Autoradiographic evidence for decrease in binding of μ- and δ-opioid receptors after subchronic [D-Ala2,D-Leu5]enkephalin treatment in rats

Pao Luh Tao, Virginia S. Seybold, Horace H Loh

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10 Scopus citations


Tolerance to the antinociceptive effect of [D-Ala2,D-Leu5]enkephalin (DADLE) develops in Sprague-Dawley rats given the peptide chronically. δ-Opioid receptor binding is significantly reduced in P2 membranes from various brain areas after 1-3 days' treatment. μ-Opioid receptor binding, however, is reduced only in striatum, and only after 5 days. To study this finding further, receptor autoradiography was used to quantity μ- and δ-opioid binding sites in rat brain sections after subchronic DADLE treatment. Autoradiograms were made following equilibrium binding of the highly selective opioid radioligands, [3H]Tyr-D-Ala-Gly-MePhe-Gly-ol ([3H]DAMGO) and [3H][D-Pen2,5]enkephalin ([3H]DPDPE) to brain sections. Computerized grain counting was applied to discrete regions of the autoradiograms corresponding to caudate and interpeduncular nuclei. We found that [3H]DAMGO binding decreased in caudate after 3 days of DADLE treatment and [3H]DPDPE binding decreased in the interpeduncular nucleus, rostal portion, after 1-day DADLE treatment. These autoradiographic changes are consistent with our earlier results for biochemical binding, although we now detected an earlier change in μ-opioid receptor binding, by using autoradiography.

Original languageEnglish (US)
Pages (from-to)145-149
Number of pages5
JournalEuropean Journal of Pharmacology
Issue number2
StatePublished - Feb 9 1993

Bibliographical note

Copyright 2014 Elsevier B.V., All rights reserved.


  • (Rat)
  • ([D-Ala,D-Leu]enkephalin)
  • Autoradiography
  • Opioid receptors
  • Tolerance


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