Abstract
The research is dedicated to in-depth study of neurotrophic and antiepileptic properties of original potential anticonvulsant agents from 4-thiazolidinones – LES-2658 (5-(3-nitro-benzylidene)-2-(thiazol-2-ylimino)-thiazolidin-4-one) and LES-1205 ([2,4-dioxo-5-(thiazol-2-ylcarbamoylmethyl)-thiazolidin-3-yl]-acetic acid ethyl ester), synthesized at the Department of Pharmaceutical, Organic and Bioorganic Chemistry of Danylo Halytsky Lviv National Medical University, Ukraine. Studying of sleep - wakefulness cycle characteristics in animals with chronic epileptic syndrome in conditions of 4-thiazolidinones derivatives LES-2658 and LES-1205 use was performed. The kindling syndrome was induced in Wistar rats via daily pentylenetetrazol (PTZ) (30 mg/kg, i.p.) administrations during three weeks and sleep - wakefulness cycle was studied under conditions of LES-2658 and LES-1205 administrations at doses 25.0and 100.0 mg/kg i.p.. Total wakefulness, non - rapid eye movement sleep, rapid eye movement sleep, falling asleep latency, REM - onset latency and also number of REM sleep episodes have been determined by behavioral characteristics of experimental animals. It was established that 4-thiazolidinone derivatives Les-1205 and Les-2658 reduce REM sleep fragmentation and increase its duration in PTZ-kindled rats. Les-1205 compound at dose 100.0 mg/kg show a clear correcting influence on kindling - induced sleep disturbances.
Highlights
Epilepsy is the most common neurological disorder and its prevalence worldwide is estimated at 0.5–1 % [1]
The durations of total wakefulness, non-rapid eye movement sleep (NREM) and rapid eye movement sleep (REM) sleep were given in % compared to the overall experiment duration (100 %); falling asleep latency (FAL) and REM – onset latency (RL) in minutes
The changes were observed in sleep pattern of experimental animals under kindling conditions
Summary
Epilepsy is the most common neurological disorder and its prevalence worldwide is estimated at 0.5–1 % [1]. Despite the substantial progress in research and development of efficient anticonvulsants the search of new original anticonvulsant agents remains still open problem, especially in the context of pharmacoresistance and significant side effects under long use [3, 4]. The model of chronic epileptization of brain formed by repeated application of a subthreshold dose of pentylenetetrazol (PTZ) adequately reflects the signs of clinical forms of disease, including the disorders of sleep – wakefulness cycle [5, 6]. The study of the cycle allows estimate the brain mechanisms that control anxiety, to solve which mechanisms ensure its individual phases and to assess the influence of pharmacological agents on brain structure [5, 6].
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