C. E. Peishoff, M.A. Lago, E. H. Ohlstein and J. D. Elliottt* Pages 425 - 440 ( 16 )
The endothelins (ET-1, 2 and 3) are potent vasoactive peptides known to elicit their actions through activation of two well-characterized receptor subtypes, ETA and ETB, belonging to the G protein coupled, seven transmembrane spanning superfamily. Since the elucidation of the structure of ET-1 in 1988, there have been many reports suggestive of a role for the endothelins in the etiology of disease. Much of the early evidence was indirect, linking elevated endogenous endothelin levels with pathophysiological states and it is only since the discovery and characterization of receptor specific antagonists that a compelling case has been developed. The present review will focus on recently developed non-peptide endothelin receptor antagonists with an introductory section covering peptide antagonists of these receptors.