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<div class="pre-content"><div><div class="bk_prnt"><p class="small">NCBI Bookshelf. A service of the National Library of Medicine, National Institutes of Health.</p><p>Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013. </p></div><div class="iconblock clearfix whole_rhythm no_top_margin bk_noprnt"><a class="img_link icnblk_img" title="Table of Contents Page" href="/books/n/micad/"><img class="source-thumb" src="/corehtml/pmc/pmcgifs/bookshelf/thumbs/th-micad-lrg.png" alt="Cover of Molecular Imaging and Contrast Agent Database (MICAD)" height="100px" width="80px" /></a><div class="icnblk_cntnt eight_col"><h2>Molecular Imaging and Contrast Agent Database (MICAD) [Internet].</h2><a data-jig="ncbitoggler" href="#__NBK109897_dtls__">Show details</a><div style="display:none" class="ui-widget" id="__NBK109897_dtls__"><div>Bethesda (MD): <a href="https://www.ncbi.nlm.nih.gov/" ref="pagearea=page-banner&amp;targetsite=external&amp;targetcat=link&amp;targettype=publisher">National Center for Biotechnology Information (US)</a>; 2004-2013.</div></div><div class="half_rhythm"><ul class="inline_list"><li style="margin-right:1em"><a class="bk_cntns" href="/books/n/micad/">Contents</a></li></ul></div><div class="bk_noprnt"><form method="get" action="/books/n/micad/" id="bk_srch"><div class="bk_search"><label for="bk_term" class="offscreen_noflow">Search term</label><input type="text" title="Search this book" id="bk_term" name="term" value="" data-jig="ncbiclearbutton" /> <input type="submit" class="jig-ncbibutton" value="Search this book" submit="false" style="padding: 0.1em 0.4em;" /></div></form></div></div><div class="icnblk_cntnt two_col"><div class="pagination bk_noprnt"><a class="active page_link prev" href="/books/n/micad/MK-1312-18F/" title="Previous page in this title">&lt; Prev</a><a class="active page_link next" href="/books/n/micad/FMAU18F/" title="Next page in this title">Next &gt;</a></div></div></div></div></div>
<div class="main-content lit-style" itemscope="itemscope" itemtype="http://schema.org/CreativeWork"><div class="meta-content fm-sec"><h1 id="_NBK109897_"><span class="title" itemprop="name">1-(2-{(2R)-1-[(2-[<sup>18</sup>F]Fluorophenyl)sulfonyl]pyrrolidin-2-yl}ethyl)-4-methylpiperidine</span></h1><div itemprop="alternativeHeadline" class="subtitle whole_rhythm">[<sup>18</sup>F]-2FP3</div><p class="contrib-group"><span itemprop="author">Kam Leung</span>, PhD.</p><a data-jig="ncbitoggler" href="#__NBK109897_ai__" style="border:0;text-decoration:none">Author Information and Affiliations</a><div style="display:none" class="ui-widget" id="__NBK109897_ai__"><div class="contrib half_rhythm"><span itemprop="author">Kam Leung</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></div><p class="small">Created: <span itemprop="datePublished">July 20, 2012</span>; Last Update: <span itemprop="dateModified">November 1, 2012</span>.</p></div><div class="jig-ncbiinpagenav body-content whole_rhythm" data-jigconfig="allHeadingLevels: ['h2'],smoothScroll: false" itemprop="text"><div id="F18-2FP3.T.nc_chemical_name122r1218ff" class="table"><p class="large-table-link" style="display:none"><span class="right"><a href="/books/NBK109897/table/F18-2FP3.T.nc_chemical_name122r1218ff/?report=objectonly" target="object">View in own window</a></span></p><div class="large_tbl" id="__F18-2FP3.T.nc_chemical_name122r1218ff_lrgtbl__"><table><tbody><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
<b>Chemical name:</b>
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">1-(2-{(2R)-1-[(2-[<sup>18</sup>F]Fluorophenyl)sulfonyl]pyrrolidin-2-yl}ethyl)-4-methylpiperidine</td><td rowspan="9" colspan="1" style="text-align:center;vertical-align:middle;">
