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Related Experiment Videos

Decrease in delta and mu opioid receptor binding capacity in rat brain after chronic etorphine treatment.

P L Tao, P Y Law, H H Loh

    The Journal of Pharmacology and Experimental Therapeutics
    |March 1, 1987
    PubMed
    Summary
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    Chronic etorphine treatment in rats leads to a decrease in opiate receptor binding, particularly mu opioid receptors, contributing to tolerance and withdrawal. This desensitization occurs at the receptor level, not due to drug presence.

    Area of Science:

    • Neuropharmacology
    • Receptor Biology

    Background:

    • Opioid receptor activation modulates receptor levels.
    • Understanding opioid tolerance and withdrawal mechanisms is crucial.

    Purpose of the Study:

    • To investigate the impact of chronic etorphine (an agonist) on opiate receptor binding.
    • To determine the time course and regional differences in receptor downregulation.

    Main Methods:

    • Rats received etorphine via osmotic minipumps for up to 7 days.
    • Behavioral responses (tail-flick, withdrawal signs) and opiate receptor binding ([3H]diprenorphine) were measured.
    • Regional receptor binding (cortex, midbrain, striatum) and subtype-specific binding (mu and delta) were analyzed.

    Main Results:

    Related Experiment Videos

  • Chronic etorphine caused a time-dependent increase in tolerance and withdrawal signs.
  • A significant, time-dependent decrease in [3H]diprenorphine binding was observed, maximal at 3 days.
  • The striatum showed the greatest decrease (68%) in binding; mu opioid receptor binding decreased more than delta opioid receptor binding.

    • Conclusions:

    • Continued agonist activation leads to downregulation of opiate receptors.
    • This downregulation, particularly of mu receptors, contributes to the development of opioid tolerance and withdrawal.
    • Regional differences in receptor sensitivity exist within the brain.