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<script type="text/javascript" src="/corehtml/pmc/jatsreader/ptpmc_3.22/js/jr.boots.min.js"> </script><title>18F-Labeled fluoropegylated 6-fluoroethoxy-4'-dimethylaminoflavone, 6-(2-(2-fluoro-ethoxy)-ethoxy)-4'-dimethylaminoflavone, and 6-(2-(2-(2-fluoro-ethoxy)-ethoxy)ethoxy)-4'-dimethylaminoflavone - Molecular Imaging and Contrast Agent Database (MICAD) - NCBI Bookshelf</title>
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<meta name="citation_title" content="18F-Labeled fluoropegylated 6-fluoroethoxy-4'-dimethylaminoflavone, 6-(2-(2-fluoro-ethoxy)-ethoxy)-4'-dimethylaminoflavone, and 6-(2-(2-(2-fluoro-ethoxy)-ethoxy)ethoxy)-4'-dimethylaminoflavone">
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<meta name="citation_author" content="Liang Shan">
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<meta name="DC.Title" content="18F-Labeled fluoropegylated 6-fluoroethoxy-4'-dimethylaminoflavone, 6-(2-(2-fluoro-ethoxy)-ethoxy)-4'-dimethylaminoflavone, and 6-(2-(2-(2-fluoro-ethoxy)-ethoxy)ethoxy)-4'-dimethylaminoflavone">
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stroke-linecap="round" style="fill:#FFF" d="m320,350a153,153 0 1,0-2,2l170,170m-91-117 110,110-26,26-110-110"></path></svg></a><a id="jr-fip-done" class="wsprkl btn" title="Dismiss find">✘</a></nav><nav id="jr-fip-info-p"><a id="jr-fip-prev" class="wsprkl btn" title="Jump to previuos match">◀</a><button id="jr-fip-matches">no matches yet</button><a id="jr-fip-next" class="wsprkl btn" title="Jump to next match">▶</a></nav></nav></div><div id="jr-epub-interstitial" class="hidden"></div><div id="jr-content"><article data-type="main"><div class="main-content lit-style" itemscope="itemscope" itemtype="http://schema.org/CreativeWork"><div class="meta-content fm-sec"><div class="fm-sec"><h1 id="_NBK82962_"><span class="title" itemprop="name"><sup>18</sup>F-Labeled fluoropegylated 6-fluoroethoxy-4'-dimethylaminoflavone, 6-(2-(2-fluoro-ethoxy)-ethoxy)-4'-dimethylaminoflavone, and 6-(2-(2-(2-fluoro-ethoxy)-ethoxy)ethoxy)-4'-dimethylaminoflavone</span></h1><div itemprop="alternativeHeadline" class="subtitle whole_rhythm">[<sup>18</sup>F]8(a–c)</div><p class="contribs">Shan L.</p><p class="fm-aai"><a href="#_NBK82962_pubdet_">Publication Details</a></p></div></div><div class="jig-ncbiinpagenav body-content whole_rhythm" data-jigconfig="allHeadingLevels: ['h2'],smoothScroll: false" itemprop="text"><div class="iconblock whole_rhythm clearfix ten_col table-wrap" id="figF188acTncchemicalname18flabeledfl"><a href="/books/NBK82962/table/F18-8a-c.T.nc_chemical_name18flabeled_fl/?report=objectonly" target="object" title="Table" class="img_link icnblk_img figpopup" rid-figpopup="figF188acTncchemicalname18flabeledfl" rid-ob="figobF188acTncchemicalname18flabeledfl"><img class="small-thumb" src="/books/NBK82962/table/F18-8a-c.T.nc_chemical_name18flabeled_fl/?report=thumb" src-large="/books/NBK82962/table/F18-8a-c.T.nc_chemical_name18flabeled_fl/?report=previmg" alt="Image " /></a><div class="icnblk_cntnt"><h4 id="F18-8a-c.T.nc_chemical_name18flabeled_fl"><a href="/books/NBK82962/table/F18-8a-c.T.nc_chemical_name18flabeled_fl/?report=objectonly" target="object" rid-ob="figobF188acTncchemicalname18flabeledfl">Table</a></h4><p class="float-caption no_bottom_margin">
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<i>In vitro</i>
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Rodents
