The future of endothelin-receptor antagonism as treatment for systemic hypertension.

Endothelin (ET) is an endogenous peptide secreted predominantly by endothelial cells that mediates its effects via vasoconstriction and hypertrophy of vascular smooth muscle. Because the role of ET has been described in multiple pathologic processes in cardiovascular disease, including hypertension, there has been a strong interest in the development of therapeutic agents that inhibit ET receptors. ET receptor antagonists have shown much promise in disease states such as pulmonary arterial hypertension, essential hypertension, and various forms of secondary hypertension. This review serves to summarize the current role of ET and ET receptor antagonists in both the pathophysiology and the treatment of hypertension.