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Selective opioid receptor agonists modulate mechanical allodynia in an animal model of neuropathic pain.

Abstract
This study evaluated the antinociceptive effects of systemically administered selective opioid agonists of mu (DAMGO), delta (BUBU) and kappa (U 69593) receptors on the vocalization threshold to paw pressure in a rat model of peripheral unilateral mononeuropathy produced by loose ligatures around the common sciatic nerve. DAMGO (0.5-2 mg/kg), BUBU (1.5-6 mg/kg) and U 69593 (0.75-3 mg/kg) injected intravenously (i.v.) produced a potent long-lasting antinociceptive effect on both hind paws. The effects on the lesioned paw were clearly and statistically more potent than for the non-lesioned paw. The selective antinociceptive effect of 2 mg/kg DAMGO, 3 mg/kg BUBU and 1.5 mg/kg U 69593 were completely prevented by prior administration of the appropriate antagonists: 0.1 mg/kg naloxone, 1 mg/kg naltrindole and 0.4 mg/kg MR 2266. The present data clearly show that an acute i.v. injection of these selective opioid agonists induces potent antinociceptive effects in a rat model of peripheral neuropathy. These data are discussed with regard to the classical view that there is opioid resistance in neuropathic pain.
AuthorsJ A Desmeules, V Kayser, G Guilbaud
JournalPain (Pain) Vol. 53 Issue 3 Pg. 277-285 (Jun 1993) ISSN: 0304-3959 [Print] United States
PMID8394563 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Analgesics
  • Benzeneacetamides
  • Benzomorphans
  • Enkephalins
  • Narcotic Antagonists
  • Oligopeptides
  • Pyrrolidines
  • Receptors, Opioid
  • Receptors, Opioid, delta
  • Receptors, Opioid, kappa
  • Receptors, Opioid, mu
  • Enkephalin, Ala(2)-MePhe(4)-Gly(5)-
  • tyrosyl-seryl(O-t-butyl)-glycyl-phenylalanyl-leucyl-threonine(O-t-butyl)
  • Naloxone
  • MR 2266
  • Naltrexone
  • naltrindole
  • U 69593
Topics
  • Analgesics (therapeutic use)
  • Animals
  • Benzeneacetamides
  • Benzomorphans (pharmacology)
  • Disease Models, Animal
  • Drug Interactions
  • Enkephalin, Ala(2)-MePhe(4)-Gly(5)-
  • Enkephalins (therapeutic use)
  • Male
  • Naloxone (pharmacology)
  • Naltrexone (analogs & derivatives, pharmacology)
  • Narcotic Antagonists (pharmacology)
  • Oligopeptides (therapeutic use)
  • Pain (drug therapy)
  • Pain Measurement (drug effects)
  • Pain Threshold (drug effects)
  • Pyrrolidines (therapeutic use)
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Opioid (drug effects)
  • Receptors, Opioid, delta (drug effects)
  • Receptors, Opioid, kappa (drug effects)
  • Receptors, Opioid, mu (drug effects)
  • Vocalization, Animal (drug effects)

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