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Trends Pharmacol Sci. 2004 Feb;25(2):76-85.

From 'gills to pills': urotensin-II as a regulator of mammalian cardiorenal function.

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Department of Vascular Biology, Cardiovascular and Urogenital Centre of Excellence for Drug Discovery, GlaxoSmithKline, PO Box 1539, 709 Swedeland Road, King of Prussia PA 19406-0939, USA.


The identification of a human homolog of urotensin-II (U-II) and a novel, specific G-protein-coupled receptor by Ames et al. in 1999 changed the perception that the U-II isopeptide family was an esoteric collection of 'somatostatin-like neuropeptides' present only in the nervous systems of an eclectic array of aquatic invertebrates, fish and amphibians. In this article, we review recent developments in the pharmacology of human U-II, focusing on the actions of this peptide in the mammalian cardiorenal system. The putative role of U-II in the etiology of hypertension, heart failure, renal dysfunction and diabetes is discussed, as are novel U-II receptor antagonists.

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