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| | Flumexadol Basic information |
| Product Name: | Flumexadol | | Synonyms: | Flumexadol;1841CERM;2-(α,α,α-Trifluoro-m-tolyl)morpholine;CERM-1841;Morpholine, 2-[3-(trifluoromethyl)phenyl]-;2-[3-(Trifluoromethyl)phenyl]morpholine | | CAS: | 30914-89-7 | | MF: | C11H12F3NO | | MW: | 231.21 | | EINECS: | | | Product Categories: | | | Mol File: | 30914-89-7.mol |  |
| | Flumexadol Chemical Properties |
| 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 |
| | Flumexadol Usage And Synthesis |
| 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. div> | | target | | 5-HT 2C Receptor 25 nM (Ki) | | | IC 50 | 5-HT2C 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 |
| | Flumexadol Preparation Products And Raw materials |
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