The endothelins are a family of potent vasoconstrictors, some of which
also have vasodilatory activity. In many diseases associated with tis
sue hypoxia or ischemia and in diseases in which vasoconstriction play
s role, the circulating levels of endothelin are higher than in health
y, control subjects. These findings stimulated research aimed at disco
vering endothelin receptor antagonists. This review focuses on the bin
ding potency and vascular activity of these new peptide and nonpeptide
endothelin receptor antagonists.