<a href="https://pubchem.ncbi.nlm.nih.gov/substance/147136418" title="View this structure in PubChem" class="img_link" ref="pagearea=body&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubchem"><img src="https://pubchem.ncbi.nlm.nih.gov/image/imgsrv.fcgi?t=l&amp;sid=147136418" alt="image 147136418 in the ncbi pubchem database" /></a>
</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
<b>Abbreviated name:</b>
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">[<sup>18</sup>F]-2FP3</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
<b>Synonym:</b>
</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;">
<b>Agent category:</b>
</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;">
<b>Target:</b>
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">5-HT<sub>7</sub> serotonin receptors</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
<b>Target category:</b>
</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;">
<b>Method of detection:</b>
</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;">
<b>Source of signal:</b>
</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;">
<b>Activation:</b>
</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;">
<b>Studies:</b>
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">
<ul class="simple-list"><li class="half_rhythm"><div>
<img alt="Checkbox" src="/corehtml/pmc/css/bookshelf/2.26/img/studies.checkbox.png" />
<i>In vitro</i>
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<img alt="Checkbox" src="/corehtml/pmc/css/bookshelf/2.26/img/studies.checkbox.png" /> Rodents
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<img alt="Checkbox" src="/corehtml/pmc/css/bookshelf/2.26/img/studies.checkbox.png" /> Non-primate non-rodent mammals
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Click on the above structure for additional information in <a href="http://pubchem.ncbi.nlm.nih.gov/" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">PubChem</a>.</td></tr></tbody></table></div></div><div id="F18-2FP3.Background"><h2 id="_F18-2FP3_Background_">Background</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&#x00026;db=pubmed&#x00026;details_term=2FP3%20PET" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">PubMed</a>]</p><p>5-Hydroxytryptamine (5-HT), commonly known as serotonin, has diverse physiological roles as a neurotransmitter in the central nervous system (<a class="bk_pop" href="#F18-2FP3.REF.1">1</a>). 5-HT is involved in regulation and modulation of sleep, affective and personality behaviors, and pain. It also is a regulator of smooth muscle function and platelet aggregation. The brain cortical 5-HT system has been implicated in several neuropsychiatric disorders, including major depression, anxiety, schizophrenia, and obsessive-compulsive disorder (<a class="bk_pop" href="#F18-2FP3.REF.2" data-bk-pop-others="F18-2FP3.REF.3">2, 3</a>). The effects of 5-HT are mediated by as many as seven classes of receptor populations (5-HT<sub>1</sub> to 5-HT<sub>7</sub>), many of which include several subtypes (<a class="bk_pop" href="#F18-2FP3.REF.4">4</a>). There are five receptor subtypes within the G-protein&#x02013;coupled 5-HT<sub>1</sub> receptor family: 5-HT<sub>1A</sub>, 5-HT<sub>1B</sub>, 5-HT<sub>1D</sub>, 5-HT<sub>1E</sub>, and 5-HT<sub>1F</sub>.</p><p>5-HT<sub>7</sub> receptors are abundantly present in the hippocampus, thalamus, and hypothalamus; low densities are observed in the cortex and amygdala (<a class="bk_pop" href="#F18-2FP3.REF.5" data-bk-pop-others="F18-2FP3.REF.6 F18-2FP3.REF.7">5-7</a>). 5-HT<sub>7</sub> receptors are involved in the mediation of emotion and the function of the hypothalamus. 5-HT<sub>7</sub> receptors are implicated in anxiety, depression, hallucinogenic behavior, circadian rhythms and sleep, memory, epilepsy, and pain. Thus, there is a need for selective ligands to investigate the pharmacological role of 5-HT<sub>7</sub> receptors. 