正电子心肌灌注显像剂^(18)F-TPT的合成及生物学分布  

Preparation and Biodistribution of Myocardial Perfusion Imaging Agent ^(18)F-TPT

作　　者：张晓军[1] 刘健[1] 关志伟[1] 田嘉禾[1] 孙志军[1] 张锦明[1] 

机构地区：[1]中国人民解放军总医院核医学科,北京100853

出　　处：《同位素》2013年第2期79-85,共7页Journal of Isotopes

摘　　要：采用一步亲核取代法合成18F-(4-氟苯基)三苯基磷(18F-TPT),HPLC(高效液相色谱)分离纯化,研究其在正常NH小鼠体内生物分布,以正常SD大鼠进行Micro PET/CT显像。结果显示,18 F-TPT合成时间约1h,不矫正合成效率为2.5%,放化纯度大于99.5%,体外稳定性良好。小鼠体内分布结果表明,18 F-TPT在心肌浓聚,有较长时间滞留,肝摄取低,血液中清除很快;心与肝放射性摄取比在30、60、90、120min时分别为33.1、14.8、25.7和17.3。Micro PET显像表明,心肌轮廓明显,肺、肝等非靶器官基本不显像。结果提示,18F-TPT是一种较有潜力的心肌灌注显像剂,值得进一步研究。99Tcm-sestamibi is typically used as a myocardial perfusion imaging agent for SPECT, however, the high uptake of liver and lung compromise the diagnostic accuracy. PET has higher spatial resolution and quantitative measurement of myocardial tracer up- take. The lipophilic cationic compound, （4-[TM F] fluorophenyl） triphenylphosphonium ion （18F-TPT） was synthesized as a potential positron emission tomography （PET） myocardial perfusion agent, biodistribution studies in the NH rats and Micro PET/CT imaging studies in the SD rats were performed. Total synthesis time was about 1 h and the uncorrected syn- thesis yield was 2.5%, radiochemical purity was higher than 99.5%, the product had good stability at room temperature. Biodistribution data in rats showed high levels of accumula- tion in the heart with stable retention and rapid blood clearance, Heart-to-liver ratios at 30, 60, 90, andl20 min were 33.1, 14.8, 25.7 and 17.3, respectively; Micro PET/CT imaging in the SD rat showed intense cardiac uptake and non-target tissues as liver, lung uptakewere washed out quickly. The result show that 18F-TPT may have potential as a myocardial perfusion imaging agent for PET.

关 键 词：心肌灌注显像剂 亲脂性阳离子 18F—TPT 

分 类 号：R817[医药卫生—影像医学与核医学] TQ464.7[医药卫生—放射医学]