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<script type="text/javascript" src="/corehtml/pmc/jatsreader/ptpmc_3.22/js/jr.boots.min.js"> </script><title>3-N-(2-[18F]Fluoroethyl)spiperone - Molecular Imaging and Contrast Agent Database (MICAD) - NCBI Bookshelf</title>
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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="_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="contribs">Leung K.</p><p class="fm-aai"><a href="#_NBK23473_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="figFESP18FTncchemicalname3n218ffluoroet"><a href="/books/NBK23473/table/FESP18F.T.nc_chemical_name3n218ffluoroet/?report=objectonly" target="object" title="Table" class="img_link icnblk_img" rid-ob="figobFESP18FTncchemicalname3n218ffluoroet"><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="FESP18F.T.nc_chemical_name3n218ffluoroet"><a href="/books/NBK23473/table/FESP18F.T.nc_chemical_name3n218ffluoroet/?report=objectonly" target="object" rid-ob="figobFESP18FTncchemicalname3n218ffluoroet">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="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="bibr" href="#FESP18F.REF.1" rid="FESP18F.REF.1 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="bibr" href="#FESP18F.REF.3" rid="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="bibr" href="#FESP18F.REF.4" rid="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="bibr" href="#FESP18F.REF.5" rid="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="bibr" href="#FESP18F.REF.6" rid="FESP18F.REF.6 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="bibr" href="#FESP18F.REF.8" rid="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="bibr" href="#FESP18F.REF.9" rid="FESP18F.REF.9 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="bibr" href="#FESP18F.REF.12" rid="FESP18F.REF.12 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="bibr" href="#FESP18F.REF.12" rid="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="bibr" href="#FESP18F.REF.8" rid="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="bibr" href="#FESP18F.REF.16" rid="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="bibr" href="#FESP18F.REF.17" rid="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="bibr" href="#FESP18F.REF.16" rid="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="bibr" href="#FESP18F.REF.16" rid="FESP18F.REF.16 FESP18F.REF.17 FESP18F.REF.18 FESP18F.REF.19 FESP18F.REF.20 FESP18F.REF.21">16-21</a>). Coenen et al. (<a class="bibr" href="#FESP18F.REF.18" rid="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="bibr" href="#FESP18F.REF.22" rid="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="bibr" href="#FESP18F.REF.19" rid="FESP18F.REF.19">19</a>) and 37.5 ± 11.5 pmol/g (<a class="bibr" href="#FESP18F.REF.21" rid="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="bibr" href="#FESP18F.REF.20" rid="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="bibr" href="#FESP18F.REF.23" rid="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="bibr" href="#FESP18F.REF.16" rid="FESP18F.REF.16 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="bibr" href="#FESP18F.REF.16" rid="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="bibr" href="#FESP18F.REF.25" rid="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="bibr" href="#FESP18F.REF.26" rid="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="bibr" href="#FESP18F.REF.27" rid="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="bibr" href="#FESP18F.REF.28" rid="FESP18F.REF.28">28</a>).</p></div><div id="FESP18F.References"><h2 id="_FESP18F_References_">References</h2><dl class="temp-labeled-list"><dl class="bkr_refwrap"><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.
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<em>Learning networks in health and Parkinson's disease: reproducibility and treatment effects.</em>
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<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></dl><dl class="bkr_refwrap"><dt>2.</dt><dd><div class="bk_ref" id="FESP18F.REF.2">Chesselet M.F., Delfs J.M.
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<em>Basal ganglia and movement disorders: an update.</em>
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<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></dl><dl class="bkr_refwrap"><dt>3.</dt><dd><div class="bk_ref" id="FESP18F.REF.3">Stoof J.C., Kebabian J.W.
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<em>Two dopamine receptors: biochemistry, physiology and pharmacology.</em>
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<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></dl><dl class="bkr_refwrap"><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.
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<em>Human brain D1 and D2 dopamine receptors in schizophrenia, Alzheimer's, Parkinson's, and Huntington's diseases.</em>
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<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></dl><dl class="bkr_refwrap"><dt>5.</dt><dd><div class="bk_ref" id="FESP18F.REF.5">Lucki I.
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<em>The spectrum of behaviors influenced by serotonin.</em>
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<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></dl><dl class="bkr_refwrap"><dt>6.</dt><dd><div class="bk_ref" id="FESP18F.REF.6">Abi-Dargham A., Laruelle M., Aghajanian G.K., Charney D., Krystal J.
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<em>The role of serotonin in the pathophysiology and treatment of schizophrenia.</em>
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<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></dl><dl class="bkr_refwrap"><dt>7.</dt><dd><div class="bk_ref" id="FESP18F.REF.7">Charney D.S.
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<em>Monoamine dysfunction and the pathophysiology and treatment of depression.</em>
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<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></dl><dl class="bkr_refwrap"><dt>8.</dt><dd><div class="bk_ref" id="FESP18F.REF.8">Goffinet A.M., Leysen J., Labar D.
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<em>In vitro pharmacological profile of 3-N-(2-fluoroethyl)spiperone.</em>
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|
<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></dl><dl class="bkr_refwrap"><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.
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<em>Repetitive, non-invasive imaging of the dopamine D2 receptor as a reporter gene in living animals.</em>
|
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<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></dl><dl class="bkr_refwrap"><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.
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<em>Direct correlation between positron emission tomographic images of two reporter genes delivered by two distinct adenoviral vectors.</em>
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<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></dl><dl class="bkr_refwrap"><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.