1-(2-{(2R)-1-[(2-[<sup>18</sup>F]Fluorophenyl)sulfonyl]pyrrolidin-2-yl}ethyl)-4-methylpiperidine ([<sup>18</sup>F]-2FP3) was evaluated as a positron emission tomography (PET) probe for 5-HT<sub>7</sub> receptors because the unlabeled 2FP3 was found to be a selective 5-HT<sub>7</sub> antagonist with nanomolar affinity for the 5-HT<sub>7</sub> receptor.</p><div id="F18-2FP3.Related_Resource_Links"><h3>Related Resource Links:</h3><ul><li class="half_rhythm"><div>Chapters in MICAD (<a href="/sites/entrez?db=Books&#x00026;cmd=Search&#x00026;term=5-HT7+AND+micad%5bbook%5d&#x00026;doptcmdl=TOCView&#x00026;log%24=booksrch&#x00026;bname=micad" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">5-HT<sub>7</sub></a>)</div></li><li class="half_rhythm"><div>Gene information in NCBI (<a href="/gene/3363" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">5-HT<sub>7</sub></a>)</div></li><li class="half_rhythm"><div>Articles in Online Mendelian Inheritance in Man (OMIM) (<a href="http://omim.org/entry/182137" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">5-HT<sub>7</sub></a>)</div></li><li class="half_rhythm"><div>Clinical trials (<a href="http://www.clinicaltrials.gov/ct2/results?term=5-HT" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">5-HT</a>)</div></li><li class="half_rhythm"><div>Drug information in Food and Drug Administration (<a href="http://google2.fda.gov/search?q=5-HT7&#x00026;client=FDAgov&#x00026;site=FDAgov&#x00026;lr=&#x00026;proxystylesheet=FDAgov&#x00026;output=xml_no_dtd&#x00026;getfields=*&#x00026;filter=1" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">5-HT<sub>7</sub></a>)</div></li></ul></div></div><div id="F18-2FP3.Synthesis"><h2 id="_F18-2FP3_Synthesis_">Synthesis</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&#x00026;db=pubmed&#x00026;details_term=2FP3%20and%20synthesis" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">PubMed</a>]</p><p>The automated radiosynthesis of [<sup>18</sup>F]-2FP3 involved standard fluoronucleophilic substitution of the corresponding nitro precursor with K[<sup>18</sup>F]F/Kryptofix2.2.2 in dimethyl sulfoxide for 10 min at 150&#x000b0;C in an automated radiosynthesis unit, followed by solid-phase extraction with C18 cartridge (<a class="bk_pop" href="#F18-2FP3.REF.8" data-bk-pop-others="F18-2FP3.REF.9">8, 9</a>). The reported overall radiochemical yield of the radiosynthesis was 48% at the end of bombardment, with a specific activity of 40&#x02013;130 MBq/nmol (1.1&#x02013;3.5 mCi/nmol) at the end of synthesis, and a radiochemical purity of &#x0003e;98%. The total synthesis time was 100&#x02013;120 min. The log <i>P</i> value for [<sup>18</sup>F]-2FP3 was 1.2&#x02013;1.4.</p></div><div id="F18-2FP3.In_Vitro_Studies_Testing_in_Cel"><h2 id="_F18-2FP3_In_Vitro_Studies_Testing_in_Cel_"><i>In Vitro</i> Studies: Testing in Cells and Tissues</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&#x00026;db=pubmed&#x00026;details_term=2FP3%20and%20in%20vitro" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">PubMed</a>]</p><p>Lemoine et al. (<a class="bk_pop" href="#F18-2FP3.REF.8">8</a>) performed <i>in vitro</i> autoradiography in rat brains with [<sup>18</sup>F]-2FP3, which exhibited radioactivity in the cingulate cortex, hippocampus, cerebellum, and thalamus. The radioactivity in the cortex and hippocampus was inhibited by SB269970 (a selective 5-HT<sub>7</sub> receptor antagonist), with 43% inhibition at 10 nM and 80% inhibition at 1,000 nM. <i>In vitro</i> binding was performed with CHO cells transfected with human recombinant 5-HT receptors. The binding affinity <i>K</i><sub>d</sub> values of [<sup>18</sup>F]-2FP3 for 5-HT<sub>7</sub> receptors was 1.43 nM with little affinity for 5-HT<sub>1A</sub> and 5-HT<sub>6</sub> receptors.