonize the excitatory effect produced by NMDA, change in firing rate: NMDA + PCP 14 percent, NMDA alone 100 percent (relative value); no effect on excitations induced by kainate and AMPA

Reference

French

Neurotoxicology and Teratology, 1994 , vol. 16, # 4 p. 355 - 362 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neurotoxicity

Endpoint of Effect (Pharmacological Data)

firing rate

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intravenous

Method (Pharmacological Data)

in vivo electrophysiology; activity of ventral tegmental (VTA) A10 dopamine neurons; single-unit extracellular recordings; chloral hydrate anesthetized rats; cumulative dose ca. 0.25 to 6 mg/kg; administration through a tail vein catheter in 0.9 percent NaCl

Further Details (Pharmacological Data)

cumulative dose-response curve

Results

increase in firing rate: change +49 percent at cumulative dose ca. 1 mg/kg; decline at doses > 1 mg/kg (ca. 2 percent at dose ca. 6 mg/kg); change in bursts activity +89 percent, spikes/bursts +71 percent at dose ca. 1 mg/kg

Reference

French

Neurotoxicology and Teratology, 1994 , vol. 16, # 4 p. 355 - 362 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male and female

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Route of Application

intraperitoneal

Concentration (Pharmacological Data)

5 mg/kg

Method (Pharmacological Data)

daily dose; chronic postnatal treatment; injections from postnatal day (PND) 5 to PND 15 (10 days of injections); effect on <3H>MK-801 binding in PND 21 rat brain (forebrain synaptosomal membranes)

Further Details (Pharmacological Data)

Scatchard plot

Results

decrease (56 percent compared to saline) the apparent density of high-affinity component of <3H>MK-801 binding; addition of Lglutamate and glycine increased <3H>MK-801 binding compared to baseline but did not differ from saline-treated controls

Reference

Sircar, Ratna; Li, Chang-Sheng

Neurotoxicology and Teratology, 1994 , vol. 16, # 4 p. 369 - 376 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

prevent of N-methyl-D-aspartate (NMDA)-induced lethality (ED50 = 0.55 mg/kg) in mice

Reference

Hays, Sheryl J.; Novak, Perry M.; Ortwine, Daniel F.; Bigge, Christopher F.; Colbry, Norman L.; et al.

Journal of Medicinal Chemistry, 1993 , vol. 36, # 6 p. 654 - 670 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

<3H>-1-(1-thienylcyclohexyl)piperidine (<3H>TCP) binding (IC50 = 36.5 nM) in rat brain homogenates in vitro, glutamate-stimulated calcium influx (IC50 = 0.20 μM) in vitro

Reference

Hays, Sheryl J.; Novak, Perry M.; Ortwine, Daniel F.; Bigge, Christopher F.; Colbry, Norman L.; et al.

Journal of Medicinal Chemistry, 1993 , vol. 36, # 6 p. 654 - 670 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

in vivo ability to prevent the lethal effects of systemically injected NMDA (mouse), ED50: 0.55 mg/kg; ataxia (mice)

Reference

Bigge; Malone; Hays; Johnson; Novak; Lescosky; Retz; Ortwine; Probert Jr.; Coughenour; Boxer; Robichaud; Brahce; Shillis

Journal of Medicinal Chemistry, 1993 , vol. 36, # 14 p. 1977 - 1995 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

in vitro <3H>TCP (1-(1-thienylcyclohexyl)piperidine) binding assay (crude rat brain synaptic membranes), IC50: 36.5 nM; in vitro inhibition of glutamate-induced accumulation of <45Ca+2> (cultured rat cortical neurons), IC50: 0.20 μM

Reference

Bigge; Malone; Hays; Johnson; Novak; Lescosky; Retz; Ortwine; Probert Jr.; Coughenour; Boxer; Robichaud; Brahce; Shillis

Journal of Medicinal Chemistry, 1993 , vol. 36, # 14 p. 1977 - 1995 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

inactive in inhibition of <3H>dichlorokynurenic acid (<3H>DCKA) binding to rat cortical membranes

Reference

Canton; Doble; Miquet; Jimonet; Blanchard

Journal of Pharmacy and Pharmacology, 1992 , vol. 44, # 10 p. 812 - 816 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

ability to inhibit <3H>1-<1-(2-thienyl)cyclohexyl>piperidine (<3H>TCP) binding at 1-(1-phenylcyclohexyl)piperidine (PCP) binding sites in rat brain tissue homogenates

Reference

Thurkauf; Mattson; Richardson; Mirsadeghi; Ornstein; Harrison Jr.; Rice; Jacobson; Monn

Journal of Medicinal Chemistry, 1992 , vol. 35, # 8 p. 1323 - 1329 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

in vitro ability to binding to phencyclidine (PCP) (rat brain, <3H>TCP as radioligand) and to σ binding sites (guinea pig brain, <3H>-(+)pentazocine as radioligand)

Reference

Costa, Brian R. de; Mattson, Mariena V.; George, Clifford; Linders, Joannes T. M.

Journal of Medicinal Chemistry, 1992 , vol. 35, # 25 p. 4704 - 4712 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

binding to Phencyclidine receptors (IC50= 52 nM)

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Reference

Tsukiyama; Hashimoto; Katayama; Nishikawa; Tobe; Maeda

Chemical and Pharmaceutical Bulletin, 1991 , vol. 39, # 6 p. 1581 - 1584 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

potency to inhibit of the stimulated T-lymphocytes proliferation

Reference

Ilagouma, A. T.; Dornand, J.; Liu, C. F.; Zenone, F.; Mani, J. C.; Kamenka, J. M.

European Journal of Medicinal Chemistry, 1990 , vol. 25, # 7 p. 609 - 615 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

ED50 = 4.7 mg/kg (stereotyped behavior), ED50 = 6.5 mg/kg (ataxia) (male rats)

Reference

Gray, Nancy M.; Cheng, Brian K.; Mick, Stephen J.; Lair, Cecelia M.; Contreras, Patricia C.

Journal of Medicinal Chemistry, 1989 , vol. 32, # 6 p. 1242 - 1248 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

failed to block 20percent or more of conditioned avoidance responding in the ratat at 1.0 mg/kg ip

Reference

Martin; Elgin Jr.; Mathiasen; Davis; Kesslick; Baldy; Shank; DiStefano; Fedde; Scott

Journal of Medicinal Chemistry, 1989 , vol. 32, # 5 p. 1052 - 1056 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

IC50 = 0.091 μM (<(3)H>-1-<1-(2-thienyl)cyclohexyl>piperidine), IC50 = 0.53 μM (<(3)H>-N-allylnormetazocine) (membrane homogenates from rat whole brain)

Reference

Gray, Nancy M.; Cheng, Brian K.; Mick, Stephen J.; Lair, Cecelia M.; Contreras, Patricia C.

Journal of Medicinal Chemistry, 1989 , vol. 32, # 6 p. 1242 - 1248 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

behavior influence in rats after intracerebroventricular administration, ED50 nmol/rat, stereotyped behavior 150, ataxia 210

Reference

Costa, Brian R. de; George, Clifford; Burke, Terrence R.; Rafferty, Michael F.; Contreras, Patricia C.; et al.

Journal of Medicinal Chemistry, 1988 , vol. 31, # 8 p. 1571 - 1575 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

binding to phenylcyclidine receptors and σ sites, Ki (apparent) nM: 91, 530

Reference

Costa, Brian R. de; George, Clifford; Burke, Terrence R.; Rafferty, Michael F.; Contreras, Patricia C.; et al.

Journal of Medicinal Chemistry, 1988 , vol. 31, # 8 p. 1571 - 1575 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

local anasthetic effect (guinea pig, intracutaneously)

Reference

Eiden; Schmidt; Buchborn

Archiv der Pharmazie, 1987 , vol. 320, # 4 p. 348 - 361 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

excitability activity (mouse, subcutaneously); mobility activity (3 mg/kg, mouse, subcutaneously); analgetic activity - ED 50: 2.8 mg/kg (mouse, intraperitoneally); Naloxon antagonistic activity (mouse, subcutaneously) - NaCl influence

Reference

Eiden; Schmidt; Buchborn

Archiv der Pharmazie, 1987 , vol. 320, # 4 p. 348 - 361 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

<3H>PCP IC50=0.25 μM; <3H>QNB IC50=30 μM on the homogenats of rat brain

Reference

Kamenka; Michaud; Geneste; et al.

European Journal of Medicinal Chemistry, 1985 , vol. 20, # 5 p. 419 - 424 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

no effects on the electrical activity at the level of cerebello-rubral system in adult rabbits of both sexes; dose: 0.5-2 mg/kg

Reference

Sagratella; Longo

Arzneimittel-Forschung/Drug Research, 1985 , vol. 35, # 1 A p. 251 - 254 Title/Abstract Full Text View citing articles Show Details

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Comment (Pharmacological Data)

LD50 against male albino mice - 258μmol/kg

Reference

Kalir; Teomy; Amir; Fuchs; Lee; Holsztynska; Rocki; Domino

Journal of Medicinal Chemistry, 1984 , vol. 27, # 10 p. 1267 - 1271 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

reversible inhibitor of butyrylcholinesterase (BChE), ED50 = 9.60μmol/kg in mice

Reference

Kalir; Teomy; Amir; Fuchs; Lee; Holsztynska; Rocki; Domino

Journal of Medicinal Chemistry, 1984 , vol. 27, # 10 p. 1267 - 1271 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

LD 50: 280 mg/kg, rotarod activity ED 50: 17.6 mg/kg (mouse, i.p.)

Reference

Cone; Vaupel; Yousefnejad

Journal of Pharmacy and Pharmacology, 1982 , vol. 34, # 3 p. 197 - 199 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

binding affinity for the phencyclidine, muscarinic, and opiate receptors in rat brain homogenates; mouse rotarod assay activity, ED50 4 mg/kg

Reference

Kamenka; Chiche; Goudal; Geneste; Vignon; Vincent; Lazdunski

Journal of Medicinal Chemistry, 1982 , vol. 25, # 4 p. 431 - 435 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

acute toxicity, LD50 (mg/kg sc) in mice: 37.5

Reference

Itzhak, Yossef; Kalir, Asher; Weissman, Ben Avi; Cohen, Sasson

Journal of Medicinal Chemistry, 1981 , vol. 24, # 5 p. 496 - 499 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

Ataxia and toxicity produced by intraperitoneal administration in the mouse, ED50: 17.6 μmol/kg

Reference

Carroll, F. Ivy; Brine, George A.; Boldt, Karl G.; Cone, Edward J.; Yousefnejad, David; et al.

Journal of Medicinal Chemistry, 1981 , vol. 24, # 9 p. 1047 - 1051 Title/Abstract Full Text View citing articles Show Details

Ecotoxicology (1) 1 of 1

Effect (Ecotoxicology)

behavioral symtoms

Species or TestSystem (Ecotoxicology)

White Carneau pigeon

Route of Application

intramuscular

Concentration (Ecotoxicology)

0.56 - 1.8 mg/kg

Kind of Dosing (Ecotoxicology)

title comp. dissolved in physiological saline; administered in a volume of 1 ml/kg body weight

Method (Ecotoxicology)

pigeons were administered with title comp. 10 min before the start of test session; repeated acquisition of response chains were evaluated by measuring errors and response rates per second per reinforcement

Further Details (Ecotoxicology)

saline control; further study: effect of coadministration of D-serine on title comp. effect

Results

title comp. produced dose-dependent increase in percent errors and decrease in rates of responding; D-serine was less effective in reversing deficits produced by title comp.; fig.

Reference

Campbell, Cory M.; Butelman, Eduardo R.; Woods, James H.

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 289, # 1 p. 521 - 527 Title/Abstract Full Text View citing articles Show Details

Use/Application

Use (54) Use Pattern

Location

Reference

Pharmaceuticals

Page/Page column title page; 235; 236

Drexel University; AJIT, Seena; SACAN, Ahmet; ALEXANDER, Guillermo; SCHWARTZMAN, Robert J.; MCDONALD, Marguerite

Patent: US2016/76098 A1, 2016 ; Title/Abstract Full Text Show Details

diagnosing complex regional pain syndrome

Page/Page column title page; 235; 236

Drexel University; AJIT, Seena; SACAN, Ahmet; ALEXANDER, Guillermo; SCHWARTZMAN, Robert J.; MCDONALD, Marguerite

Patent: US2016/76098 A1, 2016 ; Title/Abstract Full Text Show Details

diagnosing neuropathic pain

Page/Page column title page; 235; 236

Drexel University; AJIT, Seena; SACAN, Ahmet; ALEXANDER, Guillermo; SCHWARTZMAN, Robert J.; MCDONALD, Marguerite

Patent: US2016/76098 A1, 2016 ; Title/Abstract Full Text Show Details

diagnosing neuropathic pain by comparing the level of at least one microRNA in the biological sample with the level of at least one miRNA or in a comparator

Page/Page column title page; 235; 236

Drexel University; AJIT, Seena; SACAN, Ahmet; ALEXANDER, Guillermo; SCHWARTZMAN, Robert J.; MCDONALD, Marguerite

Patent: US2016/76098 A1, 2016 ; Title/Abstract Full Text Show Details

diagnosing neuropathic pain by determining the level of at least one microRNA in a biological sample

Page/Page column title page; 235; 236

Drexel University; AJIT, Seena; SACAN, Ahmet; ALEXANDER, Guillermo; SCHWARTZMAN, Robert J.; MCDONALD, Marguerite

Patent: US2016/76098 A1, 2016 ; Title/Abstract Full Text Show Details

diagnosis of inflammation

Page/Page column title page; 235; 236

Drexel University; AJIT, Seena; SACAN, Ahmet; ALEXANDER, Guillermo; SCHWARTZMAN, Robert J.; MCDONALD, Marguerite

Patent: US2016/76098 A1, 2016 ; Title/Abstract Full Text Show Details

diagnosis of pain

Page/Page column title page; 235; 236

Drexel University; AJIT, Seena; SACAN, Ahmet; ALEXANDER, Guillermo; SCHWARTZMAN, Robert J.; MCDONALD, Marguerite

Patent: US2016/76098 A1, 2016 ; Title/Abstract Full Text Show Details

predicting the responsiveness of a treatment for neuropathic pain

Page/Page column title page; 235; 236

Drexel University; AJIT, Seena; SACAN, Ahmet; ALEXANDER, Guillermo; SCHWARTZMAN, Robert J.; MCDONALD, Marguerite

Patent: US2016/76098 A1, 2016 ; Title/Abstract Full Text Show Details

N-methyl-D-aspartate (NMDA) receptor antagonist

AZAYA THERAPEUTICS, INC.

Patent: WO2007/70779 A2, 2007 ; Title/Abstract Full Text Show Details

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ; Title/Abstract Full Text Show Details

ligand which binds to a cocaine-binding site of a beta-amyloid peptide

CORNELL RESEARCH FOUNDATION, INC.

Patent: WO2008/8884 A2, 2008 ; Title/Abstract Full Text Show Details

treating or preventing Alzheimer's Disease

CORNELL RESEARCH FOUNDATION, INC.

