[发明专利]通过神经元烟碱受体配体逆转左旋多巴诱导的运动障碍无效
申请号: | 201080026720.5 | 申请日: | 2010-06-15 |
公开(公告)号: | CN102802630A | 公开(公告)日: | 2012-11-28 |
发明(设计)人: | K·G·乔丹;S·R·莱彻沃斯;M·本彻瑞弗 | 申请(专利权)人: | 塔加西普特公司 |
主分类号: | A61K31/506 | 分类号: | A61K31/506;A61K31/505;A61P25/28;A61P25/00 |
代理公司: | 中国国际贸易促进委员会专利商标事务所 11038 | 代理人: | 李华英 |
地址: | 美国北*** | 国省代码: | 美国;US |
权利要求书: | 查看更多 | 说明书: | 查看更多 |
摘要: | |||
搜索关键词: | 通过 神经元 烟碱 受体 逆转 左旋多巴 诱导 运动障碍 | ||
背景技术
运动障碍或异常不自主运动(AIMs)会在长期使用左旋多巴的大多数帕金森病(PD)患者中发展,并可能像帕金森病本身一样造成身体虚弱。Quik及其同事最近证实烟碱会使患帕金森非人灵长类动物类和啮齿动物的左旋多巴诱导的似运动障碍性运动减少~50%。目前对左旋多巴诱导的AIM的可用治疗方法非常有限。因此,特别是由于烟碱不会中和左旋多巴的抗帕金森作用,关于烟碱治疗会减少这些运动的观察可能会提供一种新的治疗选择。
烟碱通常通过刺激神经元烟碱受体(NNRs)来发挥其作用。然而,烟碱以中枢和周围神经系统和骨骼肌中的多重NNRs作为靶点。除了任何需要的反应外,这还会导致副作用。因此,鉴别可减少左旋多巴诱导的运动障碍的NNR亚型选择性(subtype-selective)药物是有益的。
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