| 规格: | 98% |
| 分子量: | 433.6 |
| 包装 | 价格(元) |
| 500ug | 电议 |
| 1mg | 电议 |
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 (Ki= 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)
m.cnreagent.com