Endothelins are endogenous vasoactive peptides that are considered among the most potent vasoconstrictor substances known. In addition to their vascular effects, endothelins and their receptors have been shown to be present in many organs and share plenty physiological and pathophysiological functions. Sarafotoxins are natural substances from the venom of snakes genus Atractaspis, structurally and pharmacologically near to endothelins. The current minireview focuses on the chemical and molecular aspects of endothelins and sarafotoxins, and their receptors in physiological and pathophysiological processes.

Endothelins are potent predominantly vasoconstricting agents that act as local autocrine and paracrine mediators. Endothelin-1 is the most potent and sustained vasoconstrictor and pressor substance yet identified. Abnormalities of the endothelin system occur in a range of diseases associated with vasoconstriction, vasospasm, and vascular hypertrophy. ET receptor antagonists were until recently regarded as drugs of great promise in patients with congestive heart failure, pulmonary hypertension and others. The aim of this article is a survey of compounds that affect the endothelin receptors and clinical trials with these agents.