AN ENDOTHELIN RECEPTOR (ETA) ANTAGONIST ISOLATED FROM STREPTOMYCES-MISAKIENSIS

被引：233

作者：

IHARA, M

FUKURODA, T

SAEKI, T

NISHIKIBE, M

KOJIRI, K

SUDA, H

YANO, M

机构：

[1] Central Research Lab., Banyu Pharmaceutical Co., Ltd., Tokyo

[2] Exploratory Research Lab., Banyu Pharmaceutical Co., Ltd., Tokyo

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 1991年 / 178卷 / 01期

关键词：

D O I：

10.1016/0006-291X(91)91789-F

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A competitive endothelin (ET) antagonist, BE-18257B, was isolated from the fermentation products of Streptomyces misakiensis. It is a novel cyclic pentapeptide, cyclo(-d-Glu-l-Ala-allo-d-Ile-l-Leu-d-Trp-), and binds to ETA receptors (ET-1 selective) in cardiovascular tissues, but not to ETB receptors (equally sensitive to isopeptides of ET family) in kidney, adrenal gland and cerebellum tissues. BE-18257B also antagonizes ET-1-induced vasoconstriction in rabbit iliac artery and pressor action in rats. Thus it is a selective ETA antagonist and should provide a valuable tool for elucidation of the pharmacological and pathophysiological roles of ET-1. © 1991.

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收藏

页码：132 / 137

页数：6

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