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SB-611812 is an antagonist of the urotensin II receptor (UTR).1 It binds to recombinant rat UTR (Ki = 121 nM) and inhibits contraction of isolated rat aorta induced by urotensin II (pA2 = 6.59) but not potassium chloride, endothelin-1, angiotensin II, or phenylephrine. SB-611812 (30 mg/kg) decreases myocardial interstitial fibrosis and the ratio of collagen I to collagen III in a rat model of ischemia induced by ligation of the left anterior descending (LAD) artery.2
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1. A role for urotensin II in restenosis following balloon angioplasty: Use of a selective UT receptor blocker. J. Mol. Cell. Cardiol. 39(5), 785-791 (2005).
2. Urotensin-