一种μ阿片肽[Dmt(1)]DALDA与吗啡的不同镇痛作用。
Differential analgesic effects of a mu-opioid peptide, [Dmt(1)]DALDA, and morphine.
作者信息
Shimoyama Megumi, Szeto Hazel H, Schiller Peter W, Tagaito Yugo, Tokairin Hideyuki, Eun Chong moon, Shimoyama Naohito
机构信息
Department of Anesthesiology, Teikyo University Chiba Medical Center, Ichihara, Chiba, Japan.
出版信息
Pharmacology. 2009;83(1):33-7. doi: 10.1159/000167878. Epub 2008 Nov 6.
AIMS
H-Dmt-D-Arg-Phe-Lys-NH(2) ([Dmt(1)]DALDA), a highly selective micro-opioid peptide, is potently analgesic after systemic and intrathecal administration but is less potent given intracerebroventricularly. This study was performed to further characterize the analgesic effects of [Dmt(1)]DALDA.
METHODS
We compared the effects of [Dmt(1)]DALDA and morphine after systemic administration in two different acute pain tests, the tail flick test and the paw withdrawal test, and examined how antagonizing the spinal opioid actions would affect their analgesic effects.
RESULTS
[Dmt(1)]DALDA was markedly more potent in the tail flick test than in the hot plate test, while the potencies of morphine were similar in the two tests. Intrathecal naloxone completely blocked the effect of systemic [Dmt(1)]DALDA in the tail flick test, while it only partially blocked the effect of morphine. At higher doses that produced analgesia in the hot plate test, the effect of [Dmt(1)]DALDA in this test was only partially blocked by naloxone.
CONCLUSION
Systemic [Dmt(1)]DALDA has a unique analgesic property clearly different from that of morphine and it has a propensity to produce spinal analgesia.
目的
H-Dmt-D-Arg-Phe-Lys-NH(2)（[Dmt(1)]DALDA），一种高度选择性的微阿片肽，经全身和鞘内给药后具有强效镇痛作用，但经脑室内给药时效力较弱。本研究旨在进一步表征[Dmt(1)]DALDA的镇痛作用。
方法
我们在两种不同的急性疼痛试验，即甩尾试验和爪部撤离试验中比较了[Dmt(1)]DALDA和吗啡经全身给药后的效果，并研究拮抗脊髓阿片类作用如何影响它们的镇痛效果。
结果
[Dmt(1)]DALDA在甩尾试验中的效力明显高于热板试验，而吗啡在这两种试验中的效力相似。鞘内注射纳洛酮完全阻断了全身给药的[Dmt(1)]DALDA在甩尾试验中的作用，而仅部分阻断了吗啡的作用。在热板试验中产生镇痛作用的较高剂量下，纳洛酮仅部分阻断了[Dmt(1)]DALDA在该试验中的作用。
结论
全身给药的[Dmt(1)]DALDA具有与吗啡明显不同的独特镇痛特性，且有产生脊髓镇痛的倾向。
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