Patent: WO2008/8884 A2, 2008 ; Title/Abstract Full Text Show Details

Chronic pain

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ; Title/Abstract Full Text Show Details

pain associated with neuropathy

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu,

Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ; Title/Abstract Full Text Show Details

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ;

pain

Title/Abstract Full Text Show Details

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ;

acute postoperative pain

Title/Abstract Full Text Show Details

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ;

severe pain

Title/Abstract Full Text Show Details

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ;

Moderate pain

Title/Abstract Full Text Show Details

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ;

cancer pain

Title/Abstract Full Text Show Details

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ;

post-surgical pain

Title/Abstract Full Text Show Details

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ;

fever

Title/Abstract Full Text Show Details

Use Pattern

Reference

inflammation of a variety of conditions

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ; Title/Abstract Full Text Show Details

rheumatic fever

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ; Title/Abstract Full Text Show Details

symptoms associated with influenza

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ; Title/Abstract Full Text Show Details

viral infections

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ; Title/Abstract Full Text Show Details

common cold

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ; Title/Abstract Full Text Show Details

low back

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ;

Title/Abstract Full Text Show Details

neck pain

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ; Title/Abstract Full Text Show Details

dysmenorrhea

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ; Title/Abstract Full Text Show Details

headache

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ; Title/Abstract Full Text Show Details

toothache

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ; Title/Abstract Full Text Show Details

sprains

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ; Title/Abstract Full Text Show Details

strains

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ; Title/Abstract Full Text Show Details

myositis

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ; Title/Abstract Full Text Show Details

neuralgia

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ; Title/Abstract Full Text Show Details

synovitis

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ; Title/Abstract Full Text Show Details

arthritis

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ; Title/Abstract Full Text Show Details

rheumatoid arthritis

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ; Title/Abstract Full Text Show Details

degenerative joint diseases

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ; Title/Abstract Full Text Show Details

osteoarthritis

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ; Title/Abstract Full Text Show Details

gout

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ; Title/Abstract Full Text Show Details

ankylosing spondylitis

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ; Title/Abstract Full Text Show Details

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ;

bursitis

Title/Abstract Full Text Show Details

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ;

burns

Title/Abstract Full Text Show Details

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ;

symptoms associated with diabetic neuropathy

Title/Abstract Full Text Show Details

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ;

injuries

Title/Abstract Full Text Show Details

Singh, Chandra Ulagaraj; Woody, David Lloyd; Nulu, Jagaveerabhadra Rao

Patent: US2008/58362 A1, 2008 ;

Anti-inflammatory/antipyretic/analgetic drug

Title/Abstract Full Text Show Details

NMDA receptor antagonist for composition for treating a sexual dysfunction

TRINITY LABORATORIES INC.

Patent: WO2008/131256 A1, 2008 ; Title/Abstract Full Text Show Details

identifying a modulator of N-methyl-D-aspartate (NMDA) receptor function

deCODE Genetics, Inc.

Patent: US2006/29546 A1, 2006 ; Title/Abstract Full Text Show Details

agent that reduces phosphorylation of an NMDA receptor complex

deCODE Genetics, Inc.

Patent: US2006/29546 A1, 2006 ; Title/Abstract Full Text Show Details

psychotic disorder associated with administration of an anesthetic

Institut National de la Sante et de la Recherche Medicale (INSERM)

Patent: EP1462117 A1, 2004 ; Title/Abstract Full Text Show Details

Alzheimer's disease

Institut National de la Sante et de la Recherche Medicale (INSERM)

Patent: EP1462117 A1, 2004 ; Title/Abstract Full Text Show Details

vascular dementia

Institut National de la Sante et de la Recherche Medicale (INSERM)

Patent: EP1462117 A1, 2004 ; Title/Abstract Full Text Show Details

Parkinson's disease

Institut National de la Sante et de la Recherche Medicale (INSERM)

Patent: EP1462117 A1, 2004 ; Title/Abstract Full Text Show Details

psychostimulant

ORION CORPORATION

Patent: WO2003/82825 A1, 2003 ; Title/Abstract Full Text Show Details

Reaxys Registry Number: 1254857

CAS Registry Number: 117208-80-7 Type of Substance: heterocyclic Molecular Formula: C17H25N Linear Structure Formula: C17H23T2N Molecular Weight: 247.376

InChI Key: JTJMJGYZQZDUJJ-YMBPORIKSA-N 2

1 prep out of 1 reactions.

Identification

Synthesize | Hide Details Find similar

Identification Substance Label (1) Label

Reference

Phencyclidin-T

Kalir et al.

Journal of Labelled Compounds and Radiopharmaceuticals, 1977 , vol. 13, p. 445,446,447 Full Text View citing articles Show Details

Chemical Name: 1-(1-d5-phenylcyclohexyl)piperidine

2 prep out of 3 reactions.

Identification Physical Data (2) Spectra (3)

Reaxys Registry Number: 1626515

CAS Registry Number: 60124-86-9 Type of Substance: heterocyclic Molecular Formula: C17H25N Linear Structure Formula: C17H20D5N Molecular Weight: 248.352

InChI Key: JTJMJGYZQZDUJJ-ZWYOJXJXSA-N

Synthesize | Hide Details Find similar Chemical Names and Synonyms 1-(1-d5-phenylcyclohexyl)piperidine, <2H5>Phencyclidin, [2H5]Phencyclidin Identification Substance Label (2) Label

Reference

d&5%-1

Masumoto; Takeuchi; Ohta; Hirobe

Chemical and Pharmaceutical Bulletin, 1989 , vol. 37, # 7 p. 1788 - 1794 Title/Abstract Full Text View citing articles Show Details

III

Fentiman; Foltz

Journal of Labelled Compounds and Radiopharmaceuticals, 1976 , vol. 12, p. 69,74 Full Text Show Details

Derivative (2) Comment (Derivative)

Reference

By formation of salt/complex with HCl. Melting point at: 224 C - 227 C

Masumoto; Takeuchi; Ohta; Hirobe

Chemical and Pharmaceutical Bulletin, 1989 , vol. 37, # 7 p. 1788 - 1794 Title/Abstract Full Text View citing articles Show Details

Hydrochlorid: F: 219-220grad

Fentiman; Foltz

Journal of Labelled Compounds and Radiopharmaceuticals, 1976 , vol. 12, p. 69,74 Full Text Show Details

Physical Data Melting Point (1) Melting Point

Solvent (Melting Point)

Reference

34 - 36 °C

ethanol H2O

Masumoto; Takeuchi; Ohta; Hirobe

Chemical and Pharmaceutical Bulletin, 1989 , vol. 37, # 7 p. 1788 - 1794 Title/Abstract Full Text View citing articles Show Details

Boiling Point (1) Boiling Point

Pressure (Boiling Point)

Reference

120 - 124 °C

0.3 Torr

Fentiman; Foltz

Journal of Labelled Compounds and Radiopharmaceuticals, 1976 , vol. 12, p. 69,74 Full Text Show Details

Spectra NMR Spectroscopy (1) Description (NMR Spectroscopy)

Nucleus (NMR Spectroscopy)

Solvents (NMR Spectroscopy)

Chemical shifts

CDCl3

Reference Masumoto; Takeuchi; Ohta; Hirobe

Chemical and Pharmaceutical Bulletin, 1989 , vol. 37, # 7 p. 1788 1794 Title/Abstract Full Text View citing articles Show Details

IR Spectroscopy (1) Description (IR Spectroscopy)

Solvent (IR Spectroscopy)

Comment (IR Spectroscopy)

Bands

KBr

2275 cm**(-1)

Reference Masumoto; Takeuchi; Ohta; Hirobe

Chemical and Pharmaceutical Bulletin, 1989 , vol. 37, # 7 p. 1788 1794 Title/Abstract Full Text View citing articles Show Details

Mass Spectrometry (1) Reference Wilson; Domino

Biomedical Mass Spectrometry, 1978 , vol. 5, # 2 p. 112 - 116 Title/Abstract Full Text View citing articles Show Details

Chemical Name: phencyclidine hydrochloride Reaxys Registry Number: 4725489

CAS Registry Number: 956-90-1 Type of Substance: heterocyclic Molecular Formula: C17H25N*ClH Linear Structure Formula: C17H25N*HCl Molecular Weight: 279.853

InChI Key: BUAJNGPDPGKBGV-UHFFFAOYSA-N

2 prep out of 4 reactions.

Synthesize | Hide Details Find similar Chemical Names and Synonyms phencyclidine hydrochloride, 1-[1-phenyl-3-cyclohexyl]piperidine hydrochloride, PCP hydrochloride, phencyclidine HCl, phencyclidine, PCP, 1-[1(phenylcyclohexyl)]piperidine hydrochloride

Identification Physical Data (8) Spectra (4) Bioactivity (91)

Identification Substance Label (15) Label

Reference

PCP

Lal; Krutak-Krol; Domino

Arzneimittel-Forschung/Drug Research, 1986 , vol. 36, # 7 p. 1075 - 1078 Title/Abstract Full Text View citing articles Show Details

Hanson; Midgley; Bush; Gibb

European Journal of Pharmacology, 1995 , vol. 278, # 2 p. 167 - 173 Title/Abstract Full Text View citing articles Show Details

Pande; Cameron; Vig; Desaiah

Toxicology, 1998 , vol. 129, # 2-3 p. 95 - 102 Title/Abstract Full Text View citing articles Show Details

Cartmell, Jayne; Monn, James A.; Schoepp, Darryle D.

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 291, # 1 p. 161 - 170 Title/Abstract Full Text View citing articles Show Details

Yonezawa, Yuji; Kuroki, Toshihide; Kawahara, Takeshi; Tashiro, Nobutada; Uchimura, Hideyuki

European Journal of Pharmacology, 1998 , vol. 341, # 1 p. 45 - 56 Title/Abstract Full Text View citing articles Show Details

Kitaichi, Kiyoyuki; Noda, Yukihiro; Hasegawa, Takaaki; Furukawa, Hiroshi; Nabeshima, Toshitaka

European Journal of Pharmacology, 1996 , vol. 318, # 1 p. 7 - 9 Title/Abstract Full Text View citing articles Show Details

Noda, Yukihiro; Miyamoto, Yoshiaki; Mamiya, Takayoshi; Kamei, Hiroyuki; Furukawa, Hiroshi; Nabeshima, Toshitaka

Journal of Pharmacology and Experimental Therapeutics, 1998 , vol. 286, # 1 p. 44 - 51 Title/Abstract Full Text View citing articles Show Details

Ator, Nancy A.; Griffiths, Roland R.

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 282, # 3 p. 1442 - 1457 Title/Abstract Full Text View citing articles Show Details

Pechnick, Robert N.; Bresee, Catherine J.; Poland, Russell E.

Life Sciences, 2006 , vol. 78, # 17 p. 2006 - 2011 Title/Abstract Full Text View citing articles Show Details

Mcclure; Wenger; Mcmillan

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 3 p. 1357 - 1367 Title/Abstract Full Text View citing articles Show Details

Mouri, Akihiro; Noda, Yukihiro; Noda, Akihiro; Nakamura, Tomonobu; Tokura, Takanobu; Yura, Yoshimitsu; Nitta, Atsumi; Furukawa, Hiroshi; Nabeshima, Toshitaka

Molecular Pharmacology, 2007 , vol. 71, # 6 p. 1598 - 1609 Title/Abstract Full Text View citing articles Show Details

Shiraishi, Eri; Suzuki, Kazunori; Harada, Akina; Suzuki, Noriko; Kimura, Haruhide

Journal of Pharmacology and Experimental Therapeutics, 2016 , vol. 356, # 3 p. 587 - 595 Title/Abstract Full Text View citing articles Show Details

Stavchansky; Loper

Journal of pharmaceutical sciences, 1982 , vol. 71, # 2 p. 194 - 196 Title/Abstract Full Text View citing articles Show Details

Ahmadi, Abbas; Khalili, Mohsen; Hajikhani, Ramin; Naserbakht, Moslem

Pharmacology Biochemistry and Behavior, 2011 , vol. 98, # 2 p. 227 - 233 Title/Abstract Full Text View citing articles Show Details

M 7364

Millan, Mark J.; Audinot, Valerie; Honore, Prisca; Bervoets, Karin; Veiga, Sylvie; Brocco, Mauricette

European Journal of Pharmacology, 2000 , vol. 388, # 1 p. 37 - 47 Title/Abstract Full Text View citing articles Show Details

PCP, Merck 7376

Valentine, John L.; Mayersohn, Michael; Wessinger, William D.; Arnold, Larry W.; Owens, S. Michael

Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 278, # 2 p. 709 - 716 Title/Abstract Full Text View citing articles Show Details

Valentine, John L.; Owens, S. Michael

Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 278, # 2 p. 717 - 724 Title/Abstract Full Text View citing articles Show Details

Merck 7364; PCP

Mazzola-Pomietto, Pascale; Aulakh, Charanjit S.; Murphy, Dennis L.

European Journal of Pharmacology, 1996 , vol. 308, # 3 p. 329 - 333 Title/Abstract Full Text View citing articles Show Details

PCP*HCl

Iorio; Molinari; Scotti de Carolis; Niglio

Farmaco, Edizione Scientifica, 1984 , vol. 39, # 7 p. 599 - 611 Title/Abstract Full Text View citing articles Show Details

Coderc, E.; Cerruti, P.; Vignon, J.; Rouayrenc, J. F.; Kamenka, J. M.

European Journal of Medicinal Chemistry, 1995 , vol. 30, # 6 p. 463 - 470 Title/Abstract Full Text View citing articles Show Details

PCP, MERCK 7364

Kitaichi, Kiyoyuki; Yamada, Kiyofumi; Yoneda, Yukio; Ogita, Kiyokazu; Hasegawa, Takaaki; et al.

Life Sciences, 1995 , vol. 56, # 7 p. 531 - 544 Title/Abstract Full Text View citing articles Show Details

Merck Index 7364

Noda; Yamada; Furukawa; Nabeshima

European Journal of Pharmacology, 1995 , vol. 286, # 3 p. 291 - 297 Title/Abstract Full Text View citing articles Show Details

PCP*HCl, Merck I.,7364.

Swedberg; Jacobsen; Honore

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 274, # 3 p. 1113 - 1121 Title/Abstract Full Text View citing articles Show Details

Tab. 1

Wiley; Cristello; Balster

European Journal of Pharmacology, 1995 , vol. 294, # 1 p. 101 - 107 Title/Abstract Full Text View citing articles Show Details

Ferle-Vidovic, A; Kastelan, M; Petrovic, D; Suman, L; Kaselj, M; et al.

European Journal of Medicinal Chemistry, 1993 , vol. 28, # 3 p. 243 - 250 Title/Abstract Full Text View citing articles Show Details

1*HCl

Iorio, Maria A.; Tomassini, Lamberto; Mattson, Mariena V.; George, Clifford; Jacobson, Arthur E.

