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常咯啉在亚细胞部位的分布

INTRACELLULAR DISTRIBUTION OF CHANGROLIN

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【作者】 屠曾宏陈恩鸿吴巍巍杨惠华

【Author】 Tu Zenghong, Chen Enhong, Wu Weiwei and Yang Huihua (Department of Pharmacology, Shanghai Institute of Materia Medica)

【机构】 中国科学院上海药物研究所中国科学院上海药物研究所

【摘要】 常咯啉(4-{3′,5′-Bis[(N-pyrrolidinyl)metbyl]-4′-Hydroxyaniline}quinazoline)。是一个有效抗心律失常药 用差离心法研究了该药在家兔心肌亚细胞部位,核、线粒体和上清液三部分的分布。发现上清液部位药物分布最多,其次是核部分。各种物化试验证明,常咯啉分布到核部分似乎是一个“物理”过程。上清液中约6.8%药物和细胞浆蛋白结合。

【Abstract】 Changrolin, 4-{3′, 5′-Bis [(Pyrrolidinyl) methyl]-4′-Hydroxy-anilino} quinazoline, is an antiarrhythmic drug. Its intracellular distribution in myocardium of rabbits has been studied by differential centrifugation. The components of cells were fractionated into three parts, nuclear, mitochondrial and supernatant fraction. Most of the drug was found in the supernatant fraction. Next is the nuclear fraction. Physico-chemical studies demonstrate that the binding of Changrolin to the nuclear fraction is a rather "physical" process. Part of the drug in the supernatant fraction has been proved to be associated with the cytoplasmic proteins.

  • 【文献出处】 药学学报 ,Acta Pharmaceutica Sinica , 编辑部邮箱 ,1979年10期
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