The role of endothelin receptor antagonists in cardiovascular pharmacotherapy.
Endothelin (ET) is a hormone produced predominantly by endothelial cells which has been recognised to play a significant role in the development of several cardiovascular disease states. In order to combat the deleterious effects of ET, several ET-receptor antagonists (ETRA) are currently in clinical development. The agents developed thus far inhibit the actions of ET through either selective inhibition of the ET(A) receptors or non-selective inhibition of both ET(A) and ET(B) receptors. However, due to the differing proportions of the two receptor subtypes in various tissues, animal models and pathologies, it remains a matter of debate whether receptor selective agents impart significant clinical benefits over non-selective agents. This paper seeks to briefly summarise the important preclinical and clinical effects that have been reported in the literature and will attempt to provide a rationale for the use of both types of ETRAs in the treatment of both systemic and pulmonary hypertension as well as chronic heart failure (CHF).
Knoll GmbH, PO Box 210805, 67008 Ludwigshafen, Germany. klaus.muenter@knoll.de
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