Mozavaptan is a benzazepine derivative that antagonizes the binding of arginine vasopressin (AVP) to vasopressin receptors located in the liver (V1; IC50 = 1.2 μM) and kidney (V2; IC50 = 14 nM). At 10-100 μg/kg, mozavaptan can inhibit the antidiuretic action of AVP, promoting aquaresis when administered intravenously to rats. The therapeutic potential of mozavaptan in ectopic antidiuretic hormone syndrome, heart failure, and other complications related to hyponatremia has been studied.
ChEBI: Mozavaptane hydrochloride is a member of benzamides.
OPC 31260 is a vasopressin V2 selective antagonist. Arginine vasopressin (AVP) plays an important part in circulatory and water homeostasis. The V2 receptor subtype is important in water retention, cardiac remodeling in congestive heart failure (CHF), and renal hemodynamic alterations, and is considered a target for polysystic kidney disease. OPC-31260 has been shown to inhibit the development of polycystic kidney disease in several animal models.
Mozavaptan (OPC-31260; 1-30 mg/kg; oral administration; hydrated conscious rats) treatment dose-dependently increases urine flow and decreased urine osmolality[1].
Mozavaptan (OPC-31260; 10-100 μg/kg; intravenous injection; male Sprague-Dawley rats) treatment inhibits the antidiuretic action of exogenously administered arginine vasopressin (AVP) in water-loaded, alcohol-anaesthetized rats in a dose-dependent manner[1].
| Animal Model: | Hydrated conscious rats (300-350 g)[1] |
| Dosage: | 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg |
| Administration: | Oral administration |
| Result: | Dose-dependently increased urine flow and decreased urine osmolality.
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