Journal of Medicinal Chemistry, 1991 , vol. 34, # 8 p. 2615 - 2623 Title/Abstract Full Text View citing articles Show Details

McQuinn; Cone; Shannon; Su

Journal of Medicinal Chemistry, 1981 , vol. 24, # 12 p. 1429 - 1432 Title/Abstract Full Text View citing articles Show Details

Itzhak, Yossef; Kalir, Asher; Weissman, Ben Avi; Cohen, Sasson

Journal of Medicinal Chemistry, 1981 , vol. 24, # 5 p. 496 - 499 Title/Abstract Full Text View citing articles Show Details

1, H in lieu of t-Bu

Manoharan, Muthiah; Eliel, Ernest L.

Tetrahedron Letters, 1984 , vol. 25, # 31 p. 3267 - 3268 Title/Abstract Full Text View citing articles Show Details

Brine; Boldt; Coleman; Carroll

Journal of Heterocyclic Chemistry, 1984 , vol. 21, # 1 p. 71 - 75 Title/Abstract Full Text View citing articles Show Details

I*HCl

Hufford; Baker; Clark

Journal of Pharmaceutical Sciences, 1981 , vol. 70, # 2 p. 155 - 158 Title/Abstract Full Text View citing articles Show Details

Patent-Specific Data (1) Location in Patent

Reference

Claim

Research Foundation of the State University of New York

Patent: US5696125 A1, 1997 ; Title/Abstract Full Text Show Details

Physical Data Melting Point (4) Melting Point

Solvent (Melting Point)

Reference

233 - 234 °C

isopropyl alcohol

Ahmadi, Abbas; Khalili, Mohsen; Abbassi, Sara; Javadi, Mozhdeh; Mahmoudi, Ali; Hajikhani, Ramin

Arzneimittel-Forschung/Drug Research, 2009 , vol. 59, # 4 p. 202 - 206 Title/Abstract Full Text View citing articles Show Details

Ahmadi, Abbas; Solati, Jalal; Hajikhani, Ramin; Onagh, Masoud; Javadi, Mojdeh

Arzneimittel-Forschung/Drug Research, 2010 , vol. 60, # 8 p. 492 - 496 Title/Abstract Full Text View citing articles Show Details

Ahmadi; Kermani; Naderi; Hajikhani; Rezaee; Javadi; Niknafs

Current Medicinal Chemistry, 2012 , vol. 19, # 5 p. 763 - 769 Title/Abstract Full Text View citing articles Show Details

233 - 234 °C

isopropyl alcohol

Ahmadi; Kermani; Naderi; Hajikhani; Rezaee; Javadi; Niknafs

Current Medicinal Chemistry, 2012 , vol. 19, # 5 p. 763 - 769 Title/Abstract Full Text View citing articles Show Details

Ahmadi, Abbas; Solati, Jalal; Hajikhani, Ramin; Pakzad, Sara

Asian Journal of Chemistry, 2011 , vol. 23, # 12 p. 5429 - 5432 Title/Abstract Full Text View citing articles Show Details

233 - 234 °C

isopropyl alcohol

Ahmadi, Abbas; Khalili, Mohsen; Hajikhani, Ramin; Naserbakht, Moslem

Pharmacology Biochemistry and Behavior, 2011 , vol. 98, # 2 p. 227 - 233 Title/Abstract Full Text View citing articles Show Details

243 - 244 °C

acetonitrile

McQuinn; Cone; Shannon; Su

Journal of Medicinal Chemistry, 1981 , vol. 24, # 12 p. 1429 - 1432 Title/Abstract Full Text View citing articles Show Details

Conformation (2)

Object of Investigation

Reference

Conformer equilibrium

Manoharan, Muthiah; Eliel, Ernest L.

Tetrahedron Letters, 1984 , vol. 25, # 31 p. 3267 - 3268 Title/Abstract Full Text View citing articles Show Details

Conformation

Manoharan, Muthiah; Eliel, Ernest L.

Tetrahedron Letters, 1984 , vol. 25, # 31 p. 3267 - 3268 Title/Abstract Full Text View citing articles Show Details

Dissociation Exponent (1) Dissociation Exponent (pK)

Dissociation Group

Temperature (Dissociation Exponent)

Solvent (Dissociation Exponent)

Method (Dissociation Exponent)

Type (Dissociation Exponent)

Comment (Dissociation Exponent)

9.73

N(+)-H

25 °C

ethanol H2O

potentiometric

a1/apparent

Ratio of solvents: 1:1

Reference Iorio; Molinari; Scotti de Carolis; Niglio

Farmaco, Edizione Scientifica, 1984 , vol. 39, # 7 p. 599 - 611 Title/Abstract Full Text View citing articles Show Details

Electrochemical Behaviour (1) Description (Electrochemical Behaviour)

Reference

Electrolytic dissociation / protonation equilibrium

Soine

Journal of Pharmaceutical Sciences, 1981 , vol. 70, # 1 p. 106 - 108 Title/Abstract Full Text View citing articles Show Details

Iorio; Molinari; Scotti de Carolis; Niglio

Farmaco, Edizione Scientifica, 1984 , vol. 39, # 7 p. 599 - 611 Title/Abstract Full Text View citing articles Show Details

Spectra NMR Spectroscopy (4) Description (NMR Spectroscopy)

Nucleus (NMR Spectroscopy)

Solvents (NMR Spectroscopy)

Temperature (NMR Spectroscopy)

Chemical shifts

13C

D2O

Iorio, Maria A.; Tomassini, Lamberto; Mattson, Mariena V.; George, Clifford; Jacobson, Arthur E.

Journal of Medicinal Chemistry, 1991 , vol. 34, # 8 p. 2615 - 2623 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

CDCl3

Brine; Boldt; Coleman; Carroll

Journal of Heterocyclic Chemistry, 1984 , vol. 21, # 1 p. 71 - 75 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

dimethylsulfoxide-d6

Brine; Boldt; Coleman; Carroll

Journal of Heterocyclic Chemistry, 1984 , vol. 21, # 1 p. 71 - 75 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

CD2Cl2

-120 °C

Bioactivity Pharmacological Data (90) 1 of 90

Comment (Pharmacological Data)

Bioactivities present

Reference

Maddox,V.H. et al.

J. Med. Chem., 1965 , vol. 8, p. 230 - 235 Title/Abstract Full Text View citing articles Show Details

Kalir; Edery; Pelah; Balderman; Porath

Journal of medicinal chemistry, 1969 , vol. 12, # 3 p. 473 - 477 Title/Abstract Full Text View citing articles Show Details

University of Kentucky Research Foundation

Patent: US5648369 A1, 1997 ; Title/Abstract Full Text Show Details

Research Foundation of the State University of New York

Reference

Manoharan, Muthiah; Eliel, Ernest L.

Tetrahedron Letters, 1984 , vol. 25, # 31 p. 3267 - 3268 Title/Abstract Full Text View citing articles Show Details

Patent: US5696125 A1, 1997 ; Title/Abstract Full Text Show Details

Brine; Boldt; Coleman; Carroll

Journal of Heterocyclic Chemistry, 1984 , vol. 21, # 1 p. 71 - 75 Title/Abstract Full Text View citing articles Show Details

Kane; Baron; Dudley; Sorensen; Staeger; Miller

Journal of Medicinal Chemistry, 1990 , vol. 33, # 10 p. 2772 - 2777 Title/Abstract Full Text View citing articles Show Details

Manoharan, Muthiah; Eliel, Ernest L.

Tetrahedron Letters, 1984 , vol. 25, # 31 p. 3267 - 3268 Title/Abstract Full Text View citing articles Show Details

Iorio, Maria A.; Tomassini, Lamberto; Mattson, Mariena V.; George, Clifford; Jacobson, Arthur E.

Journal of Medicinal Chemistry, 1991 , vol. 34, # 8 p. 2615 - 2623 Title/Abstract Full Text View citing articles Show Details

Baker; Wohlford; Bradbury; Wirth

Journal of Medicinal Chemistry, 1981 , vol. 24, # 6 p. 666 - 669 Title/Abstract Full Text View citing articles Show Details

McQuinn; Cone; Shannon; Su

Journal of Medicinal Chemistry, 1981 , vol. 24, # 12 p. 1429 - 1432 Title/Abstract Full Text View citing articles Show Details

Itzhak, Yossef; Kalir, Asher; Weissman, Ben Avi; Cohen, Sasson

Journal of Medicinal Chemistry, 1981 , vol. 24, # 5 p. 496 - 499 Title/Abstract Full Text View citing articles Show Details

Lal; Krutak-Krol; Domino

Arzneimittel-Forschung/Drug Research, 1986 , vol. 36, # 7 p. 1075 - 1078 Title/Abstract Full Text View citing articles Show Details

Bigge; Malone; Hays; Johnson; Novak; Lescosky; Retz; Ortwine; Probert Jr.; Coughenour; Boxer; Robichaud; Brahce; Shillis

Journal of Medicinal Chemistry, 1993 , vol. 36, # 14 p. 1977 - 1995 Title/Abstract Full Text View citing articles Show Details

Ferle-Vidovic, A; Kastelan, M; Petrovic, D; Suman, L; Kaselj, M; et al.

European Journal of Medicinal Chemistry, 1993 , vol. 28, # 3 p. 243 - 250 Title/Abstract Full Text View citing articles Show Details

Stavchansky; Loper

Journal of pharmaceutical sciences, 1982 , vol. 71, # 2 p. 194 - 196 Title/Abstract Full Text View citing articles Show Details

Hufford; Baker; Clark

Journal of Pharmaceutical Sciences, 1981 , vol. 70, # 2 p. 155 - 158 Title/Abstract Full Text View citing articles Show Details

Soine

Journal of Pharmaceutical Sciences, 1981 , vol. 70, # 1 p. 106 - 108 Title/Abstract Full Text View citing articles Show Details

Iorio; Molinari; Scotti de Carolis; Niglio

Farmaco, Edizione Scientifica, 1984 , vol. 39, # 7 p. 599 - 611 Title/Abstract Full Text View citing articles Show Details

Coderc, E.; Cerruti, P.; Vignon, J.; Rouayrenc, J. F.; Kamenka, J. M.

European Journal of Medicinal Chemistry, 1995 , vol. 30, # 6 p. 463 - 470 Title/Abstract Full Text View citing articles Show Details

Hanson; Midgley; Bush; Gibb

European Journal of Pharmacology, 1995 , vol. 278, # 2 p. 167 - 173 Title/Abstract Full Text View citing articles Show Details

2 of 90

Comment (Pharmacological Data)

Bioactivities present

Reference

Pande; Cameron; Vig; Desaiah

Toxicology, 1998 , vol. 129, # 2-3 p. 95 - 102 Title/Abstract Full Text View citing articles Show Details

Kitaichi, Kiyoyuki; Yamada, Kiyofumi; Yoneda, Yukio; Ogita, Kiyokazu; Hasegawa, Takaaki; et al.

Life Sciences, 1995 , vol. 56, # 7 p. 531 - 544 Title/Abstract Full Text View citing articles Show Details

Proksch, Joel W.; Gentry, W. Brooks; Owens, S. Michael

Journal of Pharmacology and Experimental Therapeutics, 1998 , vol. 287, # 2 p. 616 - 624 Title/Abstract Full Text View citing articles Show Details

Noda; Yamada; Furukawa; Nabeshima

European Journal of Pharmacology, 1995 , vol. 286, # 3 p. 291 - 297 Title/Abstract Full Text View citing articles Show Details

Kantak; Edwards; Spealman

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 274, # 2 p. 657 - 665 Title/Abstract Full Text View citing articles Show Details

Swedberg; Jacobsen; Honore

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 274, # 3 p. 1113 - 1121 Title/Abstract Full Text View citing articles Show Details

Sample; Arenal

Bulletin of Environmental Contamination and Toxicology, 1999 , vol. 62, # 6 p. 653 - 663 Title/Abstract Full Text View citing articles Show Details

Hara, Koji; Yanagihara, Nobuyuki; Minami, Kouichiro; Ueno, Susumu; Toyohira, Yumiko; Sata, Takeyoshi; Kawamura, Masaru; Bruess, Michael; Boenisch, Heinz; Shigematsu, Akio; Izumi, Futoshi

Naunyn-Schmiedeberg's Archives of Pharmacology, 1998 , vol. 358, # 3 p. 328 - 333 Title/Abstract Full Text View citing articles Show Details

Valentine, John L.; Mayersohn, Michael; Wessinger, William D.; Arnold, Larry W.; Owens, S. Michael

Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 278, # 2 p. 709 - 716 Title/Abstract Full Text View citing articles Show Details

Valentine, John L.; Owens, S. Michael

Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 278, # 2 p. 717 - 724

Title/Abstract Full Text View citing articles Show Details

Wiley; Cristello; Balster

European Journal of Pharmacology, 1995 , vol. 294, # 1 p. 101 - 107 Title/Abstract Full Text View citing articles Show Details

Mazzola-Pomietto, Pascale; Aulakh, Charanjit S.; Murphy, Dennis L.

European Journal of Pharmacology, 1996 , vol. 308, # 3 p. 329 - 333 Title/Abstract Full Text View citing articles Show Details

McMillan; Sun; Hardwick

Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 278, # 1 p. 50 - 61 Title/Abstract Full Text View citing articles Show Details

Cartmell, Jayne; Monn, James A.; Schoepp, Darryle D.

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 291, # 1 p. 161 - 170 Title/Abstract Full Text View citing articles Show Details

Yonezawa, Yuji; Kuroki, Toshihide; Kawahara, Takeshi; Tashiro, Nobutada; Uchimura, Hideyuki

European Journal of Pharmacology, 1998 , vol. 341, # 1 p. 45 - 56 Title/Abstract Full Text View citing articles Show Details

Ellison, Gaylord; Keys, Alan; Noguchi, Kevin

Pharmacology and Toxicology, 1999 , vol. 84, # 1 p. 9 - 17 Title/Abstract Full Text View citing articles Show Details

Millan, Mark J.; Audinot, Valerie; Honore, Prisca; Bervoets, Karin; Veiga, Sylvie; Brocco, Mauricette

European Journal of Pharmacology, 2000 , vol. 388, # 1 p. 37 - 47 Title/Abstract Full Text View citing articles Show Details

Jebelli, Azadeh Kokabi; Doan, Ngan; Ellison, Gaylord

Pharmacology and Toxicology, 2002 , vol. 90, # 1 p. 20 - 25 Title/Abstract Full Text View citing articles Show Details

Shelton, Keith L.; Balster, Robert L.

