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    METHODS, COMPOSITIONS, AND KITS FOR TREATING PAIN AND PRURITIS
    1.
    发明申请
    METHODS, COMPOSITIONS, AND KITS FOR TREATING PAIN AND PRURITIS 有权
    用于治疗疼痛和瘙痒的方法，组合物和用具

    公开(公告)号：US20150087714A1

    公开(公告)日：2015-03-26

    申请号：US14496629

    申请日：2014-09-25

    申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  THE GENERAL HOSPITAL CORPORATION

    发明人： Bruce P. BEAN ,  Clifford J. WOOLF

    IPC分类号： A61K31/167 ,  A61K9/00

    CPC分类号： A61K31/167 ,  A61K9/0014 ,  A61K31/085 ,  A61K31/14 ,  A61K31/165 ,  A61K45/06 ,  A61P17/04

    摘要： The invention features a method for inhibiting one or more voltage-gated ion channels in a cell by contacting the cell with (i) a first compound that activates a channel-forming receptor that is present on nociceptors and/or pruriceptors; and (ii) a second compound that inhibits one or more voltage-gated ion channels when applied to the internal face of the channels but does not substantially inhibit said channels when applied to the external face of the channels, wherein the second compound is capable of entering nociceptors or pruriceptors through the channel-forming receptor when the receptor is activated. The invention also features a quaternary amine derivative or other permanently or transiently charged derivative of a compound that inhibits one or more voltage-gated ion channels when applied to the internal face of the channels but does not substantially inhibit said channels when applied to the external face of the channels.

    摘要翻译： 本发明的特征在于通过使细胞与（i）激活存在于伤害感受器和/或抗真菌剂上的通道形成受体的第一化合物接触来抑制细胞中的一个或多个电压门控离子通道的方法; 和（ii）当施加到通道的内表面时抑制一个或多个电压门控离子通道的第二化合物，但是当施加到通道的外表面时基本上不抑制所述通道，其中第二化合物能够 当受体被激活时，通过通道形成受体进入伤害性感受器或瘙痒感受器。 本发明还具有季铵衍生物或化合物的其它永久或瞬时带电的衍生物，其当施加到通道的内表面时抑制一个或多个电压门控离子通道，但当施加到外部表面时基本上不抑制所述通道 的渠道。