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Yaksh等曾报告大鼠脊髓蛛网膜下腔(ith)注射甲啡肽400微克才能引起明显的镇痛作用,此结果得到谢国玺等的证实。推测是由于甲啡肽被迅速酶解所致。本工作在应用Bestatin抑制氨基肽酶的基础上,观察甲啡肽(MEK)、亮啡肽(LEK)和甲啡肽衍生物D-丙2-甲啡肽(DMEK)的镇痛作用。 实验中室温保持20±1℃,用辐射热-甩尾法测痛阈。测得基础痛阈后,通过事先埋置的PE-10管给大鼠ith药液15微升,给药后5,10,20,30,40,50,和60分钟测痛,与基础痛阈此较,计算痛阈变化百分数。 结果表明:(1)单纯注射MEK50微克,LEK100微克,Bestatin 50或100微
Yaksh et al. Reported that intramural subarachnoid (ith) injected with 400 micrograms of methotrexate can cause significant analgesic effect. This result was confirmed by Xie Guoxi et al. Presumably due to rapid digestion of methamidophos. In this study, we observed the analgesic effect of metatin (MEK), leupeptin (LEK) and the derivative of metoporphine, D-propionimorphine (DMEK), on the basis of Bestatin inhibition of aminopeptidase. The experiment was kept at room temperature 20 ± 1 ℃, with radiant heat - flick method to measure pain threshold. After the basal pain threshold was measured, 15 μl of rat ith liquid was preincubated with PE-10 tube, pain was measured at 5, 10, 20, 30, 40, 50, and 60 minutes after administration, Threshold comparison, calculate the percentage change of pain threshold. The results showed that: (1) MEK 50 μg, LEK 100 μg, Bestatin 50 or 100 μm