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 280, # 3 p. 1250 - 1260 Title/Abstract Full Text View citing articles Show Details

Kitaichi, Kiyoyuki; Noda, Yukihiro; Hasegawa, Takaaki; Furukawa, Hiroshi; Nabeshima, Toshitaka

European Journal of Pharmacology, 1996 , vol. 318, # 1 p. 7 - 9 Title/Abstract Full Text View citing articles Show Details

3 of 90

Comment (Pharmacological Data)

Bioactivities present

Reference

Kitaichi, Kiyoyuki; Noda, Yukihiro; Hasegawa, Takaaki; Furukawa, Hiroshi; Nabeshima, Toshitaka

European Journal of Pharmacology, 1996 , vol. 318, # 2-3 p. 205 - 211 Title/Abstract Full Text View citing articles Show Details

Shelnutt; Cornett; Owens, S. Michael

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 1 p. 574 - 581 Title/Abstract Full Text View citing articles Show Details

Noda, Yukihiro; Miyamoto, Yoshiaki; Mamiya, Takayoshi; Kamei, Hiroyuki; Furukawa, Hiroshi; Nabeshima, Toshitaka

Journal of Pharmacology and Experimental Therapeutics, 1998 , vol. 286, # 1 p. 44 - 51 Title/Abstract Full Text View citing articles Show Details

Sheridan, Robert D.; Turner, Simon R.; Cooper, Graham J.; Tattersall, John E.H.

European Journal of Pharmacology, 2005 , vol. 511, # 2-3 p. 99 - 107 Title/Abstract Full Text View citing articles Show Details

Ator, Nancy A.; Griffiths, Roland R.

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 282, # 3 p. 1442 - 1457 Title/Abstract Full Text View citing articles Show Details

Pechnick, Robert N.; Bresee, Catherine J.; Poland, Russell E.

Life Sciences, 2006 , vol. 78, # 17 p. 2006 - 2011 Title/Abstract Full Text View citing articles Show Details

Smith, James B.; Ogonowski, Alison A.

European Journal of Pharmacology, 2003 , vol. 471, # 2 p. 121 - 128 Title/Abstract Full Text View citing articles Show Details

Winger; Hursh; Casey; Woods

Journal of Pharmacology and Experimental Therapeutics, 2002 , vol. 301, # 2 p. 690 - 697 Title/Abstract Full Text View citing articles Show Details

Mcclure; Wenger; Mcmillan

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 3 p. 1357 - 1367 Title/Abstract Full Text View citing articles Show Details

Wiley, Jenny L.; Balster, Robert L.

Life Sciences, 2004 , vol. 75, # 2 p. 141 - 151 Title/Abstract Full Text View citing articles Show Details

Bujas-Bobanovic, Maja; Robertson, Harold A; Dursun, Serdar M

European Journal of Pharmacology, 2000 , vol. 409, # 1 p. 57 - 65 Title/Abstract Full Text View citing articles Show Details

Witkin, Jeffrey M.; Gasior, Maciej; Heifets, Boris; Tortella, Frank C.

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 289, # 2 p. 703 - 711 Title/Abstract Full Text View citing articles Show Details

Mouri, Akihiro; Noda, Yukihiro; Noda, Akihiro; Nakamura, Tomonobu; Tokura, Takanobu; Yura, Yoshimitsu; Nitta, Atsumi; Furukawa, Hiroshi; Nabeshima, Toshitaka

Molecular Pharmacology, 2007 , vol. 71, # 6 p. 1598 - 1609 Title/Abstract Full Text View citing articles Show Details

Ahmadi, Abbas; Khalili, Mohsen; Abbassi, Sara; Javadi, Mozhdeh; Mahmoudi, Ali; Hajikhani, Ramin

Arzneimittel-Forschung/Drug Research, 2009 , vol. 59, # 4 p. 202 - 206 Title/Abstract Full Text View citing articles Show Details

Ahmadi, Abbas; Solati, Jalal; Hajikhani, Ramin; Onagh, Masoud; Javadi, Mojdeh

Arzneimittel-Forschung/Drug Research, 2010 , vol. 60, # 8 p. 492 - 496 Title/Abstract Full Text View citing articles Show Details

Radonjic, Nevena V.; Knezevic, Iva D.; Vilimanovich, Urosh; Kravic-Stevovic, Tamara; Marina, Ljiljana V.; Nikolic, Tatjana; Todorovic, Veljko; Bumbasirevic, Vladimir; Petronijevic, Natasa D.

Neuropharmacology, 2010 , vol. 58, # 4-5 p. 739 - 745 Title/Abstract Full Text View citing articles Show Details

Arias, Hugo R.; Feuerbach, Dominik; Targowska-Duda, Katarzyna M.; Jozwiak, Krzysztof

Neurochemistry International, 2010 , vol. 57, # 2 p. 153 - 161 Title/Abstract Full Text View citing articles Show Details

Ahmadi; Kermani; Naderi; Hajikhani; Rezaee; Javadi; Niknafs

Current Medicinal Chemistry, 2012 , vol. 19, # 5 p. 763 - 769 Title/Abstract Full Text View citing articles Show Details

Ahmadi, Abbas; Solati, Jalal; Hajikhani, Ramin; Pakzad, Sara

Asian Journal of Chemistry, 2011 , vol. 23, # 12 p. 5429 - 5432 Title/Abstract Full Text View citing articles Show Details

Shebley, Mohamad; Hollenberg, Paul F.

Drug Metabolism and Disposition, 2007 , vol. 35, # 8 p. 1365 - 1371 Title/Abstract Full Text View citing articles Show Details

4 of 90

5 of 90

Comment (Pharmacological Data)

Bioactivities present

Reference

Ahmadi, Abbas; Khalili, Mohsen; Hajikhani, Ramin; Naserbakht, Moslem

Pharmacology Biochemistry and Behavior, 2011 , vol. 98, # 2 p. 227 - 233 Title/Abstract Full Text View citing articles Show Details

Pinchasi; Maayani; Sokolovsky

Biochemical Pharmacology, 1977 , vol. 26, # 18 p. 1671 - 1679 Title/Abstract Full Text Show Details

Kloog; Rehavi; Maayani; Sokolovsky

European Journal of Pharmacology, 1977 , vol. 45, # 3 p. 221 - 227 Title/Abstract Full Text Show Details

Proksch, Joel W.; Gentry, W. Brooks; Owens, S. Michael

Drug Metabolism and Disposition, 2000 , vol. 28, # 7 p. 742 - 747 Title/Abstract Full Text View citing articles Show Details

Pande; Cameron; Vig; Desaiah

Toxicology, 1998 , vol. 129, # 2-3 p. 95 - 102 Title/Abstract Full Text View citing articles Show Details

Laurenzana, Elizabeth M.; Owens, S. Michael

Drug Metabolism and Disposition, 1997 , vol. 25, # 5 p. 557 - 563 Title/Abstract Full Text View citing articles Show Details

Valentine; Mayersohn; Wessinger; Arnold; Owens

Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 278, # 2 p. 709 - 716 Title/Abstract Full Text View citing articles Show Details

Kitaichi, Kiyoyuki; Yamada, Kiyofumi; Yoneda, Yukio; Ogita, Kiyokazu; Hasegawa, Takaaki; Furukawa, Hiroshi; Nabeshima, Toshitaka

Life Sciences, 1995 , vol. 56, # 7 p. 531 - 543 Title/Abstract Full Text Show Details

Ferle-Vidovic; Kastelan; Petrovic; Suman; Kaselj; Skare; Mlinaric-Majerski

European Journal of Medicinal Chemistry, 1993 , vol. 28, # 3 p. 243 - 250 Title/Abstract Full Text Show Details

Su; Wu; Cone; Shukla; Gund; Dodge; Parish

Journal of Pharmacology and Experimental Therapeutics, 1991 , vol. 259, # 2 p. 543 - 550 Title/Abstract Full Text View citing articles Show Details

Iorio; Tomassini; Mattson; George; Jacobson

Journal of Medicinal Chemistry, 1991 , vol. 34, # 8 p. 2615 - 2623 Title/Abstract Full Text Show Details

Kilpatrick; Michel

Agents and Actions, 1991 , vol. 33, # SUPPL. p. 69 - 75 Title/Abstract Full Text View citing articles Show Details

Thurkauf; De Costa; Yamaguchi; Mattson; Jacobson; Rice; Rogawski

Journal of Medicinal Chemistry, 1990 , vol. 33, # 5 p. 1452 - 1458 Title/Abstract Full Text Show Details

Tam

European journal of pharmacology, 1985 , vol. 109, # 1 p. 33 - 41 Title/Abstract Full Text Show Details

Vickroy; Roeske; Yamamura

Journal of Pharmacology and Experimental Therapeutics, 1984 , vol. 229, # 3 p. 747 - 755 Title/Abstract Full Text View citing articles Show Details

Cook; Brine; Jeffcoat; Hill; Wall; Perez-Reyes; Di Guiseppi

Clinical Pharmacology and Therapeutics, 1982 , vol. 31, # 5 p. 625 - 634 Title/Abstract Full Text Show Details

Stavchansky; Loper

Journal of Pharmaceutical Sciences, 1982 , vol. 71, # 2 p. 194 - 196 Title/Abstract Full Text View citing articles Show Details

Itzhak; Kalir; Weissman; Cohen

Journal of Medicinal Chemistry, 1981 , vol. 24, # 5 p. 496 - 499 Title/Abstract Full Text Show Details

Collier, H O; Dinneen, L C; Johnson, C A; Schneider, C

British journal of pharmacology and chemotherapy, 1968 , vol. 32, p. 295 - 310 Title/Abstract Full Text Show Details

Type: Review, Lab: EFF_071212, Owner: EFFECT, Number: 000, Revision: 07.12.2012 00:00:00 2012 Full Text Show Details

Comment (Pharmacological Data)

Bioactivities present

Reference

Hamouda, Ayman K.; Wang, Ze-Jun; Stewart, Deirdre S.; Jain, Atul D.; Glennon, Richard A.; Cohen, Jonathan B.

Molecular Pharmacology, 2015 , vol. 88, # 1 p. 1 - 11 Title/Abstract Full Text View citing articles Show Details

Shiraishi, Eri; Suzuki, Kazunori; Harada, Akina; Suzuki, Noriko; Kimura, Haruhide

Journal of Pharmacology and Experimental Therapeutics, 2016 , vol. 356, # 3 p. 587 - 595 Title/Abstract Full Text View citing articles Show Details

Halberstadt, Adam L.; Slepak, Natalia; Hyun, James; Buell, Mahalah R.; Powell, Susan B.

Psychopharmacology, 2016 , vol. 233, # 7 p. 1215 - 1225 Title/Abstract Full Text View citing articles Show Details

Devroye, Céline; Cathala, Adeline; Haddjeri, Nasser; Rovera, Renaud; Vallée, Monique; Drago, Filippo; Piazza, Pier Vincenzo; Spampinato, Umberto

Neuropharmacology, 2016 , vol. 109, p. 59 - 68 Title/Abstract Full Text View citing articles Show Details

Hashem, Abeer; Abd_Allah, Elsayed Fathi; Alqarawi, Abdulaziz A.; Aldubise, Abdullah; Egamberdieva, Dilfuza

Journal of Plant Interactions, 2015 , vol. 10, # 1 p. 230 - 242 Title/Abstract Full Text Show Details

6 of 90

7 of 90

8 of 90

9 of 90

10 of 90

11 of 90

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Shiraishi, Eri; Suzuki, Kazunori; Harada, Akina; Suzuki, Noriko; Kimura, Haruhide

Journal of Pharmacology and Experimental Therapeutics, 2016 , vol. 356, # 3 p. 587 - 595 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Halberstadt, Adam L.; Slepak, Natalia; Hyun, James; Buell, Mahalah R.; Powell, Susan B.

Psychopharmacology, 2016 , vol. 233, # 7 p. 1215 - 1225 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Hamouda, Ayman K.; Wang, Ze-Jun; Stewart, Deirdre S.; Jain, Atul D.; Glennon, Richard A.; Cohen, Jonathan B.

Molecular Pharmacology, 2015 , vol. 88, # 1 p. 1 - 11 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Ahmadi, Abbas; Khalili, Mohsen; Hajikhani, Ramin; Naserbakht, Moslem

Pharmacology Biochemistry and Behavior, 2011 , vol. 98, # 2 p. 227 - 233 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme activity; effect on

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

female

Route of Application

subcutaneous

Concentration (Pharmacological Data)

10 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline solution; administered in the interscapular region on postnatal day 2, 6, 9, and 12

Results

no effect (related to glutathione peroxidase caudate nucleus)

Reference

Radonjic, Nevena V.; Knezevic, Iva D.; Vilimanovich, Urosh; Kravic-Stevovic, Tamara; Marina, Ljiljana V.; Nikolic, Tatjana; Todorovic, Veljko; Bumbasirevic, Vladimir; Petronijevic, Natasa D.

Neuropharmacology, 2010 , vol. 58, # 4-5 p. 739 - 745 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme activity; effect on

Species or TestSystem (Pharmacological Data)

Wistar rat

12 of 90

13 of 90

14 of 90

Sex

female

Route of Application

subcutaneous

Concentration (Pharmacological Data)

10 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline solution; administered in the interscapular region on postnatal day 2, 6, 9, and 12

Results

no effect (related to glutathione peroxidase thalamus)

Reference

Radonjic, Nevena V.; Knezevic, Iva D.; Vilimanovich, Urosh; Kravic-Stevovic, Tamara; Marina, Ljiljana V.; Nikolic, Tatjana; Todorovic, Veljko; Bumbasirevic, Vladimir; Petronijevic, Natasa D.

Neuropharmacology, 2010 , vol. 58, # 4-5 p. 739 - 745 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme activity; effect on

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

female

Route of Application

subcutaneous

Concentration (Pharmacological Data)

10 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline solution; administered in the interscapular region on postnatal day 2, 6, 9, and 12

Results

no effect (related to glutathione reductase caudate nucleus)

Reference

Radonjic, Nevena V.; Knezevic, Iva D.; Vilimanovich, Urosh; Kravic-Stevovic, Tamara; Marina, Ljiljana V.; Nikolic, Tatjana; Todorovic, Veljko; Bumbasirevic, Vladimir; Petronijevic, Natasa D.

Neuropharmacology, 2010 , vol. 58, # 4-5 p. 739 - 745 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

catalase activity; effect on

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

female

Route of Application

subcutaneous

Concentration (Pharmacological Data)

10 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline solution; administered in the interscapular region on postnatal day 2, 6, 9, and 12

Results

no effect (related to glutathione reductase dorsolateral frontal cortex)

Reference

Radonjic, Nevena V.; Knezevic, Iva D.; Vilimanovich, Urosh; Kravic-Stevovic, Tamara; Marina, Ljiljana V.; Nikolic, Tatjana; Todorovic, Veljko; Bumbasirevic, Vladimir; Petronijevic, Natasa D.

Neuropharmacology, 2010 , vol. 58, # 4-5 p. 739 - 745 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

catalase activity; effect on

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

female

15 of 90

16 of 90

17 of 90

Route of Application

subcutaneous

Concentration (Pharmacological Data)

10 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline solution; administered in the interscapular region on postnatal day 2, 6, 9, and 12

Results

no effect (related to glutathione reductase hippocampus)

Reference

Radonjic, Nevena V.; Knezevic, Iva D.; Vilimanovich, Urosh; Kravic-Stevovic, Tamara; Marina, Ljiljana V.; Nikolic, Tatjana; Todorovic, Veljko; Bumbasirevic, Vladimir; Petronijevic, Natasa D.

