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Differing stereospecificities distinguish opiate receptor subtypes.

S R Zukin

    Life Sciences
    |September 20, 1982
    PubMed
    Summary

    Stereoisomers of opiate receptor ligands show varying potency at mu, kappa, and sigma subtypes. These stereoselectivity patterns suggest distinct biochemical properties for opiate receptor subclasses.

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    Area of Science:

    • Neuroscience
    • Pharmacology
    • Biochemistry

    Background:

    • Opiate receptors are classified into proposed subtypes: mu, kappa, and sigma.
    • Stereoisomers of pharmacologically active compounds can exhibit differential binding affinities and potencies at receptor subtypes.
    • Understanding stereoselectivity is crucial for elucidating receptor structure and function.

    Purpose of the Study:

    • To investigate the stereoselectivity patterns of cyclazocine, SKF-10047, ketamine, and dexoxadrol at mu, kappa, and sigma opiate receptors.
    • To determine if observed stereoselectivity differences support the concept of biochemically distinct opiate receptor subclasses.

    Main Methods:

    • Radioligand displacement assays were employed to assess the binding affinities of stereoisomers.
    • Specific radioligands ([3H]dihydromorphine, [3H]ethylketocyclazocine, [3H]phencyclidine) were used to target different receptor subtypes.
    • Assays were controlled to account for potential cross-reactivity and isolate binding to specific receptor classes.

    Main Results:

    • (-) isomers of cyclazocine and SKF-10047 were significantly more potent displacers of [3H]dihydromorphine (mu receptor) than their (+) counterparts.
    • At kappa receptors, (-) isomers showed only moderate potency advantages over (+) isomers in displacing [3H]ethylketocyclazocine.
    • For sigma/PCP receptors, (+) ketamine was four times more potent than (-) ketamine, and dexoxadrol was significantly more potent than levoxadrol.

    Conclusions:

    • Stereoisomer potency varies considerably across mu, kappa, and sigma opiate receptor subtypes.
    • The observed stereospecificity patterns align with behavioral studies at the sigma/PCP receptor.
    • These findings provide evidence supporting the hypothesis that opiate receptor subclasses are biochemically distinct entities.

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