HETEROGENEITY OF ENDOTHELIN ET(A) RECEPTOR-MEDIATED CONTRACTIONS IN THE RABBIT SAPHENOUS-VEIN

被引：8

作者：

NISHIYAMA, M ^{[1
]}

SHAN, LH ^{[1
]}

MOROI, K ^{[1
]}

MASAKI, T ^{[1
]}

KIMURA, S ^{[1
]}

机构：

[1] KYOTO UNIV,FAC MED,DEPT PHARMACOL,KYOTO 606,JAPAN

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1995年 / 286卷 / 02期

关键词：

ENDOTHELIN; SARAFOTOXIN; BQ-123; ENDOTHELIN ET(A) RECEPTOR; SAPHENOUS VEIN; RABBIT;

D O I：

10.1016/0014-2999(95)00566-4

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The involvement of endothelin ET(A) receptors in endothelin-1-induced contractions of the rabbit saphenous vein was studied. After desensitization of endothelin ET(B) receptors by pretreatment with sarafotoxin S6c, endothelin-1 and sarafotoxin S6b and a high concentration of endothelin-3 caused dose-dependent contractions. However, endothelin-1-induced contractions were much less sensitive to an endothelin ET(A) receptor antagonist, BQ-123 (cyclo(-D-AsP-L-Pro-D-Val-L-Leu-D-Trp-)), than sarafotoxin S6b-induced responses. The pA(2) values of BQ-123 for endothelin-1- and sarafotoxin S6b-induced contractions were 5.69 and 7.65, respectively. These results suggest pharmacological heterogeneity of endothelin ET(A) receptors in the rabbit saphenous vein.

引用

页码：209 / 212

页数：4

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