@article{oai:repo.qst.go.jp:00047070,
 author = {Fujinaga, Masayuki and Xie, Lin and Yamasaki, Tomoteru and Yui, Joji and Shimoda, Yoko and Hatori, Akiko and Kumata, Katsushi and Zhang, Yiding and Nengaki, Nobuki and Kawamura, Kazunori and Zhang, Ming-Rong and 藤永 雅之 and 謝 琳 and 山崎 友照 and 由井 譲二 and 下田 陽子 and 羽鳥 晶子 and 熊田 勝志 and 張 一鼎 and 念垣 信樹 and 河村 和紀 and 張 明栄},
 issue = {3},
 journal = {Journal of Medicinal Chemistry},
 month = {Feb},
 note = {Metabotropic glutamate 1 (mGlu1) receptor is found not only in the brain but also in melanomas and breast
cancers. mGlu1 is a promising target for molecular imaging-based diagnosis and treatment of melanoma because its
overexpression induces melanocyte carcinogenesis. Here we developed three PET tracers: 4-halogeno-N-[4-[6-(isopropylamino)-
pyrimidin-4-yl]-1,3-thiazol- 2-yl]-N-[11C]methylbenzamide ([11C]4−6), which exhibited high uptake in target tumor and
decreased uptake in nontarget brain tissues. In vitro binding assay indicated high to moderate binding affinities of 4−6 (Ki, 22−
143 nM) for mGlu1 receptor. In vivo biodistribution studies in mice implanted with B16F10 melanoma cells confirmed high
radioactive uptake in tumor and low uptake in blood, skin, and muscles. Inhibition of mGlu1 receptor using an mGlu1-selective
ligand led to reduced radioactive uptake in the tumor. [11C]6 displayed the highest ratio of uptake between tumor and nontarget
tissue and may prove useful as a PET tracer for mGlu1 imaging in melanoma.},
 pages = {1513--1523},
 title = {Synthesis and Evaluation of 4‑Halogeno‑N‑[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2- yl]‑N‑[11C]methylbenzamide for Imaging of Metabotropic Glutamate 1 Receptor in Melanoma},
 volume = {58},
 year = {2015}
}