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

Abstract：

: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.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Bymaster FP,Falcone JF

doi

10.1016/s0014-2999(00)00037-6

keywords:

subject

Has Abstract

pub_date

2000-03-03 00:00:00

pages

245-8

issue

3

eissn

0014-2999

issn

1879-0712

pii

S0014299900000376

journal_volume

390

pub_type

杂志文章

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