内皮素
效力
体内
药理学
内皮素受体
受体
离体
内皮素1
化学
生物
体外
生物化学
生物技术
作者
Jerry L. Wessale,Andrew Adler,Eugene I. Novosad,Samuel V. Calzadilla,Brian D. Dayton,Kennan C. Marsh,Martin Winn,Hwan-Soo Jae,Thomas W von Geldern,Terry J. Opgenorth,Jinshyun R. Wu-Wong
出处
期刊:Clinical Science
[Portland Press]
日期:2002-09-01
卷期号:103 (s2002): 112S-117S
被引量:48
摘要
Endothelins (ETs), 21-amino-acid peptides involved in the pathogenesis of various diseases, bind to ETA and ETB receptors to initiate their effects. Based on the same core structure, we have developed four small-molecule ET receptor antagonists, ABT-627 (atrasentan), ABT-546, A-182086 and A-192621, which exhibit differences in selectivity for ETA and ETB receptors. In this report, we compare the efficacy, potency and pharmacokinetic properties of these four antagonists, including potency in inhibiting ET-1- or Sarafotoxin 6c-induced vessel constriction in isolated arteries and efficacy in antagonizing ET-1-, big ET-1- or Sarafotoxin 6c-induced pressor responses in rats.
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