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Zatosetron
Sign in to saveZatosetron (LY-277,359) is a drug which acts as an antagonist at the 5HT3 receptor It is orally active and has a long duration of action, producing antinauseant effects but without stimulating the rate of gastrointestinal transport. It is also an effective anxiolytic in both animal studies and human trials, although with some side effects at higher doses.
Chemical data
- Formula
- C19H25ClN2O2
- Molecular weight
- 348.9 g/mol
- IUPAC name
- 5-chloro-2,2-dimethyl-N-(8-methyl-8-azabicyclo[3.2.1]octan-3-yl)-3H-1-benzofuran-7-carboxamide
- SMILES
- CC1(CC2=C(O1)C(=CC(=C2)Cl)C(=O)NC3CC4CCC(C3)N4C)C
- InChIKey
- SPKBYQZELVEOLL-UHFFFAOYSA-N
- XLogP
- 3.7
- Polar surface area
- 41.6 Ų
- H-bond donors
- 1
- H-bond acceptors
- 3
- Formal charge
- 0
via PubChem
Research
28 papers- Disposition of zatosetron, a serotonin (5-HT3) receptor antagonist, in humans.Drug metabolism and disposition: the biological fate of chemicals · 1993
- In vitro metabolism of zatosetron. Interspecies comparison and role of CYP 3A.Drug metabolism and disposition: the biological fate of chemicals · 1994
- Zatosetron, a 5-HT3 receptor antagonist in a multicenter trial for acute migraine.Neuropharmacology · 1994
- Zatosetron, a potent, selective, and long-acting 5HT3 receptor antagonist: synthesis and structure-activity relationships.Journal of medicinal chemistry · 1992
- Effect of zatosetron on ipecac-induced emesis in dogs and healthy men.Journal of clinical pharmacology · 1994
via PubMed
Wikidata facts
- Subclass of
- chemical compound
- Mass
- 348.160456
Show 3 more facts
- chemical formula
- C₁₉H₂₅ClN₂O₂
- canonical SMILES
- CC1(CC2=C(O1)C(=CC(=C2)Cl)C(=O)NC3CC4CCC(C3)N4C)C
- subject has role
- serotonin antagonist
Sources (1)
via Wikidata · CC0
~1 min read
Encyclopedic overview
2 sectionsContents
- See also
- References
Zatosetron (LY-277,359) is a drug which acts as an antagonist at the 5HT3 receptor It is orally active and has a long duration of action, producing antinauseant effects but without stimulating the rate of gastrointestinal transport. It is also an effective anxiolytic in both animal studies and human trials, although with some side effects at higher doses.
== See also == Ondansetron Bemesetron Granisetron Ricasetron Tropanserin Tropisetron
Excerpted from Wikipedia’s “Zatosetron” article, available under the CC BY-SA 4.0 licence.