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<script type="text/javascript" src="/corehtml/pmc/jatsreader/ptpmc_3.22/js/jr.boots.min.js"> </script><title>18F-Labeled N-(4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-2-(2-fluoroethoxy)-5-methylbenzamide - Molecular Imaging and Contrast Agent Database (MICAD) - NCBI Bookshelf</title>
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<meta name="citation_title" content="18F-Labeled N-(4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-2-(2-fluoroethoxy)-5-methylbenzamide">
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<meta name="citation_date" content="2010/01/07">
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<meta name="citation_author" content="Arvind Chopra">
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<meta name="og:description" content="Sigma receptor (SR) subtypes 1 (Sig-1R) and 2 (Sig-2R) and are known to be present primarily in the central nervous system and the peripheral tissues. Both receptor subtypes have a different distribution in the two types of tissues, and the exact biological function of these receptors is not known (1). Of the two receptor subtypes, only the Sig-1R has been cloned, expressed, and purified (2). The Sig-2R is known to be overexpressed in various malignant tumors and is believed to promote cell proliferation, indicating that these receptors may play a role in the development of some cancers (3). As a consequence, the Sig-2R have been suggested to be biomarkers for tumor cell proliferation (4) and could be targeted for the development of different anti-cancer drugs (5) or imaging agents for tumors that overexpress Sig-2R (3, 5). Several clinical trials have been approved by the United States Food and Drug Administration for the evaluation of drugs that target the Sig-2R for the imaging and treatment of different clinical conditions. In addition, Sig-2R ligands have been used in preclinical studies to chemosensitize tumors to low doses of anti-cancer drugs that are otherwise toxic when given at high doses to animals bearing mammalian cell line tumors (6, 7).">
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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="_NBK23102_"><span class="title" itemprop="name"><sup>18</sup>F-Labeled <i>N</i>-(4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1<i>H</i>)-yl)butyl)-2-(2-fluoroethoxy)-5-methylbenzamide</span></h1><div itemprop="alternativeHeadline" class="subtitle whole_rhythm"> [<sup>18</sup>F]3c</div><p class="contribs">Chopra A.</p><p class="fm-aai"><a href="#_NBK23102_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="figF183cTncChemicalname18FLabeledN467"><a href="/books/NBK23102/table/F18_3c.T.nc_Chemical_name18FLabeled_N467/?report=objectonly" target="object" title="Table" class="img_link icnblk_img" rid-ob="figobF183cTncChemicalname18FLabeledN467"><img class="small-thumb" src="/corehtml/pmc/css/bookshelf/2.26/img/table-icon.gif" alt="Table Icon" /></a><div class="icnblk_cntnt"><h4 id="F18_3c.T.nc_Chemical_name18FLabeled_N467"><a href="/books/NBK23102/table/F18_3c.T.nc_Chemical_name18FLabeled_N467/?report=objectonly" target="object" rid-ob="figobF183cTncChemicalname18FLabeledN467">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_3c.Background"><h2 id="_F18_3c_Background_">Background</h2><p>[<a href="/pubmed?term=sigma%202%20receptor&cmd=DetailsSearch" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed]</a></p><p>Sigma receptor (SR) subtypes 1 (Sig-1R) and 2 (Sig-2R) and are known to be present primarily in the central nervous system and the peripheral tissues. Both receptor subtypes have a different distribution in the two types of tissues, and the exact biological function of these receptors is not known (<a class="bibr" href="#F18_3c.REF.1" rid="F18_3c.REF.1">1</a>). Of the two receptor