Authors:
Yong He Key Laboratory of Radiopharmaceutical, College of Chemistry, Beijing Normal University, Beijing, China

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Rui Ding Key Laboratory of Radiopharmaceutical, College of Chemistry, Beijing Normal University, Beijing, China

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Hang Liu Key Laboratory of Radiopharmaceutical, College of Chemistry, Beijing Normal University, Beijing, China

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Xiao Wang Key Laboratory of Radiopharmaceutical, College of Chemistry, Beijing Normal University, Beijing, China

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Jing-Li Xu Key Laboratory of Radiopharmaceutical, College of Chemistry, Beijing Normal University, Beijing, China

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Man Feng Key Laboratory of Radiopharmaceutical, College of Chemistry, Beijing Normal University, Beijing, China

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Yu-Rong Chen Key Laboratory of Radiopharmaceutical, College of Chemistry, Beijing Normal University, Beijing, China

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Chuan-Min Qi Key Laboratory of Radiopharmaceutical, College of Chemistry, Beijing Normal University, Beijing, China

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Cheng Peng PET Center of Xuan Wu Hospital, Beijing, China

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Zhao-Hui Zhu Department of Nuclear Medicine, PUMC Hospital, CAMS and PUMC, Beijing, 100730 China

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Yong-Hong Dang Department of Nuclear Medicine, PUMC Hospital, CAMS and PUMC, Beijing, 100730 China

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Ming Wang Key Laboratory of Radiopharmaceutical, College of Chemistry, Beijing Normal University, Beijing, China

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Yun-Chuan Ma PET Center of Xuan Wu Hospital, Beijing, China

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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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Journal of Radionalytical and Nuclear Chemistry
Language English
Size A4
Year of
Foundation
1968
Volumes
per Year
1
Issues
per Year
12
Founder Akadémiai Kiadó
Founder's
Address
H-1117 Budapest, Hungary 1516 Budapest, PO Box 245.
Publisher Akadémiai Kiadó
Springer Nature Switzerland AG
Publisher's
Address
H-1117 Budapest, Hungary 1516 Budapest, PO Box 245.
CH-6330 Cham, Switzerland Gewerbestrasse 11.
Responsible
Publisher
Chief Executive Officer, Akadémiai Kiadó
ISSN 0236-5731 (Print)
ISSN 1588-2780 (Online)