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    Method for identifying the agonistic activity of a target compound on a potassium channel
    49.
    发明申请
    Method for identifying the agonistic activity of a target compound on a potassium channel 审中-公开
    用于鉴定目标化合物在钾通道上的激动活性的方法

    公开(公告)号：US20080227819A1

    公开(公告)日：2008-09-18

    申请号：US12047989

    申请日：2008-03-13

    申请人： Timo Struenker ,  Markus Cavalar ,  Gregor Bahrenberg

    发明人： Timo Struenker ,  Markus Cavalar ,  Gregor Bahrenberg

    IPC分类号： C12Q1/02 ,  A61K31/165 ,  A61K31/444

    CPC分类号： G01N33/6872 ,  G01N33/582 ,  G01N2500/00

    摘要： A method for identifying the agonistic activity of a target compound on a potassium channel by a) providing a population of cells expressing a potassium channel and, optionally providing, a protein-based fluorescent-optical voltage sensor, b) if necessary, incubating the cells with a voltage-sensitive fluorescent dye, c) adding the target compound to the reaction batch of a) or b), d) determining a value F1 of the fluorescence intensity of the cells, e) adding potassium ions in a physiologically acceptable concentration f) determining a value F2 of the fluorescence intensity of the cells, and g) comparing the fluorescence intensity F2 with the fluorescence intensity F1 and determining the agonistic activity of the target compound on a potassium channel therefrom. A potassium channel agonist isolated and purified by this method, pharmaceutical formulations containing the same, and their use for the treatment of a disease in which potassium channels are involved.

    摘要翻译： 一种通过以下方法鉴定目标化合物在钾通道上的激动作用：a）提供表达钾通道的细胞群，并任选地提供基于蛋白质的荧光 - 光电压传感器，b）如果需要，培养细胞 使用电压敏感荧光染料，c）将目标化合物加入到a）或b）的反应批料中，d）测定细胞荧光强度的值F 1，e）加入 生理学上可接受的浓度的钾离子f）确定细胞的荧光强度的值F 2 N，g）将荧光强度F 2 N与荧光强度F 确定靶化合物在钾通道上的激动活性。 通过该方法分离和纯化的钾通道激动剂，含有其的药物制剂及其用于治疗其中涉及钾通道的疾病的用途。