@article{oai:repo.qst.go.jp:00047239, author = {Yamasaki, Tomoteru and Fujinaga, Masayuki and Maeda, Jun and Kawamura, Kazunori and Yui, Joji and Hatori, Akiko and Yoshida, Yuichirou and Nagai, Yuji and Tokunaga, Masaki and Higuchi, Makoto and Suhara, Tetsuya and Fukumura, Toshimitsu and Zhang, Ming-Rong and 山崎 友照 and 藤永 雅之 and 前田 純 and 河村 和紀 and 由井 譲二 and 羽鳥 晶子 and 吉田 勇一郎 and 永井 裕司 and 徳永 正希 and 樋口 真人 and 須原 哲也 and 福村 利光 and 張 明栄}, issue = {4}, journal = {European Journal of Nuclear Medicine and Molecular Imaging}, month = {Nov}, note = {Purpose In this study, we evaluate the utility of 4-[18F]fluoro- N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-Nmethylbenzamide ([18F]FITM) as a positron emission tomography (PET) ligand for imaging of the metabotropic glutamate receptor subtype 1 (mGluR1) in rat and monkey brains. Methods In vivo distribution of [18F]FITM in brains was evaluated by PET scans with or without the mGluR1- selective antagonist (JNJ16259685). Kinetic parameters of monkey PET data were obtained using the two-tissue compartment model with arterial blood sampling. Results In PET studies in rat and monkey brains, the highest uptake of radioactivity was in the cerebellum, followed by moderate uptake in the thalamus, hippocampus and striatum. The lowest uptake of radioactivity was detected in the pons. These uptakes in all brain regions were dramatically decreased by pre-administration of JNJ16259685. In kinetic analysis of monkey PET, the highest volume of distribution (VT) was detected in the cerebellum (VT=11.5). Conclusion [18F]FITM has an excellent profile as a PET ligand for mGluR1 imaging. PET with [18F]FITM may prove useful for determining the regional distribution and density of mGluR1 and the mGluR1 occupancy of drugs in human brains.}, pages = {632--641}, title = {Imaging for metabotropic glutamate receptor subtype 1 in rat and monkey brains using PET with [18F]FITM}, volume = {39}, year = {2011} }