Lerisetron

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IUPAC_name = 1-(phenylmethyl)-2-piperazin-1-ylbenzimidazole


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CAS_number = 143257-98-1
synonyms = Lerisetron
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PubChem = 65997
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C = 18 | H = 20 | N = 4
molecular_weight = 292.378 g/mol
smiles = C1CN(CCN1)C2=NC3=CC=CC=C3N2CC4=CC=CC=C4
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Lerisetron (F-0930-RS) is a drug which acts as an antagonist at the 5HT₃ receptor [Orjales A, Mosquera R, Labeaga L, Rodes R. New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation. "Journal of Medicinal Chemistry". 1997 Feb 14;40(4):586-93. PMID 9046349] It is a potent antinauseant [Gomez-de-Segura IA, Grande AG, De Miguel E. Antiemetic effects of Lerisetron in radiation-induced emesis in the dog. "Acta Oncologica". 1998;37(7-8):759-63. PMID 10050999] [Cooper M, Sologuren A, Valiente R, Smith J. Effects of lerisetron, a new 5-HT3 receptor antagonist, on ipecacuanha-induced emesis in healthy volunteers. "Arzneimittelforschung". 2002;52(9):689-94. PMID 12404884] and is currently in clinical trials for the treatment of nausea associated with cancer chemotherapy. [Huckle R. Lerisetron. FAES. "Current Opinion in Investigational Drugs". 2003 Jul;4(7):874-7. PMID 14619411]

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