通过正电子发射断层扫描成像研究突触密度的 [ C]UCB-J 的自动化放射性合成。
Automated radiosynthesis of [ C]UCB-J for imaging synaptic density by positron emission tomography.
机构信息
Radiopharmaceutical Unit, Wolfson Brain Imaging Centre, Department of Clinical Neurosciences, School of Clinical Medicine, University of Cambridge, Cambridge, UK.
University of Debrecen, Faculty of Medicine Department of Medical Imaging, Division of Nuclear Medicine and Translational Imaging, Department of Medical Imaging, Faculty of Medicine H-4032 Nagyerdei krt. 98, University of Debrecen, Debrecen, Hungary.
出版信息
J Labelled Comp Radiopharm. 2020 Mar;63(3):151-158. doi: 10.1002/jlcr.3828. Epub 2020 Feb 6.
An automated radiosynthesis of carbon-11 positron emission tomography radiotracer [ C]UCB-J for imaging the synaptic density biomarker synaptic vesicle glycoprotein SV2A was established using Synthra RNPlus synthesizer. Commercially available trifluoroborate UCB-J analogue was used as a radiolabelling precursor, and the desired radiolabelled product was isolated in 11 ± 2% (n = 7) nondecay corrected radiochemical yield and formulated as a 10% EtOH solution in saline with molar activities of 20 to 100 GBq/μmol. The method was based upon the palladium(0)-mediated Suzuki cross-coupling reaction and [ C]CH I as a radiolabelling synthon. The isolated product was cGMP compliant as demonstrated by the results of quality control analysis.
建立了一种使用 Synthra RNPlus 合成仪自动化合成用于成像突触密度生物标志物突触小泡糖蛋白 SV2A 的碳-11 正电子发射断层扫描放射性示踪剂 [ C]UCB-J 的方法。使用市售的三氟硼酸盐 UCB-J 类似物作为放射性标记前体，以 11±2%（n=7）的非衰变校正放射性化学产率分离得到所需的放射性标记产物，并配制成 10%乙醇在盐水中的溶液，摩尔活度为 20 至 100GBq/μmol。该方法基于钯(0)介导的 Suzuki 交叉偶联反应和 [ C]CH I 作为放射性标记合成子。通过质量控制分析的结果证明，分离得到的产物符合 cGMP 要求。
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