@article{oai:repo.qst.go.jp:00047100,
 author = {Ji, Bin and Kumata, Katsushi and Onoe, Hirotaka and Kaneko, Hiroyuki and Zhang, Ming-Rong and Seki, Chie and Ono, Maiko and Shukuri, Miho and Tokunaga, Masaki and Minamihisamatsu, Takeharu and Suhara, Tetsuya and Higuchi, Makoto and 季 斌 and 熊田 勝志 and 尾上 浩隆 and 金子 博之 and 張 明栄 and 関 千江 and 小野 麻衣子 and 宿里 充穂 and 徳永 正希 and 南久松 丈晴 and 須原 哲也 and 樋口 真人},
 journal = {Brain research},
 month = {Aug},
 note = {Cyclooxygenase-2 (COX-2) plays crucial roles in progressive neuronal death in ischemic brain injury. In the present study, we evaluated two radiolabeled COX-2 selective inhibitors, [11C]celecoxib and [11C]rofecoxib, as positron emission tomography (PET) tracers for COX-2 imaging in normal and ischemic mouse brains. We also took advantage of our newly-generated antibody highly selective for mouse COX-2 to prove accumulation of the radioligands in regions enriched with COX-2. In vitro autoradiography demonstrated specific binding of high-concentration [11C]rofecoxib but not [11C]celecoxib to the cerebellum and brain stem of normal brains wherein COX-2 immunoreactivity in neurons was most abundantly observed. Meanwhile, both of these radioligands failed to detect COX-2 expression in PET assays despite their excellent brain permeability. Hypoperfusion-induced ischemia caused marked necrotic neuron death accompanied by gliosis and enhancement of neuronal COX-2 immunoreactivity in the hippocampus. Correspondingly, in vitro autoradiographic binding of [11C]rofecoxib was increased in the injured hippocampus compared to the uninjured contralateral region, but failed in living brains of ischemia model likewise. Our work provides the rationale for monitoring COX-2 as a biomarker reflecting ischemic brain injuries and demonstrates that [11C]rofecoxib, not [11C]celecoxib, is useful for in vitro assays of COX-2, but its affinity would be insufficient for in vivo PET visualization.},
 pages = {152--162},
 title = {Assessment of radioligands for PET imaging of cyclooxygenase-2 in an ischemic neuronal injury model.},
 volume = {1533},
 year = {2013}
}