The endothelins and sarafotoxins are two structurally related families of potent vasoactive peptides. Although the exact physiological function of these peptides is not known, the endothelins are probably involved in pathophysiological conditions such as hypertension and heart failure. This article will review the biochemistry of these peptides and their receptors, with special reference to proteolytic regulation, receptor subtypes and the G protein-linked phosphoinositide signal transduction pathway.