Biochemical evidence for pharmacological similarities between alpha-adrenoreceptors and voltage-dependent Na+ and Ca++ channels |
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Authors: | C Frelin P Vigne M Lazdunski |
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Affiliation: | Centre de Biochimie du CNRS, Université de Nice, Parc Valrose, 06034 Nice Cedex, France |
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Abstract: | The α-adrenergic antagonists yohimbine, prazozin and phentolamine, but not the α-adrenergic agonists, block voltage-dependent Na+ channels of rat brain synaptosomes. The lipid-soluble neurotoxins (veratridine, aconitine, grayanotoxins and ceveratrum alkaloids), which cause a permanent activation of the Na+ channels by acting at the same receptor site as yohimbine, compete with [3H]yohimbine for its binding to rat brain α2-adrenoreceptors. The calcium channel inhibitors verapamil and D600 also block the Na+ channel and recognize α2-adrenoreceptors. |
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