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Phenobarbitone binding sites in rat brain synaptosomal membranes

M Willow, I G Morgan, G A Johnston

    Neuroscience Letters
    |July 17, 1981
    PubMed
    Summary

    Barbiturates bind to specific sites in rat brain membranes, influencing the inhibitory neurotransmitter GABA. These binding sites are distinct from GABA receptors and may explain barbiturate

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    Area of Science:

    • Neuropharmacology
    • Neurochemistry

    Background:

    • Barbiturates are widely used for their sedative, hypnotic, and anticonvulsant properties.
    • The precise molecular mechanisms underlying barbiturate action, particularly their interaction with neurotransmitter systems, remain an area of active investigation.

    Purpose of the Study:

    • To characterize the binding sites of phenobarbitone in rat brain synaptosomeal membranes.
    • To investigate the relationship between phenobarbitone binding, other barbiturates, and the binding of gamma-aminobutyric acid (GABA).
    • To elucidate the potential role of these binding sites in the pharmacological effects of barbiturates.

    Main Methods:

    • Radioligand binding assays using phenobarbitone to identify and quantify binding sites in rat brain synaptosomeal membranes.
    • Competition binding studies with various substituted barbiturates to assess their affinity for phenobarbitone binding sites.
    • Experiments to evaluate the influence of GABA and other known modulators (bicuculline methochloride, diazepam, picrotoxinin) on phenobarbitone binding.
    • Membrane extraction studies using Triton X-100 to further differentiate phenobarbitone and GABA binding sites.

    Main Results:

    • Phenobarbitone binds to a single class of low-affinity, high-density sites in rat brain synaptosomeal membranes (Kd = 100 microM, Bmax = 800 pmol/mg protein).
    • The ability of substituted barbiturates to displace phenobarbitone correlates well with their anesthetic, anticonvulsant, or depressant properties and their ability to enhance GABA binding.
    • Convulsant barbiturates show a disproportionately greater enhancement of GABA binding compared to their displacement of phenobarbitone.
    • Phenobarbitone binding is not affected by GABA, bicuculline methochloride, diazepam, or picrotoxinin, indicating distinct binding sites.
    • Triton X-100 extraction abolishes phenobarbitone binding but enhances GABA binding, further supporting the distinction between these sites.

    Conclusions:

    • The identified phenobarbitone binding sites are distinct from GABA recognition sites and GABA-activated ionophores.
    • These sites are likely involved in the potentiation of GABA-mediated synaptic inhibition by barbiturates, contributing to their pharmacological actions.
    • The differential effects of various barbiturates on GABA binding suggest complex interactions at the molecular level.

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