</p></div><div id="F18-2FP3.Animal_Studies"><h2 id="_F18-2FP3_Animal_Studies_">Animal Studies</h2><div id="F18-2FP3.Rodents"><h3>Rodents</h3><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&#x00026;db=pubmed&#x00026;details_term=2FP3%20and%20rodentia" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">PubMed</a>]</p><p><i>Ex vivo</i> stability studies of [<sup>18</sup>F]-2FP3 in the brains of rats (<i>n</i> = 3/group) were performed at 10, 20, 30, and 40 min after intravenous injection of 55.5 MBq (1.5 mCi) [<sup>18</sup>F]-2FP3. [<sup>18</sup>F]-2FP3 remained &#x0003e;95% intact at these time points as determined with HPLC (<a class="bk_pop" href="#F18-2FP3.REF.8">8</a>).</p><p>Rat brains were excised at 20 min after injection of 55.5 MBq (1.5 mCi) [<sup>18</sup>F]-2FP3. <i>Ex vivo</i> PET imaging studies (<i>n</i> = 3/group) were performed at 45 min after the brains were removed (<a class="bk_pop" href="#F18-2FP3.REF.8">8</a>). Higher radioactivity levels were observed in the cingulate cortex and hippocampus than in the striatum and cerebellum. Pretreatment with excess SB269970 (30 min, 5 mg/kg) decreased [<sup>18</sup>F]-2FP3 binding in all brain areas.</p></div><div id="F18-2FP3.Other_NonPrimate_Mammals"><h3>Other Non-Primate Mammals</h3><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&#x00026;db=pubmed&#x00026;details_term=2FP3%20and%20%28dog%20or%20pig%20or%20sheep%20or%20rabbit%29" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">PubMed</a>]</p><p>Lemoine et al. (<a class="bk_pop" href="#F18-2FP3.REF.8">8</a>) performed <i>in vivo</i> PET imaging studies in the brains of two male cats for 90 min after injection of 74 MBq (2 mCi) [<sup>18</sup>F]-2FP3. High initial radioactivity levels were observed in the cingulate cortex, thalamus, hippocampus, and cerebellum. Pretreatment with excess SB269970 (30 min, 5 mg/kg) decreased [<sup>18</sup>F]-2FP3 binding in these brain areas to background levels.</p></div><div id="F18-2FP3.NonHuman_Primates"><h3>Non-Human Primates</h3><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&#x00026;db=pubmed&#x00026;details_term=2FP3%20and%20nonhuman%20primate" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">PubMed</a>]</p><p>No publication is currently available.</p></div></div><div id="F18-2FP3.Human_Studies"><h2 id="_F18-2FP3_Human_Studies_">Human Studies</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&#x00026;db=pubmed&#x00026;details_term=2FP3%20and%20human" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">PubMed</a>]</p><p>No publication is currently available.</p></div><div id="F18-2FP3.References"><h2 id="_F18-2FP3_References_">References</h2><dl class="temp-labeled-list"><dt>1.</dt><dd><div class="bk_ref" id="F18-2FP3.REF.1">Lucki I.
<em>The spectrum of behaviors influenced by serotonin.</em>
<span><span class="ref-journal">Biol Psychiatry. </span>1998;<span class="ref-vol">44</span>(3):15162.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/9693387" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 9693387</span></a>]</div></dd><dt>2.</dt><dd><div class="bk_ref" id="F18-2FP3.REF.2">Fletcher A., Cliffe I.A., Dourish C.T.
<em>Silent 5-HT1A receptor antagonists: utility as research tools and therapeutic agents.</em>
<span><span class="ref-journal">Trends Pharmacol Sci. </span>1993;<span class="ref-vol">14</span>(12):418.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/8122313" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 8122313</span></a>]</div></dd><dt>3.</dt><dd><div class="bk_ref" id="F18-2FP3.REF.3">Hoyer D., Clarke D.E., Fozard J.R., Hartig P.R., Martin G.R., Mylecharane E.J., Saxena P.R., Humphrey P.P.
