摘要
目的：研究滇乌碱（Ｔ_１）、滇西嘟拉碱甲（Ｔ_２）及３－乙酰滇乌碱（Ｔ_３）的镇痛效应的构效关系。方法：小鼠扭体反应法和大、小鼠甲醛致痛法及急性毒性试验测试三药的镇痛作用强度及毒性。结果：镇痛作用Ｔ_１＞Ｔ_３＞Ｔ_２，毒性Ｔ_１＞Ｔ_２，Ｔ_１＞Ｔ_３，镇痛治疗指数Ｔ_３＞Ｔ_２＞Ｔ_１。结论：滇乌碱类生物碱３位上取代基与其镇痛效应及毒性关系密切。
Objective:To study the structure-activity of yunaconitine(T1)bulleyaconitine(T2)and 3-acetylaconitine(T3)on analgesia.Objective:The acetic acid test in mice;The formalin test in rats or mice;The test of acute toxicity in rats or mice,Results:The analgesic potency of these three alkaloids decreased in the order of T1>T3>T2 in terms of their median analgesic doses(ED50).The acute toxicity of T1 was more potent than that of T3or T2in terms of their sc LD50 in mice or their ip LD50 in rats.Their therapeutic index decreased in the order of T3>T2>T1.Conclusion:The different group in the 3-position of A-ring of chemical strtucture of these three alkaloids is closely related to their analgesic and toxic actions.
关键词
滇乌碱
滇西嘟拉碱甲
乙酰滇乌碱
镇痛
构效关系
bulleyaconitine Yunaconitine 3-acetylaconitine analgesia acute toxicity structure-activity relationship
