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Zatosetron
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| Systematic (IUPAC) name | |
| 5-chloro-2,2-dimethyl-N-(8-methyl-8-azabicyclo[3.2.1]octan-3-yl)-3H-1-benzofuran-7-carboxamide | |
| Identifiers | |
| CAS number | |
| ATC code | ? |
| PubChem | |
| Chemical data | |
| Formula | C19H25ClN2O2 |
| Mol. mass | 348.867 g/mol |
| SMILES | & |
| Synonyms | Zatosetron |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
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| Legal status | |
| Routes | ? |
Zatosetron (LY-277,359) is a drug which acts as an antagonist at the 5HT3 receptor1 It is orally active and has a long duration of action, producing antinauseant effects but without stimulating the rate of gastrointestinal transport.23 It is also an effective anxiolytic in both animal studies and human trials,4 although with some side effects at higher doses.56
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References
- ^ Cohen ML, Bloomquist W, Gidda JS, Lacefield W. LY277359 maleate: a potent and selective 5-HT3 receptor antagonist without gastroprokinetic activity. Journal of Pharmacology and Experimental Therapeutics. 1990 Jul;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. 1992 Jan 24;35(2):310-9. PMID 1732548
- ^ Schwartz SM, Goldberg MJ, Gidda JS, Cerimele BJ. Effect of zatosetron on ipecac-induced emesis in dogs and healthy men. Journal of Clinical Pharmacology. 1994 Mar;34(3):250-4. PMID 7517409
- ^ 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. 1999 Apr;19(2):125-31. PMID 10211913
- ^ Williams PD, Calligaro DO, Colbert WE, Helton DR, Shetler T, Turk JA, Jordan WH. General pharmacology of a new potent 5-hydroxytryptamine antagonist. Arzneimittelforschung. 1991 Mar;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. 1995 Feb;18(1):61-82. PMID 7768200
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- This page was last modified on 26 July 2008, at 01:40.
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