INVESTIGATIONS OF THE SUBTYPE OF ALPHA-2-ADRENOCEPTOR MEDIATING CONTRACTIONS OF THE HUMAN SAPHENOUS-VEIN

被引：19
|
作者：
SMITH, K [1 ]
CONNAUGHTON, S [1 ]
DOCHERTY, JR [1 ]
机构：
[1] ROYAL COLL SURG IRELAND,DEPT CLIN PHARMACOL,123 ST STEPHENS GREEN,DUBLIN 2,IRELAND
来源：
BRITISH JOURNAL OF PHARMACOLOGY | 1992年 / 106卷 / 02期
关键词：
ALPHA-2-ADRENOCEPTOR SUBTYPES; ALPHA-2B-ADRENOCEPTORS; HUMAN SAPHENOUS VEIN; PRAZOSIN; ARC-239; BRL; 44408;
D O I：
10.1111/j.1476-5381.1992.tb14354.x
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
1 We have examined the effects of a series of alpha-2-adrenoceptor antagonists against isometric contractions to noradrenaline in human saphenous vein, and correlated these potencies with affinities for the alpha-2A-ligand binding site of human platelet and the alpha-2B-ligand binding site of rat kidney. 2 The alpha-2B-selective adrenoceptor antagonists, prazosin, ARC 239 and HV 723 showed high, and the alpha-2A-selective antagonist BRL 44408 showed low, potency in human saphenous vein. 3 Potency in human saphenous vein correlated better with affinity for the alpha-2B-ligand binding site (r = 0.7 1, n = 12, P < 0.0 1) than with affinity for the alpha-2A-ligand binding site (r = 0.56, n = 12, non significant). 4 It is concluded that the postjunctional alpha-2-adenoceptor of human saphenous vein resembles an alpha-2B-ligand binding site more than an alpha-2A-ligand binding site.
引用
收藏
页码：447 / 451
页数：5
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