INCOMPLETE INHIBITION OF ENDOTHELIN-1 PRESSOR EFFECTS BY AN ENDOTHELIN ET(A)-RECEPTOR ANTAGONIST

被引：23

作者：

BIRD, JE

WALDRON, TL

机构：

[1] Department of Pharmacology, Bristol-Myers Squibb, Pharmaceutical Research Institute, Princeton

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1993年 / 240卷 / 2-3期

关键词：

ENDOTHELIN-1; MEAN ARTERIAL PRESSURE; ENDOTHELIN RECEPTOR ANTAGONIST; SARAFOTOXIN S6C;

D O I：

10.1016/0014-2999(93)90912-2

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Incomplete inhibition of endothelin-1-induced pressor effects by FR-139317, a novel, potent, ET(A) receptor antagonist, was observed in conscious, normotensive rats. Maximum inhibition by FR-139317 of the endothelin-1 pressor response (0.1, 0.3, 1.0 nmol/kg) was 49 +/- 7, 41 +/- 3, 62 +/- 5%, respectively. Two ET(B)-selective receptor ligands induced pressor responses in conscious rats. A portion of the endothelin-I pressor response may be mediated by ET(B) receptors, and ET(B)-mediated vasoconstriction may contribute to incomplete inhibition of the pressor response to endothelin-1 by an ET(A)-selective receptor antagonist.

引用

收藏

页码：295 / 298

页数：4

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