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Experimental study of analgesic mechanisms of 4-methyl-2,2-dioxo-1H-2λ6,1-benzothiazine-3-carboxylic acid derivative (compound NI-9) in rat
Author(s) -
Oxana V. Malchenko,
Н. И. Волощук,
O. V. Hrymalovska
Publication year - 2021
Publication title -
vìsnik vìnnicʹkogo nacìonalʹnogo medičnogo unìversitetu
Language(s) - English
Resource type - Journals
eISSN - 2522-9354
pISSN - 1817-7883
DOI - 10.31393/reports-vnmedical-2021-25(1)-02
Subject(s) - analgesic , prazosin , pharmacology , benzothiazine , yohimbine , medicine , (+) naloxone , nalbuphine , memantine , chemistry , anesthesia , antagonist , nmda receptor , receptor , opioid , medicinal chemistry
Annotation. The problem of effective and safe treatment of pain syndromes is a priority area of modern medicine, since pain syndrome is often accompanied by economic costs, a drop in labor productivity and an increase in the risk of other diseases. The derivative 4-methyl-2,2-dioxo-1H-2λ6,1-benzothiazine-3-carboxamide (compound NI-9) has shown a significant analgesic effect in various models of pain syndromes. The aim of this work was to experimentally study the mechanisms of the analgesic activity of compound NI-9 using pharmacological analyzers in the tail-flick test. The study was performed on 210 male Wistar rats. Statistical processing of the obtained results was performed using the software package STATISTICA 10.0 with the calculation of the mean value, standard error of the mean, confidence interval (p). The experiments used: naloxone, prazosin, clonidine, yohimbine, isoproterenol, propranolol, nalbuphine, chlorpromazine, dopamine, nakom, memantine, phenylephrine. The results showed that the opioidergic system was not involved in the antinociceptive effect of compound NI-9. At the same time, the participation of alpha-1 and alpha-2 adrenergic receptors, dopamine receptors, and also partially NMDA receptors has been proven. The data obtained serve as the basis for further preclinical studies of N- (4-methoxybenzyl) -4-methyl-2,2-dixo-1H-2Λ6,1-benzothiazine-3-carboxylic acid (compounds NI-9) as a non-narcotic analgesic, which can compete with already known drugs of this class in the treatment of diseases accompanied by inflammatory and pain syndrome.

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