扎托司琼
外观
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臨床資料 | |
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ATC碼 |
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识别信息 | |
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CAS号 | 123482-22-4 ![]() |
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CompTox Dashboard (EPA) | |
化学信息 | |
化学式 | C19H25ClN2O2 |
摩尔质量 | 348.87 g·mol−1 |
3D模型(JSmol) | |
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扎托司琼(INN:zatosetron;开发代号:LY-277,359)是一种用作5-HT3受体拮抗剂的药物。[1]它具有口服活性,作用持续时间长,能够产生止吐作用,但不刺激胃肠道运输速率。[2][3]在动物研究和人体试验中,它也是一种有效的抗焦虑药,[4]尽管高剂量下会产生一些副作用。[5][6]
参考资料
[编辑]- ^ Cohen ML, Bloomquist W, Gidda JS, Lacefield W. LY277359 maleate: a potent and selective 5-HT3 receptor antagonist without gastroprokinetic activity. The Journal of Pharmacology and Experimental Therapeutics. July 1990, 254 (1): 350–5. PMID 2366187.
- ^ Robertson DW, Lacefield WB, Bloomquist W, Pfeifer W, Simon RL, Cohen ML. Zatosetron, a potent, selective, and long-acting 5HT3 receptor antagonist: synthesis and structure-activity relationships. Journal of Medicinal Chemistry. January 1992, 35 (2): 310–9. PMID 1732548. doi:10.1021/jm00080a016.
- ^ Schwartz SM, Goldberg MJ, Gidda JS, Cerimele BJ. Effect of zatosetron on ipecac-induced emesis in dogs and healthy men. Journal of Clinical Pharmacology. March 1994, 34 (3): 250–4. PMID 7517409. S2CID 23486859. doi:10.1002/j.1552-4604.1994.tb03994.x.
- ^ Smith WT, Londborg PD, Blomgren SL, Tollefson GD, Sayler ME. Pilot study of zatosetron (LY277359) maleate, a 5-hydroxytryptamine-3 antagonist, in the treatment of anxiety. Journal of Clinical Psychopharmacology. April 1999, 19 (2): 125–31. PMID 10211913. doi:10.1097/00004714-199904000-00006.
- ^ Williams PD, Calligaro DO, Colbert WE, Helton DR, Shetler T, Turk JA, Jordan WH. General pharmacology of a new potent 5-hydroxytryptamine antagonist. Arzneimittel-Forschung. March 1991, 41 (3): 189–95. PMID 1867653.
- ^ Bendele A, Means J, Shoufler J, Schmalz C, Hanasono G, Symanowski J, Adams E. Chronic toxicity of zatosetron, a 5-HT3 receptor antagonist, in rhesus monkeys. Drug and Chemical Toxicology. February 1995, 18 (1): 61–82. PMID 7768200. doi:10.3109/01480549509017858.
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