Design and discovery of nonpeptide endothelin antagonists

Abstract

The involvement of the endothelin family of peptide vasoconstrictors has been implicated in a variety of human disease states. Several classes of endothelin antagonists are in early clinical development, and the therapeutic applications of this new mechanistic class of agents are beginning to emerge. This article reviews the different compound classes, their receptor selectivity for the endothelin receptor subtypes ETA and ETB and some important studies of selected compounds in animal models of different disease states.