扎托司琼

扎托司琼
臨床資料
ATC碼	未分配;
识别信息
	IUPAC命名法 5-chloro-2,2-dimethyl-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2,3-dihydro-1-benzofuran-7-carboxamide; ;
CAS号	123482-22-4
PubChem CID	60763;
ChemSpider	16736584;
UNII	901MC95XSB;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID8043997 ;
化学信息
化学式	C19H25ClN2O2
摩尔质量	348.87 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES CC1(Cc2cc(cc(c2O1)C(=O)N[C@H]3C[C@H]4CC[C@@H](C3)N4C)Cl)C;
	InChI InChI=1S/C19H25ClN2O2/c1-19(2)10-11-6-12(20)7-16(17(11)24-19)18(23)21-13-8-14-4-5-15(9-13)22(14)3/h6-7,13-15H,4-5,8-10H2,1-3H3,(H,21,23)/t13-,14+,15-; Key:SPKBYQZELVEOLL-QDMKHBRRSA-N;

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

^ 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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[1] 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.

[2] 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.

[3] 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.

[4] 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.

[5] 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.

[6] 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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