[3H]尼群地平标记的钙通道可区分无机钙激动剂和拮抗剂。
[3H]nitrendipine-labeled calcium channels discriminate inorganic calcium agonists and antagonists.
作者信息
Gould R J, Murphy K M, Snyder S H
出版信息
Proc Natl Acad Sci U S A. 1982 Jun;79(11):3656-60. doi: 10.1073/pnas.79.11.3656.
Abstract
[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.
摘要
[3H]尼群地平与脑膜具有高亲和力结合，其药物特异性表明与介导二氢吡啶类慢钙通道拮抗剂药物药理作用的位点相关。在脑膜中，[3H]尼群地平结合绝对依赖于钙离子的存在。阳离子与[3H]尼群地平结合位点的相互作用与其在电压依赖性钙通道上的生理作用相关。诸如锶和钡等在生理上模拟钙的离子，在增强[3H]尼群地平结合方面具有与钙相同的作用。诸如镧和钴等阻断钙作用的离子，可抑制[3H]尼群地平结合并阻断钙的刺激作用。监测离子对[3H]尼群地平结合位点上激动剂 - 拮抗剂连续体的影响的能力，提供了一种分子探针，用于探索钙和其他阳离子对细胞功能的调节。
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本文引用的文献
1
Membrane biophysics of calcium currents.钙电流的膜生物物理学
Fed Proc. 1981 Jun;40(8):2220-5.
2
[3H]-Nitrendipine, a potent calcium antagonist, binds with high affinity to cardiac membranes.[3H]-尼群地平，一种强效钙拮抗剂，与心肌膜具有高亲和力结合。
Arzneimittelforschung. 1981;31(12):2064-7.
3
High affinity binding of a calcium channel antagonist to smooth and cardiac muscle.钙通道拮抗剂与平滑肌和心肌的高亲和力结合。
Biochem Biophys Res Commun. 1982 Feb 26;104(4):1604-9. doi: 10.1016/0006-291x(82)91436-x.
4
The interaction of [3H]nitrendipine with receptors for calcium antagonists in the cerebral cortex and heart of rats.[3H]尼群地平与大鼠大脑皮层及心脏中钙拮抗剂受体的相互作用。
Biochem Biophys Res Commun. 1982 Feb 11;104(3):937-43. doi: 10.1016/0006-291x(82)91339-0.
5
Calcium antagonist receptor binding sites labeled with [3H]nitrendipine.用[3H]尼群地平标记的钙拮抗剂受体结合位点。
Eur J Pharmacol. 1982 Jan 22;77(2-3):201-2. doi: 10.1016/0014-2999(82)90021-8.
6
Calcium channel blocking agents in the treatment of cardiovascular disorders. Part II: Hemodynamic effects and clinical applications.钙通道阻滞剂在心血管疾病治疗中的应用。第二部分：血流动力学效应及临床应用。
Ann Intern Med. 1980 Dec;93(6):886-904. doi: 10.7326/0003-4819-93-6-886.
7
Calcium channel.钙通道
Annu Rev Neurosci. 1981;4:69-125. doi: 10.1146/annurev.ne.04.030181.000441.
8
Calcium channel blocking agents in the treatment of cardiovascular disorders. Part I: Basic and clinical electrophysiologic effects.钙通道阻滞剂在心血管疾病治疗中的应用。第一部分：基础与临床电生理效应
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9
Comparative pharmacology of calcium antagonists: nifedipine, verapamil and diltiazem.钙拮抗剂的比较药理学：硝苯地平、维拉帕米和地尔硫䓬。
Am J Cardiol. 1980 Dec 1;46(6):1047-58. doi: 10.1016/0002-9149(80)90366-5.
10
Divalent cations as charge carriers in excitable membranes.二价阳离子作为可兴奋膜中的电荷载体。
Prog Biophys Mol Biol. 1973;26:1-43. doi: 10.1016/0079-6107(73)90016-3.
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