L.E. Borodkina, V.V. Bagmetova, I.N. Tyurenkov

Many structural analogues and derivatives of GABA possess neuroprotective activity - phenotropil, phenibut, pikamilon, and others. On their base there were worked out anticonvulsants: vigabatrin, gabapentin, pregabalin. The creation of compositions of linear and cyclic GABA analogues with organic carboxylic acids proved to cause potentiation of pharmacological action of the base substance. The comparative study of neuroprotective and anticonvulsant action of cyclic analogues of GABA pyracetam, phenotropil and phepiron, as well as the new compositions of phepiron with organic carboxylic acids: citric, succinic, glutaminic, and nicotinic. The experiments were carried out on white non-linear male rats using models of primarily generalized epilepsy: 1) electroconvulsive shock with the evaluation of the influence of substances and compositions on the intensity of convulsions and behavioral state of animals in the open field, conditioned avoidance response and extrapolatory deliverance tests; 2) maximal electric shock with the evaluation of the influence on the duration of coma of clonic and tonic phases, as well as on the general convulsions duration. Statistical results analysis: Kruskal - Wallis, Newman-Keuls, chi square criteria. The cyclic analogues of GABA phenotropil > phepiron > pyracetam, as well as the compositions of phepiron with succinic > citric > nicotinic, glutaminic acids possess anticonvulsant, neuroprotective and nootropic properties on convulsions models caused by electric shock: they reduce the intensity of convulsive disorder, postconvilsive disorders of locomotor, exploratory behavior behavior and cognitive functions. The composition of phepiron with citric and, to a greater extent, with succinic acid surpass pyracetam, the base substance, in effectiveness; and phenotropil in the influence on a number of rates, which makes them perspective for the further study in the capacity of neuroprotectors.