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目的 :本文对人工定向合成的三个胺基环己醇类衍生物 Fs- 812 5、Fs- 82 0 6、Fs- 870 2的镇痛活性进行研究 ,以期获得定向设计高效非成瘾性镇痛药物的可靠科学依据。方法 :用热板测痛法测定给药前和给药后 5～ 10 m in内的痛阈值 ,以 ED5 0值为比较对象 ,研究三个环己醇类衍生物对小白鼠的镇痛活性。结果 :1脑室给药 (ic)的镇痛 ED5 0 值显示 :Fs- 870 2 (ED5 0 值为1.8± 0 .6 2 ug· kg- 1 )的镇痛活性最强 ,而 Fs- 82 0 6略强于 Fs- 812 5 ,且二者无显著差别。 2腹腔给药 (ip)的 ED5 0 值。显示 Fs- 870 2镇痛活性最强 ,Fs- 812 5次之 ,Fs- 82 0 6最弱。 3ic/ip的比值提示 :Fs- 812 5的比值最大 ,脂溶性最强 ,最易通过血脑屏障 ,Fs- 870 2次之 ,Fs- 82 0 6的比值最小 ,最难通过血脑屏障。 4与吗啡的镇痛活性相比 ,Fs- 870 2为吗啡的 40倍 ,Fs-812 5和 Fs- 82 0 6都约为吗啡的 10倍。 5与吗啡的镇痛作用持续时间相比 ,Fs- 870 2最长 ,Fs- 82 0 6次之 ,Fs- 812 5最短。
OBJECTIVE: In this paper, the analgesic activity of three aminocyclohexanol derivatives Fs-812 5, Fs-82 0 6, Fs-870 2 synthesized by artificial targeting was studied in order to obtain a highly effective and non-addictive Reliable scientific basis for pain medicine. Methods: The pain thresholds of 5 ~ 10 mins before and after administration were determined by hot plate analgesia. The ED50 value was used as the comparison object to study the analgesic activity of three cyclohexanol derivatives on mice . Results: 1 Analgesic ED50 values of intracerebroventricular (ic) administration showed that the analgesic activity of Fs-870 2 (ED5 0 1.8 ± 0.62 ug · kg -1) was the strongest and Fs-82 0 6 slightly stronger than Fs-812 5, and no significant difference between the two. 2 ip administered ED50 values. Fs-870 2 showed the strongest analgesic activity, Fs-812 5 times, Fs-82 0 6 weakest. The ratio of 3ic / ip suggests that the ratio of Fs-8125 is the largest, the fat-soluble is the strongest, the most easy to cross the blood-brain barrier, the second is Fs-870, and the second is Fs- 82 0. 4 Compared with the analgesic activity of morphine, Fs-870 2 is 40 times more morphine, and both Fs-812 5 and Fs-82 0 6 are about 10 times more than morphine. Compared with the duration of morphine analgesia, Fs-870 2 had the longest, Fs-82 0 6 and Fs-812 5 the shortest.