{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,7]],"date-time":"2026-10-07T05:15:56Z","timestamp":1791350156025,"version":"4.3.1"},"reference-count":33,"publisher":"Wiley","issue":"1","license":[{"start":{"date-parts":[[2013,10,16]],"date-time":"2013-10-16T00:00:00Z","timestamp":1381881600000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Labelled Comp Radiopharmac"],"published-print":{"date-parts":[[2014,1]]},"abstract":"<jats:p>Alzheimer's disease (AD) is the most common cause of dementia. Senile plaques, consisting of <jats:italic>\u03b2<\/jats:italic>\u2010amyloid, and neurofibrillary tangles (NFTs), composed of tau protein, are representative pathological hallmarks of AD. It is believed that the accumulation of NFTs precedes the onset of clinical symptoms of AD and correlates with the progression of memory dysfunction. Thus, the use of noninvasive detection techniques including radiolabeled probes and positron emission tomography (PET) will facilitate early diagnosis or staging of AD. In this study, we synthesized and evaluated novel hydroxylated 2\u2010arylquinoline derivatives as tau imaging PET probes. The binding affinities of compounds for tau were evaluated by fluorescent staining of the AD hippocampal section and a competitive binding assay using [<jats:sup>18<\/jats:sup>F]THK\u2010523. THK\u2010951 showed high binding affinity for tau pathology in an AD brain section and K18\u0394280K fibrils (K<jats:sub>i<\/jats:sub>\u2009=\u200920.7\u2009nM); thus, we radiosynthesized a <jats:sup>11<\/jats:sup>C\u2010labeled THK\u2010951 and further studied its potential as a tau PET probe. The [<jats:sup>11<\/jats:sup>C]THK\u2010951 demonstrated excellent kinetics in a normal mouse brain (3.23% ID\/g at 2\u2009min postinjection and 0.15% ID\/g at 30\u2009min postinjection) and showed the labeling of NFTs in an AD brain section by autoradiography assay. These findings indicate the availability of [<jats:sup>11<\/jats:sup>C]THK\u2010951 for in vivo PET imaging of tau pathology in AD. Copyright \u00a9 2013 John Wiley &amp; Sons, Ltd.<\/jats:p>","DOI":"10.1002\/jlcr.3133","type":"journal-article","created":{"date-parts":[[2013,10,16]],"date-time":"2013-10-16T07:34:53Z","timestamp":1381908893000},"page":"18-24","source":"Crossref","is-referenced-by-count":29,"title":["Synthesis and preliminary evaluation of 2\u2010arylhydroxyquinoline derivatives for tau imaging"],"prefix":"10.1002","volume":"57","author":[{"given":"Tetsuro","family":"Tago","sequence":"first","affiliation":[{"name":"Cyclotron and Radioisotope Center (CYRIC) Tohoku University  Sendai 980\u20108578 Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Shozo","family":"Furumoto","sequence":"additional","affiliation":[{"name":"Cyclotron and Radioisotope Center (CYRIC) Tohoku University  Sendai 980\u20108578 Japan"},{"name":"Department of Pharmacology Tohoku University School of Medicine  Sendai 980\u20108575 Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Nobuyuki","family":"Okamura","sequence":"additional","affiliation":[{"name":"Department of Pharmacology Tohoku University School of Medicine  Sendai 980\u20108575 Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ryuichi","family":"Harada","sequence":"additional","affiliation":[{"name":"Department of Pharmacology Tohoku University School of Medicine  Sendai 980\u20108575 Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yoichi","family":"Ishikawa","sequence":"additional","affiliation":[{"name":"Cyclotron and Radioisotope Center (CYRIC) Tohoku University  Sendai 980\u20108578 Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hiroyuki","family":"Arai","sequence":"additional","affiliation":[{"name":"Department of Geriatrics &amp; Gerontology, Institute of Development, Aging and Cancer Tohoku University  Sendai 980\u20108575 Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Kazuhiko","family":"Yanai","sequence":"additional","affiliation":[{"name":"Department of Pharmacology Tohoku University School of Medicine  Sendai 980\u20108575 Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ren","family":"Iwata","sequence":"additional","affiliation":[{"name":"Cyclotron and Radioisotope Center (CYRIC) Tohoku University  Sendai 980\u20108578 Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yukitsuka","family":"Kudo","sequence":"additional","affiliation":[{"name":"Innovation of New Biomedical Engineering Center Tohoku University  Sendai 980\u20108574 Japan"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2013,10,16]]},"reference":[{"key":"e_1_2_7_2_1","first-page":"243","volume":"134","author":"Ogomori K.","year":"1989","journal-title":"Am. 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