目的：通过初步动物实验，评价4-氯-2-叔丁基-5-[[6-[[4-(2-氟-18F-乙基)-1H-1，2，3-三唑-1-基]甲基]-2-吡啶基]甲氧基]-3(2H)-哒嗪酮(18F-FPTP2)用于心肌灌注发射型正电子断层显像(PET)的可能性。方法：采用18F-F-取代OTs前体的方法进行标记，通过HPLC非梯度洗脱进行纯化，并通过HPLC确认标记化合物结构。中华小型猪经静脉注射18F-FPTP2(37 MBq/15 kg)，并于注射后2 min、10 min、20 min、30 min、40 min、50 min和60 min分别进行PET/CT扫描。结果：18F-FPTP2制备的总时间为70 min，未校正的放化产率为(25±7.2)%，放射化学纯度＞98%。PET研究表明，18F-FPTP2在中华小型猪中的心肌摄取随时间的延长而增加，靶器官与非靶器官比值亦随之增加。注射后2 min，心和(或)肝以及心和(或)肺放射性摄取比值分别为0.65±0.10和3.47±0.29。注射后60 min，心和(或)肝以及心和(或)肺放射性摄取比值分别为0.92±0.13和9.28±0.77。结论：18F-FPTP2能够被心肌组织摄取而显影清晰，但心和(或)肝放射性摄取比值需要进一步提高。%Objective: To preliminarily evaluate the potential of 2-tert-butyl-4-chloro-5-((6-((4-(2-[18F]fluroethyl)-1H-1,2,3-triazol-1-yl)methyl)-2-pyridinyl)methoxy)-3(2H)-pyridazinone ([18F]FPTP2) as a myocardial perfusion imaging agent, by animal positron emission tomography(PET) imaging. Methods:[18F]FPTP2 was prepared by substituting tosyl of precursor with 18F, purified and confirmed by HPLC. [18F] FPTP2 (37 MBq/15 kg) was injected into Chinese mini-swines intravenously by a venous catheter. The cardiac PET scans were performed at 2, 10, 20, 30, 40, 50 and 60 min after injection. Results:The total radio-synthesis time was 70 min, radiochemical yield was 25±7.2% without correction. The radiochemical purities (RCP) were >98% after purification. In PET imaging study, the heart uptake and target-to-nontarget uptake ratios increased with time. The heart/liver and heart/lung ratios were 0.65±0.10 and 3.47±0.29 at 2 min post injection, 0.92±0.13 and 9.28±0.77 at 60 min post injection respectively. Conclusion:Although the higher uptake of [18F]FPTP2 were shown in myocardium, the heart/liver ratio still need to be improved in future study.
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