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(S)-2-((S)-2-(4-(3-[18F]fluoropropyl)benzamido)-3-phenylpropanamido)pentanedioic acid labeled with 18F

Abstract

As degradation product of Antineoplaston A10 in vivo, phenylacetyl glutamine showed antitumor activities. According to literatures, we designed and radiosynthesized a phenylacetyl glutamine derivative, which was achieved under a mild reaction condition. Evaluations in vitro and in vivo were performed on tumor bearing mice. Excitingly, the radiochemical purity of (S)-2-((S)-2-(4-(3-fluoropropyl)benzamido)-3-phenylpropanamido)pentanedioic acid ([18F]FBPPA) was 98%, and besides the best radiochemical yield was up to 46%. T/Bl (Tumor/Blood) and T/M (Tumor/Muscle) ratios of [18F]FBPPA at 60 min post injection were 2.33 and 3.51. Meanwhile, it showed satisfied stability in vitro and in vivo, compared with 2-[18F]fluorodeoxyglucose ([18F]FDG). Although [18F]FBPPA deserved further studies to make optimizations on its structure, the results revealed it might become a potential PET imaging agent for detecting tumors.

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Abbreviations

[18F]FBPPA:

(S)-2-((S)-2-(4-(3-fluoropropyl)benzamido)-3-phenylpropanamido)pentanedioic acid

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Acknowledgments

We acknowledged with thanks for financial supports from the National Natural Science Foundation of China (No.20371009 and No.20671014), Key laboratory of Radioactive Medicine of Ministry Education and Beijing Municipal Commission of Education.

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Correspondence to Chuan-Min Qi.

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He, Y., Ding, R., Liu, H. et al. (S)-2-((S)-2-(4-(3-[18F]fluoropropyl)benzamido)-3-phenylpropanamido)pentanedioic acid labeled with 18F. J Radioanal Nucl Chem 286, 135–140 (2010). https://doi.org/10.1007/s10967-010-0633-2

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Keywords

  • 18F
  • PET
  • Tumor