Competitive and silent antagonism of recombinant 5-HT1B receptors by amiloride

被引：7

作者：

Pauwels, PJ

机构：

[1] Centre de Recherche Pierre Fabre, Lab. of Cell. and Molec. Neurbio., 81106 Castres Cédex, 17, Avenue Jean Moulin

来源：

GENERAL PHARMACOLOGY-THE VASCULAR SYSTEM | 1997年 / 29卷 / 05期

关键词：

5-HT1B receptor (recombinant; human); cAMP; sumatriptan; amiloride; stably transfected CHO-K1 cell line;

D O I：

10.1016/S0306-3623(97)00008-6

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

1. The cyclic adenosine monophosphate (cAMP) response of the diuretic amiloride was compared with sumatriptan at recombinant human 5-HT1B (h5-HT1B) receptor sites in stably transfected Chinese hamster ovary (CHO-K1) cells. 2. Amiloride, free of intrinsic activity (pEC(50)<3.0), competitively antagonized the sumatriptan-mediated inhibition (pEC(50): 7.37) of 100 mu M forskolin-induced cAMP formation with a pA(2) value of 4.46. 3. The antagonist feature was not shared by the amiloride derivative ethylisopropylamiloride, not-withstanding a slightly higher 5'HT1B receptor-binding affinity (pK(i): 4.87) than that of amiloride (pK(i): 4.70). (C) 1997 Elsevier Science Inc.

引用

页码：749 / 751

页数：3

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