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Mozavaptan is an orally bioavailable antagonist of vasopressin V2 receptors (Ki = 9.42 nM in HeLa cells expressing the human receptor).1,2 It is selective for vasopressin V2 over V1 receptors (IC50s = 14 and 1,200 nM, respectively) in radioligand binding assays using rat kidney and rat liver membranes that endogenously express high levels of vasopressin V2 and V1 receptors, respectively.1 Mozavaptan (10-30 mg/kg, p.o.) increases urine volume and decreases urine osmolality, indicating aquaresis, in conscious rats. It reduces decreases in urine flow and increases in urine osmolality induced by arginine vasopressin (AVP; Item No. 24154) in anesthetized rats when administered intravenously at doses ranging from 10 to 100 µg/kg.
WARNING This product is not for human or veterinary use.
1. Characterization of a novel aquaretic agent, OPC-
2. Binding affinities of mozavaptan hydrochloride (OPC-