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: ≥ 3 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[4] Carles Villabona. Vasopressin receptor antagonists: the vaptans
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