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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="#__NBK23043_dtls__">Show details</a><div style="display:none" class="ui-widget" id="__NBK23043_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/PIPAM518F/" title="Previous page in this title">< Prev</a><a class="active page_link next" href="/books/n/micad/FPHCys18F/" 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="_NBK23043_"><span class="title" itemprop="name">L-3,4-Dihydroxy-6-[<sup>18</sup>F]fluorophenylalanine</span></h1><div itemprop="alternativeHeadline" class="subtitle whole_rhythm">[<sup>18</sup>F]FDOPA</div><p class="contrib-group"><span itemprop="author">Kam Leung</span>, PhD.</p><a data-jig="ncbitoggler" href="#__NBK23043_ai__" style="border:0;text-decoration:none">Author Information and Affiliations</a><div style="display:none" class="ui-widget" id="__NBK23043_ai__"><div class="contrib half_rhythm"><span itemprop="author">Kam Leung</span>, PhD<div class="affiliation small">National Center for Biotechnology Information, NLM, NIH, Bethesda, MD<div><span class="email-label">Email: </span><a href="mailto:dev@null" data-email="vog.hin vog.hin.mln.ibcn@dacim" class="oemail">vog.hin vog.hin.mln.ibcn@dacim</a></div></div><div class="small">Corresponding author.</div></div></div><p class="small">Created: <span itemprop="datePublished">March 21, 2005</span>; Last Update: <span itemprop="dateModified">December 21, 2011</span>.</p></div><div class="jig-ncbiinpagenav body-content whole_rhythm" data-jigconfig="allHeadingLevels: ['h2'],smoothScroll: false" itemprop="text"><div id="FDOPA.T.nc_chemical_namel34dihydroxy618f" class="table"><p class="large-table-link" style="display:none"><span class="right"><a href="/books/NBK23043/table/FDOPA.T.nc_chemical_namel34dihydroxy618f/?report=objectonly" target="object">View in own window</a></span></p><div class="large_tbl" id="__FDOPA.T.nc_chemical_namel34dihydroxy618f_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;">L-3,4-Dihydroxy-6-[<sup>18</sup>F]fluorophenylalanine</td><td rowspan="9" colspan="1" style="text-align:center;vertical-align:middle;">
|
||
<a href="https://pubchem.ncbi.nlm.nih.gov/substance/235" 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=235" alt="image 235 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>
|
||
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:middle;">6-[<sup>18</sup>F]Fluoro-L-DOPA, [<sup>18</sup>F]FDOPA, FDOPA</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;">
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<b>Agent category:</b>
|
||
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:middle;">Amino acid</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;">Aromatic L-amino acid decarboxylase; L-type amino acid transporter system</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
|
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<b>Target category:</b>
|
||
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:middle;">Enzyme; transporter</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Method of detection:</b>
|
||
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:middle;">Positron emission tomography (PET)</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
|
||
<b>Source of signal:</b>
|
||
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align: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-primate non-rodent mammals
|
||
</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="FDOPA.Background"><h2 id="_FDOPA_Background_">Background</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=FDOPA%5BAll%20Fields%5D" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Parkinson’s disease (PD) is associated with a loss of dopamine-containing neurons in striatum of the brain (<a class="bk_pop" href="#FDOPA.REF.1" data-bk-pop-others="FDOPA.REF.2">1, 2</a>). PD is caused by a shortage of dopamine. Dopamine, a neurotransmitter, plays an important role in the mediation of movement, cognition and emotion. Dopamine also plays a role in various neuropsychiatric disorders, such as schizophrenia, autism, attention deficit hyperactivity disorder, and drug abuse.