Pharmacological Potential of Endothelin Receptors Agonists and Antagonists

Abstract

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.

Keywords

• Endothelin
• Endothelin receptor
• Endothelin receptor agonist
• Endothelin receptor antagonist
• Bosentan
• Pulmonary hypertension treatment