Contrasting actions of endothelin ET_A and ET_B receptors in cardiovascular disease

Schneider, M.P., Boesen, E.I. and Pollock, D.M. (2007) Contrasting actions of endothelin ET_A and ET_B receptors in cardiovascular disease. Annual Review of Pharmacology and Toxicology, 47, pp. 731-759. (doi: 10.1146/annurev.pharmtox.47.120505.105134)

Abstract

First identified as a powerful vasoconstrictor, endothelin has an extremely diverse set of actions that influence homeostatic mechanisms throughout the body. Two receptor subtypes, ET_A and ET_B, which usually have opposing actions, mediate the actions of endothelin. ET_A receptors function to promote vasoconstriction, growth, and inflammation, whereas ET_B receptors produce vasodilation, increases in sodium excretion, and inhibit growth and inflammation. Potent and selective receptor antagonists have been developed and have shown promising results in the treatment of cardiovascular diseases such as pulmonary arterial hypertension, acute and chronic heart failure, hypertension, renal failure, and atherosclerosis. However, results are often contradictory and complicated because of the tissue-specific vasoconstrictor actions of ET_B receptors and the fact that endothelin is an autocrine and paracrine factor whose activity is difficult to measure in vivo. Considerable questions remain regarding whether ET_A-selective or nonselective ET_A/ET_B receptor antagonists would be useful in a range of clinical settings.

• Item Type: Articles
• Status: Published
• Refereed: Yes
• Glasgow Author(s) Enlighten ID: Schneider, Dr Markus
• Authors: Schneider, M.P., Boesen, E.I., and Pollock, D.M.
• College/School: College of Medical Veterinary and Life Sciences > School of Cardiovascular & Metabolic Health
• Journal Name: Annual Review of Pharmacology and Toxicology
• ISSN: 0362-1642
• ISSN (Online): 1545-4304
• Published Online: 01 September 2006