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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="#__NBK23473_dtls__">Show details</a><div style="display:none" class="ui-widget" id="__NBK23473_dtls__"><div>Bethesda (MD): <a href="https://www.ncbi.nlm.nih.gov/" ref="pagearea=page-banner&targetsite=external&targetcat=link&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/F18-6b/" title="Previous page in this title">< Prev</a><a class="active page_link next" href="/books/n/micad/FEatCIT18F/" title="Next page in this title">Next ></a></div></div></div></div></div>
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<div class="main-content lit-style" itemscope="itemscope" itemtype="http://schema.org/CreativeWork"><div class="meta-content fm-sec"><h1 id="_NBK23473_"><span class="title" itemprop="name">3-<i>N</i>-(2-[<sup>18</sup>F]Fluoroethyl)spiperone</span></h1><div itemprop="alternativeHeadline" class="subtitle whole_rhythm">[<sup>18</sup>F]FESP</div><p class="contrib-group"><span itemprop="author">Kam Leung</span>, PhD.</p><a data-jig="ncbitoggler" href="#__NBK23473_ai__" style="border:0;text-decoration:none">Author Information and Affiliations</a><div style="display:none" class="ui-widget" id="__NBK23473_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">October 7, 2005</span>; Last Update: <span itemprop="dateModified">January 18, 2012</span>.</p></div><div class="jig-ncbiinpagenav body-content whole_rhythm" data-jigconfig="allHeadingLevels: ['h2'],smoothScroll: false" itemprop="text"><div id="FESP18F.T.nc_chemical_name3n218ffluoroet" class="table"><p class="large-table-link" style="display:none"><span class="right"><a href="/books/NBK23473/table/FESP18F.T.nc_chemical_name3n218ffluoroet/?report=objectonly" target="object">View in own window</a></span></p><div class="large_tbl" id="__FESP18F.T.nc_chemical_name3n218ffluoroet_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:middle;">3-<i>N</i>-(2-[<sup>18</sup>F]Fluoroethyl)spiperone</td><td rowspan="9" colspan="1" style="text-align:center;vertical-align:middle;">
|
||
<a href="https://pubchem.ncbi.nlm.nih.gov/substance/121" title="View this structure in PubChem" class="img_link" ref="pagearea=body&targetsite=entrez&targetcat=link&targettype=pubchem"><img src="https://pubchem.ncbi.nlm.nih.gov/image/imgsrv.fcgi?t=l&sid=121" alt="image 121 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:middle;">[<sup>18</sup>F]FESP</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:middle;"></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:middle;">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:middle;">D<sub>2</sub> dopamine receptor and 5-HT<sub>2</sub> serotonin receptor</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:middle;">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:middle;">PET</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
|
||
<b>Source of signal / contrast:</b>
|
||
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:middle;"><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:middle;">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>
|
||
|
||
</div></li><li class="half_rhythm"><div>
|
||
<img alt="Checkbox" src="/corehtml/pmc/css/bookshelf/2.26/img/studies.checkbox.png" /> Rodents
|
||
</div></li><li class="half_rhythm"><div>
|
||
<img alt="Checkbox" src="/corehtml/pmc/css/bookshelf/2.26/img/studies.checkbox.png" /> Non-human primates
|
||
</div></li><li class="half_rhythm"><div>
|
||
<img alt="Checkbox" src="/corehtml/pmc/css/bookshelf/2.26/img/studies.checkbox.png" /> Humans
|
||
</div></li></ul>
|
||
</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&targetsite=external&targetcat=link&targettype=uri">PubChem</a>.</td></tr></tbody></table></div></div><div id="FESP18F.Background"><h2 id="_FESP18F_Background_">Background</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=%223-N-%282-fluoroethyl%29spiperone%22%5BSubstance%20Name%5D" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Dopamine, a neurotransmitter, plays an important role in the mediation of movement, cognition, and emotion (<a class="bk_pop" href="#FESP18F.REF.1" data-bk-pop-others="FESP18F.REF.2">1, 2</a>). Dopamine shortage plays a role in various neuropsychiatric disorders, such as Parkinson’s disease (PD), schizophrenia, autism, attention deficit hyperactivity disorder, and drug abuse. Two subtypes of dopamine receptors, D<sub>1</sub> and D<sub>2</sub>, were well-characterized pharmacologically and biochemically (<a class="bk_pop" href="#FESP18F.REF.3">3</a>). D<sub>2</sub> dopamine receptors have been implicated in the pathophysiology of PD, Alzheimer's disease, and schizophrenia (<a class="bk_pop" href="#FESP18F.REF.4">4</a>).</p><p>Serotonin (5-hydroxytryptamine, 5-HT) has diverse physiological roles as a neurotransmitter in the central nervous system (<a class="bk_pop" href="#FESP18F.REF.5">5</a>). 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, obsessive-compulsive disorder, and schizophrenia (<a class="bk_pop" href="#FESP18F.REF.6" data-bk-pop-others="FESP18F.REF.7">6, 7</a>).</p><p>Spiperone and its analog, 3-<i>N</i>-(2-fluoroethyl)spiperone (FESP) are high-affinity D<sub>2</sub> dopamine and 5-HT<sub>2</sub> serotonin receptor antagonists, showing a low affinity for α1-adrenergic receptors and marginal binding to other receptors (<a class="bk_pop" href="#FESP18F.REF.8">8</a>). 3-<i>N</i>-(2-[<sup>18</sup>F]Fluoroethyl)spiperone ([<sup>18</sup>F]FESP) has been studied as a positron emission tomography (PET) tracer for imaging D<sub>2</sub> and 5HT<sub>2</sub> receptor densities. It has also used as a reporter probe for dopamine D<sub>2</sub> receptor in imaging transgene expression in rodents (<a class="bk_pop" href="#FESP18F.REF.9" data-bk-pop-others="FESP18F.REF.10 FESP18F.REF.11">9-11</a>).