</p><p>Dopamine is synthesized within nerve cells (<a class="bk_pop" href="#FDOPA.REF.3">3</a>). L-tyrosine is converted to dihydroxyphenylalanine (L-DOPA) and then to dopamine in a two-step process. The first, rate limiting step is catalyzed by tyrosine 3-monoxygenase (tyrosine hydroxylase or TH). The second step is catalyzed by aromatic L-amino acid decarboxylase (L-DOPA decarboxylase, AAAD). In parts of the nervous system that release dopamine as a neurotransmitter (dopaminergic neurons), no further metabolism occurs and dopamine is stored in vesicles in the presynaptic nerve terminals by virtue of the dopamine reuptake transporter, DAT.</p><p>6-[<sup>18</sup>F]Fluoro-L-DOPA (FDOPA) is a radiolabeled analog of L-DOPA used to evaluate the central dopaminergic function of pre-synaptic neurons using positron emission tomography (PET) (<a class="bk_pop" href="#FDOPA.REF.4" data-bk-pop-others="FDOPA.REF.5">4, 5</a>). FDOPA PET reflects DOPA transport into the neurons, DOPA decarboxylation and dopamine storage capacity. The tracer is converted to 6-[<sup>18</sup>F]fluorodopamine (FDA) by AAAD and retained in the striatum. FDA can be O-methylated by catechol-O-methyltransferase (COMT) to 3-O-methyl-6-[<sup>18</sup>F]fluoro-L-dopa (3-OMFD), which is uniformly distributed throughout the brain. FDA is also metabolized via monoamine oxidase to yield [<sup>18</sup>F]6-fluoro-3,4-dihydroxyphenylacetic acid (FDOPAC) and subsequently by COMT to yield [<sup>18</sup>F]6-fluorochomovanillic acid (FHVA). AAAD and COMT are also present in peripheral tissues such as liver, kidneys, and lung. In clinical studies, AAAD is commonly inhibited with carbidopa, whereas COMT is blocked by entacapone and nitecapone. These two types of inhibitors enhance the availability of FDOPA in the brain.</p><div id="FDOPA.Related_Resource_Links"><h3>Related Resource Links:</h3><ul><li class="half_rhythm"><div>Chapters in MICAD (<a href="/sites/entrez?Db=books&Cmd=DetailsSearch&Term=amino%20acid%20(transporter%20OR%20transporters)+AND+micad%5Bbook%5D" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">Amino acid transporters</a>, <a href="/books/?term=Dopamine+AND+micad%5Bbook%5D&view=chapter&p%24a=&p%24l=PBooksLayout&p%24st=books" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">dopamine</a>)</div></li><li class="half_rhythm"><div>Gene information in NCBI (<a href="/gene/23428" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">L-type amino acid transporter</a>, <a href="/gene/1644" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">aromatic L-amino acid decarboxylase</a>)</div></li><li class="half_rhythm"><div>Articles in Online Mendelian Inheritance in Man (OMIM) (<a href="/omim?Db=omim&Cmd=DetailsSearch&Term=amino%5BAll+Fields%5D+AND+acid%5BAll+Fields%5D+AND+transporter%5BAll+Fields%5D" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">Amino acid transporters</a>, <a href="http://omim.org/entry/107930" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">aromatic L-amino acid decarboxylase</a>)</div></li><li class="half_rhythm"><div>Clinical trials (<a href="http://www.clinicaltrials.gov/ct2/results?term=amino+acid+transporters" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">Amino acid transporters</a>, <a href="http://www.clinicaltrials.gov/ct2/results?term=FDOPA" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">FDOPA</a>)</div></li><li class="half_rhythm"><div>Drug information in FDA (<a href="http://google2.fda.gov/search?q=amino+acid+transporters&client=FDAgov&site=FDAgov&lr=&proxystylesheet=FDAgov&output=xml_no_dtd&getfields=*&x=13&y=15" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">Amino acid transporters</a>, <a href="http://google2.fda.gov/search?q=FDOPA&client=FDAgov&site=FDAgov&lr=&proxystylesheet=FDAgov&output=xml_no_dtd&getfields=*&x=9&y=10" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">FDOPA</a>)</div></li></ul></div></div><div id="FDOPA.Synthesis"><h2 id="_FDOPA_Synthesis_">Synthesis</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=FDOPA%5BAll%20Fields%5D%20AND%20synthesis%5BAll%20Fields%5D" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>FDOPA can be synthesized by either electrophilic or nucleophilic process (<a class="bk_pop" href="#FDOPA.REF.6">6</a>). Regioselective electrophilic fluorodemetallation of either a mercuryl or a trimethylstannyl precursor is rapid and simple. Electrophilic fluorination of <span class="small-caps">l</span>-methyl-<i>N</i>-acetyl-[methoxy-4-acetoxyphenyl]alanine with [<sup>18</sup>F]acetyl hypofluorite to provide FDOPA in 8% radiochemical yield at the end of bombardment after hydrolysis and high-performance liquid chromatography (HPLC) purification (<a class="bk_pop" href="#FDOPA.REF.7">7</a>). An overall synthesis time is 100 min