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Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
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More detailed introduction
The urotensin-II (U-II) receptor (UT, nomenclature as agreed by the NC-IUPHAR Subcommittee on the Urotensin receptor [12,14,37]) is activated by the endogenous dodecapeptide urotensin-II (UTS2, O95399), originally isolated from the urophysis, the endocrine organ of the caudal neurosecretory system of teleost fish [3,36]. Several structural forms of U-II exist in fish and amphibians [37]. The goby orthologue was used to identify U-II as the cognate ligand for the predicted receptor encoded by the rat gene gpr14 [1,8,22,25,27]. Human urotensin-II (UTS2, O95399), an 11-amino-acid peptide [8], retains the cyclohexapeptide sequence of goby U-II that is thought to be important in ligand binding [4,16,21]. This sequence is also conserved in the deduced amino-acid sequence of rat urotensin-II (14 amino-acids) and mouse urotensin-II (14 amino-acids), although the N-terminal is more divergent from the human sequence [7]. A second endogenous ligand for the UT has been discovered in rat [32]. This is the urotensin II-related peptide (UTS2B, Q765I0), an octapeptide that is derived from a different gene, but shares the C-terminal sequence (CFWKYCV) common to U-II from other species. Identical sequences to rat urotensin II-related peptide (UTS2B, Q765I0) are predicted for the mature mouse and human peptides [13]. UT exhibits relatively high sequence identity with somatostatin, opioid and galanin receptors [37]. The urotensinergic system displays an unprecedented repertoire of four or five ancient UT in some vertebrate lineages and five U-II family peptides in teleost fish [35].
UT receptor
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Database page citation (select format):
Davenport AP, Douglas SA, Fournier A, Giaid A, Krum H, Lambert DG, Leprince J, MacLean MR, Ohlstein EH, Thomas WG, Tostivint H, Vaudry D, Vaudry H, Webb DJ. Urotensin receptor in GtoPdb v.2023.1. IUPHAR/BPS Guide to Pharmacology CITE. 2023; 2023(1). Available from: https://doi.org/10.2218/gtopdb/F65/2023.1.
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Christopoulos A, Davenport AP, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: G protein-coupled receptors. Br J Pharmacol. 180 Suppl 2:S23-S144.
In the human vasculature, human urotensin-II (UTS2, O95399) elicits both vasoconstrictor (pD2 9.3-10.1, [23]) and vasodilator (pIC50 10.3-10.4, [31]) responses.