An antagonist of UTR (IC50s = 3.6 and 1,475 nM for CHO cell membranes expressing human and rat recombinant receptors, respectively); inhibits urotensin II-induced contraction of isolated rat aortic rings in a concentration-dependent manner; reduces plasma endothelin-1, urotensin II, and TGF-β1 levels, as well the main pulmonary arterial pressure and right ventricular hypertrophy index in a monocrotaline-induced rat model of PAH at 300 mg/kg twice per day; reduces serum glucose, cholesterol, and triglyceride levels and increases survival in an STZ-induced rat model of diabetes at 300 mg/kg per day; decreases albuminuria and global kidney lesion scores in STZ-induced diabetic rats