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Urotensin receptor ligands act on the urotensin II receptor (UT), a G protein-coupled receptor. In 1999, three groups showed that the cyclic peptide urotensin II is the endogenous ligand of the orphan G protein-coupled receptor 14 (GPR14), now named UT. Human urotensin II constricts isolated arteries strongly, and the receptor is found in heart, blood vessels, kidney and brain. Urotensin II-related peptide (URP) is a second endogenous ligand of the receptor. UT ligands are used in research on vascular tone, cardiac remodeling and kidney function. Palosuran, SB-706375 and SB-611812 are nonpeptide antagonists, and urantide is a peptide antagonist. Urotensin II-related peptide and human urotensin II (114-124) are listed as agonist peptides.
UPG-108 is a peptide compound that acts as a non-competitive allosteric modulator of Urotensin II receptors (UTR). It enhances the efficacy of UTR agonists while concurrently reducing their potency. UPG-108 has been shown to efficiently induce calcium release without causing contraction in rat aortic rings that possess intact endothelium. This compound is valuable for research into diseases associated with the angiotensinergic system.
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