ザトステロン

ザトステロン
IUPAC命名法による物質名
	IUPAC名 5-chloro-2,2-dimethyl-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2,3-dihydro-1-benzofuran-7-carboxamide;
識別
CAS番号;	123482-22-4
ATCコード	none
PubChem	CID: 60763
ChemSpider	16736584
UNII	901MC95XSB
化学的データ
化学式	C19H25ClN2O2
分子量	348.87 g·mol−1
	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;
	テンプレートを表示

ザトステロン(Zatosetron, LY-277,359)は、5-HT3受容体のアンタゴニストとして作用する^[1]。経口で活性を持ち、活性時間が長く、腸管輸送の速度を刺激することなく、制吐薬としての作用を持つ^[2]^[3]。また、動物実験とヒトの臨床試験において、多量でも副作用なく^[4]^[5]、抗不安薬の作用が示された^[6]。

出典[編集]

^ “LY277359 maleate: a potent and selective 5-HT3 receptor antagonist without gastroprokinetic activity”. The Journal of Pharmacology and Experimental Therapeutics 254 (1): 350-5. (July 1990). PMID 2366187.
^ “Zatosetron, a potent, selective, and long-acting 5HT3 receptor antagonist: synthesis and structure-activity relationships”. Journal of Medicinal Chemistry 35 (2): 310-9. (January 1992). doi:10.1021/jm00080a016. PMID 1732548.
^ “Effect of zatosetron on ipecac-induced emesis in dogs and healthy men”. Journal of Clinical Pharmacology 34 (3): 250-4. (March 1994). doi:10.1002/j.1552-4604.1994.tb03994.x. PMID 7517409.
^ “General pharmacology of a new potent 5-hydroxytryptamine antagonist”. Arzneimittel-Forschung 41 (3): 189-95. (March 1991). PMID 1867653.
^ “Chronic toxicity of zatosetron, a 5-HT3 receptor antagonist, in rhesus monkeys”. Drug and Chemical Toxicology 18 (1): 61-82. (February 1995). doi:10.3109/01480549509017858. PMID 7768200.
^ “Pilot study of zatosetron (LY277359) maleate, a 5-hydroxytryptamine-3 antagonist, in the treatment of anxiety”. Journal of Clinical Psychopharmacology 19 (2): 125-31. (April 1999). doi:10.1097/00004714-199904000-00006. PMID 10211913.

[1] “LY277359 maleate: a potent and selective 5-HT3 receptor antagonist without gastroprokinetic activity”. The Journal of Pharmacology and Experimental Therapeutics 254 (1): 350-5. (July 1990). PMID 2366187.

[2] “Zatosetron, a potent, selective, and long-acting 5HT3 receptor antagonist: synthesis and structure-activity relationships”. Journal of Medicinal Chemistry 35 (2): 310-9. (January 1992). doi:10.1021/jm00080a016. PMID 1732548.

[3] “Effect of zatosetron on ipecac-induced emesis in dogs and healthy men”. Journal of Clinical Pharmacology 34 (3): 250-4. (March 1994). doi:10.1002/j.1552-4604.1994.tb03994.x. PMID 7517409.

[4] “General pharmacology of a new potent 5-hydroxytryptamine antagonist”. Arzneimittel-Forschung 41 (3): 189-95. (March 1991). PMID 1867653.

[5] “Chronic toxicity of zatosetron, a 5-HT3 receptor antagonist, in rhesus monkeys”. Drug and Chemical Toxicology 18 (1): 61-82. (February 1995). doi:10.3109/01480549509017858. PMID 7768200.

[6] “Pilot study of zatosetron (LY277359) maleate, a 5-hydroxytryptamine-3 antagonist, in the treatment of anxiety”. Journal of Clinical Psychopharmacology 19 (2): 125-31. (April 1999). doi:10.1097/00004714-199904000-00006. PMID 10211913.

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関連項目[編集]

出典[編集]