128486-54-4
Chemical Structure
Lurosetron
Synonym(s): GR-87442
- CAS No.: 128486-54-4
- Formula:C17H17FN4O
- Molecular Weight:312.34
IUPAC Name: 6-fluoro-5-methyl-2-((5-methyl-1H-imidazol-4-yl)methyl)-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indol-1-one
InChIKey: NUMKWGDDRWJQMY-UHFFFAOYSA-N
SMILES: O=C1C2=C(CCN1CC3=C(NC=N3)C)N(C)C4=C2C=CC=C4F
Biological Activity: 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].
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Lurosetron | 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.. | |||||||||||||||||||||
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- [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. [Content Brief]
Keywords