with a 95% chemical purity and a specific activity of 7.4 GBq/mmol (200 mCi/mmol) at the end of synthesis (EOS). A robotic synthesis was performed using [<sup>18</sup>F]F<sub>2</sub>/neon gas and the trimethylstannyl precursor in about 110 min (<a class="bk_pop" href="#FDOPA.REF.8">8</a>). The radiochemical purity was >97% and the specific activity was 2.59 GBq/mmol (70 mCi/mmol) at the EOS. The radiochemical yield was about 8.2% (uncorrected for decay)</p><p>A multi-step synthesis, based on the nucleophilic displacement of a nitro group using the standard [<sup>18</sup>F] potassium Kryptofix complex, has been reported (<a class="bk_pop" href="#FDOPA.REF.9">9</a>). The chemical purity was >96% with the specific activity of 1 Ci/μmol (37 GBq//μmol) at the EOS. The overall radiochemical yield was 23% at the EOS. The total synthesis time was 90 min. Nucleophilic methods using [<sup>18</sup>F]fluoride ion have the potential to provide a higher yield and a higher specific activity.</p></div><div id="FDOPA.In_Vitro_Studies_Testing_in_Cells"><h2 id="_FDOPA_In_Vitro_Studies_Testing_in_Cells_"><i>In Vitro</i> Studies: Testing in Cells and Tissues</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=FDOPA%5BAll%20Fields%5D%20AND%20%28%22in%20vitro%22%5BMeSH%20Terms%5D%20OR%20in%20vitro%5BText%20Word%5D%29" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>The enzyme kinetic parameters for AAAD of DOPA and FDOPA were determined <i>in vitro</i> (<a class="bk_pop" href="#FDOPA.REF.10">10</a>). The <i>K</i><sub>m</sub> and <i>k</i><sub>cat</sub> values for DOPA were 0.091 mM and 9.1 s<sup>-1</sup>, respectively. The <i>K</i><sub>m</sub> and <i>k</i><sub>cat</sub> values for FDOPA were 0.7 mM and 8.2 s<sup>-1</sup>, respectively. The presence of fluorine at ring position 6 decreased binding to the active site of AAAD without significantly affecting the enzyme activity of AAAD.</p><p>Unlabeled FDOPA (50 μM) reduced [<sup>3</sup>H]L-DOPA (25 nM) uptake by 69% and 49% in rat striatal and cortical synaptosomes, respectively. L-DOPA showed a higher inhibition than FDOPA (<a class="bk_pop" href="#FDOPA.REF.11">11</a>). In another study, 3-OMFD, L-DOPA and unlabeled FDOPA inhibited the uptake of [<sup>3</sup>H]trytophan (0.1 μM) into cells transfected with human L-type amino acid transporter with IC<sub>50</sub> of 84, 46, and 878 μM, respectively (<a class="bk_pop" href="#FDOPA.REF.12">12</a>).</p></div><div id="FDOPA.Animal_Studies"><h2 id="_FDOPA_Animal_Studies_">Animal Studies</h2><div id="FDOPA.Rodents"><h3>Rodents</h3><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=FDOPA%5BAll%20Fields%5D%20AND%20rodentia" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p><i>Ex vivo</i> iodistribution studies showed a high uptake of radioactivity in the kidneys (5.6% ID/organ), pancreas (0.9% ID/organ) and liver (0.7% ID/organ) of mice at 1 h post injection of FDOPA (<a class="bk_pop" href="#FDOPA.REF.13">13</a>).</p><p>Total extracellular [<sup>18</sup>F] radioactivity in rat striatum was observed to peak at 30 min after injection of FDOPA and declined with clearance half-life of 2 h (<a class="bk_pop" href="#FDOPA.REF.14">14</a>). In the extracellular space, the dominant FDOPA metabolite at early times was FDOPAC, followed by FHVA at 50 min. F-sulfoconjugates appeared at 70 min, and finally 3-OMFD appeared later. Analysis of the striatal tissue confirmed the intraneuronal localization of FDA, most likely stored in vesicles, slowing its cerebral clearance.</p><p>In rat brain, carbidopa pretreatment increased striatal FDA (700%) and 3-OMFD (230%) at 30 min postinjection of FDOPA and cerebellum FDA (370%) and 3-OMFD (300%) (<a class="bk_pop" href="#FDOPA.REF.15">15</a>). FDOPA plasma levels were increased by 20% and 3-OMFD plasma levels by 220%. FDOPAC and FDA were not detected. FHVA levels (>5%) were not changed by carbidopa pretreatment. Carbidopa restricted peripheral FDOPA metabolism to 3-OMFD formation and increased FDOPA bioavailability to the brain, resulting in greater FDA accumulation in the striatum.</p><p>The uptake of FDOPA was studied in a rat model of PD (<a class="bk_pop" href="#FDOPA.REF.16">16</a>). The brains of these rats were unilaterally lesioned with an intranigral injection of 6-hydroxydopamine. The uptake in the lesioned side was 16-31% lower than the sham controls and intact side of the striatum and substantia nigra. The uptake data correlated with the behavioral tests and the number of nigral dopaminergic neurons.