Spinal and supraspinal opioid analgesia in the mouse: the role of subpopulations of opioid binding sites

Geoffrey S.F. Ling, Gavril W. Pasternak

Research output: Contribution to journalArticle

Abstract

The selective in vivo blockade of high affinity (mu1) opioid binding sites in mice by naloxazone reduced the analgesic potency of opiates and opioid peptides, evidenced by a shift of their analgesic ED50 values. However, the extent of these shifts varied significantly between a series of opioid drugs, ranging from 12-fold for morphine to 4-fold for d-Ala2-d-Leu5-enkephalin. These findings suggested that analgesia in naloxazone-treated animals is mediated through a different subpopulation of receptors than in normal controls. Correlating these analgesic shifts for a series of opioids with their affinity for different [3H]opioid binding sites suggested an analgesic role for delta sites. Additional studies in mice with spinal transections suggested that mu1 analgesia was primarily supraspinal.

Original languageEnglish (US)
Pages (from-to)152-156
Number of pages5
JournalBrain research
Volume271
Issue number1
DOIs
StatePublished - Jul 18 1983

Keywords

  • analgesia
  • delta receptor
  • enkephalin
  • mu receptor
  • naloxazone
  • opiate

ASJC Scopus subject areas

  • Neuroscience(all)
  • Molecular Biology
  • Clinical Neurology
  • Developmental Biology

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