科研之友
微信
新浪微博
Facebook
分享链接
摘要
Objective: Carbon-11-raclopride (C-11-R) is a positron-emitting radiotracer successfully used for the study of cognitive control and widely applied in PET imaging. A simple automated preparation of C-11-R by using the reaction of carbon-11-methyl triflate (C-11-MeOTF) or C-11-methyl iodide (C-11-Mel) with demethylraclopride is described. Methods: Specifically we used a simple setup applied an additional "U" reaction vessel for C-11-MeOTf compared with C-11-Mel and assessed the influence of several solvents and of the amount of the percussor for C-11-methylation of demethylraclopride by the bubbling method. The reversal of retention order between product and its precursor has been achieved for C-11-R, enabling collection of the purified-C-11-R by using the HPLC column after shorter retention time. Results: By the improved radiosynthesis and purification strategy, C-11-R could be prepared with higher radiochemical yield than that of the previous studies. The yield for C-11-MeOTf was 76% and for C-11-CH3I >26% and with better radiochemical purity (>99% based on both C-11-MeOTf and C-11-Mel) as compared to the previously obtained purity of C-11-R using HPLC method with acetonitrile as a part of mobile phase. Furthermore, by using ethanol as the organic modifier, residual solvent analysis prior to human injection could be avoided and C-11-R could be injected directly following simple dilution and sterile filtration. Conclusion: Improved radiosynthesis and HPLC purification in combination with ethanol containing eluent, extremely shortened the time for preparation of C-11-R, gave a higher radiochemical yield and purityfor C-11-R and can be used for multiple and faster synthesis of C-11-R and probably for other C-11-labeled radiopharmaceuticals.
- 出版日期2015-9
- 单位浙江大学