subtypes, only the Sig-1R has been cloned, expressed, and purified (<a class="bibr" href="#F18_3c.REF.2" rid="F18_3c.REF.2">2</a>). The Sig-2R is known to be overexpressed in various malignant tumors and is believed to promote cell proliferation, indicating that these receptors may play a role in the development of some cancers (<a class="bibr" href="#F18_3c.REF.3" rid="F18_3c.REF.3">3</a>). As a consequence, the Sig-2R have been suggested to be biomarkers for tumor cell proliferation (<a class="bibr" href="#F18_3c.REF.4" rid="F18_3c.REF.4">4</a>) and could be targeted for the development of different anti-cancer drugs (<a class="bibr" href="#F18_3c.REF.5" rid="F18_3c.REF.5">5</a>) or imaging agents for tumors that overexpress Sig-2R (<a class="bibr" href="#F18_3c.REF.3" rid="F18_3c.REF.3 F18_3c.REF.5">3, 5</a>). Several <a href="http://clinicaltrials.gov/ct2/results?term=sigma+2+receptor" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">clinical trials</a> have been approved by the United States Food and Drug Administration for the evaluation of drugs that target the Sig-2R for the imaging and treatment of different clinical conditions. In addition, Sig-2R ligands have been used in preclinical studies to <a href="http://mct.aacrjournals.org/content/2/8/805.full.pdf+html" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">chemosensitize</a> tumors to low doses of anti-cancer drugs that are otherwise toxic when given at high doses to animals bearing mammalian cell line tumors (<a class="bibr" href="#F18_3c.REF.6" rid="F18_3c.REF.6 F18_3c.REF.7">6, 7</a>).</p><p>Investigators have developed and characterized several SR ligands, but most of them are either selective only for the Sig-1R or have similar affinity for both SR subtypes, therefore limiting their use as anti-cancer drugs that target the Sig-2R or as detection and imaging agents for this receptor (<a class="bibr" href="#F18_3c.REF.3" rid="F18_3c.REF.3 F18_3c.REF.7">3, 7</a>). In an effort to develop a ligand with high specificity for Sig-2R, Tu et al. synthesized a series of <sup>18</sup>F-labeled benzamide analogs and evaluated these radiolabeled compounds with positron emission tomography (PET) and computed tomography (CT) imaging of mice bearing allograft tumors expressing the receptor (<a class="bibr" href="#F18_3c.REF.3" rid="F18_3c.REF.3">3</a>). Among the various compounds tested, <i>N</i>-(4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1<i>H</i>)-yl)butyl)-2-(2-[<sup>18</sup>F]-fluoroethoxy)-5-methylbenzamide (designated [<sup>18</sup>F]3c) and another analog, <i>N</i>-(4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1<i>H</i>)-yl)butyl)-2-(2-[<sup>18</sup>F]-fluoroethoxy)-5-iodo-3-methoxybenzamide (designated [<sup>18</sup>F]3f), were determined to be most suitable for the detection of solid tumors expressing Sig-2R with the use of PET and CT imaging. This chapter describes the <i>in vitro</i> characterization and <i>in vivo</i> biodistribution of [<sup>18</sup>F]3c and the PET/CT imaging with [<sup>18</sup>F]3c. The <i>in vitro</i> and <i>in vivo</i> characterization of [<sup>18</sup>F]3f are described in a separate chapter in MICAD (<a href="http://www.micad.nih.gov/" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">www.micad.nih.gov</a>) (<a class="bibr" href="#F18_3c.REF.8" rid="F18_3c.REF.8">8</a>).</p><div id="F18_3c.other"><h3>Other sources of information regarding SRs</h3><p>Other SR imaging agents in <a href="/sites/entrez?db=Books&cmd=Search&term=sigma+receptor++AND+micad%5Bbook%5D&doptcmdl=TOCView&log%24=booksrch&bname=micad" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">MICAD</a>.</p><p>Sigma receptors in <a href="/omim?term=sigma%20receptors" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">OMIM</a> (Online Mendelian Inheritance in Man).