Neuropharmacology, 2010 , vol. 58, # 4-5 p. 739 - 745 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme activity; effect on

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

female

Route of Application

subcutaneous

Concentration (Pharmacological Data)

10 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline solution; administered in the interscapular region on postnatal day 2, 6, 9, and 12

Results

no effect (related to catalase caudate nucleus)

Reference

Radonjic, Nevena V.; Knezevic, Iva D.; Vilimanovich, Urosh; Kravic-Stevovic, Tamara; Marina, Ljiljana V.; Nikolic, Tatjana; Todorovic, Veljko; Bumbasirevic, Vladimir; Petronijevic, Natasa D.

Neuropharmacology, 2010 , vol. 58, # 4-5 p. 739 - 745 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme activity; effect on

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

female

Route of Application

subcutaneous

Concentration (Pharmacological Data)

10 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline solution; administered in the interscapular region on postnatal day 2, 6, 9, and 12

Results

no effect (related to catalase thalamus)

Reference

Radonjic, Nevena V.; Knezevic, Iva D.; Vilimanovich, Urosh; Kravic-Stevovic, Tamara; Marina, Ljiljana V.; Nikolic, Tatjana; Todorovic, Veljko; Bumbasirevic, Vladimir; Petronijevic, Natasa D.

Neuropharmacology, 2010 , vol. 58, # 4-5 p. 739 - 745 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

analgesic

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

male

18 of 90

19 of 90

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

6 mg/kg

Kind of Dosing (Pharmacological Data)

in saline

Further Details (Pharmacological Data)

tail immersion test

Type (Pharmacological Data)

effective dose

Value of Type (Pharmacological Data)

6 mg/kg

Reference

Ahmadi, Abbas; Khalili, Mohsen; Abbassi, Sara; Javadi, Mozhdeh; Mahmoudi, Ali; Hajikhani, Ramin

Arzneimittel-Forschung/Drug Research, 2009 , vol. 59, # 4 p. 202 - 206 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

cognitive function; impairment of

Species or TestSystem (Pharmacological Data)

ddY mouse

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

10 mg/kg

Kind of Dosing (Pharmacological Data)

dissolved in saline; once a day for 14 days

Method (Pharmacological Data)

4 days after last dosing mice were subjected to training trial of water-finding test; 24 h later entering and finding latencies measured in test trial; after training trial prefrontal cortex tissue extracts were prepared and assayed by Western blot

Further Details (Pharmacological Data)

CaMKII: Ca(2+)/calmodulin-dependent protein kinase (phosphorylation of threonine 286 of α-subunit assessed); NR1: N-methyl-Daspartate receptor ζ subunit; NR1 phosphorylation ratio: phospho-NR1 (Ser897) contents in total and membrane-enriched extracts

Results

repeated title comp. treatment induced impairment of latent learning; the effect was accompanied with reduced levels of phosphorylated CaMKII and decreased NR1 phosphorylation ratio compared with saline-treated mice; no effect 24 h after single dose

Reference

Mouri, Akihiro; Noda, Yukihiro; Noda, Akihiro; Nakamura, Tomonobu; Tokura, Takanobu; Yura, Yoshimitsu; Nitta, Atsumi; Furukawa, Hiroshi; Nabeshima, Toshitaka

Molecular Pharmacology, 2007 , vol. 71, # 6 p. 1598 - 1609 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

hormone releasing; effect on

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

1 - 10 mg/kg

Kind of Dosing (Pharmacological Data)

dissolved in saline

Method

60 min after title comp. treatment rats sacrificed; trunk blood collected; plasma removed; plasma hormone levels measured by radioimmunoassay

(Pharmacological Data)

20 of 90

21 of 90

22 of 90

Further Details (Pharmacological Data)

control: 0.9 percent NaCl

Results

title comp. caused significant increases in plasma levels of adrenocorticotropin (13-fold at 10 mg/kg) and corticosterone and significant decreases in plasma levels of prolactin

Reference

Pechnick, Robert N.; Bresee, Catherine J.; Poland, Russell E.

Life Sciences, 2006 , vol. 78, # 17 p. 2006 - 2011 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

action potential; effect on

Species or TestSystem (Pharmacological Data)

sheep cardiac Purkinje fiber

Sex

male

Concentration (Pharmacological Data)

0.05 - 5 μmol/l

Kind of Dosing (Pharmacological Data)

formulated in DMSO; added cumulatively

Method (Pharmacological Data)

after 30 min. treatment with title comp. fibers placed to two-channel recording chamber with two silver stimulation electrodes; 1 Hz; square-wave constant voltage pulses ca. 0.05 ms; cardiac action potentials (AP) monitored

Further Details (Pharmacological Data)

analysed parameters: AP duration at 50 percent or 90 percent repolarisation, maximum rate of rise in AP upstroke, upstroke amplitude, diastolic membrane potential; further investigation with dl-sotalol, human ether-a-go-go related gene/K(1+) current blocker

Results

title comp. induced prolongation of AP duration at 50 percent and 90 percent repolarisation in conc.-dependent manner (figure, table)

Reference

Sheridan, Robert D.; Turner, Simon R.; Cooper, Graham J.; Tattersall, John E.H.

European Journal of Pharmacology, 2005 , vol. 511, # 2-3 p. 99 - 107 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)

0.3 - 3 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in 0.9 percent saline

Method (Pharmacological Data)

rats trained to discriminate diazepam from vehicle; rats injected with diazepam 2.5 mg/kg or vehicle and 30 min later treated with title comp.; diazepam-lever responding observed

Further Details (Pharmacological Data)

reference comp.: diazepam

Results

title comp. at dose 3 mg/kg significantly decreased response rate; reference comp. fully dose-dependently substituted for training dose (figure)

Reference

Wiley, Jenny L.; Balster, Robert L.

Life Sciences, 2004 , vol. 75, # 2 p. 141 - 151 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

23 of 90

24 of 90

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

0.3 - 5.6 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. in saline, admin. in four to five doses

Method (Pharmacological Data)

rats in Gerbands model C rat chambers; rats maintained under FR120 SFD; after stable response, admin. with title comp. 15 min prior to expt. session; title comp. effect on overall rate of responding under FR120 SFD detd.

Further Details (Pharmacological Data)

FR120: 120-response fixed ratio; SFD: schedule of food delivery; further study with title comp. (3 mg/kg) in combination with L-arginine, L-NAME, 7-nitroindazole, aminoguanidine, molsidomine, nitroprusside, AP5

Results

title comp. decreased FR120 responding at largest doses; title comp. effect not affected by L-arginine, 7-nitroindazole, molsidomine, nitroprusside, aminoguanidine, L-NAME, AP5; diagrams

Reference

Smith, James B.; Ogonowski, Alison A.

European Journal of Pharmacology, 2003 , vol. 471, # 2 p. 121 - 128 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neurotoxicity

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

female

Route of Application

subcutaneous

Kind of Dosing (Pharmacological Data)

continuous administration for 5 days (5.45 mg/day) by minipumps implanted s.c. during 2nd (days 8-13) or 3rd (days 16-21) trimester of gestation

Method (Pharmacological Data)

rats 60-80 d of age, 280-350 g weight; 12 h light/dark cycle; pups fixed immed. after birth; brains removed and silver stained; number of stained cells counted

Further Details (Pharmacological Data)

control - saline; free access to food and water before treatment; nutritive supplement 10 cc/day during treatment

Results

in pups signif. increase in number of degener. cells in entorhinal cortex and subiculum; effect greater when title comp. applied during 2nd trimester; in ventromedial nucl. of hypothalamus degenerating cells fewer than in control in both groups

Reference

Jebelli, Azadeh Kokabi; Doan, Ngan; Ellison, Gaylord

Pharmacology and Toxicology, 2002 , vol. 90, # 1 p. 20 - 25 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

female

Kind of Dosing (Pharmacological Data)

continuous administration for 5 days (5.45 mg/day) by minipumps implanted s.c. during 2nd (days 8-13) or 3rd (days 16-21) trimester of gestation

Method (Pharmacological Data)

45-60 day old female pups from female rats exposed to title comp. during gestation; behavioural deviation of pups tested in open field, on Radial Arm Maze using Win-Shift task and on rotorod

Further Details (Pharmacological Data)

control - saline

25 of 90

26 of 90

27 of 90

Results

rotorod and open field revealed decrease of motor coordination and hyperactivity of pups from rats exposed to title comp. during 3rd trimester; minimal alterations in 2nd trimester pups

Reference

Jebelli, Azadeh Kokabi; Doan, Ngan; Ellison, Gaylord

Pharmacology and Toxicology, 2002 , vol. 90, # 1 p. 20 - 25 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

rhesus monkey

Sex

male and female

Route of Application

intravenous

Concentration (Pharmacological Data)

1 - 1.8 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in physiological saline and made up in conc. between 1 and 10 mg/ml

Method (Pharmacological Data)

monkeys admin. with title comp.; behavior obsd. for 1-320 min; behavioral symptoms recorded based on reaction to environment, posture, salivation, nystagmus; total impairment scores recorded

Further Details (Pharmacological Data)

MR: maximum response

Results

title comp. produced variable but clear effect within 1 min; rapidly increased over next 2 min; effect maintained or increased if it was not max. at 10 min, gradually decreased to complete recovery (100-178 min); smaller dose did not produce MR; diagram

Reference

Winger; Hursh; Casey; Woods

Journal of Pharmacology and Experimental Therapeutics, 2002 , vol. 301, # 2 p. 690 - 697 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

reinforcing

Species or TestSystem (Pharmacological Data)

rhesus monkey

Sex

male

Route of Application

intravenous

Concentration (Pharmacological Data)

0.003 - 0.03 mg/kg/injection

Kind of Dosing (Pharmacological Data)

title comp. dissolved in physiological saline and admin. in each session of 130 min

Method (Pharmacological Data)

monkeys individually housed in cages with response levers and stimulus lights; implanted with catheter; self-admin. title comp.; FR of title comp. availability varied from 1 to 1000; ROR, title comp. intake, normalized demand functions detd.

Further Details (Pharmacological Data)

normalized demand functions: Pmax (measure of the elasticity of demand), Omax; ROR: rates of responding; FR: fixed ratio

Results

title comp. maintained rapid peak ROR; ROR were slow at small FR, increased to max. as FR increased, declined with further increases in FR; title comp. intake (1.98 mg/kg) was highest at largest dose and smallest FR; Pmax: 231; Omax: 7261; diagrams

Reference

Winger; Hursh; Casey; Woods

Journal of Pharmacology and Experimental Therapeutics, 2002 , vol. 301, # 2 p. 690 - 697 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological

Wistar rat

Data)

28 of 90

29 of 90

Sex

male

Route of Application

subcutaneous

Kind of Dosing (Pharmacological Data)

dissolved in sterile water

Method (Pharmacological Data)

rats of 220-230 g housed in sawdust-lined cages with unrestricted access to rat chow and water; 12 h/12 h light/dark cycle; spontaneous tail-flicks (STFs) after 30 min of administration; MOE=max. observed effect; ANOVA

Type (Pharmacological Data)

Emin

Value of Type (Pharmacological Data)

5.0 mg/kg

Results

MOE 34.1/5 min

Reference

Millan, Mark J.; Audinot, Valerie; Honore, Prisca; Bervoets, Karin; Veiga, Sylvie; Brocco, Mauricette

European Journal of Pharmacology, 2000 , vol. 388, # 1 p. 37 - 47 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor; binding activity

Species or TestSystem (Pharmacological Data)

Wistar rat frontal cortex

Sex

male

Method (Pharmacological Data)

NMDA sites labeled with 3H-MK 801 (1 nM); incubation for 120 min at 22 deg C; ANOVA

Type (Pharmacological Data)

pIC50

Value of Type (Pharmacological Data)

7.38 dimensionless

Reference

Millan, Mark J.; Audinot, Valerie; Honore, Prisca; Bervoets, Karin; Veiga, Sylvie; Brocco, Mauricette

European Journal of Pharmacology, 2000 , vol. 388, # 1 p. 37 - 47 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)

5 mg/kg

Kind of Dosing (Pharmacological Data)

dissolved in saline; administered in volume 0.1 ml/100 g body weight

Method (Pharmacological Data)

rats i.p. injected with 5 - 25 mg/kg L-NAME or saline; after 15 min title comp. administered; behaviour observed for 1 h

Further Details (Pharmacological Data) Results

L-NAME: NG-nitro-L-arginine methyl ester

title comp. sign. increased locomotor activity and induced stereotyped behaviours consisting of head weaving, turning and backpedalling; effect was markedly potentiated by L-NAME

30 of 90

31 of 90

32 of 90

Reference

Bujas-Bobanovic, Maja; Robertson, Harold A; Dursun, Serdar M

European Journal of Pharmacology, 2000 , vol. 409, # 1 p. 57 - 65 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)

5 mg/kg

Kind of Dosing (Pharmacological Data)

dissolved in saline; administered in volume 0.1 ml/100 g body weight

Method (Pharmacological Data)

rats i.p. injected with 5 - 25 mg/kg L-NAME or saline; after 15 min title comp. administered; after 1 h brains removed, fixed and sectioned; c-fos expression in different brain regions analyzed by immunocytochemistry method using light microscope

Further Details (Pharmacological Data)

L-NAME: NG-nitro-L-arginine methyl ester

Results

title comp. induced differential c-fos expression in brain regions (maximum in cortical regions); effect was potentiated by L-NAME (increased expression in frontal, retrosplenial granular cortex, cerebellum, thalamic, subtalamic nuclei, caudate putamen)

Reference

Bujas-Bobanovic, Maja; Robertson, Harold A; Dursun, Serdar M

European Journal of Pharmacology, 2000 , vol. 409, # 1 p. 57 - 65 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

effect on behavior

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

1 - 10 mg/kg

Method (Pharmacological Data)

rats (250-300 g) received title comp.; motor activities monitored 30 min later for 60-min period

Further Details (Pharmacological Data)

measures of ambulations (pattern of beam breaks indicating that rat relocated its entire body), fine movements (nonambulatory beam breaks) and time at rest (total seconds in 60-min session in which no new beams broken, measured at 1-s intervals)

Results

title comp. evoked dose-dependent increases in ambulations, fine movements and reductions in time at rest; graphical representation

Reference

Cartmell, Jayne; Monn, James A.; Schoepp, Darryle D.

