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

中华核医学与分子影像杂志 Pub Date : 2020-02-25 DOI:10.3760/CMA.J.ISSN.2095-2848.2020.02.004

Ya-wen Wang, Kai Han, Zuoquan Zhao

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Abstract

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 adjacent organs. Advantages in early imaging and wide diagnostic time window make it a promising PET MPI tracer. Key words: Myocardial perfusion imaging; MyoZone; Fluorine radioisotopes; Positron-emission tomography; Swine

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新型18F标记心肌灌注显像示踪剂18F MyoZone PET显像的实验研究

目的研究4-氯-2-叔丁基-5-[2-[[1-[2-[2-18F-氟乙氧基]乙氧基甲基]-1H-1,2,3-三唑-4-基]甲基]苯基甲氧基]-3（2H）-哒嗪酮（18F-MyoZone）的生物分布，评价其作为小型猪心肌灌注显像（MPI）示踪剂的临床应用潜力。方法制备18F MyoZone。12头巴马小型猪静脉注射约111MBq的18F MyoZone，以评估PET成像特征。在注射后5、20、40、60和120分钟进行全身PET扫描，以测量健康动物（n=6）多个器官中与时间相关的平均标准摄取值（SUVmean）。然后计算心肌/肝和心肌/肺随时间的SUV平均比值。利用诱发急性心肌梗死的小型猪（n=3）和伴随健康小型猪（n=3）的慢性心肌缺血的小型猪来评估18F MyoZone PET MPI的诊断能力。结果18F MyoZone的典型衰变校正放射化学产率达到（52.0±4.3）%（n=3），放射化学纯度较高（>98%）。在生物分布研究中，观察到高的初始心肌摄取（注射后5分钟SUVmean=10.40±2.40）和显著的心肌滞留（注射后120分钟SUV均值=9.30±2.00）。邻近器官（如肝和肺）显示示踪剂摄取低，清除快。心/肝和心/肺SUV平均比值在注射后5min分别为4.77±0.91和17.14±5.84，在注射后120min分别增加到11.16±1.38和21.69±7.09。在小型猪的MPI研究中，正常心肌表现出均匀的示踪剂分布，心肌边界清晰可见，梗死心肌和严重缺血心肌表现出强烈的静息灌注缺陷，缺血心肌通过应力/静息MPI表现出可逆的灌注缺陷。心肌图像质量在注射后120分钟内保持稳定。结论含18F肌带的MPI表现出较高的初始心肌摄取和较低的心外活动。早期成像和宽诊断时间窗口的优势使其成为一种有前途的PET MPI示踪剂。关键词：心肌灌注成像；MyoZone；氟放射性同位素；正电子发射断层扫描；猪

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来源期刊

中华核医学与分子影像杂志核医学，分子影像

自引率

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发文量

5088

期刊介绍： Chinese Journal of Nuclear Medicine and Molecular Imaging (CJNMMI) was established in 1981, with the name of Chinese Journal of Nuclear Medicine, and renamed in 2012. As the specialized periodical in the domain of nuclear medicine in China, the aim of Chinese Journal of Nuclear Medicine and Molecular Imaging is to develop nuclear medicine sciences, push forward nuclear medicine education and basic construction, foster qualified personnel training and academic exchanges, and popularize related knowledge and raising public awareness. Topics of interest for Chinese Journal of Nuclear Medicine and Molecular Imaging include: -Research and commentary on nuclear medicine and molecular imaging with significant implications for disease diagnosis and treatment -Investigative studies of heart, brain imaging and tumor positioning -Perspectives and reviews on research topics that discuss the implications of findings from the basic science and clinical practice of nuclear medicine and molecular imaging - Nuclear medicine education and personnel training - Topics of interest for nuclear medicine and molecular imaging include subject coverage diseases such as cardiovascular diseases, cancer, Alzheimer’s disease, and Parkinson’s disease, and also radionuclide therapy, radiomics, molecular probes and related translational research.