基于AllinOne合成模块自动化合成^(18)F-MK-6240并初步用于阿尔茨海默病  

Automatic synthesis of ^(18)F-MK-6240 with AllinOne synthesis module and preliminary application in Alzheimer disease

作　　者：黄政海 任超[2] 吴美其 张现忠 霍力[2] HUANG Zhenghai;REN Chao;WU Meiqi;ZHANG Xianzhong;HUO Li(Institute of Clinical Medicine,Peking Union Medical College Hospital,Chinese Academy of Medical Science and Peking Union Medical College,Beijing 100730,China;Department of Nuclear Medicine,Peking Union Medical College Hospital,Chinese Academy of Medical Science and Peking Union Medical College,Beijing 100730,China)

机构地区：[1]中国医学科学院北京协和医学院北京协和医院临床医学研究所,北京100730 [2]中国医学科学院北京协和医学院北京协和医院核医学科,北京100730

出　　处：《中国医学影像技术》2024年第12期1909-1913,共5页Chinese Journal of Medical Imaging Technology

基　　金：北京协和医院中央高水平医院临床科研专项(2022-PUMCH-B-071)。

摘　　要：目的采用AllinOne合成模块自动化合成^(18)F-MK-6240,初步观察其用于阿尔茨海默病(AD)的价值。方法基于AllinOne合成模块使^(18)F-MK-6240前体与^(18)F-发生亲核反应而形成^(18)F标记中间体^(18)F-MK-6240-Boc,再经酸水解、高效液相色谱法分离及固相萃取纯化获得^(18)F-MK-6240;对其进行质量控制。前瞻性对1例AD及1例非AD认知障碍患者行^(18)F-MK-6240 PET/CT扫描;观察其初步应用价值。结果基于AllinOne合成模块成功自动合成^(18)F-MK-6240,合成时间为80 min,不校正合成效率为20.74%±2.31%,放射化学纯度>95%,无菌检测、细菌内毒素检测、异常毒性检测及溶剂残留检测均符合国家标准。^(18)F-MK-6240 PET/CT显示AD患者双侧额叶、顶叶、颞叶及岛叶tau蛋白沉积,非AD认知障碍患者颅内未见tau蛋白沉积。结论基于AllinOne合成模块可自动化合成^(18)F-MK-6240且产品质量合格,用于AD具有临床价值。Objective To observe the preliminary application value of^(18)F-MK-6240 automatically synthesized with AllinOne synthesis module in Alzheimer disease(AD).Methods Based on AllinOne synthesis module,^(18)F-labeled intermediate^(18)F-MK-6240-Boc was formed with^(18)F-MK-6240 precursor through nucleophilic reaction with^(18)F-.After hydrolyzed by acid,separated by high performance liquid chromatography and purified by solid-phase extraction,^(18)F-MK-6240 was obtained,and quality control was performed.^(18)F-MK-6240 PET/CT scanning was performed in 1 AD patient and 1 non-AD patient with cognitive impairment who were prospectively enrolled,and the preliminary application value of the product was observed.Results^(18)F-MK-6240 was successfully automatically synthesized based on AllinOne synthesis module,the synthesis time was 80 min,no-corrected synthesis efficiency was 20.74%±2.31%,radiochemical purity was greater than 95%,and sterility test,bacterial endotoxins test,abnormal toxicity test and solvent residual test all met national standards.^(18)F-MK-6240 PET/CT showed tau protein deposition of bilateral frontal,parietal,temporal and insular lobes in AD patients,while no tau protein deposition was observed in non-AD patients with cognitive impairment.Conclusion^(18)F-MK-6240 could be automatically synthesized based on AllinOne synthesis module,with qualified product quality and clinical application value in AD.

关 键 词：阿尔茨海默病 TAU蛋白质类 正电子发射断层显像和计算机体层摄影术 ^(18)F-MK-6240 

分 类 号：R742[医药卫生—神经病学与精神病学] R817.4[医药卫生—临床医学]