Biological ActivityUrotensin-II (UT) receptor ligand; behaves as a silent antagonist in most in vitro assays and in vivo, but does retain small residual agonist activity under certain conditions in some assays. Competitively antagonizes U-II induced contractions in the rat aorta (pIC50 = 7.46) and prevents plasma extravasation elicited by U-II in mice in vivo.
(Modifications: X-2 = Pen, Trp-4 = D-Trp, X-5 = Dab, Disulfide bridge between 2 - 7)
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In vitro and in vivo pharmacological characterization of the novel UT receptor ligand [Pen5,DTrp7,Dab8]urotensin II(4-11) (UFP-803).
Camarda et al.
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