心肌灌注显像剂18F-BMS747158-02的自动化合成与心肌缺血模型显像  

Automatic Synthesis of Myocardial Perfusion Imaging Agent 18F-BMS747158-02 and Imaging of Myocardial Ischemia Model

作　　者：何玉林[1] 刘子钰 王文瑞 贾凯丽 王相成[1] 王雪梅[1] HE Yulin;LIU Ziyu;WANG Wenrui;JIA Kaili;WANG Xiangcheng;WANG Xuemei(Nuclear Medicine Department,The Affiliated Hospital of Inner Mongolia Medical University,Key Laboratory of Molecular Imaging,Inner Mongolia Autonomous Region,Hohhot 010050,China)

机构地区：[1]内蒙古医科大学附属医院核医学科内蒙古自治区分子影像重点实验室,呼和浩特010050

出　　处：《同位素》2020年第6期417-422,共6页Journal of Isotopes

基　　金：国家自然科学基金(81660295,81960318)。

摘　　要：18F-BMS747158-02是氟-18标记的哒螨灵衍生物,是一种靶向线粒体复合物-Ⅰ的新型正电子核素心肌灌注显像剂。本研究进行18F-BMS747158-02的全自动化合成及其急性心肌缺血模型动物的显像,并与国内常用心肌灌注显像剂13N-NH3·H2O进行比较。18F-BMS747158-02的合成经亲核取代、高效液相分离和固相萃取三步完成,总合成时间约60 min、未经衰减校正的合成产率为(15.3±2.1)%(n=5)、放化纯度大于99%。显像研究发现18F-BMS747158-02心肌首次提取率高、心肌摄取快、血流灌注相关性好、心肌滞留时间长、放射性摄取均匀、肝内摄取低、图像对比度高的特点,证实其有心肌灌注PET显像的独特潜力。18F-BMS747158-02 is a fluorine-18-labeled pyridaben derivative and a new positron radionuclide myocardial perfusion imaging tracer targeting mitochondrial complex-Ⅰ.In this study,18F-BMS747158-02 was synthesized fully automatically and applied in the imaging of acute myocardial ischemia model animals.Its imaging performance was compared with 13N-NH3·H2O,a commonly used myocardial perfusion imaging agent in China.The synthesis of 18F-BMS747158-02 was completed by three steps:nucleophilic substitution,high-performance liquid phase separation and solid phase extraction.The total synthesis time was about 60 min.The synthesis yield was(15.3±2.1)%(EOB,n=5).The radiochemical purity was greater than 99%.Imaging studies found that the 18F-BMS747158-02 myocardium had a high primary myocardial uptake rate,fast myocardial uptake,good correlation with blood perfusion,long myocardial retention time,uniform radioactive uptake,low intrahepatic uptake,and high image contrast,which confirmed the unique potential of the agent in myocardial perfusion PET imaging.

关 键 词：18F-BMS747158-02 13N-NH3·H2O 心肌灌注显像 

分 类 号：TL923[核科学技术—核燃料循环与材料] R817.9[医药卫生—影像医学与核医学]