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.}

target

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