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.
D000818:Animals; D001711:Biotransformation; D001921:Brain / Q000378:metabolism; D002250:Carbon Radioisotopes; D002794:Choline / Q000096:biosynthesis; D002855:Chromatography, Thin Layer; D003510:Cyclohexanes / Q000378:metabolism*; D003642:Deanol / Q000378:metabolism*; D004983:Ethanolamines / Q000378:metabolism*; D007668:Kidney / Q000378:metabolism; D007700:Kinetics; D008099:Liver / Q000378:metabolism; D008168:Lung / Q000378:metabolism; D010743:Phospholipids / Q000378:metabolism; D011422:Propionates / Q000378:metabolism*; D051381:Rats; D013552:Swine
D002250:Carbon Radioisotopes; D003510:Cyclohexanes; D004983:Ethanolamines; D010743:Phospholipids; D011422:Propionates; D003642:Deanol; D002794:Choline