Lurosetron
Lurosetron (GR-87442) is a 6-fluoro analogue of Alosetron. 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].
Product Specifications
CAS Number
128486-54-4
Product Name Alternative
GR-87442
UNSPSC
12352005
Target
5-HT Receptor
Type
Reference compound
Related Pathways
GPCR/G Protein; Neuronal Signaling
Applications
Neuroscience-Neuromodulation
Field of Research
Neurological Disease
Assay Protocol
https://www.medchemexpress.com/lurosetron.html
Smiles
O=C1C2=C(CCN1CC3=C(NC=N3)C)N(C)C4=C2C=CC=C4F
Molecular Formula
C17H17FN4O
Molecular Weight
312.34
References & Citations
[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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
Lactoferrin
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