@article{oai:repo.qst.go.jp:00047267, author = {Tiwari, Anjani and Ji, Bin and Yui, Joji and Fujinaga, Masayuki and Yamasaki, Tomoteru and Xie, Lin and Luo, Rui and Shimoda, Yoko and Kumata, Katsushi and Zhang, Yiding and Hatori, Akiko and Maeda, Jun and Higuchi, Makoto and Wang, Feng and Zhang, Ming-Rong and ティワリ アンジャニ and 季 斌 and 由井 譲二 and 藤永 雅之 and 山崎 友照 and 謝 琳 and 下田 陽子 and 熊田 勝志 and 張 一鼎 and 羽鳥 晶子 and 前田 純 and 樋口 真人 and 張 明栄}, issue = {9}, journal = {Theranostics}, month = {May}, note = {We evaluated the efficacy of 2-[5-(4-[(18)F]fluoroethoxy-2-oxo-1,3-benzoxazol-3(2H)-yl)-N-methyl-N-phenylacetamide] ([(18)F]FEBMP) for positron emission tomography (PET) imaging of translocator protein (18 kDa, TSPO). Dissection was used to determine the distribution of [(18)F]FEBMP in mice, while small-animal PET and metabolite analysis were used for a rat model of focal cerebral ischemia. [(18)F]FEBMP showed high radioactivity uptake in mouse peripheral organs enriched with TSPO, and relatively high initial brain uptake (2.67 ± 0.12% ID/g). PET imaging revealed an increased accumulation of radioactivity in the infarcted striatum, with a maximum ratio of 3.20 ± 0.12, compared to non-injured striatum. Displacement with specific TSPO ligands lowered the accumulation levels in infarcts to those on the contralateral side. This suggests that the increased accumulation reflected TPSO-specific binding of [(18)F]FEBMP in vivo. Using a simplified reference tissue model, the binding potential on the infarcted area was 2.72 ± 0.27. Metabolite analysis in brain tissues showed that 83.2 ± 7.4% and 76.4 ± 2.1% of radioactivity was from intact [(18)F]FEBMP at 30 and 60 min, respectively, and that this ratio was higher than in plasma (8.6 ± 1.9% and 3.9 ± 1.1%, respectively). In vitro autoradiography on postmortem human brains showed that TSPO rs6971 polymorphism did not affect binding sites for [(18)F]FEBMP. These findings suggest that [(18)F]FEBMP is a promising new tool for visualization of neuroinflammation.}, pages = {961--969}, title = {[(18)F]FEBMP: Positron Emission Tomography Imaging of TSPO in a Model of Neuroinflammation in Rats, and in vitro Autoradiograms of the Human Brain.}, volume = {5}, year = {2015} }