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    • 15. 发明申请
    • SCREENING, DIAGNOSTIC AND/OR DOSAGE METHOD AND DEVICE OF AN AGONIST AND/OR ANTAGONIST FOR A CALCIUM-COUPLED RECEPTOR
    • 筛选,诊断和/或剂量方法和用于钙联合受体的激动剂和/或拮抗剂的装置
    • WO2002075273A2
    • 2002-09-26
    • PCT/EP2002/003121
    • 2002-03-20
    • EUROSCREEN S.A.DUPRIEZ, VincentPARMENTIER, Marc
    • DUPRIEZ, VincentPARMENTIER, Marc
    • G01N
    • G01N33/5091C07K14/705G01N33/5008G01N33/502G01N2333/726
    • The present invention relates to a screening, diagnostic and/or dosage method of a known or unknown agonist (full agonist or partial agonist) and/or a known or unknown antagonist (neutral antagonist or inverse agonist) for a calcium-coupled receptor, comprising following steps:incubating one or more cells expressing apoaequorin and said calcium-coupled receptor with "coelenterazine i" having the formula as depicted in Figure 3 or a derivative thereof, in order to reconstitute active aequorin by said cells; contacting said cell(s) with the agonist and/or antagonist of said receptor on a solid support, and,measuring light emitted by said cell(s), allowing the screening, diagnosis and/or dosage of said agonist and/or antagonist of said receptor, and, possibly, recovering said agonist or antagonist of said receptor from the reaction mixture. The present invention also relates to a corresponding device allowing the performance of said method and to the agonist and/or antagonist of said calcium-coupled receptor identified by said method and device.
    • 本发明涉及用于钙偶联受体的已知或未知的激动剂(全激动剂或部分激动剂)和/或已知或未知的拮抗剂(中性拮抗剂或反向激动剂)的筛选,诊断和/或剂量方法,包括 以下步骤:将一种或多种表达载脂蛋白和所述钙偶联受体的细胞与具有如图3所示的配方或其衍生物的“肠培养液i”一起孵育,以便由所述细胞重建活性水母发光蛋白; 使所述细胞与所述受体的激动剂和/或拮抗剂在固体支持物上接触,以及测量由所述细胞发射的光,允许所述激动剂和/或拮抗剂的筛选,诊断和/或剂量 所述受体,并且可能从所述反应混合物中回收所述受体的所述激动剂或拮抗剂。 本发明还涉及允许所述方法和由所述方法和装置鉴定的所述钙偶联受体的激动剂和/或拮抗剂的表现的相应装置。