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Journal of Radioanalytical and Nuclear Chemistry
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, and Yun-Chuan Ma

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 Radioanalytical and Nuclear Chemistry
Authors: Gu-Cai Li, Duan-Zhi Yin, Deng-Feng Cheng, Ming-Qiang Zheng, Yan-Jiang Han, Han-Chen Cai, Jiao-Yun Xia, Sheng Liang, Wan-Bang Xu, and Yong-Xian Wang

Abstract  

3-(4-[18F]fluorobenzyl)-8-hydroxy-1,2,3,4-tetrahydrochromeno[3,4-c]pyridin-5-one ([18F]FHTP) was in vitro and in vivo evaluated as a putative dopamine D4 receptor radioligand. Its inhibition constant (K i) for cloned human dopamine D4.2 receptor was determined to be 2.9 nM and it displayed a 2000-fold D4-selectivity over the D2long subtype. Its partition coefficient (logP) was measured to be 1.11. Biodistribution, blocking distribution and metabolism studies in rats demonstrated that the specific distribution of [18F]FHTP in brain regions, suggesting that [18F]FHTP may be a suitable PET imaging agent for in vivo studies of the dopamine D4 receptor.

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