</p></div><div id="FDOPA.Other_NonPrimate_Mammals"><h3>Other Non-Primate Mammals</h3><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=FDOPA%20AND%20%28dog%20OR%20rabbit%20OR%20pig%20OR%20sheep%29" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>In dogs, FDOPA uptake was greatest in the pituitary, followed by the liver, spleen and kidneys at 1 h post injection. The uptake in the brain cortex, striatum, thalamus and cerebellum was <50% of the liver uptake (<a class="bk_pop" href="#FDOPA.REF.17">17</a>).</p><p>FDOPA metabolism of immature brain was studied in newborn piglets (<a class="bk_pop" href="#FDOPA.REF.18">18</a>). The estimated values of FDOPA decarboxylation in the basal ganglia were similar to values calculated in adult animals and humans. However, a significant FDOPA decarboxylation was also found in the frontal cortex and the cerebellum. HPLC analysis of brain samples also revealed extensive and rapid metabolism of FDOPA in the frontal cortex, caudate/putamen, midbrain, and cerebellum. At 8 min after tracer injection, about 80% of FDOPA was already converted to FDA and its metabolites. Surprisingly, a rather high fraction (16-21%) of [<sup>18</sup>F]fluoro-3-methoxytyramine was found, indicating a low storage capacity of vesicular dopamine at this perinatal stage. In a later study, it was found that the metabolism of FDOPA in young pigs was significantly faster than in newborns (<a class="bk_pop" href="#FDOPA.REF.19">19</a>).</p></div><div id="FDOPA.NonHuman_Primates"><h3>Non-Human Primates</h3><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=fdopa%20AND%20primate%20NOT%20human" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>FDOPA PET studies in non-human primates have provided useful assessment of the dopaminergic function in the brain. The major metabolite detected in the periphery was 3-OMFD (<a class="bk_pop" href="#FDOPA.REF.15">15</a>). Carbidopa pretreatment increased FDOPA bioavailability to the brain and increased FDOPA metabolism to FDA and 3-OMFD. In the striatum, FDA and 3-OMFD were the major FDOPA metabolites with lower levels of FDOPAC and FHVA. In contrast, the cerebellum and cortex had mainly FDOPA and 3-OMFD accumulation (<a class="bk_pop" href="#FDOPA.REF.20" data-bk-pop-others="FDOPA.REF.21 FDOPA.REF.22">20-22</a>).</p><p>Carbidopa pretreatment of monkeys showed inhibition of peripheral decarboxylation of FDOPA and higher uptake in the striatum and cortex than the control monkeys (<a class="bk_pop" href="#FDOPA.REF.15">15</a>). There was no change in the FDOPA influx constant. Therefore, the higher uptake was because of higher FDOPA bioavailability for transport into the brain.</p><p>FDOPA metabolites from putamen of normal and 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated monkeys were measured to correlate FDOPA metabolism with those of the endogenous dopamine system (<a class="bk_pop" href="#FDOPA.REF.23">23</a>). There were less than 2% of control FDOPA and dopamine levels in the MPTP-treated putamen, which had 80% 3-OMFD as the major metabolite. FDA metabolism was increased for the lesioned putamen as measured by FHVA/FDA ratios (6:1 vs. 0.38:1). At 60 min post FDOPA injection, similar plasma activity for FDOPA and its metabolites were found for both control and lesioned monkeys. The results suggested that PET studies with FDOPA in PD patients could provide kinetic evaluation of striatal biochemistry and evidence of in vivo dopamine turnover changes.</p></div></div><div id="FDOPA.Human_Studies"><h2 id="_FDOPA_Human_Studies_">Human Studies</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=fdopa%20AND%20human" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Human dosimetry was estimated based on murine and human biodistribution data (<a class="bk_pop" href="#FDOPA.REF.13" data-bk-pop-others="FDOPA.REF.17">13, 17</a>). The bladder wall receives the highest dose (0.215 mGy/MBq or 0.797 rad/mCi). Other organs receiving high doses are the kidneys (0.089 mGy/MBq or 0.329 rad/mCi) and pancreas (0.030 mGy/MBq or 0.110 rad/mCi). The brain, liver and lungs receive <0.008 mGy/MBq (0.029 rad/mCi). Effective dose equivalent of 0.026 mSv/MBq (96 mrem/mCi) was estimated in the intravenous administration of FDOPA.