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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| Published in | 同位素 Vol. 26; no. 2; pp. 79 - 85 |
|---|---|
| Main Author | |
| Format | Journal Article |
| Language | Chinese |
| Published |
中国人民解放军总医院核医学科,北京,100853
2013
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| Subjects | |
| Online Access | Get full text |
| ISSN | 1000-7512 |
| DOI | 10.7538/tws.2013.26.02.0079 |
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| 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。 |
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| AbstractList | 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。 R817%TQ464.7; 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lh,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、120 min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,18 F-TPT是一种较有潜力的心肌灌注显像剂,值得进一步研究. |
| Author | 张晓军 刘健 关志伟 田嘉禾 孙志军 张锦明 |
| AuthorAffiliation | 中国人民解放军总医院核医学科,北京100853 |
| AuthorAffiliation_xml | – name: 中国人民解放军总医院核医学科,北京,100853 |
| Author_FL | GUAN Zhi-peng SUN Zhi-jun TIAN Jia-he LIU Jian ZHANG Jin-ming ZHANG Xiao-jun |
| Author_FL_xml | – sequence: 1 fullname: ZHANG Xiao-jun – sequence: 2 fullname: LIU Jian – sequence: 3 fullname: GUAN Zhi-peng – sequence: 4 fullname: TIAN Jia-he – sequence: 5 fullname: SUN Zhi-jun – sequence: 6 fullname: ZHANG Jin-ming |
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| ClassificationCodes | R817%TQ464.7 |
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| Copyright | Copyright © Wanfang Data Co. Ltd. All Rights Reserved. |
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| DOI | 10.7538/tws.2013.26.02.0079 |
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| DocumentTitleAlternate | Preparation and Biodistribution of Myocardial Perfusion Imaging Agent 18F-TPT |
| DocumentTitle_FL | Preparation and Biodistribution of Myocardial Perfusion Imaging Agent 18F-TPT |
| EndPage | 85 |
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| Keywords | 心肌灌注显像剂 亲脂性阳离子 18F-TPT |
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| Notes | 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 |
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| Publisher | 中国人民解放军总医院核医学科,北京,100853 |
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| SubjectTerms | 18F—TPT 亲脂性阳离子 心肌灌注显像剂 |
| Title | 正电子心肌灌注显像剂18F-TPT的合成及生物学分布 |
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