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</p></div></div><div id="F18-8a-c.Background"><h2 id="_F18-8a-c_Background_">Background</h2><p>[<a href="/pubmed/?term=molecular%20imaging%20and%20Alzheimer%u2019s%20disease%20and%20%u03B2-amyloid%20" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p><sup>18</sup>F-Labeled fluoropegylated 6-fluoroethoxy-4'-dimethylaminoflavone (compound 8a), 6-(2-(2-fluoro-ethoxy)-ethoxy)-4'-dimethylaminoflavone (compound 8b), and 6-(2-(2-(2-fluoro-ethoxy)-ethoxy)ethoxy)-4'-dimethylaminoflavone (compound 8c), abbreviated as [<sup>18</sup>F]8a, [<sup>18</sup>F]8b, and [<sup>18</sup>F]8c, respectively, are flavone derivatives synthesized by Ono et al. for positron emission tomography (PET) of Alzheimer’s disease (AD) by targeting β-amyloid (Aβ) (<a class="bibr" href="#F18-8a-c.REF.1" rid="F18-8a-c.REF.1">1</a>).</p><p>AD is characterized in pathology by the presence of extracellular Aβ plaques, intraneuronal neurofibrillary tangles, and neuronal loss in the cerebral cortex (<a class="bibr" href="#F18-8a-c.REF.2" rid="F18-8a-c.REF.2 F18-8a-c.REF.3">2, 3</a>). Of them, Aβ deposit is the earliest neuropathological marker and is relatively specific to AD and closely related disorders. Aβ plaques are composed of abnormal paired helical filaments 5–10 nm in size. These filaments are largely made of insoluble Aβ peptides that are 40 or 42 amino acids in length (<a class="bibr" href="#F18-8a-c.REF.4" rid="F18-8a-c.REF.4">4</a>).</p><p>In recent years, molecular imaging by targeting the extracellular Aβ has been intensively investigated in attempts to detect early AD, assess Aβ content <i>in vivo</i>, determine the timing of anti-plaque therapy, and evaluate the therapeutic efficacy (<a class="bibr" href="#F18-8a-c.REF.4" rid="F18-8a-c.REF.4">4</a>). Radiolabeled Aβ40 peptides were tested first, but they showed poor penetration ability to cross the blood–brain barrier (BBB) (<a class="bibr" href="#F18-8a-c.REF.4" rid="F18-8a-c.REF.4">4</a>). Based on the fact that Aβ can be specifically stained <i>in vitro</i> with dyes of Congo red, chrysamine G, and thioflavin-T, an effort was made to develop imaging agents with these dyes. This effort, however, was in general unsuccessful because the bulky ionic groups of heteroatoms in these dyes prevent them from crossing the BBB (<a class="bibr" href="#F18-8a-c.REF.2" rid="F18-8a-c.REF.2">2</a>). Importantly, a large class of derivatives (e.g., aminonaphthalenes, benzothiazoles, stilbenes, and imidazopyridines) was synthesized with these dyes as templates (<a class="bibr" href="#F18-8a-c.REF.4" rid="F18-8a-c.REF.4">4</a>). Clinical and preclinical studies have shown that these derivatives not only possess a high binding affinity with Aβ plaques as their parent compounds, but also exhibit good penetration ability through the BBB and rapid washout from brain with low to no plaque deposits.</p><p>Ono et al. first synthesized a class of radioiodinated flavone derivatives that present a high binding affinity with Aβ plaques and good penetration ability through the BBB (<a class="bibr" href="#F18-8a-c.REF.5" rid="F18-8a-c.REF.5">5</a>). However, these flavone derivatives display poor clearance from the brain, which leads to a high brain background. The investigators then explored another class of flavonoids with aurone as the core structure (<a class="bibr" href="#F18-8a-c.REF.1" rid="F18-8a-c.REF.1 F18-8a-c.REF.6">1, 6</a>). Aurone is a heterocyclic chemical compound that contains a benzofuran element associated with a benzylidene linked in position 2 and a chalcone-like group being closed into a five-member ring. The aurone derivatives possess a nucleophilic group (NH<sub>2</sub>, NHMe, or NMe<sub>2</sub>) at the 4' position