@article{oai:repo.qst.go.jp:00049007,
 author = {Tang, Dewei and Fujinaga, Masayuki and Hatori, Akiko and Zhang, Yiding and Yamasaki, Tomoteru and Xie, Lin and Mori, Wakana and Kumata, Katsushi and Liu, Jianjun and Charles, Manning H. and Huang, Gang and Zhang, Ming-Rong and 藤永 雅之 and 羽鳥 晶子 and 張 一鼎 and 山崎 友照 and 謝 琳 and 森 若菜 and 熊田 勝志 and 張 明栄},
 journal = {European Journal of Medicinal Chemistry},
 month = {Feb},
 note = {Translocator Protein (18 kDa, TSPO) is regarded as a useful biomarker for neuroinflammation imaging. TSPO PET imaging could be used to understand the role of neuroinflammation in brain diseases and as a tool for evaluating novel therapeutic effects. As a promising TSPO probe, [18F]DPA-714 is highly specific and offers reliable quantification of TSPO in vivo. In this study, we further radiosynthesized and evaluated another novel TSPO probe, 2-(7-butyl-2-(4-(2-[18F]fluoroethoxy)phenyl)-5-methylpyrazolo[1,5-a]pyrimidin-3-yl)-N,N-diethylacetamide ([18F]VUIIS1018A), which features a 700-fold higher binding affinity for TSPO than that of [18F]DPA-714. We evaluated the performance of [18F]VUIIS1018A using dynamic in vivo PET imaging, radiometabolite analysis, in vitro autoradiography assays, biodistribution analysis, and blocking assays. In vivo study using this probe demonstrated high signal-to-noise ratio, binding potential (BPND), and binding specificity in preclinical neuroinflammation studies. Taken together, these findings indicate that [18F]VUIIS1018A may serve as a novel TSPO PET probe for neuroinflammation imaging.},
 pages = {1--8},
 title = {Evaluation of the novel TSPO radiotracer 2-(7-butyl-2-(4-(2-([18F]fluoroethoxy)phenyl)-5-methylpyrazolo[1,5-a]pyrimidin-3-yl)-N,N-diethylacetamide in a preclinical model of neuroinflammation},
 volume = {150},
 year = {2018}
}