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    • 1. 发明授权
    • Compositions and methods for selective inhibition of nicotine acetylcholine receptors
    • 用于选择性抑制尼古丁乙酰胆碱受体的组合物和方法
    • US08980923B2
    • 2015-03-17
    • US13526076
    • 2012-06-18
    • Roger L. PapkeNicole A. HorensteinMichael M. FrancisKyung Il Choi
    • Roger L. PapkeNicole A. HorensteinMichael M. FrancisKyung Il Choi
    • A61K31/4465C07D211/44
    • C07D211/44
    • The present invention concerns methods for treating or preventing neurological disorders characterized by dysfunction of nicotinic acetylcholine receptors by administering 2,2,6,6-tetramethylpiperidin-4-yl heptanoate (TMPH), or a pharmaceutically acceptable salt thereof, to the patient. In another aspect, the present invention pertains to pharmaceutical compositions containing TMPH, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. In another aspect, the present invention pertains to methods for selectively inhibiting nicotinic acetylcholine receptors that lack an α5, α6, or β3 subunit by contacting an effective amount of TMPH, or a pharmaceutically acceptable salt thereof, to the receptor. The method for selectively inhibiting nicotinic acethylcholine receptors that lack an α5 subunit can be carried out in vivo or in vitro.
    • 本发明涉及通过向患者施用2,2,6,6-四甲基哌啶-4-基庚酸酯(TMPH)或其药学上可接受的盐来治疗或预防特征为烟碱乙酰胆碱受体功能障碍的神经障碍的方法。 另一方面,本发明涉及含有TMPH或其药学上可接受的盐和药学上可接受的载体的药物组合物。 另一方面,本发明涉及通过使有效量的TMPH或其药学上可接受的盐与受体接触来选择性地抑制缺乏α5,α6或αb亚基的烟碱乙酰胆碱受体的方法。 选择性抑制缺乏α5亚基的烟碱型乙酰胆碱受体的方法可以在体内或体外进行。