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<em>Micro-positron emission tomography imaging of cardiac gene expression in rats using bicistronic adenoviral vector-mediated gene delivery.</em>
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<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></dl><dl class="bkr_refwrap"><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.
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<em>No-carrier-added 3-(2'-[18F]fluoroethyl)spiperone, a new dopamine receptor-binding tracer for positron emission tomography.</em>
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<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></dl><dl class="bkr_refwrap"><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.
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<em>3-(2'-[18F]fluoroethyl)spiperone, a potent dopamine antagonist: synthesis, structural analysis and in-vivo utilization in humans.</em>
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<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></dl><dl class="bkr_refwrap"><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.
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<em>Synthesis of no-carrier-added N-([18F]fluoroalkyl)spiperone derivatives.</em>
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<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></dl><dl class="bkr_refwrap"><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.
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<em>Syntheses and D2 receptor affinities of derivatives of spiperone containing aliphatic halogens.</em>
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<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></dl><dl class="bkr_refwrap"><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.
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<em>3-(2'-[18F]fluoroethyl)spiperone: in vivo biochemical and kinetic characterization in rodents, nonhuman primates, and humans.</em>
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<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></dl><dl class="bkr_refwrap"><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.
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<em>3-N-(2-[18F]-fluoroethyl)-spiperone: a novel ligand for cerebral dopamine receptor studies with pet.</em>
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<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></dl><dl class="bkr_refwrap"><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.
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<em>PET measurement of D2 and S2 receptor binding of 3-N-[(2'-18F]fluoroethyl)spiperone in baboon brain.</em>
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<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></dl><dl class="bkr_refwrap"><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.
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<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>
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<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></dl><dl class="bkr_refwrap"><dt>20.</dt><dd><div class="bk_ref" id="FESP18F.REF.20">Jovkar S., Wienhard K., Coenen H.H., Pawlik G., Heiss W.D.
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<em>Quantification of baboon cortical S2 serotonin receptors in vivo with 3-N-(2'-F18)fluoroethylspiperone and positron emission tomography.</em>
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<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></dl><dl class="bkr_refwrap"><dt>21.</dt><dd><div class="bk_ref" id="FESP18F.REF.21">Jovkar S., Wienhard K., Pawlik G., Coenen H.H.
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<em>The quantitative analysis of D2-dopamine receptors in baboon striatum in vivo with 3-N-[2'-18F]fluoroethylspiperone using positron emission tomography.</em>
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<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></dl><dl class="bkr_refwrap"><dt>22.</dt><dd><div class="bk_ref" id="FESP18F.REF.22">Schetz J.A., Kim O.J., Sibley D.R.
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<em>Pharmacological characterization of mammalian D1 and D2 dopamine receptors expressed in Drosophila Schneider-2 cells.</em>
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<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></dl><dl class="bkr_refwrap"><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.
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<em>Quantification of the whole-body distribution of PET radiopharmaceuticals, applied to 3-N-([18F]fluoroethyl)spiperone.</em>
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<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></dl><dl class="bkr_refwrap"><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.
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<em>Models for in vivo kinetic interactions of dopamine D2-neuroreceptors and 3-(2'-[18F]fluoroethyl)spiperone examined with positron emission tomography.</em>
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<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></dl><dl class="bkr_refwrap"><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.
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<em>PET studies of dopamine receptor distribution using [18F]fluoroethylspiperone: findings in disorders related to the dopaminergic system.</em>
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<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></dl><dl class="bkr_refwrap"><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.
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<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>
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<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></dl><dl class="bkr_refwrap"><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.
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<em>Effects of fluvoxamine treatment on the in vivo binding of [F-18]FESP in drug naive depressed patients: a PET study.</em>
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<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></dl><dl class="bkr_refwrap"><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.
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<em>Differentiation of clinically non-functioning pituitary adenomas from meningiomas and craniopharyngiomas by positron emission tomography with [18F]fluoro-ethyl-spiperone.</em>
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<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></dl></div><div id="bk_toc_contnr"></div></div></div><div class="fm-sec"><h2 id="_NBK23473_pubdet_">Publication Details</h2><h3>Author Information and Affiliations</h3><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><h3>Publication History</h3><p class="small">Created: <span itemprop="datePublished">October 7, 2005</span>; Last Update: <span itemprop="dateModified">January 18, 2012</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>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></p></div><div class="small-screen-prev"><a href="/books/n/micad/F18-6b/?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/FEatCIT18F/?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="figobFESP18FTncchemicalname3n218ffluoroet"><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;">
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<b>Chemical name:</b>
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</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;">
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<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>
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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:middle;">[<sup>18</sup>F]FESP</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:middle;"></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:middle;">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: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;">
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<b>Target Category:</b>
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</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;">
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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:middle;">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:middle;"><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:middle;">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><li class="half_rhythm"><div>
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<img alt="Checkbox" src="/corehtml/pmc/css/bookshelf/2.26/img/studies.checkbox.png" /> Non-human primates
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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" /> Humans
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</div></li></ul>
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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&targetsite=external&targetcat=link&targettype=uri">PubChem</a>.</td></tr></tbody></table></div></div></article></div><div id="jr-scripts"><script src="/corehtml/pmc/jatsreader/ptpmc_3.22/js/libs.min.js"> </script><script src="/corehtml/pmc/jatsreader/ptpmc_3.22/js/jr.min.js"> </script></div></div>
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