正电子心肌灌注显像剂18F-TPT的合成及生物学分布

doi:10.7538/tws.2013.26.02.0079

摘要/Abstract

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，¹⁸F-TPT合成时间约1 h，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。

关键词: font-family: 宋体">心肌灌注显像剂font-family: 'Times New Roman'">, font-family: 宋体">亲脂性阳离子font-family: 'Times New Roman'">, ¹⁸F-TPT

Abstract:

⁹⁹Tc^m-sestamibi is typically used as amyocardial perfusion imaging agent for SPECT, however, the high uptake of liverand lung compromise the diagnostic accuracy. PET has higher spatial resolutionand quantitative measurement of myocardial tracer uptake. The lipophiliccationic compound, (4-[¹⁸F]fluorophenyl)triphenylphosphoniumion (¹⁸F-TPT)was synthesized as a potential positron emission tomography (PET) myocardialperfusion agent, biodistribution studies in the NH rats and Micro PET/CTimaging studies in the SD rats were performed. Total synthesis time was about 1h and the uncorrected synthesis yield was 2.5%, radiochemical purity was higherthan 99.5%, the product had good stability at room temperature. Biodistributiondata in rats showed high levels of accumulation in the heart with stableretention and rapid blood clearance, Heart-to-liver ratios at 30, 60, 90,and120 min were 33.1, 14.8, 25.7 and 17.3, respectively; Micro PET/CT imagingin the SD rat showed intense cardiac uptake and non-target tissues as liver,lung uptake were washed out quickly. The result show that ¹⁸F-TPT may have potential as amyocardial perfusion imaging agent for PET.

Key words: font-family: 'Times New Roman'">myocardial perfusion imaging agent, lipophiliccationic compound, ¹⁸F-TPT

张晓军;刘健;关志伟;田嘉禾;孙志军;张锦明. 正电子心肌灌注显像剂¹⁸F-TPT的合成及生物学分布[J]. 同位素, 2013, 26(2): 79-85.

ZHANG Xiao-jun;LIU Jian;GUAN Zhi-peng;TIAN Jia-he;SUN Zhi-jun;ZHANG Jin-ming. Preparation andBiodistribution of Myocardial Perfusion Imaging Agent ¹⁸F-TPT[J]. Journal of Isotopes, 2013, 26(2): 79-85.

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正电子心肌灌注显像剂¹⁸F-TPT的合成及生物学分布

Preparation andBiodistribution of Myocardial Perfusion Imaging Agent ¹⁸F-TPT

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