Potent and selective competitive vasopressin V2
receptor antagonist (Ki
values are 0.06 and 12.3 nM for V2
receptors respectively). Decreases urine osmolality and increases serum sodium concentrations. Delays the onset of end-stage renal disease in a mouse model of polycystic kidney disease. Exhibits myocardial and renal protective effects in hypertensive heart failure rats. Orally active.
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All Tocris products are intended for laboratory research use only.
7-Chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoyl-amino)benzoyl ]-2,3,4,5-tetrahydro-1H-1-benzazepine (OPC-41061): a potent, orally active nonpeptide arginine vasopressin V2 receptor antagonist.
Kondo et al.
Ghali et al.
Nat.Rev.Drug Discov., 2009;8:611
Tolvaptan delays the onset of end-stage renal disease in a polycystic kidney disease model by suppressing increases in kidney volume and renal injury.
Aihara et al.
Chronic administration of oral vasopressin type 2 receptor antagonist tolvaptan exerts both myocardial and renal protective effects in rats with hypertensive heart failure.
Morooka et al.
The citations listed below are publications that use Tocris products. Selected citations for Tolvaptan include:
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