Biokinetics of gidazepam, derivatives of peptideaminobenzophenones and their metabolites.

Results of a comparative study of biokinetics of two prodrugs gidazepam (I) and the derivative of peptideaminobenzophenone, 2-N-carbobenzylglycyl-glycylamido-5-bromobenzophenone (II) and their main physiologically active metabolite-7-brom-5-phenyl-dihydro-3H-1,4-benzodiazepine (III) were investigated in mice. It was shown earlier that I undergoes intensive N1-desalkylation with the formation of a metabolite: (III) and products of its further oxidation. Metabolism of II is characterized by hydrolysis of the peptide fragment and subsequent intramolecular condensation resulting in the formation of III, its oxi- and metoxylated derivatives and other minor metabolites.

[Biokinetics of a new prodrug gidazepam and its metabolite].

Pharmacodynamics and pharmacokinetics of a novel tranquilizing agent--gidazepam (I), a prodrug, and its physiologically active metabolite--7-bromo-5-phenyl-1,2-di-hydro-3H-1,4- benzodiazepine-2-one (II) in mice organism were studied. The form of relationship was determined between the dynamics of the anticonvulsant effect of labelled (2-14C-) I and II and the kinetics of the content of 14C-compounds in the experimental animals brain. It was noted that the biophase of the effect and the effector fragment of the scheme of biokinetics for I and II are identical.