Mozavaptan

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Mozavaptan (OPC-31260) 是一种有效的、选择性非肽加压素 V2 受体拮抗剂，IC50 为 14 nM； VP1 的效力低 100 倍 (IC50=1.2 uM)。

Mozavaptan (OPC-31260) is a potent, selective nonpeptide vasopressin V2 receptor antagonist with IC50 of 14 nM; 100-fold less potent for VP1 (IC50=1.2 uM); dose-dependently increases urine flow and decreases urine osmolality in normal conscious rats; orally effective.Other Indication Approved(In Vitro):Mozavaptan (OPC-31260) inhibits AVP binding to binding to rat liver (V1 receptor) and kidney (V2 receptor) plasma membranes in a competitive manner and that it is about 100 times more selective for V2 receptors. Kd value for [3H]-AVP in rat liver is 1.1 nM; in rat kidney is 1.38 nM. The Kd of [3H]-AVP is reduced significantly in both rat liver and kidney in the presence of Mozavaptan (Kd of 2.47 nM and 5.51 nM for V1 receptor at the doses of 0.3 μM and 1 μM.respectively; Kd of 2.4 nM and 4.03 nM for V2 receptor at the doses of 0.3 μM and 1 μM.respectively). (In Vivo):Mozavaptan (OPC-31260; 1-30 mg/kg; oral administration; hydrated conscious rats) treatment dose-dependently increases urine flow and decreased urine osmolality.Mozavaptan (OPC-31260; 10-100 μg/kg; intravenous injection; male Sprague-Dawley rats) treatment inhibits the antidiuretic action of exogenously administered arginine vasopressin (AVP) in water-loaded, alcohol-anaesthetized rats in a dose-dependent manner.

Mozavaptan (OPC-31260) inhibits AVP binding to binding to rat liver (V1 receptor) and kidney (V2 receptor) plasma membranes in a competitive manner and that it is about 100 times more selective for V2 receptors. Kd value for [3H]-AVP in rat liver is 1.1 nM; in rat kidney is 1.38 nM. The Kd of [3H]-AVP is reduced significantly in both rat liver and kidney in the presence of Mozavaptan (Kd of 2.47 nM and 5.51 nM for V1 receptor at the doses of 0.3 μM and 1 μM.respectively; Kd of 2.4 nM and 4.03 nM for V2 receptor at the doses of 0.3 μM and 1 μM.respectively).

Mozavaptan (OPC-31260; 1-30 mg/kg; oral administration; hydrated conscious rats) treatment dose-dependently increases urine flow and decreased urine osmolality.Mozavaptan (OPC-31260; 10-100 μg/kg; intravenous injection; male Sprague-Dawley rats) treatment inhibits the antidiuretic action of exogenously administered arginine vasopressin (AVP) in water-loaded, alcohol-anaesthetized rats in a dose-dependent manner. Animal Model:Hydrated conscious rats (300-350 g) Dosage:1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg Administration:Oral administration Result:Dose-dependently increased urine flow and decreased urine osmolality.

OPC-31260

GPCR/G Protein

Vasopressin Receptor

Vasopressinreceptor1|Vasopressinreceptor2

Other Indications

Other Disease

137975-06-5

427.5381

C27H29N3O2

>98% (HPLC)

DMSO: 6.2 mg/mL (Need warming)

CN(C)C1CCCN(C(=O)C2=CC=C(NC(=O)C3=CC=CC=C3C)C=C2)C2=CC=CC=C12

Benzamide, N-[4-[[5-(dimethylamino)-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl]phenyl]-2-methyl-

(-20℃)

With Ice Pack

≥ 2 years