Sivachenko A. Comparative pharmacological characteristics cynazepam and gidazepam - prodrugs of the 1,4-benzodiazepine structures

The dissertation is devoted to studying a neuropharmacologycal spectrum of action of a new tranquilizer - cynazepam, prodrug gidazepam and their active metabolites. Studying of pharmacological effects of the cynazepam has shown, that the given preparation has characteristic for tranquilizers a spectrum of activity, possesses high anticonvulsion activity in relation to convulsions of different mechanism of origin, sedative and myorelaxive the effects similar to action phenazepam. The contents 3-oximetabolites in the brain of mice on the order exceed a level of an initial preparation. It is revealed high antiepileptic effect of the cynazepam and gidazepam on experimental models of epilepsy, the caused application of the strychnine and tiosemikarbazide. The izodynamical analysis of dependences a "doze effect" and "time - effect" MED of strychnine has revealed insignificant increase of effect and fast achievement of the maximal effect already at small dozes, irrespective of structure of entered connection.The comparative pharmacological characteristic of the cynazepam is resulted, gidazepam and them metabolites and the place of new prodrugs - of the cynazepam is determined in a number of other tranquilizers 1,4-benzodiazepine lines.