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128486-54-4

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128486-54-4 Structure

128486-54-4 Structure

Identification	Back Directory
[Name] Lurosetron
[CAS] 128486-54-4
[Synonyms] Lurosetron Lurosetron [inn:ban] 6-fluoro-5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-3,4-dihydropyrido[4,3-b]indol-1-one 1H-Pyrido[4,3-b]indol-1-one, 6-fluoro-2,3,4,5-tetrahydro-5-methyl-2-[(4-methyl-1H-imidazol-5-yl)methyl]-
[Molecular Formula] C17H17FN4O
[MDL Number] MFCD00865544
[MOL File] 128486-54-4.mol
[Molecular Weight] 312.34

Chemical Properties	Back Directory
[Boiling point ] 650.1±55.0 °C(Predicted)
[density ] 1.40±0.1 g/cm3(Predicted)
[pka] 14.01±0.10(Predicted)

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[Uses] Lurosetron (GR-87442) is a 6-fluoro analogue of Alosetron (HY-70050A). Lurosetron is a serotonin 5-HT3 receptor antagonist. Lurosetron inhibits recombinant (rbt) CYP1A2, with an IC50 of 0.1 μM. Lurosetron also inhibits other CYP isoforms, including rbtCYP2C9 and rbtCYP3A4 with IC50s ranging between 3.5 μM and 16 μM.[1].
[IC 50] 5-HT₃ Receptor
[References] [1] Somers GI, et al. The metabolism of the 5HT3 antagonists ondansetron, alosetron and GR87442 I: a comparison of in vitro and in vivo metabolism and in vitro enzyme kinetics in rat, dog and human hepatocytes, microsomes and recombinant human enzymes. Xenobiotica. 2007 Aug;37(8):832-54. DOI:10.1080/00498250701485575

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