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目的 探讨新型18F标记心肌灌注显像(MPI)药物4-氯-2-叔丁基-5[2-[[1-[2-[2-氟-18F-乙氧基]乙氧基]-1H-1,2,3-三唑-4-基]甲基]苯基甲氧基]-3(2H)-哒嗪酮(18F-MyoZone)在小型猪体内的生物分布特点及其PET MPI的性能.方法 制备18F-MyoZone.选择6只健康巴马小型猪,静脉注射18F-MyoZone 111 MBq,注射后5、20、40、60和120 min分别行PET全身显像,测量各组织器官平均标准摄取值(SUVmean)及心/肝、心/肺放射性摄取比值,并观察其随时间的变化.制备急性心肌梗死(n=3)和慢性心肌缺血(n=3)小型猪模型,与健康小型猪(n=3)同行PET MPI,评价18F-MyoZone的MPI性能.结果 18F-MyoZone校正的放化产率为(52.0±4.3)％(n=3),纯化后的放化纯＞98％.18F-MyoZone注射后早期,心肌即有较高摄取,给药后5 min心肌SUVmean即达10.40±2.40,且在120min内有较稳定的滞留(9.30±2.00).心脏邻近的非靶器官,如肝、肺摄取较低,清除快,注射后5min的心/肝、心/肺放射性比值分别为4.77±0.91和17.14±5.84,注射后120 min达11.16±1.38和21.69±7.09.PET MPI显示,正常心肌对18F-MyoZone呈现分布均匀的高摄取,梗死心肌和严重缺血心肌呈现放射性缺损改变,部分缺血心肌可见负荷/静息显像的可逆性改变.18 F-MyoZone注射后120 min内心肌图像质量均保持稳定.结论 18 F-MyoZone心肌摄取较高,且快速、持久,非靶器官干扰小,在早期显像和提供较宽的诊断时间窗等方面具有优势,是一种生物学性能较为优良的PET MPI药物.“,”Objective To investigate the biodistribution of 4-chloro-2-tert-butyl-5-[2-[[1-[2-[2-18 F-fluroethoxy] ethoxymethyl]-1H-1,2,3-triazol-4-yl] methyl] phenylmethoxy]-3(2H)-pyridazinone (18F-MyoZone) and evaluate its clinical potential as a PET myocardial perfusion imaging (MPI) tracer in miniswine.Methods 18F-MyoZone was prepared.Twelve Bama mini-swine were intravenously injected with approximately 111 MBq of 18F-MyoZone to evaluate PET imaging characteristics.Whole-body PET scans were performed at the timing of 5,20,40,60 and 120 min postinjection to measure time-dependent mean stand-ardized uptake value (SUVmean) in multiple organs of health animals (n =6).SUVmean ratios of myocardium/liver and myocardium/lung over time were then calculated.Mini-swine with induced acute myocardial infarction (n =3) and chronic myocardial ischemia (n =3) accompanying with health mini-swine (n =3) were utilized to evaluate the diagnostic capability of 18F-MyoZone PET MPI.Results The typical decay-corrected radiochemical yield of 18 F-MyoZone reached (52.0±4.3)％ (n =3) with a high radiochemical purity (＞98％).In the biodistribution study,high initial myocardial uptake (SUVmean =10.40±2.40 at 5 min postinjection) and remarkable myocardial retention (SUVmean =9.30±2.00 at 120 min postinjection) were observed.The adjacent organs (like the liver and lungs) indicated low tracer uptake and rapid clearance.The heart/liver and heart/lung SUVmean ratios were 4.77±0.91 and 17.14±5.84 respectively at 5 min postinjection,with an increase to 11.16± 1.38 and 21.69±7.09 at 120 min postinjection.In the MPI study of miniswine,normal myocardium demonstrated uniform tracer distribution with clearly visualizable myocardial boundary,infarct myocardium and severe ischemia myocardium performed intense resting perfusion defect,and ischemia myocardium revealed reversible perfusion defect by stress/rest MPI.The myocardial image quality remained stable within 120 min postinjection.Conclusions MPI with 18F-MyoZone exhibits high initial myocardial uptake and low extracardiac activities in adjacent organs.Advantages in early imaging and wide diagnostic time window make it a promising PET MPI tracer.