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P-913 - new Analgesics Nitrosulfonamides With Tranquilizer Activity

Published online by Cambridge University Press:  15 April 2020

H.T. Zlenko
Affiliation:
Dnepropetrovsk State Medical Academy, Dnepropetrovsk, Ukraine
V.A. Palchikov
Affiliation:
Organic Chemistry, Oles Honchar Dnepropetrovsk National University, Dnepropetrovsk, Ukraine
V.E. Rybalko
Affiliation:
Organic Chemistry, Oles Honchar Dnepropetrovsk National University, Dnepropetrovsk, Ukraine

Abstract

Objectives

The problem of pain and search of new analgesics remains the actual problem for theoretical and clinical medicine. The well-known analgesics possess a number of sides properties, from which the convulsive activity characteristic for narcotic analgesics takes special seat.

Methods

Experiments were carried out upon white mice (20–30 g). The two new derivatives with 4-nitrobenzenesulfonamide fragment (N-bicyclo[2.2.1]hept-5-en-2-yl)-4-nitrobenzenesulfonamide and 3-(4-nitrophenylsulfonyl)-3-azabicyclo [3.2.1]oct-6-ene) having a middle acute toxicity (LD50 268 and 500 mg/kg) has been synthesized. In experiments the pains thresholds were determined at the thermal irritation (method «hot plate»). The tranquilizer action of preparations was studied under the test of increase in duration of barbiturate dream caused by the hexenale prepared ex tempore. Activity estimated in % in relation to the control group of animals.

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Results

Investigated new 4-nitrobenzenesulfonamide-containing compound demonstrates analgesic (69 and 55%) and tranquilizer (130 and 223%) activity. Thereby, observed effects enable to consider the examined compounds as perspective substance for therapy of pain syndrome in the conditions of enhanceable tranquilizer readiness.

Conclusions

It is necessary to mark that new compounds under investigation along with high tranquilizing action demonstrates middle analgesic activity. Further research can ground its introduction in clinical practice.

Type
Abstract
Copyright
Copyright © European Psychiatric Association 2012
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