Department of Nuclear Medicine, The First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, China.
Clin Nucl Med. 2012 Aug;37(8):743-7. doi: 10.1097/RLU.0b013e31824c5fae.
Fully automated synthesis of 11C-labeled 2β-carbomethoxy-3β-(4-fluorophenyl)tropane (11C CFT) as a dopamine transporter positron emission tomography (PET) tracer is performed with Sep-Pak purification, which cannot separate 11C CFT from nor-β-CFT and will result in the residual precursor nor-β-CFT in the final 11C CFT injection. The aim of this study is to estimate the influence of the residual precursor nor-β-CFT in the 11C CFT injection on the Parkinson disease (PD) diagnosis results.
Automated synthesis of 11C CFT was performed using the different chemical amounts (0.10, 0.20, 0.25, and 0.30 mg) of nor-β-CFT with Sep-Pak purification. According to the given different amounts of nor-β-CFT in the radiosynthesis, clinically suspected 25 PD patients were randomly divided into the following 4 groups: 0.10 mg, 0.20 mg, 0.25 mg, and 0.30 mg, which had 5, 9, 5, and 6 cases, respectively. A normal control group with 0.10 mg of nor-β-CFT included 2 volunteers. After the brain PET images of the subjects were acquired, the regions of interests of striatum and cerebellum were drawn, and the standard uptake values of these regions were calculated. Finally, comparing the 18F FDG PET and clinical diagnosis, the coincidence rates of 11C CFT PET imaging for PD patients were determined.
Given 0.25 mg of the precursor nor-β-CFT, high radiochemical yield (59.4%) and high radiochemical purity of 11C CFT were obtained using Sep-Pak purification within a short synthesis time. The 11C CFT standard uptake value ratios of striatum to cerebellum had no statistically significant difference (P > 0.05) between the 4 suspected PD groups. However, there was statistically significant difference (P < 0.05) between the suspected PD groups and the control group. Also, the coincidence rates between the PD diagnosis using 11C CFT PET imaging for different dose groups and the final clinical diagnosis result were greater than 80%, but difference between the coincidence rates was not statistically significant (P = 0.955).
A simple, rapid, and efficient automated synthesis of 11C CFT using 0.25 mg of nor-β-CFT with Sep-Pak purification is afforded, providing enough radioactivity for PD PET imaging routinely. The residual nor-β-CFT in the 11C CFT injection is not inhibit 11C CFT binding to dopamine transporter, and also has no influence on PET diagnosis results of PD.
使用 Sep-Pak 纯化进行 11C 标记的 2β- carbomethoxy-3β-(4-fluorophenyl)tropane(11C CFT)的全自动合成,无法将 11C CFT 与 nor-β-CFT 分离,并且会导致最终的 11C CFT 注射中残留前体 nor-β-CFT。本研究的目的是评估 11C CFT 注射中残留前体 nor-β-CFT 对帕金森病(PD)诊断结果的影响。
使用不同量(0.10、0.20、0.25 和 0.30 mg)的 nor-β-CFT 进行 11C CFT 的自动化合成,并使用 Sep-Pak 纯化。根据放射合成中给定的 nor-β-CFT 的不同量,将 25 名临床疑似 PD 患者随机分为以下 4 组:0.10 mg、0.20 mg、0.25 mg 和 0.30 mg,分别有 5、9、5 和 6 例。包括 2 名志愿者在内的 0.10 mg nor-β-CFT 的正常对照组。在获得受试者的脑 PET 图像后,绘制纹状体和小脑的感兴趣区域,并计算这些区域的标准摄取值。最后,通过比较 18F FDG PET 和临床诊断,确定 PD 患者 11C CFT PET 成像的符合率。
在短的合成时间内,使用 Sep-Pak 纯化,当给予 0.25 mg 前体 nor-β-CFT 时,可获得 59.4%的高放射化学产率和 11C CFT 的高放射化学纯度。4 个疑似 PD 组之间纹状体与小脑的 11C CFT 标准摄取值比无统计学差异(P>0.05)。然而,疑似 PD 组与对照组之间存在统计学差异(P<0.05)。此外,不同剂量组使用 11C CFT PET 成像进行 PD 诊断的符合率均大于 80%,但符合率之间无统计学差异(P=0.955)。
使用 Sep-Pak 纯化从 0.25 mg nor-β-CFT 中获得了简单、快速、高效的 11C CFT 自动化合成,为 PD PET 成像常规提供了足够的放射性。11C CFT 注射中的残留 nor-β-CFT 不会抑制 11C CFT 与多巴胺转运体结合,也不会对 PD 的 PET 诊断结果产生影响。