Endothelin Antagonists

Endothelin Antagonists

A endothelin receptor antagonist (ERA) is a drug which blocks endothelin receptors. Two main kinds of ERAs exist: First Selective ERA (e.g. sitaxsentan), which affect endothelin A. Second Dual ERAs, which affect both endothelin A and B.

Endothelin Receptor

There are at least three known endothelin receptors, ETA, ETB1 and ETB2, all of which are G protein-coupled receptors whose activation result in elevation of intracellular-free calcium. t is associated with ABCD syndrome[2] and some forms of Waardenburg syndrome.

Endothelin Antagonists

There are 2 types of endothelin receptors: ETA, which causes vasoconstriction, and ETB, which causes both constriction and vasodilation. Some endothelin receptor antagonists block the ETA receptor and others block both ETA and ETB receptors. Endothelin receptor antagonists being examined for treatment of CHF include darusentan, sitaxsentan, tezosentan, and bosentan. Sitaxsentan and tezosentan are available only for intravenous use.