Ono Koh, Matsumori Akira
Department of Cardiovascular Medicine, Kyoto University Graduate School of Medicine, Kyoto Japan 606-8297.
Cardiovasc Drug Rev. 2002 Winter;20(1):1-18. doi: 10.1111/j.1527-3466.2002.tb00078.x.
Endothelin receptor antagonists have been proposed for the treatment of a variety of disorders in which the endothelins may act as pathogenic mediators, such as hypertension, congestive heart failure, and cerebral vasospasm. Bosentan is a nonpeptide competitive antagonist, which can be a good tool for studying the endothelin system. It is specific for the endothelin system and blocks the actions of endothelin at both mammalian receptors (A and B). Bosentan has recently moved into Phase III clinical trial. This review will attempt to overview the experimental and clinical effects of bosentan.
内皮素受体拮抗剂已被提议用于治疗多种疾病，其中内皮素可能作为致病介质起作用，如高血压、充血性心力衰竭和脑血管痉挛。波生坦是一种非肽类竞争性拮抗剂，它可能是研究内皮素系统的良好工具。它对内皮素系统具有特异性，可阻断内皮素在哺乳动物的两种受体（A和B）上的作用。波生坦最近已进入III期临床试验。本综述将试图概述波生坦的实验和临床效果。
