Sullivan A F, Dickenson A H
Department of Pharmacology, University College London, U.K.
Brain Res. 1988 Sep 27;461(1):182-5. doi: 10.1016/0006-8993(88)90738-x.
The intrathecal administration of dermorphin, an endogenous heptopeptide first discovered in amphibia, produces dose-dependent selective inhibitions of C fibre-evoked responses in rat dorsal horn nociceptive neurones (ED50 0.11 micrograms). Naloxone (10 micrograms) but not ICI 174,864 (125 micrograms) antagonised the effects of the peptide. A beta-fibre-evoked activity was relatively unaffected. Thus dermorphin can profoundly inhibit nociceptive afferent input in the spinal cord, and in this preparation is more potent (approximately 40X) than morphine.
鞘内注射皮啡肽(一种最初在两栖动物中发现的内源性七肽)可对大鼠背角伤害性神经元中C纤维诱发的反应产生剂量依赖性的选择性抑制(半数有效剂量为0.11微克)。纳洛酮(10微克)而非ICI 174,864(125微克)可拮抗该肽的作用。β纤维诱发的活动相对未受影响。因此,皮啡肽可深刻抑制脊髓中的伤害性传入输入,并且在此制剂中比吗啡更有效(约40倍)。