Противосудорожная и мембранотропная активность соединения РУ-1205

The anticonvulsant activity of benzimidazole derivative RU-1205 (9-(2-morpholinoethyl)-2-(4-fluorophenyl)imidazo[1,2- a ]benzimidazole dihydrochloride) in comparison to reference drug (carbamazepine) was studied using the test of maximal electroshocki (MES) nduced convulsions in mice. The ED 50 values for RU-1205 and carbamazepine were found to be 11.4 and 14.1 mg/kg (i.p.), respectively. The antiepileptiform activity of RU-1205 (23.7 mM) was determined by the method of direct cortical stimulation in conscious rats (voltage, 120 V; frequency 50 Hz; duration 10 sec). Compound RU-1205 in a concentration of 23.7 μM effectively suppressed the electro-induced seizures and restored the normal rhythmogenesis of the neuronal columns of the somatosensory cortex. The reversible inhibition of sodium ( I Na ) and calcium ( I Ca ) ion currents by RU-1205 at concentrations of 1, 10, 100, and 1000 μM was studied by method of intracellular dialysis and membrane potential on isolated neurons of Lymnaea stagnalis snall. Compound RU-1205 at 1000 μM concentration produced maximum reversible suppression of both ion currents by 77.0 and 58.7%, respectively ( p < 0.05).