Zatosetron

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]

Zatosetron
Clinical data
ATC code
  • none
Identifiers
  • 5-chloro-2,2-dimethyl-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2,3-dihydro-1-benzofuran-7-carboxamide
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC19H25ClN2O2
Molar mass348.87 g·mol−1
3D model (JSmol)
  • CC1(Cc2cc(cc(c2O1)C(=O)N[C@H]3C[C@H]4CC[C@@H](C3)N4C)Cl)C
  • InChI=1S/C19H25ClN2O2/c1-19(2)10-11-6-12(20)7-16(17(11)24-19)18(23)21-13-8-14-4-5-15(9-13)22(14)3/h6-7,13-15H,4-5,8-10H2,1-3H3,(H,21,23)/t13-,14+,15-
  • Key:SPKBYQZELVEOLL-QDMKHBRRSA-N
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See also

References
  1. Cohen ML, Bloomquist W, Gidda JS, Lacefield W (July 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.
  2. Robertson DW, Lacefield WB, Bloomquist W, Pfeifer W, Simon RL, Cohen ML (January 1992). "Zatosetron, a potent, selective, and long-acting 5HT3 receptor antagonist: synthesis and structure-activity relationships". Journal of Medicinal Chemistry. 35 (2): 310–9. doi:10.1021/jm00080a016. PMID 1732548.
  3. Schwartz SM, Goldberg MJ, Gidda JS, Cerimele BJ (March 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. S2CID 23486859.
  4. Smith WT, Londborg PD, Blomgren SL, Tollefson GD, Sayler ME (April 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.
  5. Williams PD, Calligaro DO, Colbert WE, Helton DR, Shetler T, Turk JA, Jordan WH (March 1991). "General pharmacology of a new potent 5-hydroxytryptamine antagonist". Arzneimittel-Forschung. 41 (3): 189–95. PMID 1867653.
  6. Bendele A, Means J, Shoufler J, Schmalz C, Hanasono G, Symanowski J, Adams E (February 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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