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

Trends Pharmacol Sci. 2004 Feb;25(2):76-85. doi: 10.1016/


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.

Publication types

  • Review

MeSH terms

  • Animals
  • Heart / drug effects*
  • Humans
  • Hypertension / etiology
  • Kidney / drug effects*
  • Kidney / physiology
  • Receptors, G-Protein-Coupled / antagonists & inhibitors*
  • Species Specificity
  • Urotensins* / antagonists & inhibitors
  • Urotensins* / pharmacology
  • Urotensins* / physiology


  • Receptors, G-Protein-Coupled
  • UTS2R protein, human
  • Urotensins
  • urotensin II