新型^(18)F标记心肌灌注显像剂的PET显像实验研究

The preliminary experimental study of a novel ^(18)F-labeled myocardial perfusion imaging agent for PET imaging

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(37MBq/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）-lH-1,2,3-triazol-l-yl）methyl）-2-pyridinyl）methoxy）-3 （2H）-pyridazinone （[18F] FPTP2） as a myocardial perfusion imaging＇agent, by animal positron emfssion tomography（PET） imaging.Metllods： [18F]FPTP2,,vas prepared by substituting tosyl of precursor with 18F, purified and corffirmed by HPLC.[18F] FPTP2 （37MBq/15kg） 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 rain 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.