多巴胺转运蛋白显像剂^(11)C-β-CFT的全自动化合成  

Full Automated Synthesis of ^(11)C-β-CFT as a Dopamine Transporter Imaging Agent

作　　者：文富华[1] 邓怀福[1] 王红亮[1] 易畅[1] 杨云英[1] 吴克宁[1] 史新冲[1] 唐刚华[1] 

机构地区：[1]中山大学附属第一医院核医学科PET-CT中心,广东广州510080

出　　处：《同位素》2011年第4期193-197,共5页Journal of Isotopes

基　　金：中山大学"百人计划"引进人才科研启动基金(编号:80000-3126132);国家高技术研究发展计划(863计划)专题课题(编号:2008AA02Z430)

摘　　要：通过对反应条件的优化及合成模块的改进,探索了一种高效、全自动化合成11C-β-CFT的方法。以11CO2为起始原料与LiAlH4、HI或HBr反应生成11CH3I(或11CH3Br),再转化成Triflate-11CH3,最后与nor-β-CFT进行甲基化反应合成11C-β-CFT。整个合成工艺实现了全自动化,产品校正放化产率为70.2%±1.8%,放化纯度大于95%。用新方法合成的11C-β-CFT无菌注射液经pH测定、HPLC检测、内毒素检查、细菌培养及异常毒性检查,均符合注射液要求。用制备的11C-β-CFT对正常志愿者与帕金森病患者进行PET显像,PET显像显示正常对照者双侧纹状体影像清晰,帕金森病患者双侧纹状体不对称性摄取减低。该工艺实现了11C-β-CFT全自动化,放化产率高,工艺简单,有利于工作人员放射防护,显像效果良好,可满足临床需要。To develop an automatic and efficient synthesis of ^11C-β-CFT as a dopamine transporter imaging agent for clinical use, ^11C-β-CFT was prepared from ^11C-Triflate-CH3 by methylation with nor-β-CFT,and then purified by a C-18 Sep-Pak. Fully automated radiosynthesis of ^11C-β-CFT was carried out. The corrected radiochemical yield of ^11C-β-CFT was 70.2%±1. 8% from nCH3I or ^11CH3Br, and the radiochemical purity was above 95%. PET imaging was performed on healthy volunteers and patients with Parkinson＇s Disease （PD）. PET imaging showed high radioactivity uptake of ^11C-β-CFT in the bilateral striatums symmetrically for the healthy volunteers, but lower radioactivity uptake in the bilateral striatums asymmetrically for the PD patients. This simple automated synthesis of ^11C-β-CFT is efficient with high yields, helpful with the radiation protection of personnel, and satisfactory to clinical applications.

关 键 词：11C-β-CFT 多巴胺转运蛋白 自动化合成 

分 类 号：R817.9[医药卫生—影像医学与核医学]