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Related Experiment Videos

Naltrexone-induced opiate receptor supersensitivity.

R S Zukin, J R Sugarman, M L Fitz-Syage

    Brain Research
    |August 12, 1982
    PubMed
    Summary

    Chronic naltrexone (a narcotic antagonist) use significantly increases brain opiate receptors, particularly in key brain regions. This suggests the brain

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    Area of Science:

    • Neuroscience
    • Pharmacology
    • Receptor Biology

    Background:

    • Opiate receptors are crucial for pain perception and reward pathways.
    • Naltrexone is a long-acting opioid antagonist used in addiction treatment.

    Purpose of the Study:

    • To investigate the effects of chronic versus acute naltrexone administration on brain opiate receptor density and function.
    • To identify brain regions with significant changes in opiate receptor expression.

    Main Methods:

    • Chronic and acute administration of naltrexone to subjects.
    • Radioligand binding assays using various opiate agonists and antagonists ([3H]dihydromorphine, [3H]naloxone, [3H]D-Ala2,D-Leu5-enkephalin, [3H]etorphine).
    • Assessment of guanyl nucleotide sensitivity in agonist binding.

    Main Results:

    • Chronic naltrexone administration led to a marked increase in brain opiate receptor density across multiple receptor subtypes.
    • Agonist binding sensitivity to guanyl nucleotide inhibition significantly increased.
    • Acute naltrexone did not alter opiate receptor binding.
    • The most significant increases in receptor number were observed in the mesolimbic and frontal cortex areas.

    Conclusions:

    • The opiate receptor system exhibits plasticity in response to chronic antagonist treatment.
    • These changes in receptor density and sensitivity may be linked to specific functional pathways.
    • Chronic naltrexone therapy induces adaptive changes in the central nervous system's opioid system.

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