</p><div id="FESP18F.Related_Resource_Links"><h3>Related Resource Links:</h3><ul><li class="half_rhythm"><div>Chapters in MICAD (<a href="/sites/entrez?db=Books&cmd=Search&term=5-HT2A+AND+micad%5bbook%5d&doptcmdl=TOCView&log%24=booksrch&bname=micad" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">5-HT<sub>2A</sub></a>, <a href="/sites/entrez?Db=books&Cmd=DetailsSearch&Term=dopamine%20(receptors%20OR%20receptor)+%20AND+Table+AND+micad%5Bbook%5D" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">Dopamine receptors</a>)</div></li><li class="half_rhythm"><div>Gene information in NCBI (<a href="/gene/3356" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">5-HT<sub>2A</sub></a>, <a href="/gene/1813" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">D<sub>2</sub> receptor,</a><a href="/gene/1814" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">D<sub>3</sub> receptor</a>)</div></li><li class="half_rhythm"><div>Articles in Online Mendelian Inheritance in Man (OMIM) (<a href="/omim/182135" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">5-HT<sub>2A</sub></a>, <a href="/omim/126450" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">D<sub>2</sub> receptor</a>, <a href="/omim/126451" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">D<sub>3</sub> receptor</a>)</div></li><li class="half_rhythm"><div>Clinical trials (<a href="http://www.clinicaltrials.gov/ct2/results?term=5-HT2A" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">5-HT<sub>2A</sub></a>, <a href="http://www.clinicaltrials.gov/ct2/results?term=dopamine+receptor" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">Dopamine receptors</a>)</div></li><li class="half_rhythm"><div>Drug information in Food and Drug Administration (<a href="http://google2.fda.gov/search?q=5-HT2a&client=FDAgov&site=FDAgov&lr=&proxystylesheet=FDAgov&output=xml_no_dtd&getfields=*&x=8&y=1" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">5-HT<sub>2A</sub></a>, <a href="http://google2.fda.gov/search?q=dopamine+receptor&client=FDAgov&site=FDAgov&lr=&proxystylesheet=FDAgov&output=xml_no_dtd&getfields=*&x=6&y=12" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">Dopamine receptors</a>)</div></li></ul></div></div><div id="FESP18F.Synthesis"><h2 id="_FESP18F_Synthesis_">Synthesis</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=%223-N-%282-fluoroethyl%29spiperone%22%5BSubstance%20Name%5D%20AND%20synthesis%5BAll%20Fields%5D" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p> [<sup>18</sup>F]FESP can be synthesized by either N-alkylation or nucleophilic substitution (<a class="bk_pop" href="#FESP18F.REF.12" data-bk-pop-others="FESP18F.REF.13 FESP18F.REF.14 FESP18F.REF.15">12-15</a>). Alkylation of the amide nitrogen in spiperone by [<sup>18</sup>F]fluorobromoethane in the presence of NaOH provided [<sup>18</sup>F]FESP in 35-40% radiochemical yield (5-8% overall radiochemical yield). [<sup>18</sup>F]Fluorobromoethane was easily prepared by the reaction of 1,2-bromoethane with potassium [<sup>18</sup>F]fluoride Kryptofix complex in 15-20% radiochemical yield. The radiochemical purity of [<sup>18</sup>F]FESP was found to be >99% by high-performance liquid chromatography (HPLC). The specific activity was 185-370 GBq/μmol (5-10 Ci/μmol) at the end of synthesis with a total synthesis time of 70 min.</p><p>A one-step, one-pot synthesis of [<sup>18</sup>F]FESP using nucleophilic fluorination of 3-(2'-bromoethyl)spiperone or 3-(2'-methylsulfonyloxyethyl)spiperone with K[<sup>18</sup>F]F/Kryptofix2.2.2 in acetonitrite in <60 min was performed (<a class="bk_pop" href="#FESP18F.REF.12">12</a>). This method provided a 99% chemical purity and a specific activity of 74-370 GBq/μmol (2-10 Ci/μmol) at the end of synthesis (EOS). The radiochemical yield was 30-40% (EOS).</p></div><div id="FESP18F.In_Vitro_Studies_Testing_in_Cell"><h2 id="_FESP18F_In_Vitro_Studies_Testing_in_Cell_"><i>In Vitro</i> Studies: Testing in Cells and Tissues</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=%223-N-%282-fluoroethyl%29spiperone%22%5BSubstance%20Name%5D%20AND%20in%20vitro" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>FESP was reported to have selective binding affinity to D<sub>2</sub> (striatum) and 5-HT<sub>2</sub> (frontal cortex) receptor sites in homogenates of rat brain membranes (<a class="bk_pop" href="#FESP18F.REF.8">8</a>). The <i>K</i><sub><i>i</i></sub> values for D<sub>2</sub> and 5-HT<sub>2</sub> were 0.44 n<span class="small-caps">m</span> and 0.57 n<span class="small-caps">m</span>, respectively. It has a <i>K</i><sub><i>i</i></sub> value of 23 n<span class="small-caps">m</span> for the α1-adrenergic receptor in rat forebrain membrane and negligible binding to other sites.</p></div><div id="FESP18F.Animal_Studies"><h2 id="_FESP18F_Animal_Studies_">Animal Studies</h2><div id="FESP18F.Rodents"><h3>Rodents</h3><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=%223-N-%282-fluoroethyl%29spiperone%22%5BSubstance%20Name%5D%20AND%20rodentia" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Biodistribution studies in rats showed a high uptake of radioactivity in the lung (1.80% injected dose (ID)/g), kidney (1.00% ID/g), spleen (0.97% ID/g), and liver (0.82% ID/g) at 15 min after injection of [<sup>18</sup>F]FESP (<a class="bk_pop" href="#FESP18F.REF.16">16</a>). The brain had a low uptake of 0.18% ID/g. Low radioactivity was observed in bone tissue, indicating little defluorination. [<sup>18</sup>F]FESP remained 90% intact in the brain striatum, 32% in the cerebellum, and 46% in the frontal cortex for up to 4 h after injection. In mice, [<sup>18</sup>F]FESP remained 90% intact in the brain striatum, and 62% in the cerebellum for up to 3.5 h after injection (<a class="bk_pop" href="#FESP18F.REF.17">17</a>). [<sup>18</sup>F]FESP was metabolized peripherally with only 11% intact [<sup>18</sup>F]FESP in rat plasma at 2 h after injection (<a class="bk_pop" href="#FESP18F.REF.16">16</a>).