Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiamen 361005, China.
Department of Nuclear Medicine, Beijing Anzhen Hospital, Capital Medical University, Beijing 100029, China.
Sci Rep. 2016 Sep 20;6:33450. doi: 10.1038/srep33450.
This study reports three novel (18)F-labeled pyridaben analogues for potential myocardial perfusion imaging (MPI). Three precursors and the corresponding nonradioactive compounds were synthesized and characterized. The radiolabeled tracers were obtained by substituting tosyl with (18)F. The total radiosynthesis time of these tracers was 70-90 min. Typical decay-corrected radiochemical yields were 47-58%, with high radiochemical purities (>98%). Tracers were evaluated as MPI agents in vitro, ex vivo and in vivo. In the mouse biodistribution study, all three radiotracers showed high initial heart uptake (34-54% ID/g at 2 min after injection) and fast liver clearance. In the microPET imaging study, [(18)F]Fmpp2 produced heart images with good quality in both mice and rats. In the whole-body PET/CT images of mini-swine, [(18)F]Fmpp2 showed excellent initial heart standardized uptake value (SUV) (7.12 at 5 min p.i.) and good retention (5.75 at 120 min p.i.). The heart/liver SUV ratios were 4.12, 5.42 and 5.99 at 30, 60 and 120 min after injection, respectively. The favorable biological properties of [(18)F]Fmpp2 suggest that it is worth further investigation as a potential MPI agent.
本研究报告了三种新型（18）F 标记的哒螨灵类似物，用于潜在的心肌灌注成像（MPI）。合成并表征了三种前体和相应的非放射性化合物。用（18）F 取代甲苯磺酰基得到放射性标记示踪剂。这些示踪剂的总放射合成时间为 70-90 分钟。典型的放射性化学产率为 47-58%，放射化学纯度>98%。在体外、离体和体内评估了示踪剂作为 MPI 试剂的性能。在小鼠生物分布研究中，所有三种放射性示踪剂在注射后 2 分钟时均显示出较高的初始心脏摄取（34-54% ID/g）和快速的肝脏清除率。在 microPET 成像研究中，[（18）F]Fmpp2 在小鼠和大鼠中均产生了高质量的心脏图像。在小型猪的全身 PET/CT 图像中，[（18）F]Fmpp2 在 5 分钟（注射后）时显示出优异的初始心脏标准化摄取值（SUV）（7.12）和良好的保留（注射后 120 分钟时为 5.75）。注射后 30、60 和 120 分钟时，心脏/肝脏 SUV 比值分别为 4.12、5.42 和 5.99。[（18）F]Fmpp2 的良好生物学特性表明，它作为一种潜在的 MPI 试剂值得进一步研究。
