The exchange of monoamines during the experimental neurosis on the background of using of amide "2-hydroxy-n-naphthalen-1-yl-2-(2-oxo-,2-dihydroindol-3-ylidene)".

INTRODUCTION: Incessant increase in the frequency and distribution of anxiety disorders stipulates searching, research and study of the mechanism of action of new substances for their correction, including the group of 2-oxoindolin-3-glyoxylic acid derivatives. THE AIM: To research the effect of N-(1-naphthyl) amide-2-oxoindolin-3-glyoxylic acid on monoaminergic system of subjected to experimental neurosis of rats. MATERIALS AND METHODS: The experiments were performed on male Wistar rats, who have weight 180-220g and were researching the effect of 2-hydro-N-naphthalen-1-yl-2-(2-oxy-1,2-dihydroindol-3-ylidene)-acetamide (compound 18) at a dose (12 mg/kg), by intragastric drug injection of subjected to experimental neurosis rats, during 30 days (1 time in three days), for monoamines content (epinephrine, norepinephrine, dopamine and serotonin) in the blood, their decay products (homovanillic acid, vanillylmandelic acid and 5-oxyindolacetic acid) in the urine and the ratio of end products of the reaction to their predecessors. RESEARCH: It was established that during the preventive-therapeutic application of N-(1-naphthyl)amide-2-oxoindolin-3-glyoxylic acid, it effectively adjusts the level of monoamines, reducing the content of adrenaline and increasing the content of noradrenaline, dopamine and 5-HT in the blood. The compound also reduces the content of products exchange of mediators (HVA,VMA and 5-OIAA) in the urine. The 2-oxoindolin derivatives reduces the ratio between HVA/dopamine, VMA/(noradrenaline + adrenaline) and 5-OIAA/5-HT, it testifies about the normalizing of enzymes activity, which are involved in the process of exchange and maintaining the constancy of monoamines. The results show that in the mechanisms of anxiolytic action of compound 18, a significant role plays the normalization of content and exchange of neurotransmitters in the organism, which caused an experimental neurosis. CONCLUSION: Compound 2-hydro-N-naphthalen-1-yl-2-(2-oxo-1,2-dihydroindol-3-ylidene)-acetamide by the experimental 30-day neurosis, was reducing the expression of neurotransmitter imbalance in the blood, apparently due to correction of enzymatic synthesis links and biotransformation of monoamines.

Anhedonia at experimental models of chronic stress and its correction.

INTRODUCTION: Different types of chronic stress lead to neurotic and depressive disorders. Key symptoms of these disorders are anhedonia and correction of which will indicate the efficacy of proposed therapy. The aim of the paper is to investigate the influence of amide 2-hydroxy-N-naftalen-1-il-2-(2-oxo-1,2-dihidro-indole-3-iliden) and ethyl ether 4-[2-hydroxy-2-(2-oxo-1,2-dihidro-indole-3-iliden)-acetamin]-butyric acid on anhedonia after the experimental neurosis and chronic moderate stress in rats. MATERIALS AND METHODS: It was studied the influence of therapeutic and preventive administration of substances 18 and E-38 in the dosage of 12mg/kg during chronic mild stress "conflict of afferent activation" during 30 days and depression-like behavior chronic mild stress that modeled 8 weeks. Results of investigation: Experimental neurosis caused decrease of number of comings to drinking-bowl, decrease of total number of drank sucrose and decrease of the percent of drank water with sugar in comparison with intact animals. Analogical but more significant changes were noticed during depression-like behavior. The use of amide 2-oxoindolin-3-glyoxylic acid based on neurosis counters effectively the development of anhedonia. Substance 18 increased the number of comings to drinking-bowl with sucrose and increased the amount of the number of drank water with sucrose in comparison with control pathology without correction. The substance possibly assists in use of solution with sucrose among water and does not compromise reference-preparation such as diazepam. The administration of ethyl ether of 2-oxoindolin-3-glyoxylic acid at chronic mild stress possibly increased the number of comings to the drinking-bowl and increased the number of drank sucrose in comparison with control pathology and it was more effective than imipramine and countered anhedonia. CONCLUSIONS: It was indicated that during 30 day experimental neurosis and 8 week depression-like behavior cause the development of anhedonia. Therapeutic use of amide 2-hydroxy-N-naftalen-1-il-2-(2-oxo-1,2-dihidro-indole-3-iliden) and ethyl ether 4-[2-hydroxy-2-(2-oxo-1,2-dihidro-indole-3-iliden)-acetamin]-butyric acid corrected effectively anhedonia after experimental neurosis and chronic mild stress in rats.

Research of the protection actions of derived 2-oxoindole in acute stress.

INTRODUCTION: Correction of pathological anxiety and stress level of frustration leads to the development of new anxiolytics, notably including derivatives of 2-oksoyndolyn- 3-hlyoksylic acid. The aim of work - to study the effect of 2-oksyindolin-3-hlyoksylic acid on emotional and behavioral reactions of rats subjected to behavioral stress tests of different averiability. MATERIALS AND METHODS: In experiments on 150 white mature male rats Wistar investigated the effects of 2-oksoindolin (2-hydroxy-N-naphthalene-1-yl-2-(2-hydroxy-1,2- dihydro-indole-3-ylidene)-acetamide) with laboratory codes 18 when intraperitoneally administered to acute immobilization stress on Sel'ye on emotional and behavioral responses of animals to test «open field¼, «a raised cross maze¼ and test «conflict behavior¼ (option Vogel). RESULTS: Established that the prophylactic use of the compound 18 in a test of "open field" warned the stress changes in the latent period of the first movement, likely increased the number of exits to the center installation, warned breach vertical and horizontal motor activity and significantly increased the number of acts of grooming and reduced the number of boluses compared with stress without correction. Revealed changes suggest that the substance 18 prevents anxiety disorders conduct stress genesis. In the test «a raised cross maze¼ of 2-oksoindolin significantly increased the number of outputs rats in open arms maze and reduced the number of fecal balls compared with those in the control disorders. In the study antyconflict action found that the compound increased the number of approaches to the drinkers, but the activity in this test yielded diazepam. CONCLUSION: Installed conservation action anksyolityc 2-hydroxy-N-naphthalene-1-yl-2-(2-hydroxy-1,2-dihydro-indole-3-ylidene)-atsetamidu acute stress may be associated with indirect stimulation of GABA - benzdiazepin receptor complex, by strengthening endogenous GABA affinity to the receptors and/or indirect stimulation of GABA receptors by other neurotransmitter systems, including serotonergic, which makes compounds for further study the possibility of post stress with anxiety disorders.