^(11)C-β-CFT:多巴胺转运蛋白显像剂的合成及其在帕金森病诊断中的应用  

Synthesis of dopamine transporter imaging agent^(11)C-β-CFT and its application in the diagnosis of Parkinson's disease

作　　者：王慧 刘子钰 白侠[2] 包宝亮[2] 何玉林[2] WANG Hui;LIU Ziyu;BAI Xia;BAO Baoliang;HE Yulin(School of Pharmacy,Inner Mongolia Medical University,Hohhot 010050,China;Department of Nuclear Medicine,the Affiliated Hospital of Inner Mongolia Medical University,Hohhot 010050,China)

机构地区：[1]内蒙古医科大学药学院,内蒙古呼和浩特010050 [2]内蒙古医科大学附属医院核医学科,内蒙古呼和浩特010050

出　　处：《分子影像学杂志》2023年第4期605-608,共4页Journal of Molecular Imaging

基　　金：国家自然科学基金(82060323);内蒙古自治区高等学校“青年科技英才支持计划”项目(NJYT22003);内蒙古自治区自然科学基金(2022MS08003)。

摘　　要：目的探讨脑多巴胺转运蛋白显像剂^(11)C-甲基-N-2β-甲基酯-3β-(4-F-苯基)托烷(^(11)C-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^(11)C-CH_(3)I在线转换成Triflate-^(11)CH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^(11)C-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^(11)C-β-CFT后约60min后对其进行脑部PET/CT显像。结果^(11)C-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^(11)C-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^(11)C-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。Objective To investigate the clinical value of PET/CT imaging of cerebral dopamine transporter imaging agent^(11)C-methyl-N-2β-carbomethoxy-3β-(4-flurophenyl)tropanel(^(11)C-β-CFT)in the early diagnosis of Parkinson's disease.Methods The^(11)C-CH_(3)I generated by the first step of the reaction was converted into Triflate-^(11)CH_(3) 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^(11)C-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^(11)C-β-CFT.Results The total synthesis time of^(11)C-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^(11)C-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^(11)C-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.

关 键 词：帕金森病 多巴胺转运蛋白 11C-β-CFT 正电子发射断层显像 

分 类 号：R742.5[医药卫生—神经病学与精神病学] R817.4[医药卫生—临床医学]