Radiosynthesis and preliminary biological evaluation of the 2-[18F]fluoropropionic acid enantiomers for tumor PET imaging

被引:0
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作者
Zhanwen Zhang
Shaoyu Liu
Xiaolan Tang
Dahong Nie
Ganghua Tang
Aixia Sun
Ying Xiong
Hui Ma
Fuhua Wen
Ping Hu
机构
[1] Sun Yat-Sen University,Department of Nuclear Medicine, Guangdong Engineering Research Center for Translational Application of Medical Radiopharmaceuticals, The First Affiliated Hospital
[2] Sun Yat-Sen University,Department of Nuclear Medicine,The Sixth Affiliated Hospital
[3] South China Agricultural University,School of Materials and Energy
关键词
2-[; F]fluoropropionic acid; Optically pure tracer; Fatty acid; Prostate cancer; Positron emission tomography;
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摘要
The aim of this study was to synthesize the optically pure [18F]FPA, and to investigate the diagnostic value of different isomers. Semi-automated radiosynthesis of R-[18F]FPA or S-[18F]FPA was respectively from the chiral precursor (S)- or (R)-ethyl 2-(((trifluoromethyl)sulfonyl)oxy)propanoate via a two-step reaction and performed on the commercial FDG synthesizer. The improved radiochemical yields of R-[18F]FPA and S-[18F]FPA were 30–40% (decay-uncorrected, n = 10) in 35 min. There was no significant difference on the biodistribution of two enantiomers in normal mice (P > 0.05), but positron emission tomography imaging demonstrated that R-[18F]FPA was more suitable for PC3 tumor imaging than S-[18F]FPA and [18F]FDG.
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页码:153 / 159
页数:6
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