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12-α-[³H]-地高辛与完整人红细胞膜结合的特性:与地高辛治疗的相关性。

The characteristics of the binding of 12-alpha-[3H]-digoxin to the membranes of intact human erythrocytes: relevance to digoxin therapy.

作者信息

Ford A R, Aronson J K, Grahame-Smith D G, Rose J A

出版信息

Br J Clin Pharmacol. 1979 Aug;8(2):115-24. doi: 10.1111/j.1365-2125.1979.tb05809.x.

Abstract

1 The characteristics of the binding of 12-alpha-[3H]-digoxin to the membranes of intact human erythrocytes are described. 2 Only one class of binding site can be demonstrated. Binding is time- and temperature-dependent, saturable and slowly reversible; it is inhibited by other cardiac glycosides and by potassium. 3 Pre-incubation with unlabelled digoxin reduces the subsequent binding of 12-alpha-[3H]-digoxin in stoichiometric fashion. 4 The possible application of the measurement of the binding of 12-alpha-[3H]-digoxin to the study of biochemical pharmacological events occurring during digoxin therapy is discussed.

摘要
  1. 本文描述了12-α-[³H]-地高辛与完整人红细胞膜结合的特性。2. 仅能证明存在一类结合位点。结合具有时间和温度依赖性、可饱和且可逆性缓慢;它受到其他强心苷和钾的抑制。3. 与未标记的地高辛预孵育以化学计量方式降低随后12-α-[³H]-地高辛的结合。4. 讨论了测定12-α-[³H]-地高辛结合在研究地高辛治疗期间发生的生化药理事件中的可能应用。

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本文引用的文献

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Binding of the cardiac glycoside ouabain to intact cells.强心苷哇巴因与完整细胞的结合。
J Physiol. 1972 Jul;224(2):441-62. doi: 10.1113/jphysiol.1972.sp009904.

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