</p></div><div id="FESP18F.Other_NonPrimate_Mammals"><h3>Other Non-Primate Mammals</h3><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=%223-N-%282-fluoroethyl%29spiperone%22%5BSubstance%20Name%5D%20AND%20%28dog%20or%20pig%20or%20rabbit%20or%20sheep%29" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>No publication is currently available.</p></div><div id="FESP18F.NonHuman_Primates"><h3>Non-Human Primates</h3><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=%223-N-%282-fluoroethyl%29spiperone%22%5BSubstance%20Name%5D%20AND%20primate%20not%20human" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p> [<sup>18</sup>F]FESP PET studies in non-human primates have provided useful assessment of the D<sub>2</sub> and 5-HT<sub>2</sub> receptor in the brain (<a class="bk_pop" href="#FESP18F.REF.16" data-bk-pop-others="FESP18F.REF.17 FESP18F.REF.18 FESP18F.REF.19 FESP18F.REF.20 FESP18F.REF.21">16-21</a>). Coenen et al. (<a class="bk_pop" href="#FESP18F.REF.18">18</a>) showed a selective uptake in striatum (0.048% ID/cm<sup>3</sup>) over the frontal cortex (0.0088% ID/cm<sup>3</sup>) and in the cerebellum (0.0056% ID/cm<sup>3</sup>) in baboon brains at 4 h after injection. The striatum D<sub>2</sub> receptor sites in the striatum were saturable. The striatum [<sup>18</sup>F]FESP uptake was blocked by pretreatment with excess unlabeled FESP (0.5 mg/kg) and (+)-butaclamol (0.5 mg/kg), a D<sub>1</sub>/D<sub>2</sub> antagonist (<a class="bk_pop" href="#FESP18F.REF.22">22</a>). Ritanserin and ketanserin, 5-HT<sub>2</sub> antagonists, had no effect on [<sup>18</sup>F]FESP uptake in the striatum and blocked only 15-20% [<sup>18</sup>F]FESP uptake in the frontal cortex. [<sup>18</sup>F]FESP arterial plasma activity rapidly decreased to 25% at 1 h and 8% at 4 h after injection. D<sub>2</sub> receptor density (<i>B</i><sub>max</sub>) was estimated by two PET studies to be 25.9 ± 12.7 pmol/g (<a class="bk_pop" href="#FESP18F.REF.19">19</a>) and 37.5 ± 11.5 pmol/g (<a class="bk_pop" href="#FESP18F.REF.21">21</a>). Using serial PET scans, 5-HT<sub>2</sub> receptor density was estimated to be 35.6 ± 10.9 pmol/g in the baboon frontal cortex (<a class="bk_pop" href="#FESP18F.REF.20">20</a>).</p></div></div><div id="FESP18F.Human_Studies"><h2 id="_FESP18F_Human_Studies_">Human Studies</h2><p>[[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=%223-N-%282-fluoroethyl%29spiperone%22%5BSubstance%20Name%5D%20AND%20humans" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Human dosimetry was estimated based on human dynamic PET scans after injection of 37 MBq (1 mCi) [<sup>18</sup>F]FESP (<a class="bk_pop" href="#FESP18F.REF.23">23</a>). The gallbladder received the highest dose (0.207 mGy/MBq or 797 mrad/mCi). Other organs that received high doses were the urinary bladder (0.083 mGy/MBq or 308 mrad/mCi) and liver (0.065 mGy/MBq or 110 mrad/mCi). The total body dose was 0.0119 mGy/MBq (44 mrad/mCi).</p><p> [<sup>18</sup>F]FESP PET studies of D<sub>2</sub> receptor distribution in human brain were reported, showing a localization of radioactivity in the striatum (<a class="bk_pop" href="#FESP18F.REF.16" data-bk-pop-others="FESP18F.REF.24 FESP18F.REF.25">16, 24, 25</a>). Only about 1% of [<sup>18</sup>F]PESP entered the brain. [<sup>18</sup>F]FESP was metabolized peripherally with 54% intact [<sup>18</sup>F]FESP in arterial plasma at 2 h after injection (<a class="bk_pop" href="#FESP18F.REF.16">16</a>). Striatal-to-cerebellum ratio and kinetic constants are commonly used as analytical parameters in [<sup>18</sup>F]FESP PET studies. Wienhard et al. (<a class="bk_pop" href="#FESP18F.REF.25">25</a>) reported on [<sup>18</sup>F]FESP PET studies in 30 patients with various disorders related to the dopaminergic system and in 6 normal subjects. PET brain scans of normal subjects showed that the highest uptake was in the caudate and pituitary, followed by the cortex and cerebellum at 3 h after injection of 185 MBq (5 mCi) [<sup>18</sup>F]FESP. PET scans of patients showed decreases in the number of available D<sub>2</sub> receptors in the striatum and striatum-to-cerebellum ratio. Patients with brain damage also showed both low [<sup>18</sup>F]FDG and [<sup>18</sup>F]FESP uptake in the striatum.</p><p>5-HT<sub>2</sub> receptor distribution in human brain were studied by [<sup>18</sup>F]FESP PET in 20 healthy volunteers and 34 patients with unipolar depression (<a class="bk_pop" href="#FESP18F.REF.26">26</a>) There was a significant reduction of binding capacity in 19 non-drug-treated patients as compared with healthy controls in the cortical regions but not in the striatum. In paroxetine-treated patients (<i>n</i> = 15), there was no significant difference between the drug-treated patients and healthy volunteers. Paroxetine is a specific serotonin reuptake inhibitor. Paroxetine treatment led to remission in these patients. Chronic treatment with fluvoxamine (<a class="bk_pop" href="#FESP18F.REF.27">27</a>), another specific serotonin reuptake inhibitor, significantly increased the <i>in vivo</i> binding of [<sup>18</sup>F]FESP in the frontal and occipital cortex but not in the striatum of drug-naïve, unipolar, depressed patients (<i>n</i> = 9).</p><p> [<sup>18</sup>F]FESP PET is useful for objective monitoring of D<sub>2</sub> and 5-HT<sub>2</sub> receptor sites in patients with serotonergic and dopaminergic disorders. It revealed stage-related changes in depression and dopaminergic disorders. [<sup>18</sup>F]FESP has also demonstrated its usefulness as a PET tracer in the imaging of non-functioning pituitary adenomas from meningiomas and craniopharyngiomas (<a class="bk_pop" href="#FESP18F.REF.28">28</a>).</p></div><div id="FESP18F.References"><h2 id="_FESP18F_References_">References</h2><dl class="temp-labeled-list"><dt>1.</dt><dd><div class="bk_ref" id="FESP18F.REF.1">Carbon M., Ghilardi M.F., Feigin A., Fukuda M., Silvestri G., Mentis M.J., Ghez C., Moeller J.R., Eidelberg D.
