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Flumexadol

CAS No.30914-89-7
Chemical Name:Flumexadol
CBNumber:CB51178778
Molecular Formula:C11H12F3NO
Formula Weight:231.21
MOL File:30914-89-7.mol

Flumexadol Property

Boiling point 132 °C(Press: 10 Torr)
Density 1.2081 (estimate)
storage temp. Store at -20°C
solubility DMSO: 100 mg/mL (432.51 mM)
pka 8.41±0.40(Predicted)
form Liquid
color Colorless to light yellow
FDA UNII V9783UEL0F

Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal wordDanger
Hazard statements H318-H315-H312-H332-H335-H302
Precautionary statements P280-P305+P351+P338-P310-P261-P271-P304+P340-P312-P264-P270-P301+P312-P330-P501-P264-P280-P302+P352-P321-P332+P313-P362-P280-P302+P352-P312-P322-P363-P501

Flumexadol Chemical Properties,Usage,Production

Uses Flumexadol is a selective and affinity 5-HT2C receptor agonist with a Ki of 25 nM for the (+)-enantiomer of Flumexadol, and is 40-fold selective over the 5-HT2A receptor. Flumexadol is an orally active non-narcotic analgesic[1][2].
Biological Activity Flumexadol is an orally active non-narcotic analgesic. It is a selective and affinity agonist of the 5-HT2C receptor with a Ki of 25 nM for the (+)-enantiomer of Flumexadol, 40-fold more selective than the 5-HT2A receptor.
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.}

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target

5-HT _2C Receptor

25 nM (Ki)
IC 50 5-HT_2C Receptor: 25 nM (Ki)
References [1] Hache J, et al. The pharmacology of 1841 CERM, a new analgesic. Arzneimittelforschung. 1978;28(4):642-5. PMID:312104
[2] Nilsson BM. 5-Hydroxytryptamine 2C (5-HT2C) receptor agonists as potential antiobesity agents. J Med Chem. 2006 Jul 13;49(14):4023-34. DOI:10.1021/jm058240i
[3] Kucharczyk N, et al. Metabolites of 2-(3-trifluoromethylphenyl)tetrahydro-1,4-oxazine (CERM) 1841) in rats and dogs. Xenobiotica. 1979 Nov;9(11):703-11. DOI:10.3109/00498257909042338