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Related Experiment Videos

Para-substituted amphetamines and brain serotonin.

K Magyar, J Knoll

    Polish Journal of Pharmacology and Pharmacy
    |October 1, 1975
    PubMed
    Summary
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    V-111, a para-substituted amphetamine, selectively inhibits neurotransmitter reuptake and release. Its (+) isomer shows greater potency for dopamine and norepinephrine, suggesting potential for targeted amphetamine effects.

    Area of Science:

    • Neuroscience
    • Pharmacology
    • Medicinal Chemistry

    Background:

    • Amphetamines are widely studied for their psychoactive effects.
    • Understanding structure-activity relationships is crucial for developing targeted therapeutics.
    • Para-substituted amphetamines exhibit diverse neurochemical profiles.

    Purpose of the Study:

    • To investigate the neurochemical effects of V-111, a para-substituted amphetamine.
    • To determine the stereoselective actions of V-111 on monoamine transporters.
    • To explore the potential for selective serotonergic and catecholaminergic modulation by V-111.

    Main Methods:

    • Inhibition assays measuring synaptosomal reuptake of radiolabeled serotonin (3H-5-HT), norepinephrine (3H-NA), and dopamine (3H-DA).
    • Assessment of V-111's potency in releasing preloaded monoamines from synaptosomes.

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  • Comparison of the effects of V-111's optical isomers on reuptake and release.

    • Main Results:

    • V-111 demonstrated potent inhibition of 3H-5-HT reuptake, with both isomers being equally effective.
    • The (+) isomer of V-111 was a more potent inhibitor of 3H-NA and 3H-DA reuptake.
    • Both isomers effectively released 3H-5-HT, while the (+) isomer showed greater potency for releasing 3H-NA and 3H-DA.

    Conclusions:

    • V-111 exhibits stereoselective effects on monoamine transporter systems.
    • The differential potency of V-111 isomers suggests potential for developing amphetamines with selective serotonergic or catecholaminergic actions.
    • In vivo irreversible uptake inhibition may be mediated by V-111 metabolites.