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目的：研究孤啡肽（ＯＦＱ）对痛与阿片镇痛的影响．方法：脑室（ｉｃｖ）与鞘内（ｉｔｈ）给药，以大鼠甩尾模型测痛．结果：小剂量ＯＦＱ（０１μｇ）ｉｃｖ及ｉｔｈ给药对痛反应均无影响；较大剂量ＯＦＱ（０５－１０μｇ）可使痛反应增强．ＯＦＱ１－１０（ＯＦＱ的一个片段）ｉｃｖ对痛反应无影响．μ受体激动剂芬太尼（１μｇ）、δ激动剂ＤＳＬＥＴ（５μｇ）ｉｃｖ或ｉｔｈ给药，以及κ激动剂Ｕ５０４８８Ｈ（１μｇ）ｉｔｈ给药，可使痛阈明显增加．０１μｇ或１μｇＯＦＱ与上述药物合用后，痛阈增加明显减少（除鞘内与ＤＳＬＥＴ合用外）．结论：ＯＦＱ可增强大鼠的痛反应，在脑内对抗由μ和δ受体介导的阿片镇痛，在脊髓对抗由κ和μ但不是由δ受体介导的镇痛．
Objective: To study the effects of OFQ on pain and opioid analgesia. Methods: Intracerebroventricular (icv) and intrathecal (ith) administration were performed with a rat tail flick model. RESULTS: Small doses of OFQ (01μg) icv and ith administration had no effect on the pain response. Higher doses of OFQ (05-10μg) increased the pain response. OFQ1-10 (a fragment of OFQ) icv had no effect on pain response. μ agonist fentanyl (1μg), δ agonist DSLET (5μg) icv or ith administration, and κ agonist U50488H (1μg) ith administration, the pain threshold can be significantly increased. 0 1μg or 1μgOFQ combined with the above drugs, the pain threshold increased significantly reduced (except for intrathecal and DSLET). CONCLUSION: OFQ enhances the pain response in rats, counteracts opioid analgesia mediated by μ-and δ-receptors in the brain, antagonizes both the Îμ-and μ-but not β-γ-mediated township in the spinal cord pain.