|
||
<em>Learning networks in health and Parkinson's disease: reproducibility and treatment effects.</em>
|
||
<span><span class="ref-journal">Hum Brain Mapp. </span>2003;<span class="ref-vol">19</span>(3):197–211.</span> [<a href="/pmc/articles/PMC6871830/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC6871830</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/12811735" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 12811735</span></a>]</div></dd><dt>2.</dt><dd><div class="bk_ref" id="FESP18F.REF.2">Chesselet M.F., Delfs J.M.
|
||
<em>Basal ganglia and movement disorders: an update.</em>
|
||
<span><span class="ref-journal">Trends Neurosci. </span>1996;<span class="ref-vol">19</span>(10):417–22.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/8888518" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 8888518</span></a>]</div></dd><dt>3.</dt><dd><div class="bk_ref" id="FESP18F.REF.3">Stoof J.C., Kebabian J.W.
|
||
<em>Two dopamine receptors: biochemistry, physiology and pharmacology.</em>
|
||
<span><span class="ref-journal">Life Sci. </span>1984;<span class="ref-vol">35</span>(23):2281–96.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/6390056" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 6390056</span></a>]</div></dd><dt>4.</dt><dd><div class="bk_ref" id="FESP18F.REF.4">Seeman P., Bzowej N.H., Guan H.C., Bergeron C., Reynolds G.P., Bird E.D., Riederer P., Jellinger K., Tourtellotte W.W.
|
||
<em>Human brain D1 and D2 dopamine receptors in schizophrenia, Alzheimer's, Parkinson's, and Huntington's diseases.</em>
|
||
<span><span class="ref-journal">Neuropsychopharmacology. </span>1987;<span class="ref-vol">1</span>(1):5–15.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/2908095" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 2908095</span></a>]</div></dd><dt>5.</dt><dd><div class="bk_ref" id="FESP18F.REF.5">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):151–62.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/9693387" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 9693387</span></a>]</div></dd><dt>6.</dt><dd><div class="bk_ref" id="FESP18F.REF.6">Abi-Dargham A., Laruelle M., Aghajanian G.K., Charney D., Krystal J.
|
||
<em>The role of serotonin in the pathophysiology and treatment of schizophrenia.</em>
|
||
<span><span class="ref-journal">J Neuropsychiatry Clin Neurosci. </span>1997;<span class="ref-vol">9</span>(1):1–17.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/9017523" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 9017523</span></a>]</div></dd><dt>7.</dt><dd><div class="bk_ref" id="FESP18F.REF.7">Charney D.S.
|
||
<em>Monoamine dysfunction and the pathophysiology and treatment of depression.</em>
|
||
<span><span class="ref-journal">J Clin Psychiatry. </span>1998;<span class="ref-vol">59</span> Suppl 14:11–4.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/9818625" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 9818625</span></a>]</div></dd><dt>8.</dt><dd><div class="bk_ref" id="FESP18F.REF.8">Goffinet A.M., Leysen J., Labar D.
|
||
<em>In vitro pharmacological profile of 3-N-(2-fluoroethyl)spiperone.</em>
|
||
<span><span class="ref-journal">J Cereb Blood Flow Metab. </span>1990;<span class="ref-vol">10</span>(1):140–2.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/2137131" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 2137131</span></a>]</div></dd><dt>9.</dt><dd><div class="bk_ref" id="FESP18F.REF.9">MacLaren D.C., Gambhir S.S., Satyamurthy N., Barrio J.R., Sharfstein S., Toyokuni T., Wu L., Berk A.J., Cherry S.R., Phelps M.E., Herschman H.R.
|
||
<em>Repetitive, non-invasive imaging of the dopamine D2 receptor as a reporter gene in living animals.</em>
|
||
<span><span class="ref-journal">Gene Ther. </span>1999;<span class="ref-vol">6</span>(5):785–91.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/10505102" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 10505102</span></a>]</div></dd><dt>10.</dt><dd><div class="bk_ref" id="FESP18F.REF.10">Yaghoubi S.S., Wu L., Liang Q., Toyokuni T., Barrio J.R., Namavari M., Satyamurthy N., Phelps M.E., Herschman H.R., Gambhir S.S.
