Flumexadol

Flumexadol is a selective and affinity 5-HT 2C receptor agonist with a K i of 25 nM for the (+)-enantiomer of Flumexadol, and is 40-fold selective over the 5-HT 2A receptor. Flumexadol is an orally active non-narcotic analgesic In Vivo In rats and dogs dosed with 14 C-Flumexadol (CERM1841), the 14 C is excreted in the urine. The 14 C eliminated in the faeces of dog is significantly higher than for rat. Conjugated metabolites, mostly glucuronides, accounted for the greater part of the urinary radioactivity in both species. Biotransformation products are predominantly acids in both species, follows by significant amounts of basic metabolites, with very little neutral substances. The major urinary metabolite in rats is 3-trifluoromethylbenzoic acid and 3-trifluoromethylhipuric acid. In the dog it is 3-trifluoromethylmandelic acid in addition to the benzoic acid and its conjugate. The basic products identified in the urine of both species are unchanged drug and 1-amino-2-hydroxy-2-(3-trifluoromethylphenyl)ethane, with the first predominating. MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:5-HT 2C Receptor 25 nM (Ki)

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