Zatosetron
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Zatosetron
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
ATC code ?
Chemical data
Mol. mass 348.867 g/mol
SMILES &
Synonyms Zatosetron
Pharmacokinetic data
Therapeutic considerations
Routes ?
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]
This pharmacology-related article is a stub. You can help Wikipedia by expanding it.[edit] 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
