Characteristics of mu and delta opioid binding sites in striatal slices of morphine-tolerant and -dependent mice

Eur J Pharmacol. 1991 Jun 6;198(2-3):157-63. doi: 10.1016/0014-2999(91)90615-w.

Abstract

Previously, we demonstrated the enhanced affinity of opioid receptors for naloxone in striatal slices from morphine-dependent mice. In our present study, binding characteristics of the mu opioid receptor agonists, [D-Ala2,MePhe4,Gly-ol5]enkephalin (DAMGO) and dihydromorphine, the delta opioid receptor agonist, [D-Ala2, D-Leu5]enkephalin (DADLE), and the opioid antagonist, naloxone, were examined in striatal slices from morphine-tolerant and -dependent mice. Striatal slices from mice that were implanted with a morphine pellet for 3,7 and 21 days displayed significant decreases in Kd values (5.1, 4.6 and 5.5 nM, respectively) of [3H]DAMGO when compared to those in slices from control animals that were not implanted or implanted with placebo pellets (9.6 and 9.3 nM, respectively). Also, a significant increase in the binding affinity of naloxone, but not that of dihydromorphine, was observed in striatal slices of mice that were implanted with a morphine pellet for 3 days. Significant increases in the Bmax of delta binding sites in striatal slices of mice that were implanted with a morphine pellet for 3, 7 and 21 days (20.7, 18.1 and 17.7 pmol/mg tissue, respectively) were observed when compared to that in slices from control mice that were implanted with placebo pellets (11.4 pmol/mg tissue). The enhancement in the binding affinity of DAMGO and naloxone and the increased density of DADLE binding sites paralleled the development of morphine tolerance and dependence and [D-Pen2,D-Pen5]enkephalin cross-tolerance in whole animals. An antinociceptive potentiation between morphine and DAMGO was observed in morphine-tolerant and -dependent mice whereas in naive animals the effects of the two drugs were additive.(ABSTRACT TRUNCATED AT 250 WORDS)

Publication types

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

MeSH terms

  • Analgesics
  • Animals
  • Binding Sites
  • Corpus Striatum / metabolism*
  • Drug Interactions
  • Drug Tolerance
  • Enkephalin, Ala(2)-MePhe(4)-Gly(5)-
  • Enkephalin, Leucine-2-Alanine / metabolism
  • Enkephalins / metabolism
  • Enkephalins / pharmacology
  • Male
  • Mice
  • Morphine / pharmacology*
  • Morphine Dependence / metabolism*
  • Naloxone / metabolism
  • Naloxone / pharmacology
  • Pain / drug therapy
  • Receptors, Opioid / drug effects
  • Receptors, Opioid / metabolism*

Substances

  • Analgesics
  • Enkephalins
  • Receptors, Opioid
  • Enkephalin, Ala(2)-MePhe(4)-Gly(5)-
  • Naloxone
  • Enkephalin, Leucine-2-Alanine
  • Morphine