Endothelin ETA Receptor Antagonists

EDNRA and EDNRB (endothelin A and B receptors, respectively) are members of the rhodopsin-like 7-transmembrane receptor family. EDNRA binds endothelins ET-1 and ET-2 preferentially, and is expressed on vascular smooth muscle where it mediates vasoconstriction. EDNRB binds all three endothelin forms equally, and is expressed on endothelial cells where it mediates vasodilation.