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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 Uvol over the AVP-treated vehicle group by 438, 1018, and 1133%, respectively, while Uosm 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.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Clinical Compound Library | Drug Repurposing Compound Library | Anti-Cardiovascular Disease Compound Library | Endocrinology Compound Library | Orally Active Compound Library | Targeted Diversity Library | Rare Diseases Drug Library | Human Metabolite Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | Balovaptan | Felypressin acetate | Lazuvapagon | Mozavaptan hydrochloride | d[Cha4]-AVP | Terlipressin acetate | WAY-151932 | Fuscoside | Antagonist G | (Phe2,Orn8)-Oxytocin | Desamino(D-3-(3′-pyridyl)-Ala2,Arg8)-Vasopressin | 2-(3-Trifluoromethylphenyl)glycine hydrochloride | Atosiban acetate | Conivaptan hydrochloride | D[LEU4,LYS8]-VP TFA | RG7713 | Big Endothelin-1 (1-38), human | SR 49059 | Tolvaptan-d7 | Argipressin | [Asu1,6-Arg8]Vasopressin | Enuvaptan | SKF 100398 | TC OT 39
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货号: HY-14185
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