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Mozavaptan (OPC-31260) is a novel, orally effective, nonpeptide vasopressin V2 receptor antagonist. 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. Mozavaptan (OPC-31260) inhibited the antidiuretic action of exogenously administered AVP in water-loaded, alcohol-anaesthetized rats in a dose-dependent manner. Mozavaptan (OPC-31260) caused a competitive displacement of [3H]-AVP binding to both V1 and V2 receptors with IC50 values of 1.2 ± 0.2 × 10-6 M and 1.4 ± 0.2 × 10-8 M, respectively.
Molecular Weight | 427.53 |
Formula | C27H29N3O2 |
CAS Number | 137975-06-5 |
Solubility (25°C) | DMSO 5 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[4] Carles Villabona. Vasopressin receptor antagonists: the vaptans
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