Department of Oncology, University of Alberta, Edmonton, Canada.
Bioorg Med Chem Lett. 2012 Mar 15;22(6):2291-5. doi: 10.1016/j.bmcl.2012.01.083. Epub 2012 Feb 2.
A new synthesis of O-(2-[(18)F]fluoroethyl)-L-tyrosine [(18)F]FET was developed using a NanoTek® microfluidic synthesis system (Advion BioSciences, Inc.). Optimal reaction conditions were studied through screening different reaction parameters like temperature, flow rate, reaction time, concentration of the labeling precursor, and the applied volume ratio between the labeling precursor and [(18)F]fluoride. [(18)F]FET was obtained after HPLC purification with 50% decay-corrected radiochemical yield starting from as little as 40 μg of labeling precursor. Small animal PET studies in EMT-6 tumor bearing mice showed radioactivity accumulation in the tumor (SUV(60min) 1.21±0.2) resulting in an slightly increasing tumor-to-muscle ratio over time.
一种新的 O-(2-[(18)F]氟乙基)-L-酪氨酸 [(18)F]FET 合成方法是使用 NanoTek®微流控合成系统(Advion BioSciences,Inc.)开发的。通过筛选不同的反应参数,如温度、流速、反应时间、标记前体的浓度以及标记前体与 [(18)F]氟化物的应用体积比,研究了最佳的反应条件。通过 HPLC 纯化,从少至 40μg 的标记前体开始,获得了 50%衰减校正的放射性化学产率的 [(18)F]FET。在 EMT-6 荷瘤小鼠的小动物 PET 研究中,放射性示踪剂在肿瘤中积累(SUV(60min)为 1.21±0.2),导致肿瘤与肌肉的比值随时间略有增加。