Urotensin receptor (UT) is a G-protein coupled receptor which binds the peptide hormoneurotensin. The urotensin-II (UT) receptor is a Gq/11-protein-coupled receptor that mediates complex hemodynamic effects and influences neuromuscular physiology. The UT receptor displays greatest expression levels in the peripheral vasculature, heart and kidney, although they are found elsewhere, notably the central nervous system, at lower levels.
An overview of urotensin receptor
Urotensin receptor (UT) is a G-protein coupled receptor which binds the peptide hormoneurotensin. UT in the center is mainly distributed in the medulla, cortex, hippocampus, thalamus and hypothalamus, and the periphery is mainly distributed in the heart, kidney, liver, pancreas, skeletal muscle and other organs. And its mRNA is expressed in the cerebral cortex, hypothalamus, medullary medulla, vascular tissue, kidney, heart and other organs.
Inhibition of urotensin receptor
UT's peptide antagonists are mainly characterized by strong affinity and short-term decline, so the peptide antagonists are used as tools to study the physiological and pathological functions of Urotensin ll (UII)/UT system, including urantide , UFP 803, SB-710411, BIM-23127 and GSK248451. The results show that these peptide UT antagonists retain the UII's C-terminal ring-shaped domain, which determines its affinity with UT. For example, Urantide is a complete antagonist of UT whose primary activity is selective antagonism of rat aortic ring contraction by UII, and agonist activity expresses recombinant hUT in cells. In the whole animal level, urantide can also reduce the proportion of myocardial infarction/ischemic area in rats with myocardial ischemia-reperfusion injury, and inhibit the elevation of ST segment and T wave.
Urotensin receptor and diseases
In recent years, many animal experiments and clinical reports show that the protein expression level of UII/UT system is closely related to many cardiovascular diseases , liver diseases, kidney diseases and some other diseases. The expression of Urotensin ll (UII) and UT receptor mRNA in renal tissue of rats with acute renal injury increased significantly after 15 days of modeling, and the level of UII in plasma of type II diabetic nephropathy increased with the aggravation of diabetic nephropathy. The total bilirubin, blood anhydride, plasma UII and end-stage liver disease models of the type II hepatorenal syndrome death group were higher than the survival group. And the expression of UII and UT in pancreas of type II diabetic rats increased markedly.