Clozapine is a partial agonist at cloned, human serotonin 5-HT1A receptors

被引：104

作者：

NewmanTancredi, A

Chaput, C

Verriele, L

Millan, MJ

机构：

[1] Department of Psychopharmacology, Institut de Recherches Servier, 78290 Croissysur-Seine, Paris

来源：

NEUROPHARMACOLOGY | 1996年 / 35卷 / 01期

关键词：

clozapine; WAY; 100635; 5-HT1A receptor; G-protein; S-35]GTP gamma S; haloperidol;

D O I：

10.1016/0028-3908(95)00170-0

中图分类号：

Q189 [神经科学];

学科分类号：

071006 ;

摘要：

Clozapine exhibited 10-fold higher affinity than haloperidol for human 5-HT1A receptors expressed in Chinese Hamster Ovary cells (CHO-h5-HT1A) (K(i)s = 160 and 1910 nM respectively). Whereas haloperidol did not alter the basal binding of [S-35]GTP gamma S to CHO-h5HT(1A) membranes, clozapine stimulated it with an EC(50) of 2320 nM and an efficacy of 49% (compared to 5-HT). The stimulation was antagonized by the selective 5-HT1A receptor antagonist, WAY 100635 (1 nM).

引用

页码：119 / 121

页数：3

共 10 条

[1] COMPETITIVE ANTAGONISM OF SEROTONIN (5-HT)(2C) AND 5-HT2A RECEPTOR-MEDIATED PHOSPHOINOSITIDE (PI) TURNOVER BY CLOZAPINE IN THE RAT - A COMPARISON TO OTHER ANTIPSYCHOTICS [J].