|
||
<em>Direct correlation between positron emission tomographic images of two reporter genes delivered by two distinct adenoviral vectors.</em>
|
||
<span><span class="ref-journal">Gene Ther. </span>2001;<span class="ref-vol">8</span>(14):1072–80.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/11526454" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 11526454</span></a>]</div></dd><dt>11.</dt><dd><div class="bk_ref" id="FESP18F.REF.11">Chen I.Y., Wu J.C., Min J.J., Sundaresan G., Lewis X., Liang Q., Herschman H.R., Gambhir S.S.
|
||
<em>Micro-positron emission tomography imaging of cardiac gene expression in rats using bicistronic adenoviral vector-mediated gene delivery.</em>
|
||
<span><span class="ref-journal">Circulation. </span>2004;<span class="ref-vol">109</span>(11):1415–20.</span> [<a href="/pmc/articles/PMC4154818/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC4154818</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/15007006" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 15007006</span></a>]</div></dd><dt>12.</dt><dd><div class="bk_ref" id="FESP18F.REF.12">Satyamurthy N., Bida G.T., Barrio J.R., Luxen A., Mazziotta J.C., Huang S.C., Phelps M.E.
|
||
<em>No-carrier-added 3-(2'-[18F]fluoroethyl)spiperone, a new dopamine receptor-binding tracer for positron emission tomography.</em>
|
||
<span><span class="ref-journal">Int J Rad Appl Instrum B. </span>1986;<span class="ref-vol">13</span>(6):617–24.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/3494003" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 3494003</span></a>]</div></dd><dt>13.</dt><dd><div class="bk_ref" id="FESP18F.REF.13">Satyamurthy N., Barrio J.R., Bida G.T., Huang S.C., Mazziotta J.C., Phelps M.E.
|
||
<em>3-(2'-[18F]fluoroethyl)spiperone, a potent dopamine antagonist: synthesis, structural analysis and in-vivo utilization in humans.</em>
|
||
<span><span class="ref-journal">Int J Rad Appl Instrum [A] </span>1990;<span class="ref-vol">41</span>(2):113–29.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/2158942" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 2158942</span></a>]</div></dd><dt>14.</dt><dd><div class="bk_ref" id="FESP18F.REF.14">Chi D.Y., Kilbourn M.R., Katzenellenbogen J.A., Brodack J.W., Welch M.J.
|
||
<em>Synthesis of no-carrier-added N-([18F]fluoroalkyl)spiperone derivatives.</em>
|
||
<span><span class="ref-journal">Int J Rad Appl Instrum [A] </span>1986;<span class="ref-vol">37</span>(12):1173–80.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/3028983" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 3028983</span></a>]</div></dd><dt>15.</dt><dd><div class="bk_ref" id="FESP18F.REF.15">Kiesewetter D.O., Eckelman W.C., Cohen R.M., Finn R.D., Larson S.M.
|
||
<em>Syntheses and D2 receptor affinities of derivatives of spiperone containing aliphatic halogens.</em>
|
||
<span><span class="ref-journal">Int J Rad Appl Instrum [A] </span>1986;<span class="ref-vol">37</span>(12):1181–8.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/3028984" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 3028984</span></a>]</div></dd><dt>16.</dt><dd><div class="bk_ref" id="FESP18F.REF.16">Barrio J.R., Satyamurthy N., Huang S.C., Keen R.E., Nissenson C.H., Hoffman J.M., Ackermann R.F., Bahn M.M., Mazziotta J.C., Phelps M.E.
|
||
<em>3-(2'-[18F]fluoroethyl)spiperone: in vivo biochemical and kinetic characterization in rodents, nonhuman primates, and humans.</em>
|
||
<span><span class="ref-journal">J Cereb Blood Flow Metab. </span>1989;<span class="ref-vol">9</span>(6):830–9.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/2531146" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 2531146</span></a>]</div></dd><dt>17.</dt><dd><div class="bk_ref" id="FESP18F.REF.17">Coenen H.H., Laufer P., Stocklin G., Wienhard K., Pawlik G., Bocher-Schwarz H.G., Heiss W.D.
|
||
<em>3-N-(2-[18F]-fluoroethyl)-spiperone: a novel ligand for cerebral dopamine receptor studies with pet.</em>
|
||
<span><span class="ref-journal">Life Sci. </span>1987;<span class="ref-vol">40</span>(1):81–8.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/2948091" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 2948091</span></a>]</div></dd><dt>18.</dt><dd><div class="bk_ref" id="FESP18F.REF.18">Coenen H.H., Wienhard K., Stocklin G., Laufer P., Hebold I., Pawlik G., Heiss W.D.
|
||
<em>PET measurement of D2 and S2 receptor binding of 3-N-[(2'-18F]fluoroethyl)spiperone in baboon brain.</em>
|
||
<span><span class="ref-journal">Eur J Nucl Med. </span>1988;<span class="ref-vol">14</span>(2):80–7.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/2968911" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 2968911</span></a>]</div></dd><dt>19.</dt><dd><div class="bk_ref" id="FESP18F.REF.19">Huang S.C., Bahn M.M., Barrio J.R., Hoffman J.M., Satyamurthy N., Hawkins R.A., Mazziotta J.C., Phelps M.E.
|
||
<em>A double-injection technique for in vivo measurement of dopamine D2-receptor density in monkeys with 3-(2'-[18F]fluoroethyl)spiperone and dynamic positron emission tomography.</em>
|
||
<span><span class="ref-journal">J Cereb Blood Flow Metab. </span>1989;<span class="ref-vol">9</span>(6):850–8.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/2531148" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 2531148</span></a>]</div></dd><dt>20.</dt><dd><div class="bk_ref" id="FESP18F.REF.20">Jovkar S., Wienhard K., Coenen H.H., Pawlik G., Heiss W.D.
|
||
<em>Quantification of baboon cortical S2 serotonin receptors in vivo with 3-N-(2'-F18)fluoroethylspiperone and positron emission tomography.</em>
|
||
<span><span class="ref-journal">Eur J Nucl Med. </span>1991;<span class="ref-vol">18</span>(3):158–63.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/2040338" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 2040338</span></a>]</div></dd><dt>21.</dt><dd><div class="bk_ref" id="FESP18F.REF.21">Jovkar S., Wienhard K., Pawlik G., Coenen H.H.
