Lerisetron

Lerisetron (code name F-0930-RS) is a drug which acts as an antagonist at the 5-HT3 receptor.[1] It is a potent antiemetic[2][3] and was in clinical trials for the treatment of nausea associated with cancer chemotherapy.[4]

Lerisetron
Clinical data
Other namesF-0930-RS
ATC code
  • None
Identifiers
IUPAC name
  • 1-Benzyl-2-piperazin-1-yl-1H-benzimidazole
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC18H20N4
Molar mass292.386 g·mol−1
InChI
  • InChI=1S/C18H20N4/c1-2-6-15(7-3-1)14-22-17-9-5-4-8-16(17)20-18(22)21-12-10-19-11-13-21/h1-9,19H,10-14H2 Y
  • Key:PWWDCRQZITYKDV-UHFFFAOYSA-N Y
 NY (what is this?)  (verify)

See also

References

  1. Orjales A, Mosquera R, Labeaga L, Rodes R (February 1997). "New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation". Journal of Medicinal Chemistry. 40 (4): 586–93. doi:10.1021/jm960442e. PMID 9046349.
  2. Gomez-de-Segura IA, Grande AG, De Miguel E (1998). "Antiemetic effects of Lerisetron in radiation-induced emesis in the dog". Acta Oncologica. 37 (7–8): 759–63. doi:10.1080/028418698430160. PMID 10050999.
  3. Cooper M, Sologuren A, Valiente R, Smith J (2002). "Effects of lerisetron, a new 5-HT3 receptor antagonist, on ipecacuanha-induced emesis in healthy volunteers". Arzneimittel-Forschung. 52 (9): 689–94. doi:10.1055/s-0031-1299952. PMID 12404884.
  4. Huckle R (July 2003). "Lerisetron. FAES". Current Opinion in Investigational Drugs. 4 (7): 874–7. PMID 14619411.
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