A neuropeptide with diverse biological activities
货号:ajcx22994
CAS:N/A
分子式:C27H23D6N3O2
分子量：433.6
溶解度:Acetonitrile:Methanol (1:1): Soluble,DMF: Soluble,DMSO: Soluble
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Mozavaptan-d₆is intended for use as an internal standard for the quantification of mozavaptan by GC- or LC-MS. Mozavaptan is an orally bioavailable antagonist of vasopressin V₂receptors (K_i= 9.42 nM in HeLa cells expressing the human receptor).^1,2It is selective for vasopressin V₂over V₁receptors (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 V₂and V₁receptors, respectively.¹Mozavaptan (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 in anesthetized rats when administered intravenously at doses ranging from 10 to 100 µg/kg.

1.Yamamura, Y., Ogawa, H., Yamashita, H., et al.Characterization of a novel aquaretic agent, OPC-31260, as an orally effective, nonpeptide vasopressin V2 receptor antagonistBr. J. Pharmacol.105(4)787-791(1992) 2.Nakamura, S., Itoh, S., Fujiki, H., et al.Binding affinities of mozavaptan hydrochloride (OPC-31260) for vasopressin receptorsJap. Pharmacol. Ther.34(7)827-834(2006)