选择性和竞争性 urotensin II 受体拮抗剂
Selective and competitive urotensin-II (UT) receptor antagonist (pKB = 8.3). Blocks hU-II induced contractions in thoracic aorta ex vivo. Exhibits no effect on noradrenaline or endothelin 1-induced contraction or on acetylcholine-induced relaxation. Behaves as a partial agonist in a calcium mobilization assay (in CHO cells expressing hUT receptors).
Patacchini et al (2003) Urantide: an ultrapotent urotensin II antagonist peptide in the rat aorta. Br.J.Pharmacol. 140 1155 PMID:14645137 |Carotenuto et al (2014) Lead optimization of P5U and urantide: discovery of novel potent ligands at the urotensin-II receptor. J.Med.Chem. 57 5965 PMID:24992374
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