</p><p>The first FDOPA PET study of human brain was reported in 1983 (<a class="bk_pop" href="#FDOPA.REF.24">24</a>), showing the localization of radioactivity in the striatum. Only about 1% of FDOPA entered the brain. Striatal-to-occipital ratio, FDOPA influx constant, and AAAD activity constant are commonly used as analytical parameters in FDOPA PET studies. In patients with established bilateral PD, FDOPA PET showed bilateral influx constant reductions in the caudate, putamen, striatal nigra, and midbrain tegmentum. The decline in FDOPA uptake was more rapid in PD than normal subjects (<a class="bk_pop" href="#FDOPA.REF.25">25</a>). In PD patients, AAAD activity was reduced in striatum, putamen, and caudate and no change in frontal and occipital cortices (<a class="bk_pop" href="#FDOPA.REF.26">26</a>).</p><p>In carbidopa-pretreated subjects, peripheral FDOPA was rapidly metabolized by COMT to 3-OMFD. There were significant increases in FDOPA plasma levels for 30 min, but FHVA level decreased. Inhibition of COMT by entacapone in mild to moderate PD patients prolonged the circulation time of FDOPA in the plasma (<a class="bk_pop" href="#FDOPA.REF.27">27</a>). but did not change rate constants for striatal FDOPA influx or decarboxylation. In advanced PD patients pretreated with entacapone, the FDOPA influx constant decreased significantly in the caudate and putamen, and no change in healthy controls. This may be because of the advanced disease, decreased storage capacity, or both (<a class="bk_pop" href="#FDOPA.REF.28">28</a>).</p><p>FDOPA PET permits objective monitoring of PD progression and neuroprotection therapies [<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=fdopa%20AND%20Parkinson%27s%20disease" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]. It allows diagnosis of PD in early disease stages. In recent studies, FDOPA has also demonstrated its usefulness as in the imaging of brain tumors (<a class="bk_pop" href="#FDOPA.REF.29">29</a>) and neuroendocrine metastatic lesions in bone (<a class="bk_pop" href="#FDOPA.REF.30">30</a>).</p></div><div id="FDOPA.References"><h2 id="_FDOPA_References_">References</h2><dl class="temp-labeled-list"><dt>1.</dt><dd><div class="bk_ref" id="FDOPA.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="FDOPA.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="FDOPA.REF.3">Barrio J.R., Huang S.C., Phelps M.E.
|
||
<em>Biological imaging and the molecular basis of dopaminergic diseases.</em>
|
||
<span><span class="ref-journal">Biochem Pharmacol. </span>1997;<span class="ref-vol">54</span>(3):341–8.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/9278092" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 9278092</span></a>]</div></dd><dt>4.</dt><dd><div class="bk_ref" id="FDOPA.REF.4">Heiss W.D., Hilker R.
|
||
<em>The sensitivity of 18-fluorodopa positron emission tomography and magnetic resonance imaging in Parkinson's disease.</em>
|
||
<span><span class="ref-journal">Eur J Neurol. </span>2004;<span class="ref-vol">11</span>(1):5–12.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/14692881" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 14692881</span></a>]</div></dd><dt>5.</dt><dd><div class="bk_ref" id="FDOPA.REF.5">Thobois S., Guillouet S., Broussolle E.
|
||
<em>Contributions of PET and SPECT to the understanding of the pathophysiology of Parkinson's disease.</em>
|
||
<span><span class="ref-journal">Neurophysiol Clin. </span>2001;<span class="ref-vol">31</span>(5):321–40.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/11817273" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 11817273</span></a>]</div></dd><dt>6.</dt><dd><div class="bk_ref" id="FDOPA.REF.6">Luxen A., Guillaume M., Melega W.P., Pike V.W., Solin O., Wagner R.
|
||
<em>Production of 6-[18F]fluoro-L-dopa and its metabolism in vivo--a critical review.</em>
|
||
<span><span class="ref-journal">Int J Rad Appl Instrum B. </span>1992;<span class="ref-vol">19</span>(2):149–58.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/1601668" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 1601668</span></a>]</div></dd><dt>7.</dt><dd><div class="bk_ref" id="FDOPA.REF.7">Adam M.J., Ruth T.J., Grierson J.R., Abeysekera B., Pate B.D.
|
||
<em>Routine synthesis of L-[18F]6-fluorodopa with fluorine-18 acetyl hypofluorite.</em>
|
||
<span><span class="ref-journal">J Nucl Med. </span>1986;<span class="ref-vol">27</span>(9):1462–6.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/3091786" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 3091786</span></a>]</div></dd><dt>8.</dt><dd><div class="bk_ref" id="FDOPA.REF.8">Chang C.W., Wang H.E., Lin H.M., Chtsai C.S., Chen J.B., Liu R.S.
