多巴胺转运蛋白显像剂^11C-β—CFT的全自动化合成

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...

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Bibliographic Details
Published in同位素 Vol. 24; no. 4; pp. 193 - 197
Main Author 文富华 邓怀福 王红亮 易畅 杨云英 吴克宁 史新冲 唐刚华
Format Journal Article
LanguageChinese
Published 中山大学附属第一医院核医学科PET-CT中心,广东广州,510080 2011
Subjects
11C-β-CFT多巴胺转运蛋白
自动化合成
多巴胺转运蛋白
11C-β-CFT
自动化合成
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Summary: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。
Bibliography:11-2566/TL
11C-β-CFT dopamine transporter ; automated synthesis
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.
WEN Fu-hua, DENG Huai-fu, WANG Hong-liang, YI Cha
ISSN:1000-7512