</p><p>Protein sequences of human SR1, <a href="/protein/NP_005857.1?ordinalpos=3&itool=EntrezSystem2.PEntrez.Sequence.Sequence_ResultsPanel.Sequence_RVDocSum" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">isoform1</a> and <a href="/protein/NP_671513.1?ordinalpos=2&itool=EntrezSystem2.PEntrez.Sequence.Sequence_ResultsPanel.Sequence_RVDocSum" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">isoform 2</a>.</p><p>Nucleotide (mRNA) sequences of SR1, <a href="/nuccore/NM_005866.2?ordinalpos=4&itool=EntrezSystem2.PEntrez.Sequence.Sequence_ResultsPanel.Sequence_RVDocSum" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">variant 1</a> and <a href="/nuccore/NM_147157.1?ordinalpos=3&itool=EntrezSystem2.PEntrez.Sequence.Sequence_ResultsPanel.Sequence_RVDocSum" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">variant 2</a>.</p></div></div><div id="F18_3c.Synthesis"><h2 id="_F18_3c_Synthesis_">Synthesis</h2><p>[<a href="/pubmed?term=18F-3c%5BAll%20Fields%5D%20AND%20%28%22metabolism%22%5BMeSH%20Terms%5D%20OR%20%22metabolism%22%5BAll%20Fields%5D%20OR%20%22synthesis%22%5BAll%20Fields%5D%29&cmd=DetailsSearch&log$=details" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>The synthesis and <sup>18</sup>F-labeling of 3c has been described by Tu et al. (<a class="bibr" href="#F18_3c.REF.3" rid="F18_3c.REF.3">3</a>). The total time of synthesis to obtain [<sup>18</sup>F]3c was ~2 h with a decay-corrected yield of ~35%. The radiochemical purity of the labeled compound was >99% as determined with analytical high-performance liquid chromatography with a specific activity of >74.07 TBq/mmol (2,000 Ci/mmol). The entire procedure, including purification, was completed in approximately 2 h. The stability and conditions used to store [<sup>18</sup>F]3c were not reported.</p></div><div id="F18_3c.In_Vitro_Studies_Testing_in_Cells"><h2 id="_F18_3c_In_Vitro_Studies_Testing_in_Cells_"><i>In Vitro</i> Studies: Testing in Cells and Tissues</h2><p>[<a href="/pubmed?term=18F-3c%20in%20vitro&cmd=DetailsSearch" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p><i>In vitro</i> receptor binding studies with [<sup>18</sup>F]3c were performed by Tu et al. (<a class="bibr" href="#F18_3c.REF.3" rid="F18_3c.REF.3">3</a>) using membranes isolated from liver homogenates as described elsewhere (<a class="bibr" href="#F18_3c.REF.9" rid="F18_3c.REF.9">9</a>). The affinity of 3c for the two SR subtypes was determined by competition studies using [<sup>3</sup>H](+)-pentazocine (for Sig-1R) and [<sup>3</sup>H]1,3-di(2-tolyl)guanidine in the presence of unlabeled (+)-pentazocine (for Sig-2R). The affinity of 3c, as determined with Scatchard plot analysis, was reported to be 330 ± 25 and 6.95± 1.63 nM for Sig-1R and Sig-2R, respectively, with a Sig-1R/Sig-2R ratio of 48. For comparison, the affinity of 3f was reported to be 2,150 ± 410 and 0.26 ± 0.07 nM, respectively for the two receptor subtypes, with a Sig-1R/Sig-2R ratio of 8,190.</p></div><div id="F18_3c.Animal_Studies"><h2 id="_F18_3c_Animal_Studies_">Animal Studies</h2><div id="F18_3c.Rodents"><h3>Rodents</h3><p>[<a href="/pubmed?term=18F-3c%20rodentia&cmd=DetailsSearch" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Tu et al. studied the biodistribution of [<sup>18</sup>F]3c in BALB/c mice bearing mouse mammary adenocarcinoma EMT-6 cell (these cells express high levels of the SRs (<a class="bibr" href="#F18_3c.REF.10" rid="F18_3c.REF.10">10</a>)) tumors (<a class="bibr" href="#F18_3c.REF.3" rid="F18_3c.REF.3">3</a>). The animals were injected with the labeled compound through the tail vein and euthanized at predetermined time points up to 120 min after the treatment (the number of animals used per time point was not indicated). After euthanasia, tissues from major organs of the animals were removed, weighed, and counted for accumulated radioactivity, and the data were presented as