正电子心肌灌注显像剂18F-TPT的合成及生物学分布

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MicroPET／CT显像。结果显示，18F—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，18F—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。MicroPET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...

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Bibliographic Details
Published in同位素 Vol. 26; no. 2; pp. 79 - 85
Main Author 张晓军 刘健 关志伟 田嘉禾 孙志军 张锦明
Format Journal Article
LanguageChinese
Published 中国人民解放军总医院核医学科,北京,100853 2013
Subjects
18F—TPT
亲脂性阳离子
心肌灌注显像剂
心肌灌注显像剂
亲脂性阳离子
18F-TPT
Online AccessGet full text
ISSN1000-7512
DOI10.7538/tws.2013.26.02.0079

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Summary: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MicroPET／CT显像。结果显示，18F—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，18F—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。MicroPET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。
Bibliography:11-2566/TL
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
ISSN:1000-7512
DOI:10.7538/tws.2013.26.02.0079