(S)-2-((S)-2-(4-(3-[18F]fluoropropyl)benzamido)-3-phenylpropanamido)pentanedioic acid labeled with 18F |
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Authors: | Yong He Rui Ding Hang Liu Xiao Wang Jing-Li Xu Man Feng Yu-Rong Chen Chuan-Min Qi Cheng Peng Zhao-Hui Zhu Yong-Hong Dang Ming Wang Yun-Chuan Ma |
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Institution: | 1. Key Laboratory of Radiopharmaceutical, College of Chemistry, Beijing Normal University, Beijing, China 2. PET Center of Xuan Wu Hospital, Beijing, China 3. Department of Nuclear Medicine, PUMC Hospital, CAMS and PUMC, Beijing, 100730, 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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