a percentage of injected dose per gram tissue (% ID/g). At 5 min after injection, maximum uptake of radioactivity was noticed in the kidneys (29.18 ± 1.92% ID/g) followed by the liver (23.33 ± 4.22% ID/g) and lungs (10.26 ± 0.71% ID/g). In comparison, the tumor had an uptake of 3.67 ± 0.45% ID/g at this time point. By 2 h after injection, the amount of label in the kidney, liver, lungs, and tumor tissues was reduced to 0.87 ± 0.13, 2.05 ± 0.43, 0.43 ± 0.07, and 0.64 ± 0.10% ID/g, respectively. A similar trend was noticed for the uptake of [<sup>18</sup>F]3f in all the tissues, including the tumors. The tumor/muscle (T/M) and tumor/fat (T/F) ratios for [<sup>18</sup>F]3c were ~3 and ~8, respectively, at 2 h after injection. For [<sup>18</sup>F]3f, the T/M and T/F ratios were ~7 and ~6, respectively. Both [<sup>18</sup>F]3c and [<sup>18</sup>F]3f were reported to have rapid clearance from blood, indicating that both tracers were probably suitable for the detection and imaging of solid tumors expressing Sig-2R.</p><p>For blocking studies, mice were injected with [<sup>18</sup>F]3c in presence of excess (1 mg/Kg) unlabeled <i>N</i>-(4-fluorobenzyl)piperidinyl-4-(3-bromophenyl) acetamide, which has a high affinity for the two SR subtypes (<a class="bibr" href="#F18_3c.REF.3" rid="F18_3c.REF.3">3</a>), and the mice were euthanized 1 h after the treatment (the number of animals used was not reported) (<a class="bibr" href="#F18_3c.REF.3" rid="F18_3c.REF.3">3</a>). Under these conditions, the T/M and T/F ratios for this labeled compound were reduced by ~50%, indicating that the radiochemical bound selectively to the Sig-2R. Similar results were obtained with [<sup>18</sup>F]3f under these experimental conditions.</p><p>Mice bearing EMT-6 cell tumors were injected with [<sup>18</sup>F]3c as detailed above, and PET/CT imaging was performed on the animals 1 h later (<a class="bibr" href="#F18_3c.REF.3" rid="F18_3c.REF.3">3</a>). Both detection methods were reported to identify the tumors in the animals easily. Similar results were reported when [<sup>18</sup>F]3f was used as an imaging agent.</p><p>On the basis of the results obtained from these studies, the investigators concluded that both [<sup>18</sup>F]3c and [<sup>18</sup>F]3f were equally suitable for the detection and imaging of solid tumors expressing Sig-2R using PET (<a class="bibr" href="#F18_3c.REF.3" rid="F18_3c.REF.3">3</a>).</p></div><div id="F18_3c.Other_NonPrimate_Mammals"><h3>Other Non-Primate Mammals</h3><p>[<a href="/pubmed?term=18F-3c%20Other%20Non-Primate%20Mammals&cmd=DetailsSearch" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>No references are currently available.</p></div><div id="F18_3c.NonHuman_Primates"><h3>Non-Human Primates</h3><p>[<a href="/pubmed?term=18F-3c%20Non-Human%20Primates&cmd=DetailsSearch" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>No references are currently available.</p></div></div><div id="F18_3c.Human_Studies"><h2 id="_F18_3c_Human_Studies_">Human Studies</h2><p>[<a href="/pubmed?term=18F-3c%20Human%20Studies&cmd=DetailsSearch" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>No references are currently available.</p></div><div id="F18_3c.Supplemental_Information"><h2 id="_F18_3c_Supplemental_Information_">Supplemental Information</h2><p>[<a href="/books/n/micad/disclaimer/?report=reader">Disclaimers</a>]</p><p>No information is currently available.</p></div><div id="F18_3c.NIH_Support"><h2 id="_F18_3c_NIH_Support_">NIH Support</h2><p>Some studies reported in this chapter were supported by National Institutes of Health grants CA-102869 and P41RR0954.</p></div><div id="F18_3c.References"><h2 id="_F18_3c_References_">References</h2><dl class="temp-labeled-list"><dl class="bkr_refwrap"><dt>1.</dt><dd><div class="bk_ref" id="F18_3c.REF.1">Collier T.L., Waterhouse R.N., Kassiou M.
