Introduction：Basic information about CAS 137975-06-5|Mozavaptan, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Mozavaptan |
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| CAS Number | 137975-06-5 | Molecular Weight | 427.538 |
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| Density | 1.2±0.1 g/cm3 | Boiling Point | 543.0±50.0 °C at 760 mmHg |
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| Molecular Formula | C27H29N3O2 | Melting Point | / |
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| MSDS | / | Flash Point | 282.2±30.1 °C |
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Names
| Name | N-[4-[5-(dimethylamino)-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl]phenyl]-2-methylbenzamide |
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| Synonym | More Synonyms |
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Mozavaptan BiologicalActivity
| Description | Mozavaptan (OPC31260) is a orally effective, nonpeptide vasopressin V2 receptor antagonist with an IC50 of 14 nM. |
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| Related Catalog | Signaling Pathways >>GPCR/G Protein >>Vasopressin ReceptorResearch Areas >>Cancer |
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| Target | IC50: 14 nM (vasopressin receptor)[1] |
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| In Vitro | Mozavaptan causes a competitive displacement of [3H]-arginine vasopressin (AVP) binding to both V1 and V2 receptors with IC50 values of 1.2 μM and 14 nM, respectively. The Kd of [3H]-AVP is reduced significantly in both rat liver and kidney in the presence of mozavaptan (Kd=1.1 nM in liver, Kd=1.38 nM in kidney)[1]. |
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| In Vivo | Mozavaptan at doses of 10 to 100 μg/kg, i.v., inhibits the antidiuretic action of exogenously administered arginine vasopressin in water-loaded, alcohol-anaesthetized rats in a dose-dependent manner. Mozavaptan does not exert an antidiuretic activity suggesting that it is not a partial V2 receptor agonist. Mozavaptan dose-dependently increases urine flow and decreases urine osmolality after oral administration at doses of 1 to 30 mg/kg in normal conscious rats[1]. |
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| Kinase Assay | To determine binding kinetic constants, liver or kidney plasma membranes are incubated with increasing concentrations of [3H]-AVP with or without excess (1 μM) unlabelled AVP to obtain a saturation curve. To investigate whether mozavaptan interacts competitively or noncompetitively, the saturation binding of [3H]-AVP is examined in the absence and presence of mozavaptan at concentrations of 0.3 μM and 1 μM in liver membranes and 3 nM, and 10 nM in kidney membranes. Data on the saturation curve are plotted according to the method of Scatchard and fitted by a regression analysis[1]. |
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| Animal Admin | Rats: Mozavaptan is dissolved in DMSO at a concentration of 10 mM and diluted with assay buffer. Female Brattleboro rats homozygous for hypothalamic diabetes insipidus and weighing between 180 and 280g are used. Mozavaptan (30 mg/kg) and vehicle (5% gum arabic) are administered orally in a volume of 2 mL/kg and d(CH2)5Tyr(Et)VAVP (10pgkg-1) is administered in a volume of 1 mL/kg. Spontaneously voided urine is collected for 6h with metabolic cages. Both before and during the study, the rats received water and food ad libitum[1]. |
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| References | [1]. Yamamura Y, et al. Characterization of a novel aquaretic agent, OPC-31260, as an orally effective, nonpeptide vasopressin V2 receptor antagonist. Br J Pharmacol. 1992 Apr;105(4):787-91. |
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Chemical & Physical Properties
| Density | 1.2±0.1 g/cm3 |
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| Boiling Point | 543.0±50.0 °C at 760 mmHg |
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| Molecular Formula | C27H29N3O2 |
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| Molecular Weight | 427.538 |
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| Flash Point | 282.2±30.1 °C |
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| Exact Mass | 427.225983 |
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| PSA | 52.65000 |
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| LogP | 3.83 |
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| Vapour Pressure | 0.0±1.5 mmHg at 25°C |
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| Index of Refraction | 1.647 |
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| InChIKey | WRNXUQJJCIZICJ-UHFFFAOYSA-N |
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| SMILES | Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)C)c3ccccc32)cc1 |
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Safety Information
Synonyms
| 5-dimethylamino-1-[4-[(2-methylbenzoyl)amino]benzoyl]-2,3,4,5-tetrahydro-1H-benzazepine |
| N-(4-(((5RS)-5-(Dimethylamino)-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)carbonyl)phenyl)-2-methylbenzamide |
| Mozavaptan |
| Mozavaptan [INN] |
| N-(4-((5-(Dimethylamino)-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)carbonyl)phenyl)-2-methylbenzamide |
| (+/-)-5-dimethylamino-1-[4-(2-methylbenzoylamino)-benzoyl]-2,3,4,5-tetrahydro-1H-benzazepin |
| Benzamide,N-(4-((5-(dimethylamino)-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)carbonyl)phenyl)-2-methyl |
| 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- |
