Palosuran, also known as ACT-058362, a potent and specific antagonist of the human UT receptor. Urotensin inhibition with palosuran was a promising alternative in pulmonary arterial hypertension. Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues. Palosuran improves pancreatic and renal function in diabetic rats. Phase-II clinical trials for diabetic nephropathies and cardiovascular disorders were discontinued.

SB-706375 is a potent, surmountable, reversible and selective mammalian urotensin-II receptor antagonist. In rats SB-706375 provoked a pronounced diuresis and natriuresis, accompanied by modest increases in effective renal blood flow and glomerular filtration rate.