Mg2+ modulates the binding of [3H]glibenclamide to its receptor in rat cerebral cortical membranes

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    Radioligand binding studies were performed to determine the effect of various cations on the characteristics of [3H]glibenclamide binding to its high-affinity receptor in rat cerebral cortex membranes. Mg2+ was shown specifically to reduce radioligand binding to membranes pretreated with 5 mM EDTA. CaCl2 enhanced [3H]glibenclamide binding whilst MnCl2, KCl and NaCl were without significant effect. 2 mM MgCl2 induced a statistically significant rightward shift in the dissociation constant for glibenclamide obtained from both saturation and competition studies. These results suggest that Mg2+ may participate in the regulation of the sulphonylurea receptor in the rat cerebral cortex.
    Original languageEnglish
    Pages (from-to)347-351
    Number of pages5
    JournalEuropean Journal of Pharmacology
    Issue number3
    Publication statusPublished - 15 Nov 1993


    • Rats
    • Glyburide
    • Cerebral Cortex
    • Animals
    • Receptors, Drug
    • Cell Membrane
    • Cations, Divalent
    • Radioligand Assay
    • Magnesium
    • Potassium Channels


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