<em>International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin).</em>
<span><span class="ref-journal">Pharmacol Rev. </span>1994;<span class="ref-vol">46</span>(2):157203.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/7938165" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 7938165</span></a>]</div></dd><dt>4.</dt><dd><div class="bk_ref" id="F18-2FP3.REF.4">Lanfumey L., Hamon M.
<em>5-HT1 receptors.</em>
<span><span class="ref-journal">Curr Drug Targets CNS Neurol Disord. </span>2004;<span class="ref-vol">3</span>(1):110.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/14965240" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 14965240</span></a>]</div></dd><dt>5.</dt><dd><div class="bk_ref" id="F18-2FP3.REF.5">Bard J.A., Zgombick J., Adham N., Vaysse P., Branchek T.A., Weinshank R.L.
<em>Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.</em>
<span><span class="ref-journal">J Biol Chem. </span>1993;<span class="ref-vol">268</span>(31):234226.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/8226867" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 8226867</span></a>]</div></dd><dt>6.</dt><dd><div class="bk_ref" id="F18-2FP3.REF.6">Varnas K., Thomas D.R., Tupala E., Tiihonen J., Hall H.
<em>Distribution of 5-HT7 receptors in the human brain: a preliminary autoradiographic study using [3H]SB-269970.</em>
<span><span class="ref-journal">Neurosci Lett. </span>2004;<span class="ref-vol">367</span>(3):3136.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/15337256" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 15337256</span></a>]</div></dd><dt>7.</dt><dd><div class="bk_ref" id="F18-2FP3.REF.7">Martin-Cora F.J., Pazos A.
<em>Autoradiographic distribution of 5-HT7 receptors in the human brain using [3H]mesulergine: comparison to other mammalian species.</em>
<span><span class="ref-journal">Br J Pharmacol. </span>2004;<span class="ref-vol">141</span>(1):92104.</span> [<a href="/pmc/articles/PMC1574165/" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pmc">PMC free article<span class="bk_prnt">: PMC1574165</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/14656806" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 14656806</span></a>]</div></dd><dt>8.</dt><dd><div class="bk_ref" id="F18-2FP3.REF.8">Lemoine L., Andries J., Le Bars D., Billard T., Zimmer L.
<em>Comparison of 4 radiolabeled antagonists for serotonin 5-HT(7) receptor neuroimaging: toward the first PET radiotracer.</em>
<span><span class="ref-journal">J Nucl Med. </span>2011;<span class="ref-vol">52</span>(11):18118.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/21990574" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 21990574</span></a>]</div></dd><dt>9.</dt><dd><div class="bk_ref" id="F18-2FP3.REF.9">Andries J., Lemoine L., Le Bars D., Zimmer L., Billard T.
<em>Synthesis and biological evaluation of potential 5-HT(7) receptor PET radiotracers.</em>
<span><span class="ref-journal">Eur J Med Chem. </span>2011;<span class="ref-vol">46</span>(8):345561.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/21620533" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 21620533</span></a>]</div></dd></dl></div><div id="bk_toc_contnr"></div></div></div>
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<div xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance"></div><div class="portlet"><div class="portlet_head"><div class="portlet_title"><h3><span>Views</span></h3></div><a name="Shutter" sid="1" href="#" class="portlet_shutter" title="Show/hide content" remembercollapsed="true" pgsec_name="PDF_download" id="Shutter"></a></div><div class="portlet_content"><ul xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="simple-list"><li><a href="/books/NBK109897/?report=reader">PubReader</a></li><li><a href="/books/NBK109897/?report=printable">Print View</a></li><li><a data-jig="ncbidialog" href="#_ncbi_dlg_citbx_NBK109897" data-jigconfig="width:400,modal:true">Cite this Page</a><div id="_ncbi_dlg_citbx_NBK109897" style="display:none" title="Cite this Page"><div class="bk_tt">Leung K. 1-(2-{(2R)-1-[(2-[18F]Fluorophenyl)sulfonyl]pyrrolidin-2-yl}ethyl)-4-methylpiperidine. 