Исследовали влияние предварительного введения изопикамилона (ИП) и пикамилона (П) при формировании пикротоксин-вызванной судорожной активности на поведенческие проявления у мышей и поведенческие и электроэнцефалографические параметры у крыс. Выявили увеличение латентного периода и уменьшение интенсивности судорог при введении ИП и П в дозах от 10 до 100 мг/кг. При увеличении дозы до 50–100 мг/кг ИП оказывал более значительное противосудорожное действие. Показали, что введение крысам этих двух препаратов уже в дозе 20 мг/кг предотвращает генерацию генерализованных иктальных разрядов с развитием тяжелых клонико-тонических судорог. Введение ИП в дозе 50 мг/кг у крыс приводило к более эффективному уменьшению интенсивности судорог на фоне значительного снижения частоты и длительности генерализованных эпилептиформных разрядов по сравнению с П.
The investigation of neurotropic drugs — GABA-derivatives effects seems to be interesting especially taking into consideration that GABA participates in CNS functional activity regulation as well as in the cerebral circulation. Additionally it was shown its ability to penetrate through the blood-brain barrier. Both ‘picamilon’ (P) and ‘isopicamilon’ (IP) compounds were synthesized on the background of GABA. The aim of the work — the investigation of both P and IP influences on mice’s and rat’s behavioural and EEG effects under conditions of picrotoxin-induced generalized convulsive syndrome.Trials were performed in conditions of acute and chronic experiment using picrotoxin as traditional convulsive compound that decreases the GABA-induced inhibition. The experimental trials were performed via two series. The 1st devoted to mice’s behavioural convulsive
response reactions investigation after P and IP administration in the range 10–100 mg/kg. The 2nd part of the trial was devoted to rats picrotoxin-induced convulsive activity EEG registration after P and IP preliminary administration in the same dosages. It was shown that IP and P in doses 20–100 mg/kg increase the latency and diminish the intensity of seizures in mice. IP has more expressed anticonvulsant effect that has dosedependent character. Both pharmacons preliminary injections in a dose 20 mg/kg resulted in the prevention of generalized ictal discharges generation with subsequent severe clonic-tonic seizures development in rats. IP in a dose 50 mg/kg was more effective in this set of trials revealing the considerable decreasing of frequency and duration of rat’s generalized epileptiform discharges in comparison with P.
