THE STRUCTURE AND SPECIFICITY OF ENDOTHELIN RECEPTORS - THEIR IMPORTANCE IN PHYSIOLOGY AND MEDICINE

被引:179
作者
HUGGINS, JP
PELTON, JT
MILLER, RC
机构
[1] Marion Merrell Dow Research Institute, F-67046 Strasbourg Cedex
关键词
D O I
10.1016/0163-7258(93)90041-B
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
In addition to involvement in vascular endothelium-smooth muscle communication, the secretion of and receptors for, endothelins arc widely distibuted. Two cloned receptor subtypes are G-protein-coupled to several intracellular messengers, predominantly inositol phosphates. From a knowledge of structure-activity relationships and peptide conformations, details of receptor architecture and selective agents, including nonpeptides and antagonists, have been discovered. From the nature of the actions of endothelins, receptor distributions (including CNS) and plasma levels, it is concluded that they are paracrine factors normally involved in long-term cellular regulation, but which may be important in several pathologies, many of which are stress-related.
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页码:55 / 123
页数:69
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