2012 Jul 20 [Updated 2012 Nov 1]. 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></div></div></li><li><a href="/books/NBK109897/pdf/Bookshelf_NBK109897.pdf">PDF version of this page</a> (138K)</li><li><a href="/books/n/micad/toc/bin/micad.csv">MICAD summary (CSV file)</a></li></ul></div></div><div class="portlet"><div class="portlet_head"><div class="portlet_title"><h3><span>In this page</span></h3></div><a name="Shutter" sid="1" href="#" class="portlet_shutter" title="Show/hide content" remembercollapsed="true" pgsec_name="page-toc" id="Shutter"></a></div><div class="portlet_content"><ul xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="simple-list"><li><a href="#F18-2FP3.Background" ref="log$=inpage&amp;link_id=inpage">Background</a></li><li><a href="#F18-2FP3.Synthesis" ref="log$=inpage&amp;link_id=inpage">Synthesis</a></li><li><a href="#F18-2FP3.In_Vitro_Studies_Testing_in_Cel" ref="log$=inpage&amp;link_id=inpage"><i>In Vitro</i> Studies: Testing in Cells and Tissues</a></li><li><a href="#F18-2FP3.Animal_Studies" ref="log$=inpage&amp;link_id=inpage">Animal Studies</a></li><li><a href="#F18-2FP3.Human_Studies" ref="log$=inpage&amp;link_id=inpage">Human Studies</a></li><li><a href="#F18-2FP3.References" ref="log$=inpage&amp;link_id=inpage">References</a></li></ul></div></div><div class="portlet"><div class="portlet_head"><div class="portlet_title"><h3><span>Search MICAD</span></h3></div><a name="Shutter" sid="1" href="#" class="portlet_shutter" title="Show/hide content" remembercollapsed="true" pgsec_name="source-application" id="Shutter"></a></div><div class="portlet_content"><form xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" name="frmSearch" method="get" action="/books/NBK5330/" id="frmSearch"><script type="text/javascript" src="/corehtml/pmc//js/bookshelf/micad.js">/**/</script><label class="offscreen_noflow" for="txtfield">Search term</label><input id="txtfield" type="text" name="f1_term" size="22" onKeyPress="KeyPress('micad',event,'/books/NBK5330/','')" /><button name="f1_search" type="submit">Go</button><button onclick="this.form.reset();" type="reset">Clear</button><p><b>Limit my Search:</b></p><div class="clearfix"><label for="detection">Method of detection:</label><div class="right"><select name="detection" id="detection" style="width:200px"><option value="" selected="selected">Any</option><option value="(MRI OR &quot;Magnetic resonance imaging&quot; OR MRS)">MRI</option><option value="Multimodal">Multimodal imaging</option><option value="Optical">Optical imaging</option><option value="PET">PET</option><option value="Photoacoustic">Photoacoustic imaging</option><option value="(SPECT OR planar)">SPECT</option><option value="Ultrasound">Ultrasound</option><option value="(x-ray OR ct)">X-ray, CT</option></select></div></div><div class="clearfix"><label for="signal">Source of signal/contrast:</label><div class="right"><select name="signal" id="signal" style="width:200px"><option value="" selected="selected">Any</option><optgroup label="MRI agents"><option value="(Copper OR Cu)">Copper</option><option value="(Europium OR Eu3+)">Europium</option><option value="(Fluorine OR 19F)">Fluorine</option><option value="(Gadolinium OR Gd3+)">Gadolinium</option><option value="&quot;Hyperpolarized 13C&quot;">Hyperpolarized 13C</option><option value="&quot;Iron oxide&quot;">Iron oxide</option><option value="&quot;Nitroxide radicals&quot;">Nitroxide radicals</option><option value="(Oxygen OR 17O)">Oxygen</option><option value="Thulium">Thulium</option></optgroup><optgroup label="Multimodal agents"><option value="((Gadolinium OR Gd3+) AND Optical)">Gadolinium and optical</option><option value="((Gadolinium OR Gd3+) AND (Gold OR Au))">Gadolinium and Gold</option><option value="(&quot;Iron oxide&quot; AND (64Cu OR 124I OR 111In))">Iron oxide and
