Selective urotensin-II (UT) receptor antagonist (Ki
values are 61, 17, 30, 65 and 56 nM at human, monkey, cat, rat and mouse receptors respectively). Inhibits U-II-induced intracellular Ca2+
= 180 nM) and antagonizes the contractile action of U-II in isolated mammalian arteries and aortae (EC50
= 50 - 189 nM).
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Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues.
Behm et al.
Nonpeptide urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375.
Douglas et al.