Name | Mozavaptan |
Synonyms | CS-134 OPC 31260 OPC-31260 Mozavaptan OPC 31260 OPC31260L MOZAVAPTAN N-(4-(5-(Dimethylamino) -2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl) 5-(Dimethylamino)-1-[4-(2-methylbenzamido)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepine N-(4-{[5-(dimethylamino)-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl}phenyl)-2-methylbenzamide Benzamide, N-[4-[[5-(dimethylamino)-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl]phenyl]-2-methyl- |
CAS | 137975-06-5 |
EINECS | 1312995-182-4 |
InChI | InChI=1/C27H29N3O2/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) |
Molecular Formula | C27H29N3O2 |
Molar Mass | 427.54 |
Density | 1.21g/cm3 |
Melting Point | 213 - 217°C |
Boling Point | 543°C at 760 mmHg |
Flash Point | 282.2°C |
Solubility | DMSO 1 mg/mL Water <1 mg/mL Ethanol 1 mg/mL |
Vapor Presure | 7.49E-12mmHg at 25°C |
Appearance | Solid |
Color | White to Off-White |
Storage Condition | Sealed in dry,Room Temperature |
Refractive Index | 1.646 |
MDL | MFCD00908918 |
Physical and Chemical Properties | Appearance: white to off-white crystalline powder; |
In vitro study | Mozavaptan (OPC-31260) is a non-peptide, orally effective, competitive AVP inhibitor, acting on V1 and V2 receptors with a selectivity ratio of 1:25, indicating a relatively high selectivity for V2 receptors. Mozavaptan (OPC-31260) competitively inhibits AVP binding to V1 and V2 receptors. |
In vivo study | Mozavaptan (OPC-31260) inhibits the antidiuretic effect of exogenous AVP in a dose-dependent manner in rats under alcohol anesthesia. OPC-31260 Oral treatment of normal conscious rats at doses of 1 to 30 mg/kg increased urinary flow and decreased urinary osmolality in a dose-dependent manner. |