Delta opioid antagonist, naltrindole, selectively blocks analgesia induced by DPDPE but not DAGO or morphine

Pharmacol Biochem Behav. 1991 Jan;38(1):185-90. doi: 10.1016/0091-3057(91)90608-5.

Abstract

Initial reports suggest that naltrindole hydrochloride (NTI), a recently developed opioid, acts as a selective delta (delta) antagonist in vivo. Three experiments were conducted in rats to test NTI for its ability to dose-dependently and selectively block the analgesia produced by a delta-selective opioid agonist without affecting analgesia produced by mu (mu) receptor opioid agonists. Intracerebroventricular (ICV) administration of the delta-selective agonist, DPDPE (30 micrograms/rat), and the mu-selective agonist, DAGO (0.3 micrograms/rat), increased paw-lick latency (2-fold relative to baseline) in the hot-plate assay. NTI (0.01-1.0 micrograms/rat, ICV) dose-dependently attenuated DPDPE-induced analgesia (1.0 micrograms reduced paw-lick latency to baseline), but failed to affect DAGO-induced analgesia at any dose tested. A third experiment determined whether the ICV administration of NTI (1.0 micrograms/rat) would attenuate restraint stress-induced potentiation of morphine analgesia as indexed by the tail-flick assay. Rats that underwent 5 days of 1 h restraint stress and nonstressed rats were injected subcutaneously with morphine (1.0-8.0 mg/kg). The magnitude (greater than 2-fold) and duration of morphine-induced analgesia in restrained rats were significantly potentiated compared to nonstressed rats. NTI (1 microgram, ICV) failed to affect the magnitude and duration of morphine-induced analgesia regardless of restraint treatment. Thus, NTI failed to attenuate the analgesia produced by DAGO or morphine (in two assays of antinociception), whereas NTI (0.01-1.0 micrograms, ICV) antagonized dose-dependently DPDPE-induced analgesia. These results support the view that NTI is a selective delta-receptor antagonist in vivo.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Analgesia*
  • Analgesics / pharmacology*
  • Animals
  • Dose-Response Relationship, Drug
  • Enkephalin, Ala(2)-MePhe(4)-Gly(5)-
  • Enkephalin, D-Penicillamine (2,5)-
  • Enkephalins / antagonists & inhibitors*
  • Enkephalins / pharmacology
  • Indoles / pharmacology*
  • Injections, Intraventricular
  • Male
  • Morphinans / pharmacology*
  • Morphine / antagonists & inhibitors*
  • Morphine / pharmacology
  • Naltrexone* / analogs & derivatives*
  • Narcotic Antagonists / pharmacology*
  • Rats
  • Rats, Inbred Strains
  • Reaction Time / drug effects
  • Restraint, Physical
  • Stress, Psychological / psychology

Substances

  • Analgesics
  • Enkephalins
  • Indoles
  • Morphinans
  • Narcotic Antagonists
  • Enkephalin, Ala(2)-MePhe(4)-Gly(5)-
  • Naltrexone
  • Morphine
  • Enkephalin, D-Penicillamine (2,5)-
  • naltrindole