Endothelin-1 and endothelin receptor antagonists in cardiovascular remodeling

被引：59
|
作者：
Kirchengast, M
Münter, K
机构：
[1] Knoll AG, Dept Int Strateg Mkt Cardiovasc, D-67008 Ludwigshafen, Germany
[2] Knoll AG, Dept Expt & Cardiovasc Res, D-67008 Ludwigshafen, Germany
来源：
PROCEEDINGS OF THE SOCIETY FOR EXPERIMENTAL BIOLOGY AND MEDICINE | 1999年 / 221卷 / 04期
关键词：
D O I：
10.1046/j.1525-1373.1999.d01-88.x
中图分类号：
R-3 [医学研究方法]; R3 [基础医学];
学科分类号：
1001 ;
摘要：
Endothelins build a peptide family composed of three isoforms, each of them containing 21 amino acids. Endothelin-1 is the isoform mainly responsible for any cardiovascular action and therefore the sole scope of this review. Endothelin-1 is the most potent endogenous vasoconstrictor known; in addition it acts as a potent (co)mitogen. There is a substantial body of experimental evidence that endothelin-1 may contribute not only to sustained vasoconstriction, but also to remodeling within the cardiovascular system. Thus, with the help of endothelin receptor antagonists (available for a few years) the involvement of mainly ETA receptors in structural diseases such as heart failure, pulmonary hypertension, atherosclerosis, restenosis, systemic hypertension, and chronic renal failure has been shown. These data make endothelin receptor antagonists, and especially those selective for the ETA receptor, promising agents for the treatment of chronic cardiovascular diseases associated with remodeling. Currently several chemically distinct, orally available members of this novel class of therapeutic agents are under clinical investigation.
引用
收藏
页码：312 / 325
页数：14
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