ENDOTHELIN ETA AND ENDOTHELIN ETB RECEPTORS MEDIATE VASCULAR SMOOTH-MUSCLE CONTRACTION

被引：276

作者：

SUMNER, MJ ^{[1
]}

CANNON, TR ^{[1
]}

MUNDIN, JW ^{[1
]}

WHITE, DG ^{[1
]}

WATTS, IS ^{[1
]}

机构：

[1] GLAXO GRP RES LTD, DEPT CARDIOVASC & RESP PHARMACOL, PK RD, WARE SG12 0DP, HERTS, ENGLAND

来源：

BRITISH JOURNAL OF PHARMACOLOGY | 1992年 / 107卷 / 03期

关键词：

ENDOTHELIN; RECEPTOR SUBTYPES; VASCULAR SMOOTH MUSCLE CONTRACTION; ETA ANTAGONIST; BQ123;

D O I：

10.1111/j.1476-5381.1992.tb14537.x

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

1 We have investigated the receptors mediating endothelin-induced contraction of rabbit isolated jugular vein (RJV) and rat isolated thoracic aorta (RTA). 2 Endothelin-1 (ET-1) and endothelin-3 (ET-3) contracted RJV preparations with similar potency (EC50 values approximately 1 nM), whereas, ET-1 (EC50:4.5 nM) was approximately 80 fold more potent than ET-3 in contracting RTA. In addition, the ET(B) receptor-selective agonist [Ala1,3,11,15]ET-1 contracted RJV (EC50:2.1 nM) but not RTA. 3 The ETA receptor antagonist, BQ123, competitively antagonized (pA2 6.93) the contraction of RTA produced by ET-1, but had no effect (at 10 muM) on the contractile effects of either ET-1, ET-3 or [Ala1,3,11,15]ET-1 in RJV. 4 These data suggest that both ET(A) and ET(B) receptors can mediate vascular smooth muscle contraction.

引用

页码：858 / 860

页数：3

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