Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally activevasopressin V₂receptorantagonist with anIC₅₀of 14 nM. Mozavaptan shows ~85-fold selectivity forV₂receptorover V₁receptor (IC₅₀of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment^[1][2].

IC50: 14 nM (Vasopressin V₂receptor); 1.2 μM (Vasopressin V₁receptor)^[1]

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. K_dvalue for [3H]-AVP in rat liver is 1.1 nM; in rat kidney is 1.38 nM. The K_dof [3H]-AVP is reduced significantly in both rat liver and kidney in the presence of Mozavaptan (K_dof 2.47 nM and 5.51 nM for V1 receptor at the doses of 0.3 μM and 1 μM.respectively; K_dof 2.4 nM and 4.03 nM for V2 receptor at the doses of 0.3 μM and 1 μM.respectively)^[1].

Mozavaptan (OPC-31260; 1-30 mg/kg; oral administration; hydrated conscious rats) treatment dose-dependently increases urine flow and decreased urine osmolality^[1].
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^[1].

427.54

Solid

C₂₇H₂₉N₃O₂

137975-06-5

莫扎伐普坦

Room temperature in continental US; may vary elsewhere.

DMSO : 6.2 mg/mL(14.50 mM;Need warming)

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