P-912 - new Sulfonamide With Neurotropic Activity

Abstract

Objectives

Activation of nociceptive system often leads to nervous regulation disorders resulting in convulsive attacks. Meanwhile, it has been established that certain medications with analgesic effect can intensify convulsive attacks. In this connection, there arises a problem of searching for new compounds with antinociceptive and anticonvulsive effects. In current investigation we studied new endo-2-aminomethylbicyclo[2.2.1]hept-5-en derivative with sulfonamide and sulfolan fragment.

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Methods

Experiments were carried out upon white mice (22–28 g). Acute toxicity (LD50) determined by Prozorovsky modification of Litchfield & Wilcoxon method, is 730 mg/kg. Analgesic effect of the compound has been investigated by the “hot plate” method at 55°C, the data obtained were compared to initial background. Anticonvulsive activity has been established under corazole spasms test. Tranquilizing activity of the compound has been studied on the test of barbituric sleep duration increase caused by hexenale.

Results

Investigated new sulfolan-containing compound demonstrates analgesic (145%), anticonvulsant (50%) and tranquilizer (127%) activity. Its activity was estimated in percentage to the control group of animals. Thereby, observed effects enable to consider the examined compound as perspective substance for therapy of pain syndrome in the conditions of enhanceable convulsive readiness.

Conclusions

It is necessary to mark that new sulfolan-containing compound under investigation along with low tranquilizing action demonstrates analgesic and anticonvulsive activity.