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value="(&quot;Iodine 124&quot; OR 124I)">Iodine-124</option><option value="(&quot;Nitrogen 13&quot; OR 13N)">Nitrogen-13</option><option value="(&quot;Yttrium 86&quot; OR 86Y)">Yttrium-86</option><option value="(&quot;Zirconium 89&quot; OR 89Zr)">Zirconium-89</option></optgroup><optgroup label="Photoacoustic agents"><option value="(Gold OR Au)">Gold</option><option value="(&quot;Indocyanine green&quot; OR ICG)">Indocyanine green</option></optgroup><optgroup label="SPECT radionuclides"><option value="(Gallium-67 OR 67Ga)">Gallium-67</option><option value="(&quot;Indium 111&quot; OR 111In)">Indium-111</option><option value="(&quot;Iodine 123&quot; OR &quot;Iodine 125&quot; OR &quot;Iodine 131&quot; OR 123I OR 125I OR 131I)">Iodine-123, 125, 131</option><option value="(&quot;Lutetium 177&quot; OR 177Lu)">Lutetium-177</option><option value="(Rhenium OR 186Re OR 188Re)">Rhenium</option><option value="(&quot;Technetium 99m&quot; OR 99mTc)">Technetium-99m</option><option value="(&quot;Tellurium 125m&quot; OR 125mTe)">Tellurium-125m</option></optgroup><optgroup label="Ultrasound agents"><option value="Microbubbles">Microbubbles</option><option value="Nanobubbles">Nanobubbles</option></optgroup><optgroup label="X-ray and CT agents"><option value="(Bismuth OR Bi)">Bismuth</option><option value="(Gold OR Au)">Gold</option><option value="Iodine">Iodine</option></optgroup></select></div></div><div class="clearfix"><label for="agent">Agent Category:</label><div class="right"><select name="agent" id="agent" style="width:200px"><option value="" selected="selected">Any</option><option value="(antibody OR trastuzumab OR immunoglobulin)">Antibodies</option><option value="(bacteria OR bacteriophage OR coli)">Bacteria</option><option value="cell">Cells</option><option value="(compound OR &quot;amino acid&quot; OR &quot;folic acid&quot; OR &quot;cage molecule&quot; OR carbohydrate OR copolymers OR polymer OR &quot;small molecule&quot; OR macromolecule OR 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title="Show/hide content" remembercollapsed="true" pgsec_name="PBooksDiscovery_RA" id="Shutter"></a></div><div class="portlet_content"><ul><li class="brieflinkpopper two_line"><a class="brieflinkpopperctrl" href="/pubmed/23077753" ref="ordinalpos=1&amp;linkpos=1&amp;log$=relatedreviews&amp;logdbfrom=pubmed"><span xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="invert">Review</span> 3-Chloro-4-[(18)F]fluorophenyl-(4-fluoro-4-[[(5-methyl-pyrimidin-2-ylmethyl)-amino]-methyl]-piperidin-1-yl)methanone (F15599).</a><span class="source">[Molecular Imaging and Contrast...]</span><div class="brieflinkpop offscreen_noflow"><span xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="invert">Review</span> 3-Chloro-4-[(18)F]fluorophenyl-(4-fluoro-4-[[(5-methyl-pyrimidin-2-ylmethyl)-amino]-methyl]-piperidin-1-yl)methanone (F15599).<div class="brieflinkpopdesc"><em xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="author">Leung K. </em><em xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="cit">Molecular Imaging and Contrast Agent Database (MICAD). 2004</em></div></div></li><li class="brieflinkpopper two_line"><a class="brieflinkpopperctrl" href="/pubmed/23077752" ref="ordinalpos=1&amp;linkpos=2&amp;log$=relatedreviews&amp;logdbfrom=pubmed"><span xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="invert">Review</span> 3-Chloro-4-[(18)F]fluorophenyl-(4-fluoro-4-[[((5-methyl-4-methylamino-pyridin-2-ylmethyl)-amino]-methyl]-piperidin-1-yl)methanone (F13714).</a><span class="source">[Molecular Imaging and Contrast...]</span><div class="brieflinkpop offscreen_noflow"><span xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" 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