Lixivaptan利伐普坦,168079-32-1

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Lixivaptan

CAS No. : 168079-32-1

MCE 国际站：Lixivaptan

产品活性：Lixivaptan (VPA-985, WAY-VPA 985) 是具有口服活性，选择性的 vasopressin receptor V2 拮抗剂，对人和大鼠的 IC₅₀ 值分别为1.2 和 2.3 nM。

研究领域：GPCR/G Protein

作用靶点：Vasopressin Receptor

In Vitro: Lixivaptan displays competitive antagonist activity at V2 receptors.

In Vivo: In conscious dogs, water-loaded with 30 mL/kg (po) and arginine vasopressin (AVP)-treated (0.4 μg/kg in oil, sc), lixivaptan (1, 3, and 10 mg/kg po) increases U_vol over the AVP-treated vehicle group by 438, 1018, and 1133%, respectively, while U_osm decreases from 1222 mOsm/kg (water-loaded and AVP treated vehicle) to 307, 221, and 175 mOsm/kg, respectively. In homozygous Brattleboro rats lacking AVP, lixivaptan at 10 mg/kg po (i.e., 10 times the dose producing V2 antagonist activity) b.i.d. for 5 days, shows a sustained antagonist action without evidence of agonist effects. In a randomized double-blind placebo-controlled ascending single dose study, patients (deprived of fluids overnight before dosing) are dosed orally with 30, 75, or 150 mg of lixivaptan. All three doses increase urine flow and serum sodium concentrations and produced significant dose-related decreases in urinary osmolality. Phase II clinical trials in patients with congestive heart failure, liver cirrhosis with ascites or syndrome of inappropriate antidiuretic hormone have demonstrated that lixivaptan increases water clearance without affecting renal sodium excretion or activating the neurohormonal system.

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