WAY-100635 has high selectivity for serotonin 5-HT1A versus dopamine D4 receptors

被引：39

作者：

Martel, Jean-Claude

Leduc, Nathalie

Ormiere, Anne-Marie

Faucillon, Valerie

Danty, Nathalie

Culie, Charlene

Cussac, Didier

Newman-Tancredi, Adrian

机构：

[1] Ctr Rech Pierre Fabre, Div Neurobiol 2, F-81106 Castres, France

[2] Ctr Rech Pierre Fabre, Dept Cellular & Mol Biol, F-81106 Castres, France

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 2007年 / 574卷 / 01期

关键词：

WAY-100635; serotonin 5-HT1A receptor; dopamine D-4 receptor;

D O I：

10.1016/j.ejphar.2007.07.015

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The serotonin 5-HT1A receptor antagonist WAY-100635 was recently reported to have potent agonist properties at dopamine D-4 receptors (Chernel et al., 2006, Psychopharmacology 188,244-251.). Herein WAY-100635 (pK(i) at human(h) serotonin 5-HT1A receptors=9.5l;pK(i) at dopaminc hD(4.4) receptors=7.42) stimulated [S-35]GTP-gamma S incorporation in membranes of Chinese Hamster Ovary cells expressing dopamine hD4.4 receptors with only moderate potency and modest efficacy (pEC(50) = 6.63; Emax = 19% of dopamine). Moreover, in antagonism experiments, WAY-100635 had a much lower potency at dopamine hD4.4 receptors (pK(B) = 7.09), than at serotonin h5-HT1A receptors (pK(B) = 9.47). These data demonstrate that WAY-100635 has high selectivity for serotonin h5-HT1A versus doparnine hD(4.4) receptors. (C) 2007 Elsevier B.V. All rights reserved.

引用

页码：15 / 19

页数：5

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