|
||
<em>Robotic synthesis of 6-[18F]fluoro-L-dopa.</em>
|
||
<span><span class="ref-journal">Nucl Med Commun. </span>2000;<span class="ref-vol">21</span>(9):799–802.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/11065151" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 11065151</span></a>]</div></dd><dt>9.</dt><dd><div class="bk_ref" id="FDOPA.REF.9">Lemaire C., Damhaut P., Plenevaux A., Comar D.
|
||
<em>Enantioselective synthesis of 6-[fluorine-18]-fluoro-L-dopa from no-carrier-added fluorine-18-fluoride.</em>
|
||
<span><span class="ref-journal">J Nucl Med. </span>1994;<span class="ref-vol">35</span>(12):1996–2002.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/7989984" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 7989984</span></a>]</div></dd><dt>10.</dt><dd><div class="bk_ref" id="FDOPA.REF.10">Borri Voltattorni C., Bertoldi M., Bianconi S., Deng W.P., Wong K., Kim I., Herbert B., Kirk K.L.
|
||
<em>Behavior of fluorinated analogs of L-(3,4-dihydroxyphenyl)alanine and L-threo-(3,4-dihydroxyphenyl)serine as substrates for Dopa decarboxylase.</em>
|
||
<span><span class="ref-journal">Biochem Biophys Res Commun. </span>2002;<span class="ref-vol">295</span>(1):107–11.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/12083775" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 12083775</span></a>]</div></dd><dt>11.</dt><dd><div class="bk_ref" id="FDOPA.REF.11">Yee R.E., Cheng D.W., Huang S.C., Namavari M., Satyamurthy N., Barrio J.R.
|
||
<em>Blood-brain barrier and neuronal membrane transport of 6-[18F]fluoro-L-DOPA.</em>
|
||
<span><span class="ref-journal">Biochem Pharmacol. </span>2001;<span class="ref-vol">62</span>(10):1409–15.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/11709201" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 11709201</span></a>]</div></dd><dt>12.</dt><dd><div class="bk_ref" id="FDOPA.REF.12">Brust P., Vorwieger G., Walter B., Fuchtner F., Stark H., Kuwabara H., Herzau M., Opfermann T., Steinbach J., Ganapathy V., Bauer R.
|
||
<em>The influx of neutral amino acids into the porcine brain during development: a positron emission tomography study.</em>
|
||
<span><span class="ref-journal">Brain Res Dev Brain Res. </span>2004;<span class="ref-vol">152</span>(2):241–53.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/15351512" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 15351512</span></a>]</div></dd><dt>13.</dt><dd><div class="bk_ref" id="FDOPA.REF.13">Mejia A.A., Nakamura T., Itoh M., Hatazawa J., Ishiwata K., Ido T., Matsumoto M., Watabe H., Watanuki S., Seo S.
|
||
<em>Absorbed dose estimates in positron emission tomography studies based on the administration of 18F-labeled radiopharmaceuticals.</em>
|
||
<span><span class="ref-journal">J Radiat Res (Tokyo). </span>1991;<span class="ref-vol">32</span>(3):243–61.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/1838773" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 1838773</span></a>]</div></dd><dt>14.</dt><dd><div class="bk_ref" id="FDOPA.REF.14">DeJesus O.T., Haaparanta M., Solin O., Nickles R.J.
|
||
<em>6-fluoroDOPA metabolism in rat striatum: time course of extracellular metabolites.</em>
|
||
<span><span class="ref-journal">Brain Res. </span>2000;<span class="ref-vol">877</span>(1):31–6.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/10980240" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 10980240</span></a>]</div></dd><dt>15.</dt><dd><div class="bk_ref" id="FDOPA.REF.15">Melega W.P., Hoffman J.M., Luxen A., Nissenson C.H., Phelps M.E., Barrio J.R.
|
||
<em>The effects of carbidopa on the metabolism of 6-[18F]fluoro-L-dopa in rats, monkeys and humans.</em>
|
||
<span><span class="ref-journal">Life Sci. </span>1990;<span class="ref-vol">47</span>(2):149–57.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/2117691" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 2117691</span></a>]</div></dd><dt>16.</dt><dd><div class="bk_ref" id="FDOPA.REF.16">Forsback S., Niemi R., Marjamaki P., Eskola O., Bergman J., Gronroos T., Haaparanta M., Haapalinna A., Rinne J., Solin O.