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 291, # 1 p. 161 - 170 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neurotoxicity

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

female

Route of Application

subcutaneous

Kind of Dosing

5.45 mg/day (5 days) with osmotic minipump

(Pharmacological Data)

33 of 90

34 of 90

Method (Pharmacological Data)

animals (280-320 g weigths) were sacrificed by decapitation 21 days (long-term study) or 24 hours (short-term study) after title comp. administration

Further Details (Pharmacological Data)

autoradiographic study with 3H-labeled flunitrazepam, quinuclidinyl benzilate, ketanserin, α-amino-3-hydroxy-5-methylisoxazole (AMPA), piperidyl-3,4-3H(N)-TCP and mazindol

Results

changes in brain regions binding (diagrams)

Reference

Ellison, Gaylord; Keys, Alan; Noguchi, Kevin

Pharmacology and Toxicology, 1999 , vol. 84, # 1 p. 9 - 17 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

Swiss-Webster mouse

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

1 - 10 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. was dissolved in distilled water or 0.9percent NaCl; administered in a volume of 0.01 ml/g

Method (Pharmacological Data)

mice admin. with title comp.; placed on wire mesh screen elevated above the ground; after slowly inverting the screen, mice tested during 2-min trial for their ability to climb to top; TD50 calculated

Further Details (Pharmacological Data)

TD50: dose of title comp. producing screen failure in 50percent of mice tested

Type (Pharmacological Data)

TD50

Value of Type (Pharmacological Data)

4.12 mg/kg

Reference

Witkin, Jeffrey M.; Gasior, Maciej; Heifets, Boris; Tortella, Frank C.

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 289, # 2 p. 703 - 711 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

anticonvulsant

Species or TestSystem (Pharmacological Data)

Swiss-Webster mouse

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

Ca. 1 - 20 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. was dissolved in distilled water or 0.9percent NaCl; administered in a volume of 0.01 ml/g

Method (Pharmacological Data)

mice admin. with title comp.; after 120 min, admin. with cocaine (75 mg/kg, i.p.); observed for 30 min, for the presence or absence of convulsions; ED50 value calculated

Type (Pharmacological Data)

ED50

Value of Type (Pharmacological Data)

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6.59 mg/kg

Reference

Witkin, Jeffrey M.; Gasior, Maciej; Heifets, Boris; Tortella, Frank C.

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 289, # 2 p. 703 - 711 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

cardiotoxic

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

10 mg/kg

Kind of Dosing (Pharmacological Data)

test comp. dissolv. in 0.1 N saline

Exposure Period (Pharmacological Data)

12 h

Method (Pharmacological Data)

in vivo; rats weigh. 200-250 g; sacrif.; hearts removed; cardiac sarcoplasmic reticulum fractions isol. from ventricles; Ca2+ ATPase activ.

Further Details (Pharmacological Data)

Ca2+ ATPase activ. determ. colorimetrically by maes. inorganic phosphate liberated from ATP hydrolysis

Results

Ca2+ ATPase activ. signif. and irreversibly reduced; rats showed classical circling behavior

Reference

Pande; Cameron; Vig; Desaiah

Toxicology, 1998 , vol. 129, # 2-3 p. 95 - 102 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

cardiotoxic

Endpoint of Effect (Pharmacological Data)

Ca2+ ATPase activity

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat sarcoplasmic reticulum

Concentration (Pharmacological Data)

25 - 100 μmol/l

Kind of Dosing (Pharmacological Data)

test comp. dissolv. in distilled water

Method (Pharmacological Data)

in vitro; cardiac sarcoplasmic reticulum fractions prepar. from normal hearts of rats weigh. 200-250 g; kinetic analysis

Further Details (Pharmacological Data)

Ca2+ ATPase activ. determ. colorimetrically by maes. inorganic phosphate liberated from ATP hydrolysis

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

100 μmol/l

Results Reference

Ca2+ ATPase activ. signif. reduced; Vmax= 11.6; Km= 0.41 mM Pande; Cameron; Vig; Desaiah

Toxicology, 1998 , vol. 129, # 2-3 p. 95 - 102 Title/Abstract Full Text View citing articles Show Details

37 of 90

38 of 90

39 of 90

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rats

Sex

male

Route of Application

intravenous

Concentration (Pharmacological Data)

1 mg/kg

Exposure Period (Pharmacological Data)

3 h

Method (Pharmacological Data)

adult rats cannuled (right external jugular vein or right femoral vein); title compd. administration, fluid loading (lactated Ringer's soln. or NaHCO3 soln.; urine collection, anal. (radioimmunoassay)

Results

urine flow rate evaluated (diagram)

Reference

Proksch, Joel W.; Gentry, W. Brooks; Owens, S. Michael

Journal of Pharmacology and Experimental Therapeutics, 1998 , vol. 287, # 2 p. 616 - 624 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

metabolic

Species or TestSystem (Pharmacological Data)

Bovine adrenal medullary cells

Concentration (Pharmacological Data)

300 nmol/l

Method (Pharmacological Data)

Cells isolated by collagenase digestion of slices of bovine adrenal medulla; cultured cells incubated (37 deg C, 30 min, pH 7.4) with <3H>NA in the presence or absence of the title comp.; the radioactivity in the solubilized cells counted by LSC

Further Details (Pharmacological Data)

Effect of the title comp. on desipramine-sensitive uptake of <3H>NA assessed; <3H>NA=<3H>noradrenaline (1-30 μmol/l); LSC=liquid scintillation counter

Results

The title comp. inhibited <3H>NA uptake; Eadie-Hofstee analysis of curves with or without title comp.; app. Michaelis constant Km=5.6 μmol/l (control 3.1 μmol/l); the max velocity Vmax=250 (vs. 292) pmol/4E6 cells/30 min; a mixed inhibition type

Reference

Hara, Koji; Yanagihara, Nobuyuki; Minami, Kouichiro; Ueno, Susumu; Toyohira, Yumiko; Sata, Takeyoshi; Kawamura, Masaru; Bruess, Michael; Boenisch, Heinz; Shigematsu, Akio; Izumi, Futoshi

Naunyn-Schmiedeberg's Archives of Pharmacology, 1998 , vol. 358, # 3 p. 328 - 333 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

secretion stimulant

Species or TestSystem (Pharmacological Data)

Wistar rats

Sex

male

Concentration (Pharmacological Data)

100 - 500 μmol/l

Method (Pharmacological Data)

rats (250-350 g) housed 3 or 4 per cage at 22 degC, food and water ad libitum; rats anesthetized, concentric dialysis probe implanted into left medial prefrontal cortex

Further Details (Pharmacological Data)

microdialysis; extracellular dopamine (DO) levels

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42 of 90

Results

ca. DO (100/500μM) percent of basal level at 0, 30, 60 and 90 min after local administration into medial prefrontal cortex: 100, 1000/3100, 500/2200, 100/400

Reference

Yonezawa, Yuji; Kuroki, Toshihide; Kawahara, Takeshi; Tashiro, Nobutada; Uchimura, Hideyuki

European Journal of Pharmacology, 1998 , vol. 341, # 1 p. 45 - 56 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

secretion inhibition

Species or TestSystem (Pharmacological Data)

Wistar rats

Sex

male

Concentration (Pharmacological Data)

100 - 500 μmol/l

Method (Pharmacological Data)

rats (250-350 g) housed 3 or 4 per cage at 22 degC, food and water ad libitum; rats anesthetized, concentric dialysis probe implanted into left medial prefrontal cortex

Further Details (Pharmacological Data)

microdialysis; extracellular γ-aminobutiric acid (GABA) levels

Results

ca. GABA (100/500μM) percent of basal level at 0, 20, 40 and 80 min after local administration into medial prefrontal cortex: 100, 87/87, 75/70, 78/68

Reference

Yonezawa, Yuji; Kuroki, Toshihide; Kawahara, Takeshi; Tashiro, Nobutada; Uchimura, Hideyuki

European Journal of Pharmacology, 1998 , vol. 341, # 1 p. 45 - 56 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

ddY mouse

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

2 - 8 mg/kg

Kind of Dosing (Pharmacological Data)

dissolved in saline

Method (Pharmacological Data)

mice pretreated with vehicle or title comp. (10 mg/kg s.c.) for 28 d; treatment with title comp. during 6 successive days; conditioned place preference test performed every day of treatment

Further Details (Pharmacological Data)

vehicle control; further studies using tyrosine hydroxylase inhibitor (AMPT), or dopaminergic neurotoxin (6-OHDA), or dopamine D1 or D2 receptor antagonists ((+)SCH-23390 and (-)sulpiride, respectively)

Results

in naive mice title comp. induced dose-dependent place aversion, but caused place preference in mice pretreated with title comp.; effect was attenuated by AMPT, 6-OHDA, or (+)SCH-23390, but not (-)sulpride (figure)

Reference

Noda, Yukihiro; Miyamoto, Yoshiaki; Mamiya, Takayoshi; Kamei, Hiroyuki; Furukawa, Hiroshi; Nabeshima, Toshitaka

Journal of Pharmacology and Experimental Therapeutics, 1998 , vol. 286, # 1 p. 44 - 51 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transmitter releasing

Species or TestSystem (Pharmacological Data)

ddY mouse

Sex

male

Route of Application

subcutaneous

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Concentration (Pharmacological Data)

8 mg/kg

Kind of Dosing (Pharmacological Data)

dissolved in saline

Method (Pharmacological Data)

mice were treated with title comp. during 6 successive days; contents of monoamines (NA, DA, and 5-HT) in prefrontal cortex and striatum were determined; HPLC with electrochemical detection

Further Details (Pharmacological Data)

vehicle control; NA: noradrenaline; DA: dopamine; 5-HT: serotonin

Comment (Pharmacological Data)

No effect

Reference

Noda, Yukihiro; Miyamoto, Yoshiaki; Mamiya, Takayoshi; Kamei, Hiroyuki; Furukawa, Hiroshi; Nabeshima, Toshitaka

Journal of Pharmacology and Experimental Therapeutics, 1998 , vol. 286, # 1 p. 44 - 51 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

ddY mouse

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

2 - 8 mg/kg

Kind of Dosing (Pharmacological Data)

dissolved in saline

Method (Pharmacological Data)

mice pretreated with vehicle or title comp. (10 mg/kg s.c.) for 28 d; treatment with title comp. during 6 successive days; conditioned place preference test performed every day of treatment

Further Details (Pharmacological Data)

vehicle control; further studies using 14-d administration of methamphetamine, or noradrenalinergic neurotoxin (DSP-4), or serotonin2 receptor antagonist (ritanserin)

Results

in naive mice title comp. induced dose-dependent place aversion, which was inhibited by ritanserin, or methamphetamine (8-d treatment) but not DSP-4; title comp. methamphetamine-independently caused place preference after pretreatment with title comp.

Reference

Noda, Yukihiro; Miyamoto, Yoshiaki; Mamiya, Takayoshi; Kamei, Hiroyuki; Furukawa, Hiroshi; Nabeshima, Toshitaka

Journal of Pharmacology and Experimental Therapeutics, 1998 , vol. 286, # 1 p. 44 - 51 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

Long-Evans rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

1 - 4 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. diluted in saline, injected (1 ml/kg) 15 min before session

Method (Pharmacological Data)

effect of pretreatment with title comp. on ethanol (10 percent) self-administration investigated under multiple schedule for alternating 5min periods of title comp. availability; 1-h daily session (12 5-min periods of liquid availability)

Further Details

control: saline; reference comp. for drinking: 0.1 percent saccharin

(Pharmacological Data)

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47 of 90

Results

pretreatment with title comp. at 4 mg/kg decreased ethanol and saccharin self-administration compared to control (figure)

Reference

Shelton, Keith L.; Balster, Robert L.

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 280, # 3 p. 1250 - 1260 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; inhib. of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

18 mg/kg

Kind of Dosing (Pharmacological Data)

dose per day

Method (Pharmacological Data)

adult animals infused with title comp. via osmotic pumps implanted on back for 1, 3, 10 or 20 d; livers collected 24 h postinfusion; microsomes obtained; CYP2C11 protein expression determined by Western blot analysis using anti-CYP2C11 antibody

Further Details (Pharmacological Data)

control: saline (infused for 3 or 20 d); CYP: cytochrome P450

Results

after 1- and 3-d infusions title comp. decreased amount of CYP2C11 protein to 61 percent and 46 percent, respectively, vs. 3-day salineinfused control (figure)

Reference

Shelnutt; Cornett; Owens, S. Michael

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 1 p. 574 - 581 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; inhib. of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

18 mg/kg

Kind of Dosing (Pharmacological Data)

dose per day

Method (Pharmacological Data)

adult animals infused with title comp. via osmotic pumps implanted on back for 1, 3, 10 or 20 d; livers collected 24 h postinfusion; microsomes obtained; total CYP content determined

Further Details (Pharmacological Data)

control: saline (infused for 3 or 20 d); CYP: cytochrome P450

Results

title comp. significantly decreased total CYP content for 1-, 3- and 10-d infused animals (figure, table)

Reference

Shelnutt; Cornett; Owens, S. Michael

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 1 p. 574 - 581 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; inhib. of

Species or TestSystem

Sprague-Dawley rat

(Pharmacological Data)

48 of 90

49 of 90

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

18 mg/kg

Kind of Dosing (Pharmacological Data)

dose per day

Method (Pharmacological Data)

adult animals infused with title comp. for 1, 3, 10 or 20 d; livers collected; microsomes obtained and incubated with testosterone; changes in CYP2C11 function determined by measuring 2α-OH testosterone metabolites using TLC

Further Details (Pharmacological Data)

control: saline (infused for 3 or 20 d); TLC: thin-layer chromatography; CYP: cytochrome P450; 2α-OH: 4-androsten-2α,17β-diol-3-one

Results

title comp. significantly decreased CYP2C11 function to 46, 28, and 45 percent of control for 1-, 3- and 10-d infused animals (figure)

Reference

Shelnutt; Cornett; Owens, S. Michael

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 1 p. 574 - 581 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; inhib. of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

18 mg/kg

Kind of Dosing (Pharmacological Data)

dose per day

Method (Pharmacological Data)

adult animals infused with title comp. for 1, 3, 10 or 20 d; livers collected; microsomes obtained and incubated with testosterone; changes in CYP3A2 function determined by measuring 6α-OH testosterone metabolites using TLC

Further Details (Pharmacological Data)

control: saline (infused for 3 or 20 d); TLC: thin-layer chromatography; CYP: cytochrome P450; 6α-OH: 4-androsten-6α,17β-diol-3-one

Results

after 3-d title comp. infusion CYP3A2 function appeared almost nonexistent (figure)

Reference

Shelnutt; Cornett; Owens, S. Michael

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 1 p. 574 - 581 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

mRNA expression; reduction of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

18 mg/kg

Kind of Dosing (Pharmacological Data)

dose per day

Method

adult animals infused with title comp. for 1, 3, 10 or 20 d; livers collected 24 h postinfusion; total cellular RNA isolated and subjected to

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51 of 90

(Pharmacological Data)

both Northern and slot blot analysis; CYP2C11 mRNA levels determined

Further Details (Pharmacological Data)

control: saline (infused for 3 or 20 d); CYP: cytochrome P450

Results

steady-state levels of hepatic CYP2C11 mRNA were significantly reduced to 43.3, 30.6, 36.8, and 47.4 of control values in animals given 1-, 3-, 10- or 20-d title comp. infusion, respectively (figure)

Reference

Shelnutt; Cornett; Owens, S. Michael

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 1 p. 574 - 581 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

hormone release; inhibition of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

18 mg/kg

Kind of Dosing (Pharmacological Data)

dose per day

Method (Pharmacological Data)

adult animals infused with title comp. for 1, 3, 10 or 20 d; sera collected 24 h postinfusion; changes in testosterone and T3 concentrations determined using testosterone RIA kit and total T3 Coat-a-Count RIA kit, respectively

Further Details (Pharmacological Data)

control: saline (infused for 3 or 20 d); T3: triiodothyronine

Comment (Pharmacological Data)

No effect

Reference

Shelnutt; Cornett; Owens, S. Michael

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 1 p. 574 - 581 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

biotransformation

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

18 mg/kg

Kind of Dosing (Pharmacological Data)

dose per day

Method (Pharmacological Data)

adult animals infused with title comp. for 1, 3, 10 or 20 d; livers collected 24 h postinfusion; microsomes obtained and incubated with unlabeled and <3H>labeled title comp. for 20 min; formation of metabolite-protein adducts quantified

Further Details (Pharmacological Data)

control: saline (infused for 3 or 20 d)

Results

formation of reactive title comp. metabolite was significantly decreased to 36 percent and 41 percent in 1- and 3-d title comp.-infused animals vs. 3-d saline-infused control (figure)

Reference

Shelnutt; Cornett; Owens, S. Michael

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 1 p. 574 - 581 Title/Abstract Full Text View citing articles Show Details

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53 of 90

54 of 90

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

baboon

Sex

male

Route of Application

peroral

Concentration (Pharmacological Data)

0.32 - 10 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. blended for 3 min into a volume of 60 ml of a matrix prepared with 1-2 g/l of BIO-Serv Agent K in distilled water flavored with orange-drink powder (52 g/l)

Method (Pharmacological Data)

four of six baboons trained to discriminate lorazepam (1.8 mg/kg, p.o.); treated with title comp. or vehicle (quinine SO4); post 30 min lever responses counted; generalization and drug-discrimination performance determined

Further Details (Pharmacological Data)

control: without title comp.; baboons: LE, ML, MS, RA, RF (Papio anubis) and LO (Papio cynocephalus); generalization: peak mean percentage of lorazepam-lever responding by 80 percent or more

Comment (Pharmacological Data)

No effect

Reference

Ator, Nancy A.; Griffiths, Roland R.

