Experimental Study of Antispasmodic Activity of 2-Oksoindolin-3-Glyoxylic Acid Derivatives

Abstract

Clinical psychiatry and neurology requires a creation of new means with difficult many component range of psychotropic action, so psychoemotional disturbances “boundary type” and difficult mental disorders have high level of heterogeneity, various clinical manifestations, which are caused by different pathogenetic factors. One of the most often used preparation for the treatment of these diseases is anxiolytic medications. It is known that anxiolytic action combines with anticonvulsive. Perspective medications are simple amides and ethers of 2-oksoindolin-3-glyoxylic acid, which have not recognized and practically observed. The aim of this research is to determine anticonvulsant action in 2-oksoindolin-3-glyoxylic acid derivatives on the model of acute myoclonic pentylentetrazol, piktrotoxic, and bikukullin convulsions. In experiments on mature mice of both sex Wistar line were studied an influence of ethyl ester 4-[2-hydroxy-2-(2-oxo-1,2-dihydro-indol-3-ylidene)-acetylamino]-butyric acid and 2-hydroxy-N-naphthalen-1-yl-2-(2-oxo-1,2-dihydro-indol-3-ylidene)-acetamide on chemoinduced epileptogenesis. An intake of proconvulsants is accompanied by a development of syndrome convulsion, which was estimated by convulsion’s intensity (grades), latent period of convulsions (sec.), number of convulsions acts, and duration of convulsions (sec.) and number of survived animals in a group. It was showed that a combination of 2-hydroxy-N-naphthalen-1-yl-2-(2-oxo-1,2-dihydro-indol-3-ylidene)-acetamide (12 acetamide mg/kg) is similar to reference preparation diazepam in (2 mg/kg) which decreased a manifestation of syndrome convulsion. It demonstrated an increase of intensity of convulsions, decrease of latent period of the convulsion’s start which is caused by all blockers GАМКА-receptors, decrease of number convulsive acts on the background of korazol and pikrotoxin, a decrease of convulsive syndrome duration during an intake of korazol and bikukullin, and a decrease of animal’s mortality, which was caused by pikrotoxin intake.