@article{oai:repo.qst.go.jp:00082553,
 author = {Zhou, Xiaoyun and Ji, Bin and Seki, Chie and Nagai, Yuji and Minamimoto, Takafumi and Fujinaga, Masayuki and Ming-Rong, Zhang and Saito, Takashi and C Saido, Takaomi and Suhara, Tetsuya and Kimura, Yasuyuki and Higuchi, Makoto and Xiaoyun, Zhou and Ji, Bin and Chie, Seki and Yuji, Nagai and Takafumi, Minamimoto and Masayuki, Fujinaga and Zhang, Ming-Rong and Tetsuya, Suhara and Yasuyuki, Kimura and Makoto, Higuchi},
 issue = {9},
 journal = {Journal of cerebral blood flow and metabolism},
 month = {Mar},
 note = {Colony-stimulating factor 1 receptor (CSF1R) is a specific biomarker for microglia. In this study, we developed a novel PET radioligand for CSF1R, C-GW2580, and compared it to a reported CSF1R tracer, C-CPPC, in mouse models of acute and chronic neuroinflammation and a rhesus monkey. Dynamic C-GW2580- and C-CPPC-PET images were quantified by reference tissue-based models and standardized uptake value ratio. Both tracers exhibited increased uptake in the lesioned striata of lipopolysaccharide-injected mice and in the forebrains of -knock-in mice, spatially in agreement with an increased 18-kDa translocator protein radioligand retention. Moreover, C-GW2580 captured changes in CSF1R availability more sensitively than C-CPPC, with a larger dynamic range and a smaller inter-individual variability, in these model animals. PET imaging of CSF1R in a rhesus monkey displayed moderate-to-high tracer retention in the brain at baseline. Homologous blocker (i. e. unlabeled tracer) treatment reduced the uptake of C-GW2580 by ∼30% in all examined brain regions except for centrum semi-ovale white matter, but did not affect the retention of C-CPPC. In summary, our results demonstrated that C-GW2580-PET captured inflammatory microgliosis in the mouse brain with higher sensitivity than a reported radioligand, and displayed saturable binding in the monkey brain, potentially providing an imaging-based quantitative biomarker for reactive microgliosis.},
 pages = {2410--2422},
 title = {PET imaging of colony-stimulating factor 1 receptor: A head-to-head comparison of a novel radioligand, 11C-GW2580, and 11C-CPPC, in mouse models of acute and chronic neuroinflammation and a rhesus monkey},
 volume = {41},
 year = {2021}
}