and a radioiodine at the 5 position. Although these aurone derivatives exhibit a strong binding affinity with Aβ (inhibition constant (<i>K</i><sub>i</sub>) = 1.2–6.8 nM), high penetration ability through the BBB (1.9%−4.6% injected dose per gram tissue (ID/g) at 2 min), and a fast washout from the brain (0.3%−0.5% ID/g at 30 min), the pharmacokinetics of these compounds are less favorable for brain imaging than the pharmacokinetics of the agent [<sup>123</sup>I]IMPY (6-iodo-2-(4'-dimethylamino)phenyl-imidazo[1,2]pyridine), which is the only SPECT agent to be tested in humans to date (<a class="bibr" href="#F18-8a-c.REF.7" rid="F18-8a-c.REF.7 F18-8a-c.REF.8 F18-8a-c.REF.9">7-9</a>). The investigators also modified the flavone and aurone derivatives by pegylating them with 1–3 units of ethylene glycol at the 4' position or by conjugating them with the chelating agent bis-amino-bis-thiol (BAT). Favorable pharmacokinetics for brain imaging was observed for the pegylated derivatives ([<sup>18</sup>F]8(a–c)) but not for the BAT-chelated derivatives ([<sup>99m</sup>Tc]BAT-FL and [<sup>99m</sup>Tc]BAT-AR) (<a class="bibr" href="#F18-8a-c.REF.1" rid="F18-8a-c.REF.1 F18-8a-c.REF.6">1, 6</a>).</p><p>This series of chapters summarizes the data obtained with flavone and aurone derivatives, including [<sup>125</sup>I]15, [<sup>125</sup>I]9, [<sup>125</sup>I]14, [<sup>125</sup>I]16, [<sup>125</sup>I]17, [<sup>99m</sup>Tc]BAT-FL, [<sup>99m</sup>Tc]BAT-AR, [<sup>18</sup>F]8(a–c), [<sup>125</sup>I]3, and [<sup>18</sup>F]3 (<a class="bibr" href="#F18-8a-c.REF.1" rid="F18-8a-c.REF.1 F18-8a-c.REF.6 F18-8a-c.REF.7 F18-8a-c.REF.8">1, 6-8</a>). This chapter presents the data obtained with [<sup>18</sup>F]8(a–c) (<a class="bibr" href="#F18-8a-c.REF.1" rid="F18-8a-c.REF.1">1</a>).</p><div id="F18-8a-c.Related_Resource_Links"><h3>Related Resource Links:</h3><ul><li class="half_rhythm"><div>
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<a href="/books/?term=amyloid+AND+micad%5bbook%5d&view=chapter&p%24a=&p%24l=PBooksLayout&p%24st=books" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">Amyloid-targeted imaging agents in MICAD</a>
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</div></li><li class="half_rhythm"><div>
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<a href="http://clinicaltrials.gov/ct2/results?term=amyloid" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">Amyloid-targeted imaging clinical trials in ClinicalTrials.gov</a>
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</div></li><li class="half_rhythm"><div>
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<a href="/pcsubstance/?term=amyloid" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">Structures and other information of amyloid peptides in PubChem</a>
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</div></li><li class="half_rhythm"><div>
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<a href="/omim/?term=Alzheimer%27s%20disease" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">Alzheimer’s disease articles in Online Mendelian Inheritance in Man</a>
