Gorshkov N I, Miroslavov А Е, Аlekseev I Е, Lumpov А А, Мurko А Y, Gavrilova I I, Saprykina N N, Bezrukova М А, Kipper А I, Krasikov V D, Suglobov D N, Tyupina M Y, Panarin Е F
Institute of Macromolecular Compounds, Federal State Budgetary Institute of Science, Russian Academy of Sciences, St Petersburg, Russia.
Khlopin Radium Institute Joint-Stock Company, St Petersburg, Russia.
J Labelled Comp Radiopharm. 2017 May 30;60(6):302-311. doi: 10.1002/jlcr.3503.
The procedure of the directed synthesis of N-vinylpyrrolidone-N-vinylformamide (VP-VFA) copolymers with grafted iminodiacetate (IDA) chelating units is presented. The methods for labelling resulting conjugates with indium-113m were developed. The metal-copolymer conjugates were characterized by different physicochemical methods, including IR and NMR, viscometry, light scattering, and exclusion high-performance liquid chromatography. Parameters of radiochemical synthesis of the conjugates labelled with indium-113m were optimized. It was shown that the VP-VFA-IDA copolymer firmly binds indium-113m both in the acid and alkaline solutions, with pH of the reaction mixture having almost no effect on the complexation. VP-VFA-IDA-In conjugates were found to be unstable in histidine challenge reaction.
介绍了具有接枝亚氨基二乙酸（IDA）螯合单元的N-乙烯基吡咯烷酮-N-乙烯基甲酰胺（VP-VFA）共聚物的定向合成过程。开发了用铟-113m标记所得共轭物的方法。通过不同的物理化学方法对金属-共聚物共轭物进行了表征，包括红外光谱和核磁共振、粘度测定、光散射和排阻高效液相色谱。优化了用铟-113m标记的共轭物的放射化学合成参数。结果表明，VP-VFA-IDA共聚物在酸性和碱性溶液中都能牢固地结合铟-113m，反应混合物的pH值对络合几乎没有影响。发现VP-VFA-IDA-In共轭物在组氨酸激发反应中不稳定。