|
||
<em>The quantitative analysis of D2-dopamine receptors in baboon striatum in vivo with 3-N-[2'-18F]fluoroethylspiperone using positron emission tomography.</em>
|
||
<span><span class="ref-journal">J Cereb Blood Flow Metab. </span>1990;<span class="ref-vol">10</span>(5):720–6.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/2384543" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 2384543</span></a>]</div></dd><dt>22.</dt><dd><div class="bk_ref" id="FESP18F.REF.22">Schetz J.A., Kim O.J., Sibley D.R.
|
||
<em>Pharmacological characterization of mammalian D1 and D2 dopamine receptors expressed in Drosophila Schneider-2 cells.</em>
|
||
<span><span class="ref-journal">J Recept Signal Transduct Res. </span>2003;<span class="ref-vol">23</span>(1):99–109.</span> [<a href="/pmc/articles/PMC3108030/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC3108030</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/12680592" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 12680592</span></a>]</div></dd><dt>23.</dt><dd><div class="bk_ref" id="FESP18F.REF.23">Herzog H., Coenen H.H., Kuwert T., Langen K.J., Feinendegen L.E.
|
||
<em>Quantification of the whole-body distribution of PET radiopharmaceuticals, applied to 3-N-([18F]fluoroethyl)spiperone.</em>
|
||
<span><span class="ref-journal">Eur J Nucl Med. </span>1990;<span class="ref-vol">16</span>(2):77–83.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/2311622" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 2311622</span></a>]</div></dd><dt>24.</dt><dd><div class="bk_ref" id="FESP18F.REF.24">Bahn M.M., Huang S.C., Hawkins R.A., Satyamurthy N., Hoffman J.M., Barrio J.R., Mazziotta J.C., Phelps M.E.
|
||
<em>Models for in vivo kinetic interactions of dopamine D2-neuroreceptors and 3-(2'-[18F]fluoroethyl)spiperone examined with positron emission tomography.</em>
|
||
<span><span class="ref-journal">J Cereb Blood Flow Metab. </span>1989;<span class="ref-vol">9</span>(6):840–9.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/2531147" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 2531147</span></a>]</div></dd><dt>25.</dt><dd><div class="bk_ref" id="FESP18F.REF.25">Wienhard K., Coenen H.H., Pawlik G., Rudolf J., Laufer P., Jovkar S., Stocklin G., Heiss W.D.
|
||
<em>PET studies of dopamine receptor distribution using [18F]fluoroethylspiperone: findings in disorders related to the dopaminergic system.</em>
|
||
<span><span class="ref-journal">J Neural Transm Gen Sect. </span>1990;<span class="ref-vol">81</span>(3):195–213.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/2144427" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 2144427</span></a>]</div></dd><dt>26.</dt><dd><div class="bk_ref" id="FESP18F.REF.26">Messa C., Colombo C., Moresco R.M., Gobbo C., Galli L., Lucignani G., Gilardi M.C., Rizzo G., Smeraldi E., Zanardi R., Artigas F., Fazio F.
|
||
<em>5-HT(2A) receptor binding is reduced in drug-naive and unchanged in SSRI-responder depressed patients compared to healthy controls: a PET study.</em>
|
||
<span><span class="ref-journal">Psychopharmacology (Berl). </span>2003;<span class="ref-vol">167</span>(1):72–8.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/12632246" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 12632246</span></a>]</div></dd><dt>27.</dt><dd><div class="bk_ref" id="FESP18F.REF.27">Moresco R.M., Colombo C., Fazio F., Bonfanti A., Lucignani G., Messa C., Gobbo C., Galli L., Del Sole A., Lucca A., Smeraldi E.
|
||
<em>Effects of fluvoxamine treatment on the in vivo binding of [F-18]FESP in drug naive depressed patients: a PET study.</em>
|
||
<span><span class="ref-journal">Neuroimage. </span>2000;<span class="ref-vol">12</span>(4):452–65.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/10988039" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 10988039</span></a>]</div></dd><dt>28.</dt><dd><div class="bk_ref" id="FESP18F.REF.28">Lucignani G., Losa M., Moresco R.M., Del Sole A., Matarrese M., Bettinardi V., Mortini P., Giovanelli M., Fazio F.