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 282, # 3 p. 1442 - 1457 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)

0.3 - 3 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline and admin. in a volume of 1 ml/kg

Method (Pharmacological Data)

rats trained under the temporal response differentiation (TRD) 1-1.3 sec schedule; title comp. admin.; after 10 min, effect on number of responses emitted and interresponse times (IRTs) collected as performance indicators during every session

Further Details (Pharmacological Data)

control: saline; illumination of house light in ceiling, stimulus light above the right lever, signaled the beginning of the sessions; RF: relative frequency; SR: shorter response; CSC: cumulative curve slope; DEC: dose-effect curve; NR: nonreinforced

Results

distributions shifted to left (L) with SR durations occurred at 0.3 mg/kg (increased with dose); at 3.0 mg/kg, increased in RF across all NR to L of reinforcer (decreased in CSC); large shift to L between 1.7, 3.0 mg/kg corresponding with DEC; diagram

Reference

Mcclure; Wenger; Mcmillan

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 3 p. 1357 - 1367 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

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Concentration (Pharmacological Data)

0.3 - 3 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline and admin. in a volume of 1 ml/kg

Method (Pharmacological Data)

rats trained under the temporal response differentiation (TRD) 4-5.2 sec schedule; title comp. admin.; after 10 min, effect on number of responses emitted and interresponse times (IRTs) collected as performance indicators during every session

Further Details (Pharmacological Data)

control: saline; illumination of house light in ceiling, stimulus light above the right lever, signaled the beginning of the sessions; RF: relative frequency; SDR: shorter-duration response; RDD: response-duration distribution

Results

CFC showed an increased shift to left with increasing doses; RF of the RDD was an increased in SDR with bimodal pattern starting at 1.0 mg/kg; at highest doses, the curve shifted far to left and frequency of short-response durations; diagram

Reference

Mcclure; Wenger; Mcmillan

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 3 p. 1357 - 1367 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)

0.3 - 3 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline and admin. in a volume of 1 ml/kg

Method (Pharmacological Data)

rats trained under the temporal response differentiation (TRD) 10-13 sec schedule; title comp. admin.; after 10 min, effect on number of responses emitted and interresponse times (IRTs) collected as performance indicators during every session

Further Details (Pharmacological Data)

control: saline; illumination of house light in ceiling, stimulus light above the right lever, signaled the beginning of the sessions; CFC: cumulative frequency curve

Results

title comp. at low doses (1.0 and 1.7 mg/kg) showed CFC shifted to left; at highest dose, few response durations long enough to be reinforced; diagram

Reference

Mcclure; Wenger; Mcmillan

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 3 p. 1357 - 1367 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)

0.3 - 3 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline and admin. in a volume of 1 ml/kg

Method (Pharmacological Data)

rats trained under the temporal response differentiation (TRD) 1-1.3 sec schedule; title comp. admin.; after 10 min, effect on accuracy, mean interresponse time and response rate studied

Further Details (Pharmacological Data)

control: saline; MRD: mean response duration; AC: accuracy

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Results

title comp. decreased AC and MRD with increasing dose; at 1.00 and 1.70 mg/kg signif. increased response rates at low doses; table

Reference

Mcclure; Wenger; Mcmillan

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 3 p. 1357 - 1367 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)

0.3 - 3 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline and admin. in a volume of 1 ml/kg

Method (Pharmacological Data)

rats trained under the temporal response differentiation (TRD) 4-5.2 sec schedule; title comp. admin.; after 10 min, effect on accuracy, mean interresponse time and response rate studied

Further Details (Pharmacological Data)

control: saline; MRD: mean response duration; AC: accuracy

Results

title comp. decreased AC and MRD with dose; decreased the response rate only at highest dose; table

Reference

Mcclure; Wenger; Mcmillan

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 3 p. 1357 - 1367 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)

0.3 - 3 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline and admin. in a volume of 1 ml/kg

Method (Pharmacological Data)

rats trained under the temporal response differentiation (TRD) 10-13 sec schedule; title comp. admin.; after 10 min, effect on accuracy, mean interresponse time and response rate studied

Further Details (Pharmacological Data)

control: saline; MRD: mean response duration; AC: accuracy

Results

title comp. decreased AC and MRD with increasing dose; decreased response rates only at highest dose; table

Reference

Mcclure; Wenger; Mcmillan

Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 281, # 3 p. 1357 - 1367 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rats

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Sex

male

Route of Application

intravenous

Concentration (Pharmacological Data)

1 mg/kg

Method (Pharmacological Data)

adult animals (350-400 g) administered in right jugular vein; 5 min after addition of title comp. antigen binding fragment of IgG (Fab) (human or anti-PCP in 0.3, 1.0, 3-0 times of title comp.)

Further Details (Pharmacological Data)

behavioral studies in plastic cage monitoring by cameras: locomotor activity (headweaving, circling) and ataxia (in 0-4 scale) determined

Results

addition of title comp. increases locomotor activity and ataxia; anti-PCP Fab reversed title-comp. induced behaviors

Reference

Valentine, John L.; Mayersohn, Michael; Wessinger, William D.; Arnold, Larry W.; Owens, S. Michael

Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 278, # 2 p. 709 - 716 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

pharmacokinetics

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rats

Sex

male

Route of Application

intravenous

Concentration (Pharmacological Data)

1 mg/kg

Method (Pharmacological Data)

animals cannulated in jugular vein; 2 h after title comp. administration anti-PCP Fab added; title comp. serum protein binding determind by equilibrium dialysis; conc. of title comp. determined by radioimmunoassay

Further Details (Pharmacological Data)

pharmacokinetic data analysis by model-independent methods

Results

pharmacokinetic parameters given; decrease in brain 23 percent, fat 24 percent, heart 52 percent, lung 74 percent, testis 12 percent of controls, increase in liver 137 percent of controls

Reference

Valentine, John L.; Owens, S. Michael

Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 278, # 2 p. 717 - 724 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

drug interaction

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

1 mg/kg

Method (Pharmacological Data)

250 g rats (T=21 deg C; 12 h light/dark cycle); 30 min after title comp. 2.5 mg/kg i.p. m-chlorophenylpiperazine (mCPP) inj.; 24 h later challenged with 2.5 mg/kg i.p. mCPP; 30 min later sacrificed

Further Details (Pharmacological Data)

trunk blood collected; plasma adrenocorticotropic hormone (ACTH) measured with radioimmunoassay; title comp. effect on tolerance to mCPP's stimulation of ACTH studied (diagram)

Comment (Pharmacological Data)

No effect

Reference

Mazzola-Pomietto, Pascale; Aulakh, Charanjit S.; Murphy, Dennis L.

European Journal of Pharmacology, 1996 , vol. 308, # 3 p. 329 - 333 Title/Abstract Full Text View citing articles Show Details

62 of 90

63 of 90

64 of 90

Effect (Pharmacological Data)

drug discrimination

Species or TestSystem (Pharmacological Data)

White Carneaux pigeons

Sex

male

Concentration (Pharmacological Data)

0.3 - 3 mg/kg

Method (Pharmacological Data)

in vivo; pigeons (414-500 g) trained to discriminate saline from pentobarbital, morphine, d-amphetamine, then pentobarbital from damphetamine or morphine, then saline and pentobarbital keys reversed; three-key pigeon chamber

Further Details (Pharmacological Data)

compounds were injected; for discrimination 5 mg/kg title comp., 7 mg/kg morphine, 1.8 mg/kg d-amphetamine used; dose-response curve given

Results

percentage of responses: 0.3 mg/kg, 10 percent, n.g., 100 percent; 0.5 mg/kg, 12 percent, 32 percent, 55 percent; 1 mg/kg, 28 percent, 15 percent, 50 percent; 2 mg/kg, 50 percent, n.g., 10 percent; 3 mg/kg, n.g., 10 percent, n.g., pentobarbital vs. d-amphetamine or morphine, reversed keys, resp.

Reference

McMillan; Sun; Hardwick

Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 278, # 1 p. 50 - 61 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

drug discrimination

Species or TestSystem (Pharmacological Data)

White Carneaux pigeons

Sex

male

Concentration (Pharmacological Data)

0.1 - 2 mg/kg

Method (Pharmacological Data)

in vivo; pigeons (414-500 g) trained to discriminate saline from pentobarbital, then from morphine or d-amphetamine; three-key pigeon chamber

Further Details (Pharmacological Data)

compounds were injected; for discrimination 5 mg/kg pentobarbital, 7 mg/kg morphine, 1.8 mg/kg d-amphetamine used; dose-response curve given

Results

percentage of responses: 0.1 mg/kg, 0 percent, n.g., n.g. ; 0.3 mg/kg, 35 percent, 5 percent, 10 percent; 0.5 mg/ml, n.g., n.g., 50 percent; 1 mg/kg, n.g., 50 percent, 70 percent; 2 mg/kg, n.g., 75 percent, n.g., after establishing discrimination with pentobarbital, morphine, d-amphetamine, resp.

Reference

McMillan; Sun; Hardwick

Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 278, # 1 p. 50 - 61 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

drug discrimination

Species or TestSystem (Pharmacological Data)

White Carneaux pigeons

Sex

male

Concentration (Pharmacological Data)

0.1 - 2 mg/kg

Method (Pharmacological Data)

in vivo; pigeons (414-500 g) trained to discriminate saline from pentobarbital, then from morphine and finally d-amphetamine, or damphetamine and finally morphine; three-key pigeon chamber

Further Details (Pharmacological Data)

compounds were injected; for discrimination 5 mg/kg title comp., 7 mg/kg morphine, 1.8 mg/kg d-amphetamine used; dose-response curve given

Results

percentage of responses: 0.1 mg/kg, n.g., 0 percent; 0.3 mg/kg, 1 percent, 30 percent; 0.5 mg/kg, 5 percent, 35 percent; 1 mg/kg, 65 percent, 15 percent; 2 mg/kg, 65 percent, n.g., morphine - d-amphetamine, d-amphetamine - morphine, resp.

65 of 90

66 of 90

67 of 90

Reference

McMillan; Sun; Hardwick

Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 278, # 1 p. 50 - 61 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)

2 - 8 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline

Method (Pharmacological Data)

rats received title comp.; place conditioning test, including pre-conditioning test, conditioning and post-conditioning test was performed

Further Details (Pharmacological Data)

saline control

Results

title comp. produced place aversion in dose-dependent manner

Reference

Kitaichi, Kiyoyuki; Noda, Yukihiro; Hasegawa, Takaaki; Furukawa, Hiroshi; Nabeshima, Toshitaka

European Journal of Pharmacology, 1996 , vol. 318, # 1 p. 7 - 9 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)

2 - 8 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline

Method (Pharmacological Data)

rats pretreated with title comp. (10 mg/kg) for 14 or 28 days, then rats received title comp.; place conditioning test, including preconditioning test, conditioning and post-conditioning test was performed

Further Details (Pharmacological Data)

saline control

Results

in rats pretreated for 14 days, title comp. produced neither place preference nor place aversion but in rats pretreated for 28 days, title comp. at dose 4 and 8 mg/kg induced place preference in dose-dependent manner

Reference

Kitaichi, Kiyoyuki; Noda, Yukihiro; Hasegawa, Takaaki; Furukawa, Hiroshi; Nabeshima, Toshitaka

European Journal of Pharmacology, 1996 , vol. 318, # 1 p. 7 - 9 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

male

68 of 90

69 of 90

70 of 90

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

7.5 mg/kg

Kind of Dosing (Pharmacological Data)

dissolved in saline

Method (Pharmacological Data)

immediately after injection of title comp. stereotyped head-weaving behavior was observed for 45 min; number of times the rats made slow, side-to-side head movements determined

Further Details (Pharmacological Data)

reference comp.: selective title comp. binding site ligand dizocilpine; further investigations with selective σ1 receptor ligand, prototype σ receptor ligand, and σ1/σ1 receptor ligands

Results

title comp. induced head-weaving behavior; title comp. binding sites and σ receptors were involved

Reference

Kitaichi, Kiyoyuki; Noda, Yukihiro; Hasegawa, Takaaki; Furukawa, Hiroshi; Nabeshima, Toshitaka

European Journal of Pharmacology, 1996 , vol. 318, # 2-3 p. 205 - 211 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

affinity for the 1-(1-phenylcyclohexyl)piperidine (phencyclidine) receptor (IC50 = 36.9 nM) and for the dopamine transporter (IC50 = 7600 nM) on the rat brain

Reference

Coderc, E.; Cerruti, P.; Vignon, J.; Rouayrenc, J. F.; Kamenka, J. M.

European Journal of Medicinal Chemistry, 1995 , vol. 30, # 6 p. 463 - 470 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

psychotomimetic

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rats

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

5 - 15 mg/kg

Method (Pharmacological Data)

multiple administr. (6 times) of various doses at 6 h intervals, rats killed 18 h after final administr.; time-dependent response to single 15 mg/kg dose of animals killed 6, 12 or 24 h later

Further Details (Pharmacological Data)

animals killed 10, 18, 34 or 54 h after treatment; striatal neurotensin-like immunoreactivity (NTLI) content detn. by radioimmunoassay, comparing bound to free (125)iod-labeled peptide in each sample (extracellular dopamine conc.)

