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Synthesis and biological evaluation of novel radioiodinated imidazopyridine derivatives for amyloid-β imaging in Alzheimer's disease.
https://repo.qst.go.jp/records/46886
https://repo.qst.go.jp/records/46886d16cbdd3-e11d-4d2e-9e51-e5690c9f836a
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2014-10-22 | |||||
| タイトル | ||||||
| タイトル | Synthesis and biological evaluation of novel radioiodinated imidazopyridine derivatives for amyloid-β imaging in Alzheimer's disease. | |||||
| 言語 | ||||||
| 言語 | eng | |||||
| 資源タイプ | ||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
| 資源タイプ | journal article | |||||
| アクセス権 | ||||||
| アクセス権 | metadata only access | |||||
| アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
| 著者 |
Chen, Chun-Jen
× Chen, Chun-Jen× Bando, Kazunori× Ashino, Hiroki× Taguchi, Kazumi× Shiraishi, Hideaki× Fujimoto, Osuke× Kitamura, Chiemi× Matsushima, Satoshi× Fujinaga, Masayuki× Zhang, Ming-Rong× Kasahara, Hiroyuki× Minamizawa, Takao× Jiang, Cheng× Ono, Maiko× Higuchi, Makoto× Suhara, Tetsuya× Yamada, Kazutaka× Ji, Bin× 陳 忠正× 藤永 雅之× 張 明栄× 小野 麻衣子× 樋口 真人× 須原 哲也× 季 斌 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | 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. | |||||
| 書誌情報 |
Bioorganic & Medicinal Chemistry 巻 22, 号 15, p. 4189-4197, 発行日 2014-06 |
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| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0968-0896 | |||||
| PubMed番号 | ||||||
| 識別子タイプ | PMID | |||||
| 関連識別子 | 24931274 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1016/j.bmc.2014.05.043 | |||||
