多巴胺转运蛋白显像剂<sup>11</sup>C-<EM>β</EM>-CFT的全自动化合成

文富华; 邓怀福; 王红亮; 易畅; 杨云英; 吴克宁; 史新冲; 唐刚华

doi:10.7538/tws.2011.24.04.0193

多巴胺转运蛋白显像剂¹¹C-β-CFT的全自动化合成

中山大学附属第一医院核医学科PET-CT中心,广东广州510080

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出版历程
- 收稿日期: 1899-12-31
- 修回日期: 1899-12-31
- 刊出日期: 2011-11-19

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

PET-CT Center, Department of Nuclear Medicine, the First Affiliated Hospital, Sun Yat-sen University, Guangzhou 510080, China

摘要

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。
- ¹¹C-β-CFT /
- 多巴胺转运蛋白 /
- 自动化合成
Abstract: 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 ¹¹CH₃I 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.
- ¹¹C-β-CFT /
- dopamine transporter /
- automated synthesis

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参考文献(10)

[1]	Yoder KK, Hutchins GD, Mocka BH, et al. Dopamin transporter binding in rat striatum: a comparison of [O-methyl-¹¹C]β-CFT and [N-methyl-¹¹C] β-CFT [J]. Nucl Med Biol, 2009, 36: 11-16.
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多巴胺转运蛋白显像剂11C-β-CFT的全自动化合成

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

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目录

多巴胺转运蛋白显像剂¹¹C-β-CFT的全自动化合成

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