Mozavaptan (hydrochloride)

Mozavaptan is an orally bioavailable antagonist of vasopressin V2 receptors (Ki = 9.42 nM in HeLa cells expressing the human receptor). 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. 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, Cay-24154) in anesthetized rats when administered intravenously at doses ranging from 10 to 100 µg/kg.Formal Name: N-[4-[[5-(dimethylamino)-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl]phenyl]-2-methyl-benzamide, monohydrochloride. CAS Number: 138470-70-9. Synonyms: OPC 31260. Molecular Formula: C27H29N3O2 . HCl. Formula Weight: 464.0. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 25 mg/ml, Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 288 nm. SMILES: CC1=C(C(NC2=CC=C(C(N3C(C=CC=C4)=C4C(N(C)C)CCC3)=O)C=C2)=O)C=CC=C1.Cl. InChi Code: InChI=1S/C27H29N3O2.ClH/c1-19-9-4-5-10-22(19)26(31)28-21-16-14-20(15-17-21)27(32)30-18-8-13-24(29(2)3)23-11-6-7-12-25(23)30,/h4-7,9-12,14-17,24H,8,13,18H2,1-3H3,(H,28,31),1H. InChi Key: MOROBKPIULFQDC-UHFFFAOYSA-N.