Analgesic effect of endomorphin-1

Acta Pharmacol Sin. 2001 Nov;22(11):976-80.

Abstract

Aim: To study the analgesic effect of endomorphin-1 (EM-1).

Methods: The 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.

Results: 1) 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.

Conclusion: EM-1 had a definite analgesic effect and the analgesic effect of EM-1 was mediated by central mu-opioid receptor.

MeSH terms

  • Analgesics, Opioid / pharmacology*
  • Analgesics, Opioid / therapeutic use
  • Animals
  • Arthritis, Experimental / complications
  • Arthritis, Experimental / physiopathology
  • Drug Tolerance
  • Male
  • Mice
  • Nociceptors / drug effects*
  • Oligopeptides / pharmacology*
  • Oligopeptides / therapeutic use
  • Pain / drug therapy*
  • Pain / etiology
  • Pain Measurement
  • Pain Threshold / drug effects
  • Rats
  • Receptors, Opioid, mu / antagonists & inhibitors
  • Receptors, Opioid, mu / metabolism

Substances

  • Analgesics, Opioid
  • Oligopeptides
  • Receptors, Opioid, mu
  • endomorphin 1