Abstract
1466 Objectives Four 18F-labelled pyridaben analogues were synthesized and evaluated as potential myocardial perfusion imaging (MPI) agents. Methods Four precursors and corresponding nonradioactive compounds were synthesized. Radiotracers were obtained by substituting tosyl with 18F, and evaluated as MPI agents in vitro, ex vivo and in vivo. Results Total radiosynthesis time was 70-90 min. Radiochemical yields were 38-58% (corrected). After stored in water for 3 h, their radiochemical purities were still >95%. All four tracers showed high initial heart uptake (34-54 %ID/g at 2 min post injection) in mice. The heart/liver, heart/lung and heart/blood ratios of [18F]Fmpp2 were kept > 3.5 at all the time points. In Whole-Body PET imaging, [18F]Fmpp2 exhibited excellent initial heart SUV (7.12 at 2 min p.i.) and good retention (5.75 at 120 min p.i.). The heart/liver SUV ratios of [18F]Fmpp2 were 1.72, 4.12, 5.42 and 5.99 at 5, 30, 60 and 120 min, suggesting its huge potential for MPI. Conclusions Four lipophilic tracers were successfully prepared in good radiochemical yields and purities. All four tracers showed excellent stabilities in water and high initial heart uptake in mice. Among them, [18F]Fmpp2 exhibited best image quality with clear outline of heart and fast clearance of non-target tissues, suggesting it could be a novel MPI agent for further evaluation. Research Support This study was financially supported by the National Natural Science Foundation of China (81301251, 81271613).
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