A vasopressin V2 receptor antagonist (Ki = 9.42 nM in HeLa cells expressing the human receptor); selective for vasopressin V2 over V1 receptors (IC50s = 14 and 1

Mozavaptan (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
138470-70-9
Storage:
-20
UN-No:
Non-Hazardous - /

Mozavaptan is an orally bioavailable antagonist of vasopressin V2 receptors (Ki = 9.42 nM in HeLa cells expressing the human receptor).{27292,59329} 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.{27292} 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; Item No. 24154) in anesthetized rats when administered intravenously at doses ranging from 10 to 100 µg/kg.  

 

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Description

A vasopressin V2 receptor antagonist (Ki = 9.42 nM in HeLa cells expressing the human receptor); 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, respectively; increases urine volume and decreases urine osmolality in rats from 10-30 mg/kg

Formal name: N-[4-[[5-(dimethylamino)-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl]phenyl]-2-methyl-benzamide, monohydrochloride

Synonyms:  OPC 31260

Molecular weight: 464

CAS: 138470-70-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Kidney & Renal Disease||Research Area|Endocrinology & Metabolism|Hormones & Receptors

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