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Brain Uptake and Biotransformation of Remacemide Hydrochloride, a Novel Anticonvulsant

Brain Uptake and Biotransformation of Remacemide Hydrochloride, a Novel Anticonvulsant

H Heyn, D J McCarthy, S H Curry, M S Eisman, M W Anders

Drug Metab Dispos. May-Jun 1994;22(3):443-6.

PMID: 8070322

Abstract:

The brain uptake and biotransformation of remacemide hydrochloride [(+/-)-2-amino-N-(1-methyl-1,2-diphenylethyl)acetamide monohydrochloride; FPL 12924AA] were studied in the rat. The brain uptake indices (BUI) for remacemide and its pharmacologically active metabolite FPL12495 [(+/-)-1-methyl-1,2-diphenylethylamine monohydrochloride] were 51 and 130%, respectively. The BUI of [14C] remacemide and [14C]FPL12495 were not affected by increasing amounts of unlabeled remacemide or FPL12495, respectively. Likewise, the BUI of remacemide was not affected by dl-amphetamine or beta-phenethylamine. A mixture of [3H]remacemide hydrochloride (3H label in the glycine moiety) and [14C]remacemide hydrochloride (14C label in 1,2-diphenyl-2-aminopropane moiety) was administered by intracarotid injection. The ratio of 14C/3H in the brain was equal to that in the injection mixture, indicating that remacemide enters the brain intact. HPLC analysis of brain extracts of rats given [14C] remacemide hydrochloride by intracarotid injection revealed that 97.8 +/- 0.2% (mean +/- SD) of the radioactivity was present as remacemide, whereas 1.9 +/- 0.2% of the radioactivity was present as FPL12495. Finally, in vitro studies revealed that remacemide is hydrolyzed by whole-brain homogenates to the pharmacologically active metabolite FPL12495. Data indicate that remacemide enters the brain by passive diffusion and undergoes deglycination at the blood-brain barrier or within the brain to give FPL12495.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP111686794	Remacemide hydrochloride		111686-79-4	Price

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