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
收藏
页码：119 / 121
页数：3
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