Analgesic effects of new triazole compounds Ⅱ3 and their effects on the activity of cycloxygenase
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Graphical Abstract
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Abstract
Aim ：To investigate the analgesic effect of the new triazole compounds II3 and effects on cycloxygenase-1(COX-1) as well as cycloxygenase-2(COX-2). Methods ：The hot plate and the stretching settings in mice were utilized to study the effects of compounds II3 on acute pain.Radioimmunologic kits were used to assay the contents of PGE2 in macrophage and 6-keto-PGF1α in endodermis，which represents the activities of COX-2 and COX-1，respectively. Results ：Compounds II3 (15，30，60 mg/kg) prolonged the pain liminal value and the writhing response time in the initial appearance，and reduced the frequency of the writhing response in 15 min after exposure of the mice to glacial acetic acid(P<0.05，P<0.01).Compounds II3，at the concentrations of 1×10-5，1×10-6，and 1×10-7 mol/L，markedly inhibited the production of PGE2 in macrophage，and also impeded the activity of COX-2 at 1×10-6 mol/L.But the inhibition of 6-keto-PGF1α in endodermis using the same settings of compounds Ⅱ3 was found to be limited. Conclusion ：Compounds Ⅱ3 has analgesic effects on the acute pain and selective inhibition on COX-2.
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