Urantide: an ultrapotent urotensin II antagonist peptide in the rat aorta

Riccardo Patacchini, Paolo Santicioli, Sandro Giuliani, Paolo Grieco, Ettore Novellino, Paolo Rovero, Carlo Alberto Maggi
British Journal of Pharmacology 2003, 140 (7): 1155-8
In this study we describe the ability of two human urotensin-II (hU-II) derivatives [Pen5,Orn8]hU-II(4-11) and [Pen5,DTrp7,Orn8]hU-II(4-11) (urantide) to block hU-II-induced contractions in the rat isolated thoracic aorta. Both compounds competitively antagonized hU-II- induced effects with pKB=7.4+/-0.06 (n=12) and pKB=8.3+/-0.09 (n=12), respectively. In contrast, neither [Pen5,Orn8]hU-II(4-11) nor urantide (1 microm each) was able to modify noradrenaline- or endothelin 1-induced contractile effects. At micromolar concentrations, [Pen5,Orn8]hU-II(4-11) produced weak (< or =25% of hU-II maximum) agonist responses in the rat aorta, whereas urantide was totally uneffective as agonist up to 1 microm. In addition, [Pen5,Orn8]hU-II(4-11) and urantide displaced [125I]urotensin II from specific binding at hU-II recombinant receptors (UT receptors) transfected into CHO/K1 cells (pKi=7.7+/-0.05, n=4 and pKi=8.3+/-0.04, n=4, respectively). To our knowledge, urantide is the most potent UT receptor antagonist so far described, and might represent a useful tool for exploring the (patho)physiological role of hU-II in the mammalian cardiovascular system.

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