Exploring delta-receptor function using the selective opioid antagonist naltrindole

Neuropharmacology. 1989 Dec;28(12):1427-30. doi: 10.1016/0028-3908(89)90022-1.

Abstract

Until recently the only pharmacological probes for delta-receptors have been peptide enkephalin analogues. These suffer from a number of limitations including high cost, partial agonist effects and a propensity for neurotoxicity. A stable non-peptide antagonist, naltrindole, has recently become available. We have explored its intrinsic actions and found that it attenuated swim stress-induced antinociception, a model for endogenous delta-receptor activation. Naltrindole may therefore be a useful alternative to presently available delta-receptor antagonists.

MeSH terms

  • Animals
  • Behavior, Animal / drug effects
  • Indoles / pharmacology*
  • Male
  • Morphinans / pharmacology*
  • Naltrexone* / analogs & derivatives*
  • Narcotic Antagonists / pharmacology*
  • Pain / physiopathology
  • Rats
  • Rats, Inbred Strains
  • Receptors, Opioid / drug effects*
  • Receptors, Opioid / physiology
  • Receptors, Opioid, delta
  • Stress, Psychological / physiopathology

Substances

  • Indoles
  • Morphinans
  • Narcotic Antagonists
  • Receptors, Opioid
  • Receptors, Opioid, delta
  • Naltrexone
  • naltrindole