申请人:——
公开号:US05395946A1
公开(公告)日:1995-03-07
The invention related to a method of preparing a protein or a proteinaceous material labelled with a metalradionuclide and intended for diagnostic or therapeutic application, by reacting a protein or a proteinaceous material with an agent for coupling the radionuclide to the protein or the proteinaceous material, a protein conjugate being formed, and by then complexing the radionuclide with the conjugate thus formed to a radionuclide complex. A coupling agent is used which consists at least substantially of a thio compound of the general formula Y--R--S--X wherein X is a hydrogen atom or a suitable protective group, R is a branched or non-branched, optionally substituted hydrocarbon radical having 1-10 carbon atoms, which may be interrupted by one or more hereto atoms, and Y is at least one terminal reactive group capable of reacting with a functional group from the protein or the proteinaceous material; or a cyclic condensation product of the thio compound of formula I having 5-7 ring atoms, wherein X and Y together constitute a reactive group capable of reacting with a functional group from the protein or the proteinaceous material; or a water-soluble salt of this condensation product.
该发明涉及一种制备与金属放射性核素标记的蛋白质或蛋白质材料,用于诊断或治疗应用的方法,通过将蛋白质或蛋白质材料与用于将放射性核素偶联到蛋白质或蛋白质材料的试剂反应,形成蛋白质共轭物,然后将放射性核素与形成的共轭物络合成放射性核素复合物。使用至少主要由一般公式Y--R--S--X的硫化合物组成的偶联剂,其中X是氢原子或适当的保护基,R是一个分支或非分支的、可选择地取代的具有1-10个碳原子的烃基,可以被一个或多个氮原子中断,Y是至少一个能够与蛋白质或蛋白质材料的官能团反应的末端反应性基团;或者具有5-7个环原子的公式I的硫化合物的环缩聚物,其中X和Y共同构成能够与蛋白质或蛋白质材料的官能团反应的反应性基团;或者这种缩聚物的水溶性盐。