AUTHOR=Kane Emilie , Giaid Adel TITLE=Potential Clinical Implications of the Urotensin II Receptor Antagonists JOURNAL=Frontiers in Pharmacology VOLUME=2 YEAR=2011 URL=https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2011.00038 DOI=10.3389/fphar.2011.00038 ISSN=1663-9812 ABSTRACT=

Urotensin II (UII) binds to its receptor, UT, playing an important role in the heart, kidneys, pancreas, adrenal gland, and central nervous system. In the vasculature, it acts as a potent endothelium-independent vasoconstrictor and endothelium-dependent vasodilator. In disease states, however, this constriction–dilation equilibrium is disrupted. There is an upregulation of the UII system in heart disease, metabolic syndrome, and kidney failure. The increase in UII release and UT expression suggest that UII system may be implicated in the pathology and pathogenesis of these diseases by causing an increase in acyl-coenzyme A:cholesterol acyltransferase-1 (ACAT-1) activity leading to smooth muscle cell proliferation and foam cell infiltration, insulin resistance (DMII), as well as inflammation, high blood pressure, and plaque formation. Recently, UT antagonists such as SB-611812, palosuran, and most recently a piperazino-isoindolinone based antagonist have been developed in the hope of better understanding the UII system and treating its associated diseases.