|
||
<em>Differentiation of clinically non-functioning pituitary adenomas from meningiomas and craniopharyngiomas by positron emission tomography with [18F]fluoro-ethyl-spiperone.</em>
|
||
<span><span class="ref-journal">Eur J Nucl Med. </span>1997;<span class="ref-vol">24</span>(9):1149–55.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/9283109" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 9283109</span></a>]</div></dd></dl></div><div id="bk_toc_contnr"></div></div></div>
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<div class="post-content"><div><div class="half_rhythm"><a href="/books/about/copyright/">Copyright Notice</a></div><div class="small"><span class="label">Bookshelf ID: NBK23473</span><span class="label">PMID: <a href="https://pubmed.ncbi.nlm.nih.gov/20641672" title="PubMed record of this page" ref="pagearea=meta&targetsite=entrez&targetcat=link&targettype=pubmed">20641672</a></span></div><div style="margin-top:2em" class="bk_noprnt"><a class="bk_cntns" href="/books/n/micad/">Contents</a><div class="pagination bk_noprnt"><a class="active page_link prev" href="/books/n/micad/F18-6b/" title="Previous page in this title">< Prev</a><a class="active page_link next" href="/books/n/micad/FEatCIT18F/" title="Next page in this title">Next ></a></div></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/NBK23473/?report=reader">PubReader</a></li><li><a href="/books/NBK23473/?report=printable">Print View</a></li><li><a data-jig="ncbidialog" href="#_ncbi_dlg_citbx_NBK23473" data-jigconfig="width:400,modal:true">Cite this Page</a><div id="_ncbi_dlg_citbx_NBK23473" style="display:none" title="Cite this Page"><div class="bk_tt">Leung K. 3-N-(2-[18F]Fluoroethyl)spiperone. 2005 Oct 7 [Updated 2012 Jan 18]. 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/NBK23473/pdf/Bookshelf_NBK23473.pdf">PDF version of this page</a> (164K)</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="#FESP18F.Background" ref="log$=inpage&link_id=inpage">Background</a></li><li><a href="#FESP18F.Synthesis" ref="log$=inpage&link_id=inpage">Synthesis</a></li><li><a href="#FESP18F.In_Vitro_Studies_Testing_in_Cell" ref="log$=inpage&link_id=inpage"><i>In Vitro</i> Studies: Testing in Cells and Tissues</a></li><li><a href="#FESP18F.Animal_Studies" ref="log$=inpage&link_id=inpage">Animal Studies</a></li><li><a href="#FESP18F.Human_Studies" ref="log$=inpage&link_id=inpage">Human Studies</a></li><li><a href="#FESP18F.References" ref="log$=inpage&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 "Magnetic resonance imaging" 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=""Hyperpolarized 13C"">Hyperpolarized 13C</option><option value=""Iron oxide"">Iron oxide</option><option value=""Nitroxide radicals"">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="("Iron oxide" AND (64Cu OR 124I OR 111In))">Iron oxide and
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europium</option><option value="(166Ho OR 67Ga OR 68Ga OR 123I OR 124I OR 125I)">Radionuclides</option></optgroup><optgroup label="Optical agents"><option value="("Fluorescent dyes" OR protein)">Fluorescent dyes or proteins</option><option value=""Luminescent agents"">Luminescent agents</option><option value="(Metals OR Metal OR Gold OR Au)">Metals (Au)</option><option value="Nanotubes">Nanotubes</option><option value=""Quantum dots"">Quantum dots</option></optgroup><optgroup label="PET radionuclides"><option value="("Arsenic 74" OR 74As)">Arsenic-74</option><option value="("Bromine 76" OR 76Br)">Bromine-76</option><option value="("Carbon 11" OR 11C)">Carbon-11</option><option value="(Copper-60 OR Copper-61 OR Copper-62 OR Copper-64 OR 60Cu OR 61Cu OR 62Cu OR 64Cu)">Copper-60, 61, 62, 64</option><option value="("Fluorine 18" OR 18F)">Fluorine-18</option><option value="(Gallium-68 OR 68Ga)">Gallium-68</option><option value="("Iodine 124" OR 124I)">Iodine-124</option><option value="("Nitrogen 13" OR 13N)">Nitrogen-13</option><option value="("Yttrium 86" OR 86Y)">Yttrium-86</option><option value="("Zirconium 89" OR 89Zr)">Zirconium-89</option></optgroup><optgroup label="Photoacoustic agents"><option value="(Gold OR Au)">Gold</option><option value="("Indocyanine green" OR ICG)">Indocyanine green</option></optgroup><optgroup label="SPECT radionuclides"><option value="(Gallium-67 OR 67Ga)">Gallium-67</option><option value="("Indium 111" OR 111In)">Indium-111</option><option value="("Iodine 123" OR "Iodine 125" OR "Iodine 131" OR 123I OR 125I OR 131I)">Iodine-123, 125, 131</option><option value="("Lutetium 177" OR 177Lu)">Lutetium-177</option><option value="(Rhenium OR 186Re OR 188Re)">Rhenium</option><option value="("Technetium 99m" OR 99mTc)">Technetium-99m</option><option value="("Tellurium 125m" 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 "amino acid" OR "folic acid" OR "cage molecule" OR carbohydrate OR copolymers OR polymer OR "small molecule" OR macromolecule OR triiodobenzoate OR estradiol OR glycosaminoglycan)">Compounds</option><option value="ligand">Ligands</option><option value="(lipid OR liposome OR liposomes">Lipids</option><option value="metal">Metal</option><option value="(nanoparticle OR nanoparticles OR nanotubes OR "iron oxide")">Nanoparticles</option><option value="(siRNA OR "nucleic acid" OR oligonucleotide)">Nucleic acids</option><option value="peptide">Peptides</option><option value="polyeptide">Polyeptides</option><option value="(protein OR albumin OR chemokin OR immunoprotein OR luciferase OR albumin)">Proteins</option><option value="(virus OR adenovirus)">Viruses</option></select></div></div><div class="clearfix"><label for="target">Target Category:</label><div class="right"><select name="target" id="target" style="width:200px"><option value="" selected="selected">Any</option><option value="acceptor">Acceptors</option><option value=""adhesion molecule"">Adhesion molecules</option><option value="(antigen OR antibody-antigen)">Antigens</option><option value="(enzyme OR enzymes OR enzyme-substrate)">Enzymes</option><option value="(lipids OR lipophilic cation)">Lipids</option><option value="(receptor OR receptors OR receptor-ligand OR receptor-antibody OR antibody-receptor)">Receptors</option><option value="transporter">Transporters</option><option value="non-targeted">Non-targeted</option><option