A NEW HIGHLY POTENT ANTAGONIST OF BRADYKININ

被引：46

作者：

LAMMEK, B ^{[1
]}

WANG, YX ^{[1
]}

GAVRAS, I ^{[1
]}

GAVRAS, H ^{[1
]}

机构：

[1] BOSTON UNIV,SCH MED,MED CTR,SCH MED,DEPT MED,HYPERTENS & ATHEROSCLEROSIS SECT,80 E CONCORD ST,BOSTON,MA 02118

来源：

PEPTIDES | 1990年 / 11卷 / 05期

关键词：

Acylation; Adamantane-acetic acid; Bradykinin; Bradykinin inhibitor; Potency;

D O I：

10.1016/0196-9781(90)90031-Y

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：

We report that the acylation of the N-terminus of [D-Arg0,Hyp3,Thi5.8,D-Phe7]bradykinin, one of the most potent bradykinin antagonists described to date, with 1-adamantane-acetic acid, results in an analogue with more than ten times enhanced potency. The new analogue does not increase the plasma catecholamines, even when administered at doses sufficient to inhibit by more than 90% the vasodepressor response to 250 ng of exogenous bradykinin. This modification suggests new possibilities for the design of even more potent and selective bradykinin antagonists for studying the physiopathology of bradykinin. © 1990.

引用

页码：1041 / 1043

页数：3

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