Zatosetron

Zatosetron

Zatosetron
Systematic (IUPAC) name
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
?
Identifiers
CAS number
ATC code None
PubChem
ChemSpider
UNII  YesY
Chemical data
Formula C19H25ClN2O2 
Mol. mass 348.867 g/mol
 YesY   

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

  1. ^ 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.  
  2. ^ 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.  
  3. ^ 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.  
  4. ^ 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.  
  5. ^ 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.  
  6. ^ 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.