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  • 标题:[3H]nitrendipine-labeled calcium channels discriminate inorganic calcium agonists and antagonists
  • 本地全文:下载
  • 作者:R J Gould ; K M Murphy ; S H Snyder
  • 期刊名称:Proceedings of the National Academy of Sciences
  • 印刷版ISSN:0027-8424
  • 电子版ISSN:1091-6490
  • 出版年度:1982
  • 卷号:79
  • 期号:11
  • 页码:3656-3660
  • DOI:10.1073/pnas.79.11.3656
  • 语种:English
  • 出版社:The National Academy of Sciences of the United States of America
  • 摘要:[3H]Nitrendipine binds with high affinity to brain membranes with a drug specificity indicating association with sites mediating the pharmacologic actions of dihydropyridine slow-calcium-channel antagonist drugs. In brain membranes, [3H]nitrendipine binding is absolutely dependent on the presence of calcium ions. Interactions of cation with [3H]nitrendipine binding sites correlate with their physiologic actions at voltage-dependent calcium channels. Ions such as strontium and barium, which mimic calcium physiologically, share the action of calcium in enhancing [3H]nitrendipine binding. Ions such as lanthanum an cobalt, which block the effects of calcium, can inhibit [3H]nitrendipine binding and block the stimulating actions of calcium. The ability to monitor the influence of ions on an agonist-antagonist continuum at [3H]nitrendipine binding sites provides a molecular probe to explore the regulation of cellular function by calcium and other cations.
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