摘要
目的 探讨合成18F-Flurpiridaz的优化方法,评估其在正常巴马小型猪PET/CT心肌灌注显像(MPI)中的分布情况.方法 以18F取代2-叔丁基-4-氯-5-[4-(2-甲基磺酰基-乙氧基甲基)苯基甲氧基]哒嗪-3-哒嗪酮中的苯磺酸离去基团进行标记,通过高效液相色谱非梯度洗脱的方法纯化产物.5头正常巴马小型猪经耳缘静脉注射37 MBq18F-Flurpiridaz后10 min行PET/CTMPI,并于注射后30和60 min进行PET/CT全身显像,观察显像剂在其体内主要脏器的摄取情况.结果 18F-Fiurpiridaz的制备时间约为50 min,非校正放射化学产率为40%,放射化学纯度>97%.MPI图像显示心肌细胞摄取明显,肝脏仅有少量摄取,肺基本无摄取,心肌图像质量好.全身显像中,显像剂注射后30 min,心肌和肾脏摄取明显,肌肉组织中有少量摄取,而其他组织器官均无明显摄取;显像剂注射后60 min,心脏内仍有较高摄取.结论 实现并优化了18F-Flurpiridaz的自动化合成,为其临床应用奠定了基础.
Objectve To explore the synthesis method of 18F-flurpiridaz and evaluate its ability for myocardial perfusion imaging(MPI)through PET/CT and bio-distribution in normal miniature pigs.Methods 18F-Flurpiridaz was prepared through the substitution of the toluene sulfonate leaving group of tert-butyl-4-chloro-5(4-(2-methyl(sulfonyl-ethoxymethyl)phenyl)methyl)pyridazin-3-one followed by radiolabeling with 18F.The product was isolated and purified by high performance liquid chromatography(HPLC)non-gradient elution.PET/CT MPI was performed 10 min after intravenous injection of 37 MBq 18F-flurpiridaz in five normal miniature pigs,and PET/CT whole-body scans were performed 30 and 60 min after injection to observe the bio-distribution.Results The total synthesis time(including HPLC separation)of 18F-flurpiridaz was approximately 50 min.The radiochemical yield was 40%(decay uncorrected),and the radiochemical purity was>97%(after HPLC purification).MPI results demonstrated that the radioactive uptake primarily accumulated in heart muscles,whereas little radioactivity was distributed throughout the liver and lungs.Moreover,the image quality was good.The whole-body PET/CT data showed high uptake in heart muscles and kidneys,whereas the skeleton muscle only had little radioactive uptake.No evident accumulations of activity in other organs were observed.18F-Flurpiridaz had higher retention in the myocardium 60 min after injection.Conclusion The automatic synthesis of 18F-flurpiridaz is realized and optimized,which lays a foundation for its clinical application.
作者
李帅
刘天文
汪娇
张杰民
王帆
李剑明
Li Shuai;Liu Tianwen;Wang Jiao;Zhang Jiemin;Wang Fan;Li Jianming(Department of Nuclear Medicine,TEDA International Cardiovascular Hospital,Chinese Academy of Medical Sciences,Peking Union Medical College,Tianjin 300457,China;Experimental Animal Center,TEDA International Cardiovascular Hospital,Chinese Academy of Medical Sciences,Peking Union Medical College,Tianjin 300457,China)
出处
《国际放射医学核医学杂志》
2020年第3期151-155,共5页
International Journal of Radiation Medicine and Nuclear Medicine
基金
天津市自然科学基金(17JCYBJC28200)
天津市滨海新区卫生计生委科技项目(2018BWKZ007)
泰达国际心血管病医院院级课题(2017TD-002)。
