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Development of ligand screening system for neurotransmitter receptor

机译:神经递质受体配体筛选系统的开发

摘要

Provided is a screening method for substances that bind to neurotransmitter receptors, have a group structure represented by formula (II) (in the formula, Rec-Nu represents a group obtained by separating a hydrogen atom from a neurotransmitter receptor (Rec-Nu-H). Nu represents a bivalent group obtained by separating a hydrogen atom from a nucleophile group (Nu-H) possessed by the neurotransmittor receptor. L2 represents a bilavent linking group and Fl represents a marker group). A candidate substance, the fluorescence patterns of which vary between when an antagonist is bound and when an agonist is bound, and which is expected to interact with a marked neurotransmitter receptor is made to act on the receptor, the binding mode of the candidate substance and the receptor is detected by variation in the signals emitted by a marker, and screening is carried out based on those results.
机译:提供了一种结合神经递质受体,具有式(II)表示的基团结构的物质的筛选方法(式中,Rec-Nu表示通过从神经递质受体分离氢原子而获得的基团(Rec-Nu-H ).Nu表示通过将氢原子与神经递质受体所具有的亲核基团(Nu-H)分离而获得的二价基团; L2表示bilavent连接基团,F1表示标记基团)。使候选物质的荧光模式在结合拮抗剂和结合激动剂之间变化,并预期与标记的神经递质受体相互作用,从而使其作用于受体,候选物质的结合方式和结合方式。通过标记物发出的信号变化来检测受体,并根据这些结果进行筛选。

著录项

  • 公开/公告号JP6670502B2

    专利类型

  • 公开/公告日2020-03-25

    原文格式PDF

  • 申请/专利权人 国立大学法人京都大学;

    申请/专利号JP20160504151

  • 发明设计人 浜地 格;清中 茂樹;若山 翔;

    申请日2015-02-19

  • 分类号G01N33/566;G01N33/15;G01N33/50;G01N33/542;G01N21/76;G01N21/78;C09B11/28;C09B19;A61K47/50;C12Q1/02;A61K45;A61P43;A61K47/22;C07D405/14;C07D498/14;C07D491/147;A61P25;

  • 国家 JP

  • 入库时间 2022-08-21 11:33:32

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