^(18)F-T807在TRACERlab FX_(FN)合成器上合成方法的优化及生物分布研究  

Synthesis method optimization and biodistribution study of^(18)F-T807 on TRACERlab FX_(FN) synthesizer

作　　者：左峰 霍花 王治国 张国旭 石庆学 张宗鹏 ZUO Feng;HUO Hua;WANG Zhiguo;ZHANG Guoxu;SHI Qingxue;ZHANG Zongpeng(Department of Nuclear Medicine,General Hospital of Northern Theater Command,Shenyang 110840,China;Institute of Drug Clinical Trial,General Hospital of Northern Theater Command,Shenyang 110840,China)

机构地区：[1]北部战区总医院核医学科,辽宁沈阳110840 [2]北部战区总医院药物临床试验机构办公室,辽宁沈阳110840

出　　处：《药学实践杂志》2021年第6期525-528,共4页Journal of Pharmaceutical Practice

基　　金：辽宁省自然科学基金(20170540927)。

摘　　要：目的优化^(18)F-T807的合成方法,并进行初步生物分布研究。方法使用TRACERlab FX_(FN)合成器,以BOC(t-Butyloxy carbonyl)保护的^(18)F-T807前体NPPI-9为起始原料,改进实验条件进行合成,进行质量控制分析和Wistar大鼠生物分布研究。结果改进合成条件合成产率由(20.5±6.1)%提高到(25.7±5.8)%,质控符合标准,Wistar大鼠肾、肝、血分布较高,在脑、心、肺摄取最低。结论使用改进一锅法合成^(18)F-T807简便易行,产率高,可以满足科研与临床的需求。Objective To optimize the synthesis method of^(18)F-T807 and study preliminary biodistribution.Methods^(18)FT807 was synthesized using an optimized method in TRACERlab FX_(FN) synthesizer with a t-BOC(t-Butyloxy carbonyl)-protected^(18)F-T807 precursor NPPI-9 as starting material,improving experimental conditions for synthesis,then QC and biodistribution study in Wistar rats conducted.Results The improved synthesis conditions increased the synthesis yield from 20.5%±6.1%to 25.7%±5.8%.QC met the standard.Wistar rats had higher intake in kidney,liver,blood and lowest intake in brain,heart,lung.Conclusion The optimized synthesis method to synthesize^(18)F-T807 is simple and easy,and high yield,which can meet the needs of scientific research and clinical practice.

关 键 词：T807 TAU蛋白 正电子药物 正电子发射扫描 

分 类 号：R981[医药卫生—药品]