Key result
Urantide competitively antagonized hU-II-induced contractions in the rat isolated thoracic aorta (pKB=8.3+/-0.09) and displaced urotensin II from recombinant UT receptors (pKi=8.3+/-0.04).
Population
Rat isolated thoracic aorta and CHO/K1 cells transfected with hU-II recombinant receptors (UT receptors)
Design
Preclinical
Authors
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Urantide may serve as a tool for preclinical urotensin II research; leaves open translation to human cardiovascular therapeutics.
Effect estimate: pKB=8.3+/-0.09
Urantide is an ultrapotent urotensin II receptor antagonist that may serve as a useful tool for exploring the pathophysiological role of hU-II in the cardiovascular system.
Patacchini et al. (2003) studied this question. Urantide vs. [Pen5,Orn8]hU-II(4-11) was evaluated on hU-II-induced contractions in the rat isolated thoracic aorta (pKB=8.3+/-0.09). Urantide competitively antagonized hU-II-induced contractions in the rat isolated thoracic aorta (pKB=8.3+/-0.09) and displaced urotensin II from recombinant UT receptors (pKi=8.3+/-0.04).
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