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Biological evaluation of the radioiodinated imidazo[1,2-a]pyridine derivative DRK092 for amyloid-β imaging in mouse model of Alzheimer's disease.
https://repo.qst.go.jp/records/46887
https://repo.qst.go.jp/records/46887f8c3dab6-d3d2-4867-b4c1-2e0ce4f8ee87
| 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 | Biological evaluation of the radioiodinated imidazo[1,2-a]pyridine derivative DRK092 for amyloid-β imaging in mouse model of 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× Shima, Keiji× Fujimoto, Osuke× Kitamura, Chiemi× Morimoto, Yasuaki× Kasahara, Hiroyuki× Minamizawa, Takao× Jiang, Cheng× Zhang, Ming-Rong× Suhara, Tetsuya× Higuchi, Makoto× Yamada, Kazutaka× Ji, Bin× 陳 忠正× 張 明栄× 須原 哲也× 樋口 真人× 季 斌 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Non-invasive determination of amyloid-β peptide (Aβ) deposition has important significance for early diagnosis and medical intervention in Alzheimer's disease (AD). In this study, we investigated the availability of a radioiodinated imidazo[1,2-a]pyridine derivative, termed (125)I-DRK092, as single photon emission computed tomography (SPECT) ligand for in vivo detection of Aβ deposition. DRK092 showed high binding affinity for either synthetic human Aβ fibrils or brain homogenates from amyloid precursor protein transgenic (Tg) mouse (PS1-ki/JU-Tg2576) and AD patient with a dissociation constant (Kd) of one-digit nM, and excellent brain permeability (peak value of uptake: approximately 0.9% of injection dose/g rat brain). Ex vivo autoradiographic analysis showed that measurement with (125)I-DRK092 has higher sensibility for detecting Aβ accumulation than with (125)I-IMPY, a well-known amyloid SPECT ligand, in Tg mice. In vitro autoradiography with (125)I-DRK092 also confirmed higher accumulation of radioactivity in the cortical area, enriched with Aβ plaques, of Tg mouse and AD patient brains, as compared with the corresponding areas in non-Tg mouse and healthy control brains. All the data presented above lead us to draw the conclusion that radioiodinated DRK092 is a potential SPECT ligand for amyloid imaging in AD. | |||||
| 書誌情報 |
Neuroscience letters 巻 581, p. 103-108, 発行日 2014-08 |
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| 出版者 | ||||||
| 出版者 | Elsevier Scientific Publishers Ireland | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0304-3940 | |||||
| PubMed番号 | ||||||
| 識別子タイプ | PMID | |||||
| 関連識別子 | 25172571 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1016/j.neulet.2014.08.036 | |||||