|
||
<em>Uptake of 6-[18F]fluoro-L-dopa and [18F]CFT reflect nigral neuronal loss in a rat model of Parkinson's disease.</em>
|
||
<span><span class="ref-journal">Synapse. </span>2004;<span class="ref-vol">51</span>(2):119–27.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/14618679" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 14618679</span></a>]</div></dd><dt>17.</dt><dd><div class="bk_ref" id="FDOPA.REF.17">Harvey J., Firnau G., Garnett E.S.
|
||
<em>Estimation of the radiation dose in man due to 6-[18F]fluoro-L-dopa.</em>
|
||
<span><span class="ref-journal">J Nucl Med. </span>1985;<span class="ref-vol">26</span>(8):931–5.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/3928836" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 3928836</span></a>]</div></dd><dt>18.</dt><dd><div class="bk_ref" id="FDOPA.REF.18">Brust P., Bauer R., Walter B., Bergmann R., Fuchtner F., Vorwieger G., Steinbach J., Johannsen B., Zwiener U.
|
||
<em>Simultaneous measurement of [18F]FDOPA metabolism and cerebral blood flow in newborn piglets.</em>
|
||
<span><span class="ref-journal">Int J Dev Neurosci. </span>1998;<span class="ref-vol">16</span>(5):353–64.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/9829172" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 9829172</span></a>]</div></dd><dt>19.</dt><dd><div class="bk_ref" id="FDOPA.REF.19">Brust P., Walter B., Hinz R., Fuchtner F., Muller M., Steinbach J., Bauer R.
|
||
<em>Developmental changes in the activities of aromatic amino acid decarboxylase and catechol-O-methyl transferase in the porcine brain: a positron emission tomography study.</em>
|
||
<span><span class="ref-journal">Neurosci Lett. </span>2004;<span class="ref-vol">364</span>(3):159–63.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/15196667" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 15196667</span></a>]</div></dd><dt>20.</dt><dd><div class="bk_ref" id="FDOPA.REF.20">Chan G.L., Doudet D.J., Dobko T., Hewitt K.A., Schofield P., Pate B.D., Ruth T.J.
|
||
<em>Routes of administration and effect of carbidopa pretreatment on 6-[18F]fluoro-L-dopa/PET scans in non-human primates.</em>
|
||
<span><span class="ref-journal">Life Sci. </span>1995;<span class="ref-vol">56</span>(21):1759–66.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/7739350" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 7739350</span></a>]</div></dd><dt>21.</dt><dd><div class="bk_ref" id="FDOPA.REF.21">Endres C.J., DeJesus O.T., Uno H., Doudet D.J., Nickles J.R., Holden J.E.
|
||
<em>Time profile of cerebral [18F]6-fluoro-L-DOPA metabolites in nonhuman primate: implications for the kinetics of therapeutic L-DOPA.</em>
|
||
<span><span class="ref-journal">Front Biosci. </span>2004;<span class="ref-vol">9</span>:505–12.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/14766386" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 14766386</span></a>]</div></dd><dt>22.</dt><dd><div class="bk_ref" id="FDOPA.REF.22">Melega W.P., Grafton S.T., Huang S.C., Satyamurthy N., Phelps M.E., Barrio J.R.
|
||
<em>L-6-[18F]fluoro-dopa metabolism in monkeys and humans: biochemical parameters for the formulation of tracer kinetic models with positron emission tomography.</em>
|
||
<span><span class="ref-journal">J Cereb Blood Flow Metab. </span>1991;<span class="ref-vol">11</span>(6):890–7.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/1939384" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 1939384</span></a>]</div></dd><dt>23.</dt><dd><div class="bk_ref" id="FDOPA.REF.23">Melega W.P., Hoffman J.M., Schneider J.S., Phelps M.E., Barrio J.R.
|
||
<em>6-[18F]fluoro-L-dopa metabolism in MPTP-treated monkeys: assessment of tracer methodologies for positron emission tomography.</em>
|
||
<span><span class="ref-journal">Brain Res. </span>1991;<span class="ref-vol">543</span>(2):271–6.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/1905578" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 1905578</span></a>]</div></dd><dt>24.</dt><dd><div class="bk_ref" id="FDOPA.REF.24">Garnett E.S., Firnau G., Nahmias C.
|
||
<em>Dopamine visualized in the basal ganglia of living man.</em>
|
||
<span><span class="ref-journal">Nature. </span>1983;<span class="ref-vol">305</span>(5930):137–8.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/6604227" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 6604227</span></a>]</div></dd><dt>25.</dt><dd><div class="bk_ref" id="FDOPA.REF.25">Vingerhoets F.J., Snow B.J., Lee C.S., Schulzer M., Mak E., Calne D.B.
