Analgesic effects of new triazole compounds Ⅱ_3 and their effects on the activity of cycloxygenase / 中国药科大学学报

ABSTRACT

Aim: To investigate the analgesic effect of the new triazole compounds Ⅱ_3 and effects on cycloxygen-ase-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 Ⅱ_3 on acute pain. Radioimmunologic kits were used to assay the contents of PGE_2 in macrophage and 6-keto-PGF_(1α) in endodermis, which represents the activities of COX-2 and COX-1, respectively. Results: CompoundsⅡ_3( 15,30,60 mg/kg) prolonged the pain liminal value and the writ-hing 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). CompoundsⅡ_3, at the concentrations of 1×10 ~(-5),1×10 ~(-6), and 1×10 ~(-7) mol/L, markedly inhibited the production of PGE_2 in macrophage, and also impeded the activity of COX-2 at 1×10 ~(-6) mol/L But the inhibition of 6-keto-PGFla in endodermis using the same settings of compounds Ⅱ_3 was found to be limited. Conclusion: CompoundsⅡ_3 has analgesic effects on the acute pain and selective inhibition on COX-2.