新型^18F标记心肌灌注显像药物^18F-MyoZone的PET显像实验研究  

Experimental research of PET imaging with novel ^18F-labeled myocardial perfusion imaging tracer: ^18F-MyoZone

作　　者：王雅雯[1] 韩凯 赵祚全 方纬[1] Wang Yawen;Han Kai;Zhao Zuoquan;Fang Wei(Department of Nuclear Medicine,Fuwai Hospital,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100037,China)

机构地区：[1]北京协和医学院、中国医学科学院阜外医院核医学科,100037

出　　处：《中华核医学与分子影像杂志》2020年第2期82-87,共6页Chinese Journal of Nuclear Medicine and Molecular Imaging

摘　　要：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120 min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5 min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。^18F-MyoZone注射后120 min内心肌图像质量均保持稳定。结论^18F-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-^18F-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 mini-swine.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 standardized 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^18F-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 mini-swine,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

关 键 词：心肌灌注显像 MyoZone 氟放射性同位素 正电子发射断层显像术 猪 

分 类 号：R9[医药卫生—药学]