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</div></li></ul></div></div><div id="F18-8a-c.Synthesis"><h2 id="_F18-8a-c_Synthesis_">Synthesis</h2><p>[<a href="/pubmed/?term=19201614" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>The synthesis of the compound precursors with chemical yields was described in detail by Ono et al. (<a class="bibr" href="#F18-8a-c.REF.1" rid="F18-8a-c.REF.1">1</a>). [<sup>18</sup>F]8(a–c) was obtained with the reaction of the corresponding tosylate precursors with [<sup>18</sup>F]fluoride. The reaction mixture was purified with reversed phase high-performance liquid chromatography. The radiochemical purities of the final products were >99%; radiochemical yields ranged from 5% to 13%; total synthesis times were 70 min; and specific activities were 33.3–55.5 GBq/mmol (900–1,500 mCi/mmol) at the end of synthesis.</p><p>[<sup>125</sup>I]6-Iodo-4'-dimethylaminoflavone ([<sup>125</sup>I]DMFV, <i>K</i><sub>d</sub> = 12.3 nM) was prepared as the radioligand in binding assays using the standard iododestannylation reaction (<a class="bibr" href="#F18-8a-c.REF.10" rid="F18-8a-c.REF.10">10</a>). The specific activity and radiochemical purity of [<sup>125</sup>I]DMFV were 81.4 TBq/mmol (2.2 kCi/mmol) and >95%, respectively.</p></div><div id="F18-8a-c.In_Vitro_Studies_Testing_in_Cel"><h2 id="_F18-8a-c_In_Vitro_Studies_Testing_in_Cel_"><i>In Vitro</i> Studies: Testing in Cells and Tissues</h2><p>[<a href="/pubmed/?term=19201614" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>The binding of [<sup>18</sup>F]8(a–c) with Aβ aggregates was carried out with [<sup>125</sup>I]DMFV in solutions (<a class="bibr" href="#F18-8a-c.REF.1" rid="F18-8a-c.REF.1 F18-8a-c.REF.10">1, 10</a>). The <i>K</i><sub>i</sub> values were measured to be 5.3, 14.4, and 19.3 for [<sup>18</sup>F]8a, [<sup>18</sup>F]8b, and [<sup>18</sup>F]8c, respectively. The results of <i>K</i><sub>i</sub> measurement for [<sup>18</sup>F]8(a–c) and other derivatives indicate that the affinities of flavone derivatives for Aβ(1–42) aggregates were affected by the group substituted at the 4' position in the flavone structure, not by the length of ethylene glycol introduced into the flavone backbone (<a class="bibr" href="#F18-8a-c.REF.1" rid="F18-8a-c.REF.1">1</a>).</p><p>The affinity of [<sup>18</sup>F]8(a–c) for brain Aβ plaques was analyzed with brain sections of <i>Tg2576</i> transgenic mice with fluorescence staining (<a class="bibr" href="#F18-8a-c.REF.1" rid="F18-8a-c.REF.1">1</a>). Many fluorescent spots were observed, and these findings were consistent with those obtained with immunohistochemical labeling with an antibody specific for Aβ. No spots were observed in the brain sections of wild-type mice (data not shown). These results indicate that [<sup>18</sup>F]8(a–c) can bind specifically with Aβ plaques in the mouse brain.</p></div><div id="F18-8a-c.Animal_Studies"><h2 id="_F18-8a-c_Animal_Studies_">Animal Studies</h2><div id="F18-8a-c.Rodents"><h3>Rodents</h3><p>[<a href="/pubmed/?term=19201614" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>The biodistribution of [<sup>18</sup>F]8(a–c) was examined in normal mice (<i>n</i> = 4–5/time point for each agent) (<a class="bibr" href="#F18-8a-c.REF.1" rid="F18-8a-c.REF.1">1</a>). All three ligands displayed high radioactivity in the brain at 2 min after injection (2.89%–4.17% ID/g). Low radioactivity was observed at 30 min after injection (1.89%, 2.00%, and 1.31% ID/g for [<sup>18</sup>F]8a, [<sup>18</sup>F]8b, and [<sup>18</sup>F]8c, respectively). These values were equal to 45.3%, 56.5%, and 45.3% of the initial uptake peak for [<sup>18</sup>F]8a, [<sup>18</sup>F]8b, and [<sup>18</sup>F]8c, respectively, indicating a rapid initial uptake in normal brain tissue coupled with a fast washout, which is highly desirable for Aβ imaging. [<sup>18</sup>F]8(a–c) also showed high bone uptake (3.74%–6.21% ID/g) at 60 min after injection, suggesting there may be <i>in vivo</i> defluorination. However, the interference from this free fluoride is expected to be relatively low for brain imaging because the free fluorine was not taken up by brain tissue (<a class="bibr" href="#F18-8a-c.REF.1" rid="F18-8a-c.REF.1">1</a>).