New benzodiazepin-protein conjugate



PROBLEM TO BE SOLVED: To obtain the subject new conjugate which is a specific benzodiazepin- protein conjugate and used for detection of immunoassay of benzoazepin-based metabolite in the urine and useful for immunogen, for preparation of antibody having high crossreactivity to the metabolite. SOLUTION: This new benzoazepin-protein conjugate is represented by formula I {R 1 is H, methyl or a group of R {R is a group of formula II [Z is a carrier substance of a macromolecule which is active as an immunogen; (n) is 2 or 3]; R 2 is H, OH or OR; either one of R 1 and R 2 contains R; R 3 is a halogen, NO 2 or NH 2 ; X is H or a halogen}. The compound is used for immunoassay, etc., of urine concentration of a benzoazepin-based medicine, especially benzoazepin-based medicine such as tranquilizers and useful as an antigen for preparation of antibody having high crossreactivity to the metabolite. The conjugate is obtained by subjecting benzoazepin of formula III to aminoalkylation and reacting the alkylated product with an alkoxycarbonylmaleimide and reacting the prepared linker compound of formula IV with a compound of the formula Z-SH. COPYRIGHT: (C)1996,JPO
(57)【要約】 【課題】 様々なベンゾジアゼピン類、特に尿中のベン ゾジアゼピン代謝産物、に対して高い交差反応性を有す る抗体を生成しうるベンゾジアゼピン−タンパク質結合 体の形の免疫原を提供する。 【解決手段】 式I: 【化1】 〔式中、R 1 は水素、メチルまたはR基であり、R 2 は 水素、ヒドロキシルまたはOR基であり、その際R 1 か R 2 のどちらかがR基を含み、R 3 はハロゲン、NO 2 またはNH 2 であり、Xは水素またはハロゲンであり、 Rは式II: 【化2】 (式中、Zは免疫原として活性な巨大分子の担体物質で あり、nは2または3である)の基である〕で表される ベンゾジアゼピン−タンパク質結合体はベンゾジアゼピ ンに対する抗体を得るための免疫原として使用できる。




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