Results

striatal levels of NTLI signific. elevated in dose-dependent manner; not signific. altered after any of time points when animals recived single dose; significant increases in NTLI conc. at 10, 18, and 34 h after multiple dose treatment

Reference

Hanson; Midgley; Bush; Gibb

European Journal of Pharmacology, 1995 , vol. 278, # 2 p. 167 - 173 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

psychotomimetic

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rats

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

15 mg/kg

Method (Pharmacological Data)

multiple doses (5 doses); 18 h after animals killed; striatal neurotensin-like immunoreactivity (NTLI) content measured by radioimmunoassay, in nucleus accumbens, frontal cortex and substantia nigra

71 of 90

72 of 90

73 of 90

Results

title comp. increased NTLI conc. in accumbens in similar manner than in striatum; frontal cortex NTLI content decreased to 40 percent of the control; NTIL content of the substantia nigra assessed (similar than in control)

Reference

Hanson; Midgley; Bush; Gibb

European Journal of Pharmacology, 1995 , vol. 278, # 2 p. 167 - 173 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

psychotomimetic

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rats

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

15 mg/kg

Method (Pharmacological Data)

title comp. in combination with 80 mg/kg sulpiride (dopamin D2 antagonist)

Further Details (Pharmacological Data)

striatal neurotensin-like immunoreactivity (NTLI) content detn. by radioimmunoassay, comparing bound to free (125)iod-labeled peptide in each sample (extracellular dopamine conc.)

Results

combination treatment increased striatal NTLI conc. to 444 percent of control compared to increse of 165 percent and 287 percent of control (title comp. and sulpiridine)

Reference

Hanson; Midgley; Bush; Gibb

European Journal of Pharmacology, 1995 , vol. 278, # 2 p. 167 - 173 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)

10 mg/kg

Exposure Period (Pharmacological Data)

14 w

Method (Pharmacological Data)

200-300 g rats; T:22-24 deg C; RH:55 percent; 12 h light:dark cycle; 24 h after last dose 10 mg/kg i.p. title comp. given; behavior observed for 90 min postinjection

Further Details (Pharmacological Data)

motility (locomotor activity, L) measured with IR sensors; stereotyped behaviors (SB) observed: rearing (R), sniffing (S), head-waving (W), head-twitch (H), backpedalling (B), turning (T)

Results

supersensitivity to title comp.-induced hyperlocomotion, R, S; tolerance shown by diminished W, H, B, T

Reference

Kitaichi, Kiyoyuki; Yamada, Kiyofumi; Yoneda, Yukio; Ogita, Kiyokazu; Hasegawa, Takaaki; et al.

Life Sciences, 1995 , vol. 56, # 7 p. 531 - 544 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

receptor blocking agent

Species or TestSystem (Pharmacological Data)

brain from Wistar rat

Sex

male

Route of

intraperitoneal

Application

74 of 90

75 of 90

Concentration (Pharmacological Data)

10 mg/kg

Exposure Period (Pharmacological Data)

14 w

Method (Pharmacological Data)

24 h after treament, 250-300 g rats sacrificed, brains dissected; <3H>MK-801 binding to discrete areas measured with reported method <J.Pharmacol.Exp.Ther.259,86-96(91)>

Further Details (Pharmacological Data)

title comp. effect on profile of <3H>MK-801 binding in rat brain studied

Comment (Pharmacological Data)

No effect

Reference

Kitaichi, Kiyoyuki; Yamada, Kiyofumi; Yoneda, Yukio; Ogita, Kiyokazu; Hasegawa, Takaaki; et al.

Life Sciences, 1995 , vol. 56, # 7 p. 531 - 544 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

behavioural symptoms

Species or TestSystem (Pharmacological Data)

ddY mice

Sex

male

Route of Application

subcutaneous

Concentration (Pharmacological Data)

1 - 10 mg/kg

Method (Pharmacological Data)

animmals were placed individually in transparent cages immediately after title comp. treatment, 30 min later degree of sniffing, head movement and ataxia was assessed over a 3 min observation period, locomotor count was recorded over a 30 min period

Results

title comp. induced hyperlocomotion and stereotyped behaviors dose dependently, including sniffing, head movement, and ataxia, also caused marked deficit of motor coordination; diagrams are given

Reference

Noda; Yamada; Furukawa; Nabeshima

European Journal of Pharmacology, 1995 , vol. 286, # 3 p. 291 - 297 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

cocaine-like discriminative stimulant

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

Ca. 1 - 6 mg/kg

Method (Pharmacological Data)

rats trained to discriminate either a low (2 mg/kg) or a high (10 mg/kg) dose of cocaine from saline

Further Details (Pharmacological Data)

dose reduced cocaine-appropriate response rate by 50 percent: 1.9 and 3.6 mg/kg (under low and high training dose, resp.)

Type (Pharmacological Data)

ED50

Value of Type (Pharmacological Data)

2.1 mg/kg

76 of 90

77 of 90

Results

cocaine-appropriate responses in the majority of subjects under the low-dose training cond. but little effect under the high-dose training cond.; signif. reduced response rates

Reference

Kantak; Edwards; Spealman

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 274, # 2 p. 657 - 665 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

anxiolytic

Species or TestSystem (Pharmacological Data)

Wistar rats

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

1 - 6 mg/kg

Exposure Period (Pharmacological Data)

15 min

Method (Pharmacological Data)

drug discrimination experiments; operant chambers with two response levers; training and testing procedures; learning that pressing any of the two levers producing food; PTZ (17.5 mg/kg i.p.); drug lever and no drug lever assigned

Type (Pharmacological Data)

ED50

Value of Type (Pharmacological Data)

2.83 mg/kg

Results

title compd. partly reversed PTZ appropriate responding to a max. of 47 percent at 3.0 mg/kg

Reference

Swedberg; Jacobsen; Honore

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 274, # 3 p. 1113 - 1121 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

anticonvulsant

Species or TestSystem (Pharmacological Data)

DBA/2 mice

Sex

not specified

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

3 - 30 mg/kg

Exposure Period (Pharmacological Data)

30 min

Method (Pharmacological Data)

motoring impairment test; mice trained for 2 min to keep on top of rotating rod (6 rpm) as the rod rotated toward with animal; title compd. added; mice placed on the ratating rod at the appropriate intervals

Further Details (Pharmacological Data)

animals observed for 2 min; mice fell off twice or more was considered ataxic

Type (Pharmacological Data)

ED50

Value of Type (Pharmacological Data)

3.51 - 5.72 mg/kg

Results

title compd. produced motoring impairment

Reference

Swedberg; Jacobsen; Honore

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 274, # 3 p. 1113 - 1121

Title/Abstract Full Text View citing articles Show Details

78 of 90

79 of 90

80 of 90

Effect (Pharmacological Data)

anticonvulsant

Species or TestSystem (Pharmacological Data)

NMRI mice

Sex

male and female

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

3 - 30 mg/kg

Exposure Period (Pharmacological Data)

30 min

Method (Pharmacological Data)

methyl-6,7-dimethoxy-4-ethyl-β-carboline-3-carboxylate (DMCM) (15 mg/kg i.p.) administered at 30 min after adding of title compd.; mice failing to exhibit clonic seizures were considered protected

Results

title compd. produced a partial effect against DMCM-induced seizures with a max. protection of 40 percent at 10 and 30 mg/kg

Reference

Swedberg; Jacobsen; Honore

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 274, # 3 p. 1113 - 1121 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

anticonvulsant

Species or TestSystem (Pharmacological Data)

DBA/2 mice

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

0.3 - 3 mg/kg

Exposure Period (Pharmacological Data)

30 min

Method (Pharmacological Data)

title compd. administered at given time before testing; testing chamber with 4 loudspeakers; mice exposed to a 14-kHz tone at 111 Db for 30 s; audiogenic seizures; mice failing to exhibit clonic seizures were considered protected

Type (Pharmacological Data)

ED50

Value of Type (Pharmacological Data)

0.91 - 1.84 mg/kg

Results

title compd. provided a dose-depending increase in protection against audiogenic seizures

Reference

Swedberg; Jacobsen; Honore

Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 274, # 3 p. 1113 - 1121 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

anxiolytic

Species or TestSystem (Pharmacological Data)

naive ICR mice

Sex

male

Route of Application

intraperitoneal

81 of 90

82 of 90

83 of 90

84 of 90

85 of 90

86 of 90

87 of 90

88 of 90

Concentration (Pharmacological Data)

1 - 5.6 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline; injection volume: 10 ml/kg

Method (Pharmacological Data)

mice weight 15-20 g; elevated plus-maze with 2 open and 2 closed arms; 5-min test; dose 4-8 mice; observer and video; pre-session injection time: 10 min; title comp. - site-selective NMDA receptor antagonist

Further Details (Pharmacological Data)

number of open arm entries; time spent in each type of arm; untreated control

Results

title comp. increased number of open arm entries (diagram, table) - potential anxiolytic agent

Reference

Wiley; Cristello; Balster

European Journal of Pharmacology, 1995 , vol. 294, # 1 p. 101 - 107 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

LD50 = 87.9 mg/kg (mice)

Reference

Ferle-Vidovic, A; Kastelan, M; Petrovic, D; Suman, L; Kaselj, M; et al.

European Journal of Medicinal Chemistry, 1993 , vol. 28, # 3 p. 243 - 250 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

effect on the proliferative and reproductive ability of a human tumor cel strain - human cervical carcinoma (HeLa) cells and nonmalignant mouse (L929) and hamster (V79) fibroblasts in vitro; in vivo anesthetic effect: ED50 = 0.270 mmol/kg (mice)

Reference

Ferle-Vidovic, A; Kastelan, M; Petrovic, D; Suman, L; Kaselj, M; et al.

European Journal of Medicinal Chemistry, 1993 , vol. 28, # 3 p. 243 - 250 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

in vitro affinity for the PCP (1-(1-phenylcyclohexyl)piperidine) binding site, Ki (nM): 53; in vivo ataxic effect on the rotarod assay in mice (20-28 g weight), ED50 = 4.0

Reference

Iorio, Maria A.; Tomassini, Lamberto; Mattson, Mariena V.; George, Clifford; Jacobson, Arthur E.

Journal of Medicinal Chemistry, 1991 , vol. 34, # 8 p. 2615 - 2623 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

acute toxicity for cats at 3.0 mg/kg (i.v.)

Reference

Lal; Krutak-Krol; Domino

Arzneimittel-Forschung/Drug Research, 1986 , vol. 36, # 7 p. 1075 - 1078 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

severe inhibiion of respiration, but cough can still be elicited (0.32 mg/kg i.a.); both cough and respiration are supressed for several hours by 1.0 mg/kg (i.v.) in anesthetized decerebrate cats with direct electrical stimulation of cough-center

Reference

Lal; Krutak-Krol; Domino

Arzneimittel-Forschung/Drug Research, 1986 , vol. 36, # 7 p. 1075 - 1078 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

effect on the EEG (rabbit); LD 50 (acute, i.p.): 63.5 mg/kg (mouse)

Reference

Iorio; Molinari; Scotti de Carolis; Niglio

Farmaco, Edizione Scientifica, 1984 , vol. 39, # 7 p. 599 - 611 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

serum level (rhesus monkey)

Reference

Stavchansky; Loper

Journal of pharmaceutical sciences, 1982 , vol. 71, # 2 p. 194 - 196 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

great increase in locomotor activity (male mice)

Reference

Baker; Wohlford; Bradbury; Wirth

Journal of Medicinal Chemistry, 1981 , vol. 24, # 6 p. 666 - 669 Title/Abstract Full Text View citing articles Show Details

89 of 90

90 of 90

Comment (Pharmacological Data)

in vitro (rat brain) relative to PCP binding affinity; in vitro (rats) relative binding potency (discriminative stimulus test)

Reference

McQuinn; Cone; Shannon; Su

Journal of Medicinal Chemistry, 1981 , vol. 24, # 12 p. 1429 - 1432 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

anelgesic activity in the mouse writhing test, ED50 (mg/kg sc): 2.8; relative potency in activity cage (hyperactivity in mice)

Reference

Itzhak, Yossef; Kalir, Asher; Weissman, Ben Avi; Cohen, Sasson

Journal of Medicinal Chemistry, 1981 , vol. 24, # 5 p. 496 - 499 Title/Abstract Full Text View citing articles Show Details

Ecotoxicology (1) 1 of 1

Effect (Ecotoxicology)

toxicity to birds

Species or TestSystem (Ecotoxicology)

avian species

Route of Application

peroral

Method (Ecotoxicology)

number of species - 14; acute toxicity values obtained from published and unpublished studies from the Denver Wildlife Research Center, and from RTECS database; data restricted to oral exposure; simple linear regression model

Type (Ecotoxicology)

allometric scaling factor

Value of Type (Ecotoxicology)

1.133 dimensionless

Reference

Sample; Arenal

Bulletin of Environmental Contamination and Toxicology, 1999 , vol. 62, # 6 p. 653 - 663 Title/Abstract Full Text View citing articles Show Details

Reaxys Registry Number: 24868477

Molecular Formula: CH3I*C17H25N Linear Structure Formula: CH3I*C17H25N Molecular Weight: 385.332

InChI Key: GEPJDJHSHHEHLE-UHFFFAOYSA-N

no reactions.

Bioactivity (1)

no reactions.

Bioactivity (1)

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Bioactivity Pharmacological Data (1) 1 of 1

Comment (Pharmacological Data)

Bioactivities present

Reference

Kalir; Edery; Pelah; Balderman; Porath

Journal of medicinal chemistry, 1969 , vol. 12, # 3 p. 473 - 477 Title/Abstract Full Text View citing articles Show Details

Reaxys Registry Number: 25654511

Molecular Formula: C17H25NO2*C17H25N*ClH Linear Structure Formula: C17H25NO2*C17H25N*ClH Molecular Weight: 555.244

InChI Key: WFEMOAGNXOOTNF-UHFFFAOYSA-N

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Bioactivity Pharmacological Data (1) 1 of 1

Comment (Pharmacological Data)

Bioactivities present

Reference

Baker; Wohlford; Bradbury; Wirth

Journal of Medicinal Chemistry, 1981 , vol. 24, # 6 p. 666 - 669 Title/Abstract Full Text View citing articles Show Details

Reaxys Registry Number: 25654512

Molecular Formula: C17H25N*C18H27NO2*ClH Linear Structure Formula: C17H25N*C18H27NO2*ClH Molecular Weight: 569.271

InChI Key: LFZRPUVYAAIDDE-UHFFFAOYSA-N

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Bioactivity Pharmacological Data (1) 1 of 1

Comment (Pharmacological Data)

Bioactivities present

Reference

Baker; Wohlford; Bradbury; Wirth

Journal of Medicinal Chemistry, 1981 , vol. 24, # 6 p. 666 - 669 Title/Abstract Full Text View citing articles Show Details

no reactions.

Bioactivity (1)