</p></div><div id="F18-8a-c.Other_NonPrimate_Mammals"><h3>Other Non-Primate Mammals</h3><p>[<a href="/pubmed/?term=%22SUBSTANCENAME%22%5BSubstance%20Name%5D%20AND%20%28dog%20OR%20rabbit%20OR%20pig%20OR%20sheep%29" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>No references are currently available.</p></div><div id="F18-8a-c.NonHuman_Primates"><h3>Non-Human Primates</h3><p>[<a href="/pubmed/?term=%22SUBSTANCENAME%22%5BSubstance%20Name%5D%20AND%20%28primate%20NOT%20human%29" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>No references are currently available.</p></div></div><div id="F18-8a-c.Human_Studies"><h2 id="_F18-8a-c_Human_Studies_">Human Studies</h2><p>[<a href="/pubmed/?term=%22SUBSTANCENAME%22%5BSubstance%20Name%5D%20AND%20human" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>No references are currently available.</p></div><div id="F18-8a-c.References"><h2 id="_F18-8a-c_References_">References</h2><dl class="temp-labeled-list"><dl class="bkr_refwrap"><dt>1.</dt><dd><div class="bk_ref" id="F18-8a-c.REF.1">Ono M., Watanabe R., Kawashima H., Kawai T., Watanabe H., Haratake M., Saji H., Nakayama M.
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<em>18F-labeled flavones for in vivo imaging of beta-amyloid plaques in Alzheimer's brains.</em>
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<span><span class="ref-journal">Bioorg Med Chem. </span>2009;<span class="ref-vol">17</span>(5):2069–76.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/19201614" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 19201614</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>2.</dt><dd><div class="bk_ref" id="F18-8a-c.REF.2">Ono M.
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<em>Development of positron-emission tomography/single-photon emission computed tomography imaging probes for in vivo detection of beta-amyloid plaques in Alzheimer's brains.</em>
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<span><span class="ref-journal">Chem Pharm Bull (Tokyo). </span>2009;<span class="ref-vol">57</span>(10):1029–39.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/19801854" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 19801854</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>3.</dt><dd><div class="bk_ref" id="F18-8a-c.REF.3">Mathis C.A., Wang Y., Klunk W.E.
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<em>Imaging beta-amyloid plaques and neurofibrillary tangles in the aging human brain.</em>
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<span><span class="ref-journal">Curr Pharm Des. </span>2004;<span class="ref-vol">10</span>(13):1469–92.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/15134570" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 15134570</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>4.</dt><dd><div class="bk_ref" id="F18-8a-c.REF.4">Vallabhajosula S.
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<em>Positron emission tomography radiopharmaceuticals for imaging brain Beta-amyloid.</em>
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<span><span class="ref-journal">Semin Nucl Med. </span>2011;<span class="ref-vol">41</span>(4):283–99.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/21624562" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 21624562</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>5.</dt><dd><div class="bk_ref" id="F18-8a-c.REF.5">Ono M., Maya Y., Haratake M., Ito K., Mori H., Nakayama M.
