Selective ET(A) receptor antagonism with ABT-627 attenuates all renal effects of endothelin in humans.

++Endothelin (ET-1) acts as a potent vasoconstrictor in the human kidney, and this vasoconstriction could contribute to the ischemia seen in acute renal failure. In animal studies, the vasoactive properties of ET-1 are known to be ET(A) receptor-and/or ET(B) receptor-mediated; however, the receptor subtype involved in the human kidney remains to be defined. In a phase I, single-center, double-blind, randomized, three-period, crossover design, the effects of orally administered ABT-627, a selective ET(A) receptor antagonist, on renal hemodynamics during ET-1 infusion were evaluated.