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<em>Imaging sigma receptors: applications in drug development.</em>
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<span><span class="ref-journal">Curr Pharm Des. </span>2007;<span class="ref-vol">13</span>(1):51–72.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/17266588" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 17266588</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>2.</dt><dd><div class="bk_ref" id="F18_3c.REF.2">Hanner M., Moebius F.F., Flandorfer A., Knaus H.G., Striessnig J., Kempner E., Glossmann H.
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<em>Purification, molecular cloning, and expression of the mammalian sigma1-binding site.</em>
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<span><span class="ref-journal">Proc Natl Acad Sci U S A. </span>1996;<span class="ref-vol">93</span>(15):8072–7.</span> [<a href="/pmc/articles/PMC38877/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC38877</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/8755605" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 8755605</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>3.</dt><dd><div class="bk_ref" id="F18_3c.REF.3">Tu Z., Xu J., Jones L.A., Li S., Dumstorff C., Vangveravong S., Chen D.L., Wheeler K.T., Welch M.J., Mach R.H.
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<em>Fluorine-18-labeled benzamide analogues for imaging the sigma2 receptor status of solid tumors with positron emission tomography.</em>
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<span><span class="ref-journal">J Med Chem. </span>2007;<span class="ref-vol">50</span>(14):3194–204.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/17579383" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 17579383</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>4.</dt><dd><div class="bk_ref" id="F18_3c.REF.4">Wheeler K.T., Wang L.M., Wallen C.A., Childers S.R., Cline J.M., Keng P.C., Mach R.H.
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<em>Sigma-2 receptors as a biomarker of proliferation in solid tumours.</em>
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<span><span class="ref-journal">Br J Cancer. </span>2000;<span class="ref-vol">82</span>(6):1223–32.</span> [<a href="/pmc/articles/PMC2363350/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC2363350</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/10735510" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 10735510</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>5.</dt><dd><div class="bk_ref" id="F18_3c.REF.5">Hashimoto K., Ishiwata K.
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<em>Sigma receptor ligands: possible application as therapeutic drugs and as radiopharmaceuticals.</em>
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<span><span class="ref-journal">Curr Pharm Des. </span>2006;<span class="ref-vol">12</span>(30):3857–76.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/17073684" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 17073684</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>6.</dt><dd><div class="bk_ref" id="F18_3c.REF.6">Kashiwagi H., McDunn J.E., Simon P.O. Jr, Goedegebuure P.S., Vangveravong S., Chang K., Hotchkiss R.S., Mach R.H., Hawkins W.G.
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<em>Sigma-2 receptor ligands potentiate conventional chemotherapies and improve survival in models of pancreatic adenocarcinoma.</em>
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<span><span class="ref-journal">J Transl Med. </span>2009;<span class="ref-vol">7</span>:24.</span> [<a href="/pmc/articles/PMC2669042/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC2669042</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/19323815" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 19323815</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>7.</dt><dd><div class="bk_ref" id="F18_3c.REF.7">Chu W., Xu J., Zhou D., Zhang F., Jones L.A., Wheeler K.T., Mach R.H.
