Synthesis of dopamine transporter imaging agent 11C- β- CFT and its application in the diagnosis of Parkinson's disease
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摘要:
目的 探讨脑多巴胺转运蛋白显像剂11C-甲基-N-2β-甲基酯-3β-(4-F-苯基)托烷（11C-β-CFT）的PET/CT显像在早期帕金森病诊断中的临床应用价值。 方法 将第一步反应生成的11C-CH3I在线转换成Triflate-11CH3后与前体2β-甲基酯-3β-(4-F-苯基)去甲基托烷进行室温反应，反应结束后加水转移反应液到C18柱上进行纯化，产品11C-β-CFT用乙醇从C18柱上洗脱后加水混匀得到终产品。5例轻度帕金森病患者静脉注射11C-β-CFT后约60 min后对其进行脑部PET/CT显像。 结果 11C-β-CFT的总合成时间约16 min，放化纯度>98%，比活度>2 GBq/μmol，未校正合成产率为（25.0±5.0）%。轻度帕金森病患者脑PET/CT显示双侧前壳核、后壳核11C-β-CFT摄取明显减少，以患病侧壳核区域最为显著。 结论 全自动化制备11C-β-CFT的合成速度快、产率高、产品放化纯度和比活度能够满足临床需求。上述显像结果表明该显像剂可准确反映病情，有助于帕金森病的早期诊断。 Abstract:Objective To investigate the clinical value of PET/CT imaging of cerebral dopamine transporter imaging agent 11C-methyl-N-2β-carbomethoxy-3β-(4-flurophenyl) tropanel(11C-β-CFT) in the early diagnosis of Parkinson's disease. Methods The 11C-CH3I generated by the first step of the reaction was converted into Triflate-11CH3 online and the precursor 2β-carbomethoxy-3β-(4-flurophenyl) demethylatropanel was reacted at room temperature, and after the reaction was completed, the reaction solution was transferred to the C18 column with water for purification, and the product 11C-β-CFT was eluted from the C18 column with ethanol and mixed with water to obtain the final product. Five patients with mild Parkinson's disease underwent brain PET/CT imaging about 60 minutes after intravenous injection of 11C-β-CFT. Results The total synthesis time of 11C-β-CFT was about 16 minutes, the clarification purity>98%, the specific activity>2 GBq/μmol, and the uncorrected synthesis yield was (25.0±5.0)%. Brain PET/CT in patients with mild Parkinson's disease showed a significant decrease in bilateral uptake of 11C-β-CFT in the anterior and posterior shell nuclei, most notably in the diseased side of the crustal nucleus. Conclusion The synthesis speed, high yield, and purity and specific activity of the fully automated preparation of 11C-β-CFT can meet the clinical needs. The above imaging results show that the imaging agent can accurately reflect the condition and help in the early diagnosis of Parkinson's disease. -
Key words:
- Parkinson's disease /
- dopamine transporter /
- 11C-β-CFT /
- PET/CT
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图 1 患者男，57岁，震颤10年，临床诊断为PD
Figure 1. Male, 57 years old, tremor for 10 years, clinical diagnosis of PD
PET/CT showed that there was a significant decrease in imaging agent uptake in both custard nuclei of the brain, which was significant on the right side, and there was no significant decrease in the uptake of bilateral caudate nuclei, and no abnormality on brain MRI.
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