@article{oai:repo.qst.go.jp:00046886, author = {Chen, Chun-Jen and Bando, Kazunori and Ashino, Hiroki and Taguchi, Kazumi and Shiraishi, Hideaki and Fujimoto, Osuke and Kitamura, Chiemi and Matsushima, Satoshi and Fujinaga, Masayuki and Zhang, Ming-Rong and Kasahara, Hiroyuki and Minamizawa, Takao and Jiang, Cheng and Ono, Maiko and Higuchi, Makoto and Suhara, Tetsuya and Yamada, Kazutaka and Ji, Bin and 陳 忠正 and 藤永 雅之 and 張 明栄 and 小野 麻衣子 and 樋口 真人 and 須原 哲也 and 季 斌}, issue = {15}, journal = {Bioorganic & Medicinal Chemistry}, month = {Jun}, note = {Non-invasive detection for amyloid-β peptide (Aβ) deposition has important significance for the early diagnosis and medical intervention for Alzheimer's disease (AD). In this study, we developed a series of imidazopyridine derivatives as potential imaging agents for single-photon emission computed tomography (SPECT). Two of them, compounds DRK092 and DRM106, showed higher affinity for synthetic human Aβ 1-40 fibrils than did the well-known amyloid-imaging agent IMPY. A metabolite analysis revealed brain-permeable radioactive metabolites of (125)I-labeled DRK092 and IMPY; no radioactive metabolites from (125)I-labeled DRM106 ([(125)I]DRM106) were detected. In addition, in vitro autoradiography clearly demonstrated specific binding of [(125)I]DRM106 in the hippocampal region of AD enriched with Aβ plaques. Thus, our results strongly suggested that compound DRM106 can be used as an imaging agent for SPECT to detect Aβ deposition in AD brain.}, pages = {4189--4197}, title = {Synthesis and biological evaluation of novel radioiodinated imidazopyridine derivatives for amyloid-β imaging in Alzheimer's disease.}, volume = {22}, year = {2014} }