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<em>Aurones serve as probes of beta-amyloid plaques in Alzheimer's disease.</em>
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<span><span class="ref-journal">Biochem Biophys Res Commun. </span>2007;<span class="ref-vol">361</span>(1):116–21.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/17644062" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 17644062</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>6.</dt><dd><div class="bk_ref" id="F18-8a-c.REF.6">Ono M., Ikeoka R., Watanabe H., Kimura H., Fuchigami T., Haratake M., Saji H., Nakayama M.
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<em>99mTc/Re complexes based on flavone and aurone as SPECT probes for imaging cerebral beta-amyloid plaques.</em>
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<span><span class="ref-journal">Bioorg Med Chem Lett. </span>2010;<span class="ref-vol">20</span>(19):5743–8.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/20797860" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 20797860</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>7.</dt><dd><div class="bk_ref" id="F18-8a-c.REF.7">Maya Y., Ono M., Watanabe H., Haratake M., Saji H., Nakayama M.
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<em>Novel radioiodinated aurones as probes for SPECT imaging of beta-amyloid plaques in the brain.</em>
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<span><span class="ref-journal">Bioconjug Chem. </span>2009;<span class="ref-vol">20</span>(1):95–101.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/19072219" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 19072219</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>8.</dt><dd><div class="bk_ref" id="F18-8a-c.REF.8">Watanabe H., Ono M., Kimura H., Kagawa S., Nishii R., Fuchigami T., Haratake M., Nakayama M., Saji H.
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<em>A dual fluorinated and iodinated radiotracer for PET and SPECT imaging of beta-amyloid plaques in the brain.</em>
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<span><span class="ref-journal">Bioorg Med Chem Lett. </span>2011;<span class="ref-vol">21</span>(21):6519–22.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/21920750" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 21920750</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>9.</dt><dd><div class="bk_ref" id="F18-8a-c.REF.9">Newberg A.B., Wintering N.A., Plossl K., Hochold J., Stabin M.G., Watson M., Skovronsky D., Clark C.M., Kung M.P., Kung H.F.
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<em>Safety, biodistribution, and dosimetry of 123I-IMPY: a novel amyloid plaque-imaging agent for the diagnosis of Alzheimer's disease.</em>
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<span><span class="ref-journal">J Nucl Med. </span>2006;<span class="ref-vol">47</span>(5):748–54.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/16644743" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 16644743</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>10.</dt><dd><div class="bk_ref" id="F18-8a-c.REF.10">Ono M., Yoshida N., Ishibashi K., Haratake M., Arano Y., Mori H., Nakayama M.
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<em>Radioiodinated flavones for in vivo imaging of beta-amyloid plaques in the brain.</em>
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<span><span class="ref-journal">J Med Chem. </span>2005;<span class="ref-vol">48</span>(23):7253–60.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/16279784" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 16279784</span></a>]</div></dd></dl></dl></div><div id="bk_toc_contnr"></div></div></div><div class="fm-sec"><h2 id="_NBK82962_pubdet_">Publication Details</h2><h3>Author Information and Affiliations</h3><div class="contrib half_rhythm"><span itemprop="author">Liang Shan</span>, PhD<div class="affiliation small">National Center for Biotechnology Information, NLM, NIH<div><span class="email-label">Email: </span><a href="mailto:dev@null" data-email="vog.hin.mln.ibcn@dacim" class="oemail">vog.hin.mln.ibcn@dacim</a></div></div><div class="small">Corresponding author.</div></div><h3>Publication History</h3><p class="small">Created: <span itemprop="datePublished">November 30, 2011</span>; Last Update: <span itemprop="dateModified">December 28, 2011</span>.