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. |
overview | in recent years, with the cloning and sequencing of arginine vasopressin (arginine vasopressin AVP) binding receptors, many drugs that antagonize AVP have come out. these AVP preparations can act on V2 receptors in the collecting duct and enhance free excretion without obvious sodium and potassium loss, thus increasing the blood sodium concentration, it provides a new method for the treatment of edema and hyponatremia in congestive heart failure (CHF). |
use | mozavaptan is a non-peptide V2 receptor antagonist, which is mainly used for rare hyponatremia in malignant tumor-related antidiuretic hormone secretion syndrome. |
biological activity | Mozavaptan (OPC-31260) is a new and competitive vasopressin receptor antagonist that acts on V1 and V2 receptors with IC50 of 1.2 μM and 14 nM respectively. |
Target | Value |
Vasopressin receptor 2 | 14 nM |
Vasopressin receptor 1 | 1.2 μM |