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<em>New N-substituted 9-azabicyclo[3.3.1]nonan-3alpha-yl phenylcarbamate analogs as sigma2 receptor ligands: synthesis, in vitro characterization, and evaluation as PET imaging and chemosensitization agents.</em>
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<span><span class="ref-journal">Bioorg Med Chem. </span>2009;<span class="ref-vol">17</span>(3):1222–31.</span> [<a href="/pmc/articles/PMC2670245/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC2670245</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/19119012" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 19119012</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>8.</dt><dd><div class="bk_ref" id="F18_3c.REF.8">Chopra, A., <em>[18F]Labeled N-(4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-2-(2-fluoroethoxy)-5-iodo-3-methoxybenzamide ([18F]3f).</em> Molecular Imaging and Contrast agent Database (MICAD) [database online]. National Library of Medicine, NCBI, Bethesda, MD, USA. Available from <a href="http://www.micad.nih.gov/" ref="pagearea=cite-ref&targetsite=external&targetcat=link&targettype=uri">www<wbr style="display:inline-block"></wbr>​.micad.nih.gov</a>, 2004 -to current.</div></dd></dl><dl class="bkr_refwrap"><dt>9.</dt><dd><div class="bk_ref" id="F18_3c.REF.9">Xu J., Tu Z., Jones L.A., Vangveravong S., Wheeler K.T., Mach R.H.
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<em>[3H]N-[4-(3,4-dihydro-6,7-dimethoxyisoquinolin-2(1H)-yl)butyl]-2-methoxy-5 -methylbenzamide: a novel sigma-2 receptor probe.</em>
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<span><span class="ref-journal">Eur J Pharmacol. </span>2005;<span class="ref-vol">525</span>(1-3):8–17.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/16289030" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 16289030</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>10.</dt><dd><div class="bk_ref" id="F18_3c.REF.10">Colabufo N.A., Berardi F., Contino M., Fazio F., Matarrese M., Moresco R.M., Niso M., Perrone R., Tortorella V.
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<em>Distribution of sigma receptors in EMT-6 cells: preliminary biological evaluation of PB167 and potential for in-vivo PET.</em>
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<span><span class="ref-journal">J Pharm Pharmacol. </span>2005;<span class="ref-vol">57</span>(11):1453–9.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/16259778" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 16259778</span></a>]</div></dd></dl></dl></div><div id="bk_toc_contnr"></div></div></div><div class="fm-sec"><h2 id="_NBK23102_pubdet_">Publication Details</h2><h3>Author Information and Affiliations</h3><div class="contrib half_rhythm"><span itemprop="author">Arvind Chopra</span>, PhD<div class="affiliation small">National Center for Biotechnology Information, NLM, NIH, Bethesda, MD 20894<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><h3>Publication History</h3><p class="small">Created: <span itemprop="datePublished">November 18, 2009</span>; Last Update: <span itemprop="dateModified">January 7, 2010</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>Chopra A. 18F-Labeled N-(4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-2-(2-fluoroethoxy)-5-methylbenzamide. 2009 Nov 18 [Updated 2010 Jan 7]. 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/F18_3f/?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/F18-2ZHER2-477/?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="figobF183cTncChemicalname18FLabeledN467"><div id="F18_3c.T.nc_Chemical_name18FLabeled_N467" class="table"><p class="large-table-link" style="display:none"><span class="right"><a href="/books/NBK23102/table/F18_3c.T.nc_Chemical_name18FLabeled_N467/?report=objectonly" target="object">View in own window</a></span></p><div class="large_tbl" id="__F18_3c.T.nc_Chemical_name18FLabeled_N467_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 <i>N</i>-(4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1<i>H</i>)-yl)butyl)-2-(2-fluoroethoxy)-5-methylbenzamide</td><td rowspan="9" colspan="1" style="text-align:center;vertical-align:middle;">
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<span class="graphic"><img src="/books/NBK23102/bin/F183c.jpg" alt="Image F183c.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]3c</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;"></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;">Compound</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;">Sigma-2 receptor</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;">Receptor</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]3c.</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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