</p><h3>Copyright</h3><div><div class="half_rhythm"><a href="/books/about/copyright/">Copyright Notice</a></div></div><h3>Publisher</h3><p><a href="http://www.ncbi.nlm.nih.gov/" ref="pagearea=page-banner&targetsite=external&targetcat=link&targettype=publisher">National Center for Biotechnology Information (US)</a>, Bethesda (MD)</p><h3>NLM Citation</h3><p>Shan L. 18F-Labeled fluoropegylated 6-fluoroethoxy-4'-dimethylaminoflavone, 6-(2-(2-fluoro-ethoxy)-ethoxy)-4'-dimethylaminoflavone, and 6-(2-(2-(2-fluoro-ethoxy)-ethoxy)ethoxy)-4'-dimethylaminoflavone. 2011 Nov 30 [Updated 2011 Dec 28]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013. <span class="bk_cite_avail"></span></p></div><div class="small-screen-prev"><a href="/books/n/micad/Exe9-3918F/?report=reader"><svg xmlns="http://www.w3.org/2000/svg" viewBox="0 0 100 100" preserveAspectRatio="none"><path d="M75,30 c-80,60 -80,0 0,60 c-30,-60 -30,0 0,-60"></path><text x="20" y="28" textLength="60" style="font-size:25px">Prev</text></svg></a></div><div class="small-screen-next"><a href="/books/n/micad/F18_3f/?report=reader"><svg xmlns="http://www.w3.org/2000/svg" viewBox="0 0 100 100" preserveAspectRatio="none"><path d="M25,30c80,60 80,0 0,60 c30,-60 30,0 0,-60"></path><text x="20" y="28" textLength="60" style="font-size:25px">Next</text></svg></a></div></article><article data-type="table-wrap" id="figobF188acTncchemicalname18flabeledfl"><div id="F18-8a-c.T.nc_chemical_name18flabeled_fl" class="table"><p class="large-table-link" style="display:none"><span class="right"><a href="/books/NBK82962/table/F18-8a-c.T.nc_chemical_name18flabeled_fl/?report=objectonly" target="object">View in own window</a></span></p><div class="large_tbl" id="__F18-8a-c.T.nc_chemical_name18flabeled_fl_lrgtbl__"><table><tbody><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Chemical name:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><sup>18</sup>F-Labeled fluoropegylated 6-fluoroethoxy-4'-dimethylaminoflavone, 6-(2-(2-fluoro-ethoxy)-ethoxy)-4'-dimethylaminoflavone, and 6-(2-(2-(2-fluoro-ethoxy)-ethoxy)ethoxy)-4'-dimethylaminoflavone</td><td rowspan="9" colspan="1" style="text-align:center;vertical-align:middle;">
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<span class="graphic"><img src="/books/NBK82962/bin/F188ac.jpg" alt="Image F188ac.jpg" /></span>
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</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Abbreviated name:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">[<sup>18</sup>F]8(a–c)</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Synonym:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">[<sup>18</sup>F]8a, [<sup>18</sup>F]8b, [<sup>18</sup>F]8c</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Agent Category:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Compounds</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Target:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">β-amyloid (Aβ)</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Target Category:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Accepters</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Method of detection:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Positron emission tomography (PET)</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Source of signal / contrast:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><sup>18</sup>F</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Activation:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">No</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Studies:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">
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<ul class="simple-list"><li class="half_rhythm"><div>
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<img alt="Checkbox" src="/corehtml/pmc/css/bookshelf/2.26/img/studies.checkbox.png" />
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<i>In vitro</i>
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</div></li><li class="half_rhythm"><div>
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<img alt="Checkbox" src="/corehtml/pmc/css/bookshelf/2.26/img/studies.checkbox.png" /> Rodents
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</div></li></ul>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Structure of [<sup>18</sup>F]8(a–c) by Ono et al. (<a class="bibr" href="#F18-8a-c.REF.1" rid="F18-8a-c.REF.1">1</a>).</td></tr></tbody></table></div></div></article></div><div id="jr-scripts"><script src="/corehtml/pmc/jatsreader/ptpmc_3.22/js/libs.min.js"> </script><script src="/corehtml/pmc/jatsreader/ptpmc_3.22/js/jr.min.js"> </script></div></div>
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