EFFECT OF EXTRACELLULAR CALCIUM-CONCENTRATION ON POTENCY OF MUSCARINIC AGONISTS AT M1-RECEPTORS AND M2-RECEPTORS IN RABBIT VAS-DEFERENS

被引:17
作者
DORJE, F
RETTENMAYR, NM
MUTSCHLER, E
LAMBRECHT, G
机构
[1] Department of Pharmacology, University of Frankfurt, D-6000 Frankfurt/Main, Theodor-Stern-Kai 7
关键词
MUSCARINIC M1-HETERORECEPTORS (PREJUNCTIONAL); MUSCARINIC RECEPTOR AGONISTS; VAS DEFERENS (RABBIT); CA2+; PIRENZEPINE; 4-CL-MCN-A-343;
D O I
10.1016/0014-2999(91)90900-B
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The M1 potency (decrease in neurogenic response) of carbachol, oxotremorine, muscarine, arecaidine propargyl ester (APE) and 4-(4-chlorophenylcarbamoyloxy)-2-butynyltrimethylammonium iodide (4-Cl-McN-A-343) in rabbit field-stimulated vas deferens (prostatic segments) increased up to 15-fold when calcium was lowered (3.5-1.0 nM). The M2 receptor-mediated increase in twitch height in response to carbachol and the M1 affinity of pirenzepine were independent of calcium concentration (2.5 and 1.0 mM). Thus, prostatic segments of rabbit vas deferens can be used successfully at 1.0 mM calcium to determine M1 potencies of agonists and M1 affinities of antagonists without counteracting stimulation of M2 receptors.
引用
收藏
页码:417 / 420
页数:4
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