Pharmacokinetic study of maleate acid of 2-(N,N-dimethylaminoethanol-14C1)-cyclohexylpropionate (cyprodenate) and of N,N-dimethylaminoethanol-14C1 in animals

The study of the biotransformation of 2-(N,N-dimethylaminoethanol)-cyclohexylpropionate-meleate acid (cyprodenate, Actebral), a psychotonic brain stimulant, was carried out on two species of Animals (rats and pigs) with the aid of 14C-labelled molecules. Following i.v. administration in rats it was found that 14C-cyprodenate diffuses very rapidly to the principal organs (liver, brain, kidneys) preceding a hydrolysis which gives 14C-dimethylaminoethanol (DMAE). The latter undergoes N-oxidation but the major portion of DMAE goes directly into the metabolic cycle of the Phospholipids up to the formation of 14C-choline, as shown in the metabolic scheme proposed by the authors that identifies the principal labelled intermediaries: 14C-phosphoryl-DMAE (P-DMAE), 14C-glycerophosphatidyl-N,N-dimethylethanolamine (GP-DMAE), 14C-glycerophosphatidyl-choline (GP-choline). Similar results were found with the oral administration of 14C-cyprodenate in pigs, thus showing a more intense participation of the product at the level of the intermediary metabolism of Phospholipids, precursors of choline.