• Z H Li, L D Shan, X H Jiang, S Y Guo, G D Yu, T Hisamitsu, and Q Z Yin.
• Department of Physiology, School of Medicine, Showa University, Tokyo 142, Japan.
• Acta Pharmacol. Sin. 2001 Nov 1;22(11):976-80.

AimTo study the analgesic effect of endomorphin-1 (EM-1).MethodsThe experiment was performed in rats and mice to study the analgesic effect of intraperitoneal (ip) injection of EM-1 with tail stimulation-vocalization test, writhing test, adjuvant arthritis, and neuropathic pain model and to compare it with the analgesic effects produced by intracerebroventricular (icv) and intrathecal (it) administrations.Results1) EM-1 raised the pain threshold dose-dependently in tail stimulation-vocalization test in rats and inhibited the writhing responses induced by ip acetic acid in mice. EM-1 also decreased the hyperalgesia in both adjuvant arthritis and neuropathic pain model. 2) The analgesic effect induced by central (icv and it) administration of EM-1 was faster and more powerful than that induced by peripheral (ip) administration. 3) The analgesic effect of EM-1 was reversed by naloxone (opioid receptor antagonist), as well as by cyprodime (mu-opioid receptor selective antagonist). Repeated administrations of EM-1 induced tolerance.ConclusionEM-1 had a definite analgesic effect and the analgesic effect of EM-1 was mediated by central mu-opioid receptor.

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