@article{oai:repo.qst.go.jp:00085193,
 author = {Hattori, Yasushi and Tomoteru, Yamasaki and Ohashi, Tomohiro and Miyanohana, Yuhei and Kusumoto, Tomokazu and Maeda, Ryouta and Miyamoto, Maki and Debori, Yasuyuki and Hata, Akito and Zhang, Yiding and Hidekatsu, Wakizaka and Takeshi, Wakabayashi and Masayuki, Fujinaga and Yamashita, Ryo and Zhang, Ming-Rong and Koike, Tatsuki and Hattori, Yasushi and Tomoteru, Yamasaki and Zhang, Yiding and Hidekatsu, Wakizaka and Takeshi, Wakabayashi and Masayuki, Fujinaga and Zhang, Ming-Rong},
 journal = {Journal of Medicinal Chemistry},
 month = {Aug},
 note = {Diacylglycerol kinase gamma (DGKγ) is a subtype of DGK enzyme which catalyzes ATPdependent conversion of diacylglycerol to phosphatidic acid. DGKγ, localized in brain, plays some important role in central nervous system. However, its function has not been widely investigated. Positron emission tomography (PET) imaging of DGKγ validates target engagement of therapeutic DGKγ inhibitors and investigates DGKγ levels under normal and disease conditions. In this study, we designed and synthesized a series of 3-acetyl indole
derivatives as candidates for PET imaging agents for DGKγ. Among the synthesized compounds, 2-((3-acetyl-1-(6-methoxypyridin-3-yl)-2-methyl-1H-indol-5-yl)oxy)-N-methylacetamide (9) exhibited potent inhibitory activity (IC50 = 30 nM) against DGKγ and desirable physicochemical properties allowing efficient blood-brain barrier penetration and low levels of undesirable nonspecific
binding. The radio-labeling of 9 followed by PET imaging of wild-type and DGKγ-
deficient mice and rats indicated that [11C]9 ([11C]T-278) specifically binds to DGKγ and yields a high signal-noise ratio for DGKγ in rodent brains.},
 pages = {11990--12002},
 title = {Design, Synthesis, and Evaluation of 11C-Labeled 3-Acetylindole Derivatives as Novel Positron-Emission Tomography Imaging Agent for Diacylglycerol Kinase Gamma (DGKγ) in Brain},
 volume = {64},
 year = {2021}
}