Decreased binding affinity of olanzapine and clozapine for human muscarinic receptors in intact clonal cells in physiological medium

被引：44

作者：

Bymaster, FP ^{[1
]}

Falcone, JF ^{[1
]}

机构：

[1] Lilly Corp Ctr, Lilly Res Labs, Neurosci Res Div, Indianapolis, IN 46285 USA

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 2000年 / 390卷 / 03期

关键词：

muscarinic receptor; olanzapine; clozapine; binding; antipsychotic;

D O I：

10.1016/S0014-2999(00)00037-6

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The binding affinity of olanzapine, clozapine and atropine for muscarinic receptor subtypes in clonal Chinese hamster ovary (CHO) cell lines was compared in intact cells in physiological media to disrupted cells in hypotonic buffer. The affinity of olanzapine and clozapine, but not atropine, for muscarinic receptor subtypes (M-1-M-5) was significantly reduced in intact cells in physiological medium compared to disrupted cells in hypotonic buffer. The affinity of olanzapine for muscarinic M-1 receptors was most affected with a reduction of K-i value from 2.5 to 73 nM in intact cells. These data suggest that the affinity of olanzapine and clozapine for muscarinic receptors have been significantly overestimated. (C) 2000 Elsevier Science B.V. All rights reserved.

引用

页码：245 / 248

页数：4

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