Zatosetron
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| Systematic (IUPAC) name | |
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| 5-chloro-2,2-dimethyl-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2,3-dihydro-1-benzofuran-7-carboxamide | |
| Clinical data | |
| Legal status |
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| Identifiers | |
| CAS number | 123482-22-4 |
| ATC code | None |
| PubChem | CID 60763 |
| ChemSpider | 54761 |
| UNII | 901MC95XSB  |
| Chemical data | |
| Formula | C19H25ClN2O2 |
| Mol. mass | 348.867 g/mol |
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Zatosetron (LY-277,359) is a drug which acts as an antagonist at the 5HT3 receptor[1] It is orally active and has a long duration of action, producing antinauseant effects but without stimulating the rate of gastrointestinal transport.[2][3] It is also an effective anxiolytic in both animal studies and human trials,[4] although with some side effects at higher doses.[5][6]
References[edit]
- ^ Cohen, ML; Bloomquist, W; Gidda, JS; Lacefield, W (1990). "LY277359 maleate: a potent and selective 5-HT3 receptor antagonist without gastroprokinetic activity". The Journal of Pharmacology and Experimental Therapeutics 254 (1): 350–5. PMID 2366187.
- ^ Robertson, DW; Lacefield, WB; Bloomquist, W; Pfeifer, W; Simon, RL; Cohen, ML (1992). "Zatosetron, a potent, selective, and long-acting 5HT3 receptor antagonist: synthesis and structure-activity relationships". Journal of Medical Chemistry 35 (2): 310–9. doi:10.1021/jm00080a016. PMID 1732548.
- ^ Schwartz, SM; Goldberg, MJ; Gidda, JS; Cerimele, BJ (1994). "Effect of zatosetron on ipecac-induced emesis in dogs and healthy men". Journal of clinical pharmacology 34 (3): 250–4. doi:10.1002/j.1552-4604.1994.tb03994.x. PMID 7517409.
- ^ Smith, WT; Londborg, PD; Blomgren, SL; Tollefson, GD; Sayler, ME (1999). "Pilot study of zatosetron (LY277359) maleate, a 5-hydroxytryptamine-3 antagonist, in the treatment of anxiety". Journal of Clinical Psychopharmacology 19 (2): 125–31. doi:10.1097/00004714-199904000-00006. PMID 10211913.
- ^ Williams, PD; Calligaro, DO; Colbert, WE; Helton, DR; Shetler, T; Turk, JA; Jordan, WH (1991). "General pharmacology of a new potent 5-hydroxytryptamine antagonist". Arzneimittel-Forschung 41 (3): 189–95. PMID 1867653.
- ^ Bendele, A; Means, J; Shoufler, J; Schmalz, C; Hanasono, G; Symanowski, J; Adams, E (1995). "Chronic toxicity of zatosetron, a 5-HT3 receptor antagonist, in rhesus monkeys". Drug and chemical toxicology 18 (1): 61–82. doi:10.3109/01480549509017858. PMID 7768200.
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