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Related Experiment Videos

Decrease in mu-opioid receptor binding capacity in rat brain after chronic PL017 treatment.

P L Tao1, H Y Lee, L R Chang

  • 1Department of Pharmacology, National Defense Medical Center, Taipei, Taiwan.

Brain Research
|September 3, 1990
PubMed
Summary
This summary is machine-generated.

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Chronic treatment with a selective mu-opioid agonist (PL017) in rats specifically down-regulates mu-opioid receptors in the brain. This demonstrates specific receptor regulation, unlike previous studies with non-specific ligands.

Area of Science:

  • Neuroscience
  • Pharmacology
  • Molecular Biology

Background:

  • Previous studies showed non-specific opioid ligands (etorphine, DADLE) reduced both mu- and delta-opioid receptor binding during tolerance.
  • These non-specific ligands prevented determination of specific receptor down-regulation.
  • This study aimed to investigate specific mu-opioid receptor regulation.

Purpose of the Study:

  • To determine if mu-opioid receptors can be specifically down-regulated by a selective mu-opioid receptor ligand.
  • To investigate the effects of chronic PL017 treatment on opioid receptor binding capacity in rat brain.

Main Methods:

  • Sprague-Dawley rats were treated with increasing doses of the mu-opioid selective ligand PL017 (2.5-20 µg/kg, i.c.v.) for 5 days.
  • Antinociceptive and catatonic responses were measured to assess tolerance.

Related Experiment Videos

  • Mu- and delta-opioid receptor binding was quantified using radioligand binding assays ([3H]diprenorphine, [3H]DAMGO) and Scatchard analysis.

    • Main Results:

    • PL017 treatment induced significant tolerance to its antinociceptive (30-40 fold increase in AD50) and catatonic (14 fold increase in ED50) effects.
    • A 20-30% decrease in mu-opioid receptor binding was observed in all tested brain areas.
    • No significant changes in delta-opioid receptor binding were detected.
    • Scatchard analysis revealed decreased Bmax values for mu-opioid receptors, indicating down-regulation, with no change in Kd.

    Conclusions:

    • Chronic administration of the mu-opioid selective ligand PL017 specifically down-regulates mu-opioid receptors in the rat brain.
    • This provides evidence for specific ligand-induced regulation of mu-opioid receptor binding capacity.
    • These findings parallel specific delta-receptor regulation observed in cell lines.