This article provides a survey of endothelin receptor agonists and antagonists and their clinical trials in conditions such as heart failure and pulmonary hypertension.
Endothelin agents remain investigational in heart failure; leaves open optimal receptor targeting for future trials.
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.
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Patočka et al. (2005) studied this question.
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