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This study aimed to evaluate the potential of radioiodinated flavonoid derivatives for single photon emission computed tomography (SPECT) imaging of PrP<jats:sup>Sc<\/jats:sup>. <jats:italic>In vitro<\/jats:italic> binding assays using recombinant mouse PrP (rMoPrP) aggregates revealed that the 4-dimethylamino-substituted styrylchromone derivative (SC-NMe<jats:sub>2<\/jats:sub>) had higher <jats:italic>in vitro<\/jats:italic> binding affinity (<jats:italic>K<\/jats:italic><jats:sub>d<\/jats:sub>\u2009=\u200924.5\u2009nM) and capacity (<jats:italic>B<\/jats:italic><jats:sub>max<\/jats:sub>\u2009=\u200936.3\u2009pmol\/nmol protein) than three other flavonoid derivatives (flavone, chalcone and aurone). Fluorescent imaging using brain sections from mouse-adapted bovine spongiform encephalopathy (mBSE)-infected mice demonstrated that SC-NMe<jats:sub>2<\/jats:sub> clearly labelled PrP<jats:sup>Sc<\/jats:sup>-positive prion deposits in the mice brain. Two methoxy SC derivatives, SC-OMe and SC-(OMe)<jats:sub>2<\/jats:sub>, also showed high binding affinity for rMoPrP aggregates with <jats:italic>K<\/jats:italic><jats:sub>i<\/jats:sub> values of 20.8 and 26.6\u2009nM, respectively. <jats:italic>In vitro<\/jats:italic> fluorescence and autoradiography experiments demonstrated high accumulation of [<jats:sup>125<\/jats:sup>I]SC-OMe and [<jats:sup>125<\/jats:sup>I]SC-(OMe)<jats:sub>2<\/jats:sub> in prion deposit-rich regions of the mBSE-infected mouse brain. SPECT\/computed tomography (CT) imaging and <jats:italic>ex vivo<\/jats:italic> autoradiography demonstrated that [<jats:sup>123<\/jats:sup>I]SC-OMe showed consistent brain distribution with the presence of PrP<jats:sup>Sc<\/jats:sup> deposits in the mBSE-infected mice brain. In conclusion, [<jats:sup>123<\/jats:sup>I]SC-OMe appears a promising SPECT radioligand for monitoring prion deposit levels in the living brain.<\/jats:p>","DOI":"10.1038\/srep18440","type":"journal-article","created":{"date-parts":[[2015,12,16]],"date-time":"2015-12-16T10:18:14Z","timestamp":1450261094000},"update-policy":"https:\/\/doi.org\/10.1007\/springer_crossmark_policy","source":"Crossref","is-referenced-by-count":25,"title":["Characterisation of radioiodinated flavonoid derivatives for SPECT imaging of cerebral prion deposits"],"prefix":"10.1038","volume":"5","author":[{"given":"Takeshi","family":"Fuchigami","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yuki","family":"Yamashita","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Masao","family":"Kawasaki","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ayaka","family":"Ogawa","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mamoru","family":"Haratake","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ryuichiro","family":"Atarashi","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Kazunori","family":"Sano","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Takehiro","family":"Nakagaki","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Kaori","family":"Ubagai","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Masahiro","family":"Ono","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sakura","family":"Yoshida","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Noriyuki","family":"Nishida","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Morio","family":"Nakayama","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"297","published-online":{"date-parts":[[2015,12,16]]},"reference":[{"key":"BFsrep18440_CR1","doi-asserted-by":"publisher","first-page":"13363","DOI":"10.1073\/pnas.95.23.13363","volume":"95","author":"SB Prusiner","year":"1998","unstructured":"Prusiner, S. 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