Palosuran is an antagonist of the urotensin II receptor (UTR; IC
50s = 3.6 and 1,475 nM for CHO cell membranes expressing human and rat recombinant receptors, respectively).
1 It inhibits contraction of isolated rat aortic rings induced by urotensin II (Item Nos.
24711 |
24753) in a concentration-dependent manner. Palosuran (300 mg/kg twice per day) reduces plasma endothelin-1 (Item No.
24127), urotensin II, and TGF-β1 levels, as well as the main pulmonary arterial pressure and right ventricular hypertrophy index in a rat model of pulmonary arterial hypertension (PAH) induced by monocrotaline (Item No.
16666).
2 Palosuran (300 mg/kg per day) reduces serum glucose, cholesterol, and triglyceride levels and increases survival in a rat model of diabetes induced by streptozotocin (STZ; Item No.
13104).
3 It also decreases albuminuria and global kidney lesion scores in STZ-induced diabetic rats.
