Показано, что механизм действия соединения С-3 связан с активацией эффектов ГАМК-ергической системы, о чем свидетельствует увеличение содержания ГАМК в гомогенате головного
мозга крыс и уменьшение ферментативной активности ГАМК-Т. В концентрации 10-5 М макрогетероцикл способен на 50 % снижать связывание 3Н-ГАМК с мембранами фракции клеток головного мозга крыс. При сопоставлении противосудорожной активности соединения С-3 с эталонными препаратами оказалось, что ЕД50 макроцикла по методу «антагонизма с коразолом» ниже
на порядок ЕД50 дифенилгидантоина и депакина.
The aim of the work is the investigation of the GABA-ergic system role and antiseizure effects in
macrogeterocycle C-3 neurotropic effects realization.The experiments were performed on 3-month Wistar rats weighting 160–180 g and mice weighting
18–20 g.
The data obtained revealed that C-3 psychotropic activity characterizes by anticonvulsive activity
wide spectrum appearance that is quite definite from compounds with nootropic activity. Macrogeterocycle C-3 has also expressed antiamnestic efficacy.
It was shown that mode of action of compound C-3 is due to the activation of GABA-ergic system,
that confirmed by the increase of GABA content and the decrease of enzymatic activity of GABA-T in
rats brain gomogenate. The main effects of C-3 (antiamnesic, anticonvulsant) are diminished by bicuculline. Compoud C-3 in concentration of 10-5 M on 50% decreases the binding of 3H-GABA with membrane fraction of rats brain cells. Compound C-3 is more effective by its anticonvulsant activity than
that of reference drugs of depakine and diphenylgidantoine. One could conclude that one of the possible mechanism of macrogeterocycle C-3 psychotropic effects realization is GABA molecule presence that could induce its direct interaction with brain GABA-ergic receptors.
