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替泊沙林(tepoxalin)是一种有效的花生四烯酸级联反应的环氧合酶和脂氧合酶代谢抑制剂,具有抗炎、治疗多种疼痛(手术后、关节等)等多种药物活性。本文采用新的合成试剂,首次以离子液体为反应溶剂,找到了一种合成替泊沙林的新方法。利用小鼠醋酸扭体法对替泊沙林的镇痛活性进行了研究。方差分析结果表明:替泊沙林给药组和CMC对照组间扭体反应潜伏期及1h内小鼠的扭体次数均有显著性的差异(P<0.05);并且替泊沙林可剂量依赖性地延长注射冰醋酸后的扭体反应潜伏期并减少1h内小鼠的扭体次数,替泊沙林对扭体反应的潜伏期及1h内扭体次数的抑制作用和双氯酚酸钠(diclofenac sodium)无显著性差异。
Tepoxalin is a potent aromatase and lipoxygenase metabolic inhibitor of the arachidonic acid cascade and has anti-inflammatory and multi-ache (postoperative, joint, etc.) and many more Kind of drug activity. In this paper, a new synthetic reagent, the first time with ionic liquids as the reaction solvent, found a new method for the synthesis of tepu sarin. The antinociceptive activity of teicoplanar was studied using mouse acetic acid writhing method. Analysis of variance showed that there was a significant difference (P <0.05) in the latency of writhing reaction and the number of writhing in mice within 1h after administration of telmisalin and CMC control group, and the dose-dependent Extend the incubation period of writhing response after injection of glacial acetic acid and reduce the number of writhing in mice within 1h, the inhibitory effect of telmisalin on the incubation period of writhing reaction and the number of writhing in 1h and diclofenac sodium) no significant difference.