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Flumexadol is a selective 5-HT2C receptor agonist with an affinity (Ki) of 25 nM for the (+)-enantiomer and exhibits 40-fold selectivity over the 5-HT2A receptor. It is an orally active, non-narcotic analgesic.
Description | Flumexadol is a selective 5-HT2C receptor agonist with an affinity (Ki) of 25 nM for the (+)-enantiomer and exhibits 40-fold selectivity over the 5-HT2A receptor. It is an orally active, non-narcotic analgesic. |
Targets&IC50 | 5-HT2C receptor:25 nM (ki) |
In vivo | In rats and dogs dosed with 14C-Flumexadol (CERM1841), the 14C is primarily excreted in the urine. The 14C eliminated in the feces of dogs is significantly higher than that for rats. Conjugated metabolites, mostly glucuronides, accounted for the majority of the urinary radioactivity in both species. Biotransformation products are predominantly acids in both species, followed by substantial amounts of basic metabolites, with minimal neutral substances. The major urinary metabolites in rats are 3-trifluoromethylbenzoic acid and 3-trifluoromethylhippuric acid, whereas in dogs, the major metabolite is 3-trifluoromethylmandelic acid, along with 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 former predominating. |
Molecular Weight | 231.21 |
Formula | C11H12F3NO |
Cas No. | 30914-89-7 |
Relative Density. | 1.2081 g/cm3 (Estimated) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (432.51 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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