[资源] Lixivaptan（利伐普坦/利昔伐坦/ WAY-VPA-985/VPA-985）介绍

【通用名】Lixivaptan, WAY-VPA-985, VPA-985 【化学名】 N-[3-Chloro-4-(10,11-dihydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-10-ylcarbonyl)phenyl]-5-fluoro-2-methylbenzamide 【CAS登记号】168079-32-1 【分子式】C27-H21-Cl-F-N3-O2 【分子量】473.93 【化学活性】Cardiovascular Drugs, Diuretics, Heart Failure Therapy, Renal-Urologic Drugs, Vasopressin V2 Antagonists（心血管药，利尿药，治疗心力衰竭，肾，泌尿系统药物，血管加压素V2受体拮抗剂） 【开发阶段】Phase II 【研发机构】Wyeth Pharmaceuticals (Originator) 【合成路线】（见附图） 作者：Albright, J.D.; Reich, M.F.; Sum, F.-W.; Delos Santos, E.G. (American Cyanamid Co.) 来源：CA 2128956; EP 0636625; JP 1995157486; US 5516774 【药效】Lixivaptan, a highly selective, orally active, vasopressin receptor antagonist, is currently in late stage development for the treatment of hyponatremia. It is thought to antagonize the action of vasopressin (also known as antidiuretic hormone, or ADH) on the V2 receptors in the collecting duct of the kidney, causing excretion of water without loss of sodium or other electrolytes. Based on its proposed mechanism of action and as seen in early studies, lixivaptan has shown promise in treatment of disease states associated with water retention and/or electrolyte imbalance such as hypervolemic hyponatremia commonly associated with heart failure (HF) or the syndrome of inappropriate antidiuretic hormone (SIADH) 合成路线图.GIF

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