内皮素ETA受体拮抗剂对内皮素-1升压作用的不完全抑制。

Incomplete inhibition of endothelin-1 pressor effects by an endothelin ETA receptor antagonist.

作者信息

Bird J E, Waldron T L

机构信息

Department of Pharmacology, Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000.

出版信息

Eur J Pharmacol. 1993 Aug 24;240(2-3):295-8. doi: 10.1016/0014-2999(93)90912-2.

DOI:10.1016/0014-2999(93)90912-2

PMID:8243544

Abstract

Incomplete inhibition of endothelin-1-induced pressor effects by FR-139317, a novel, potent, ETA 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 ETB-selective receptor ligands induced pressor responses in conscious rats. A portion of the endothelin-1 pressor response may be mediated by ETB receptors, and ETB-mediated vasoconstriction may contribute to incomplete inhibition of the pressor response to endothelin-1 by an ETA-selective receptor antagonist.

摘要

在清醒的正常血压大鼠中观察到，新型强效内皮素A（ETA）受体拮抗剂FR-139317对内皮素-1诱导的升压作用的抑制不完全。FR-139317对内皮素-1升压反应（0.1、0.3、1.0 nmol/kg）的最大抑制率分别为49±7%、41±3%、62±5%。两种内皮素B（ETB）选择性受体配体在清醒大鼠中诱导升压反应。内皮素-1的部分升压反应可能由ETB受体介导，并且ETB介导的血管收缩可能导致ETA选择性受体拮抗剂对内皮素-1升压反应的抑制不完全。