value=""nucleic acid"">Nucleic acids</option><option value="(non-targeted OR "unknown binding site")">Others</option></select></div></div><div><input id="__micad_btn_1" type="radio" name="stage" value="vitro" /><label for="__micad_btn_1"><i>In vitro</i></label><input id="__micad_btn_2" type="radio" name="stage" value="rodents" /><label for="__micad_btn_2">Rodents</label><input id="__micad_btn_3" type="radio" name="stage" value="mammals" /><label for="__micad_btn_3">Non-primate non-rodent mammals</label><br /><input id="__micad_btn_4" type="radio" name="stage" value="primates" /><label for="__micad_btn_4">Non-human primates</label><input id="__micad_btn_5" type="radio" name="stage" value="humans" /><label for="__micad_btn_5">Humans</label><input id="__micad_btn_6" type="radio" name="stage" value="any" checked="checked" /><label for="__micad_btn_6">Any</label></div></form><form xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" name="frmGo" method="get" action="javascript:alert('frmGo:_@action_was_not_set')" id="frmGo"><input name="term" value="." type="hidden" /></form></div></div><div class="portlet"><div class="portlet_head"><div class="portlet_title"><h3><span>Related information</span></h3></div><a name="Shutter" sid="1" href="#" class="portlet_shutter" title="Show/hide content" remembercollapsed="true" pgsec_name="discovery_db_links" id="Shutter"></a></div><div class="portlet_content"><ul><li class="brieflinkpopper"><a class="brieflinkpopperctrl" href="/books/?Db=pmc&DbFrom=books&Cmd=Link&LinkName=books_pmc_refs&IdsFromResult=1512816" ref="log$=recordlinks">PMC</a><div class="brieflinkpop offscreen_noflow">PubMed Central citations</div></li><li class="brieflinkpopper"><a class="brieflinkpopperctrl" href="/books/?Db=pcsubstance&DbFrom=books&Cmd=Link&LinkName=books_pcsubstance&IdsFromResult=1512816" ref="log$=recordlinks">PubChem Substance</a><div class="brieflinkpop offscreen_noflow">Related PubChem Substances</div></li><li class="brieflinkpopper"><a class="brieflinkpopperctrl" href="/books/?Db=pubmed&DbFrom=books&Cmd=Link&LinkName=books_pubmed_refs&IdsFromResult=1512816" ref="log$=recordlinks">PubMed</a><div class="brieflinkpop offscreen_noflow">Links to PubMed</div></li></ul></div></div><div class="portlet"><div class="portlet_head"><div class="portlet_title"><h3><span>Similar articles in PubMed</span></h3></div><a name="Shutter" sid="1" href="#" class="portlet_shutter" title="Show/hide content" remembercollapsed="true" pgsec_name="PBooksDiscovery_RA" id="Shutter"></a></div><div class="portlet_content"><ul><li class="brieflinkpopper two_line"><a class="brieflinkpopperctrl" href="/pubmed/20641810" ref="ordinalpos=1&linkpos=1&log$=relatedreviews&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-N-[(11)C]Methylspiperone.</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-N-[(11)C]Methylspiperone.<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/21994970" ref="ordinalpos=1&linkpos=2&log$=relatedreviews&logdbfrom=pubmed"><span xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="invert">Review</span> N-(4-(4-(2-(2-[(18)F]Fluoroethoxy)phenyl)piperazine-1-yl)butyl)-4-(3-thienyl)benzamide.</a><span class="source">[Molecular Imaging and Contrast...]</span><div class="brieflinkpop offscreen_noflow"><span xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="invert">Review</span> N-(4-(4-(2-(2-[(18)F]Fluoroethoxy)phenyl)piperazine-1-yl)butyl)-4-(3-thienyl)benzamide.<div class="brieflinkpopdesc"><em xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="author">Leung K. </em><em xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="cit">Molecular Imaging and Contrast Agent Database (MICAD). 2004</em></div></div></li><li class="brieflinkpopper two_line"><a class="brieflinkpopperctrl" href="/pubmed/21473029" ref="ordinalpos=1&linkpos=3&log$=relatedreviews&logdbfrom=pubmed"><span xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="invert">Review</span> 2-(4-Bromo-2,5-dimethoxyphenyl)-N-(2-[(11)C]methoxybenzyl)ethanamine.</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> 2-(4-Bromo-2,5-dimethoxyphenyl)-N-(2-[(11)C]methoxybenzyl)ethanamine.<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/20641608" ref="ordinalpos=1&linkpos=4&log$=relatedreviews&logdbfrom=pubmed"><span xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="invert">Review</span> [(11)C](+)-4-N-Propyl-,3,4a,5,6,10b-hexahydro-2H-naphth[1,2-b][1,4]-oxazin-9-ol.</a><span class="source">[Molecular Imaging and Contrast...]</span><div class="brieflinkpop offscreen_noflow"><span xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="invert">Review</span> [(11)C](+)-4-N-Propyl-,3,4a,5,6,10b-hexahydro-2H-naphth[1,2-b][1,4]-oxazin-9-ol.<div class="brieflinkpopdesc"><em xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="author">Leung K. </em><em xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="cit">Molecular Imaging and Contrast Agent Database (MICAD). 2004</em></div></div></li><li class="brieflinkpopper two_line"><a class="brieflinkpopperctrl" href="/pubmed/20641295" ref="ordinalpos=1&linkpos=5&log$=relatedreviews&logdbfrom=pubmed"><span xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="invert">Review</span> (R,S)-2-(N-Propyl-N-5'-[(18)F]fluoropentyl)amino-5-hydroxytetralin.</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> (R,S)-2-(N-Propyl-N-5'-[(18)F]fluoropentyl)amino-5-hydroxytetralin.<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></ul><a class="seemore" href="/sites/entrez?db=pubmed&cmd=link&linkname=pubmed_pubmed_reviews&uid=20641672" ref="ordinalpos=1&log$=relatedreviews_seeall&logdbfrom=pubmed">See reviews...</a><a class="seemore" href="/sites/entrez?db=pubmed&cmd=link&linkname=pubmed_pubmed&uid=20641672" ref="ordinalpos=1&log$=relatedarticles_seeall&logdbfrom=pubmed">See all...</a></div></div><div class="portlet"><div class="portlet_head"><div class="portlet_title"><h3><span>Recent Activity</span></h3></div><a name="Shutter" sid="1" href="#" class="portlet_shutter" title="Show/hide content" remembercollapsed="true" pgsec_name="recent_activity" id="Shutter"></a></div><div class="portlet_content"><div xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" id="HTDisplay" class=""><div class="action"><a 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