product name Mozavaptan
Description: Mozavaptan, also known as OPC 31260, is a novel, selective, competitive vasopressin receptor antagonist for both V1 and V2 receptors with IC50 of 1.2 μM and 14 nM, respectively. It was developed and marketed by Otsuka of Japan. Mozavaptan was approved in October 2006 in Japan for hyponatremia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH) due to ADH producing tumors.
References: Blood Press. 1994 Mar;3(1-2):137-41; Br J Pharmacol. 1992 Apr;105(4):787-91.
427.54
Formula
C27H29N3O2
CAS No.
137975-06-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 1 mg/mL (2.3 mM)
Water: <1 mg/mL
Ethanol: 1 mg/mL (2.3 mM)
Solubility (In vivo)
30% Propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
Synonyms
OPC-31260
other peoduct :
| In Vitro |
In vitro activity: Mozavaptan (OPC-31260) is a nonpeptide, orally effective competitive inhibitor of AVP with a V2:V1 receptor selectivity ratio of 25:1 indicating relative V2 receptor selectivity. Mozavaptan (OPC-31260) inhibits AVP binding to V1 and V2 receptors in a competitive manner. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Mozavaptan (OPC-31260) inhibits the antidiuretic action of exogenously administered AVP in water-loaded, alcohol-anaesthetized rats in a dose-dependent manner. OPC-31260 dose-dependently increases urine flow and decreased urine osmolality after oral administration at doses of 1 to 30 mg/kg in normal conscious rats. |
| Animal model | Male Sprague-Dawley rats |
| Formulation & Dosage | Dissolved in 3% ethanol (v/v), 1.67% glucose (w/v) and 0.3% NaCl (w/v); 10, 30, 100μg/kg; i.v. injection |
| References | Blood Press. 1994 Mar;3(1-2):137-41; Br J Pharmacol. 1992 Apr;105(4):787-91. |