|
||
<em>Longitudinal fluorodopa positron emission tomographic studies of the evolution of idiopathic parkinsonism.</em>
|
||
<span><span class="ref-journal">Ann Neurol. </span>1994;<span class="ref-vol">36</span>(5):759–64.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/7979222" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 7979222</span></a>]</div></dd><dt>26.</dt><dd><div class="bk_ref" id="FDOPA.REF.26">Kuwabara H., Cumming P., Yasuhara Y., Leger G.C., Guttman M., Diksic M., Evans A.C., Gjedde A.
|
||
<em>Regional striatal DOPA transport and decarboxylase activity in Parkinson's disease.</em>
|
||
<span><span class="ref-journal">J Nucl Med. </span>1995;<span class="ref-vol">36</span>(7):1226–31.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/7790948" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 7790948</span></a>]</div></dd><dt>27.</dt><dd><div class="bk_ref" id="FDOPA.REF.27">Ishikawa T., Dhawan V., Chaly T., Robeson W., Belakhlef A., Mandel F., Dahl R., Margouleff C., Eidelberg D.
|
||
<em>Fluorodopa positron emission tomography with an inhibitor of catechol-O-methyltransferase: effect of the plasma 3-O-methyldopa fraction on data analysis.</em>
|
||
<span><span class="ref-journal">J Cereb Blood Flow Metab. </span>1996;<span class="ref-vol">16</span>(5):854–63.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/8784230" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 8784230</span></a>]</div></dd><dt>28.</dt><dd><div class="bk_ref" id="FDOPA.REF.28">Ruottinen H.M., Rinne J.O., Ruotsalainen U.H., Bergman J.R., Oikonen V.J., Haaparanta M.T., Solin O.H., Laihinen A.O., Rinne U.K.
|
||
<em>Striatal [18F]fluorodopa utilization after COMT inhibition with entacapone studied with PET in advanced Parkinson's disease.</em>
|
||
<span><span class="ref-journal">J Neural Transm Park Dis Dement Sect. </span>1995;<span class="ref-vol">10</span>(2-3):91–106.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/9620057" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 9620057</span></a>]</div></dd><dt>29.</dt><dd><div class="bk_ref" id="FDOPA.REF.29">Becherer A., Karanikas G., Szabo M., Zettinig G., Asenbaum S., Marosi C., Henk C., Wunderbaldinger P., Czech T., Wadsak W., Kletter K.
|
||
<em>Brain tumour imaging with PET: a comparison between [18F]fluorodopa and [11C]methionine.</em>
|
||
<span><span class="ref-journal">Eur J Nucl Med Mol Imaging. </span>2003;<span class="ref-vol">30</span>(11):1561–7.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/14579097" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 14579097</span></a>]</div></dd><dt>30.</dt><dd><div class="bk_ref" id="FDOPA.REF.30">Becherer A., Szabo M., Karanikas G., Wunderbaldinger P., Angelberger P., Raderer M., Kurtaran A., Dudczak R., Kletter K.
|
||
<em>Imaging of advanced neuroendocrine tumors with (18)F-FDOPA PET.</em>
|
||
<span><span class="ref-journal">J Nucl Med. </span>2004;<span class="ref-vol">45</span>(7):1161–7.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/15235062" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 15235062</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: NBK23043</span><span class="label">PMID: <a href="https://pubmed.ncbi.nlm.nih.gov/20641250" title="PubMed record of this page" ref="pagearea=meta&targetsite=entrez&targetcat=link&targettype=pubmed">20641250</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/PIPAM518F/" title="Previous page in this title">< Prev</a><a class="active page_link next" href="/books/n/micad/FPHCys18F/" 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/NBK23043/?report=reader">PubReader</a></li><li><a href="/books/NBK23043/?report=printable">Print View</a></li><li><a data-jig="ncbidialog" href="#_ncbi_dlg_citbx_NBK23043" data-jigconfig="width:400,modal:true">Cite this Page</a><div id="_ncbi_dlg_citbx_NBK23043" style="display:none" title="Cite this Page"><div class="bk_tt">Leung K. L-3,4-Dihydroxy-6-[18F]fluorophenylalanine. 2005 Mar 21 [Updated 2011 Dec 21]. 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/NBK23043/pdf/Bookshelf_NBK23043.pdf">PDF version of this page</a> (165K)</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="#FDOPA.Background" ref="log$=inpage&link_id=inpage">Background</a></li><li><a href="#FDOPA.Synthesis" ref="log$=inpage&link_id=inpage">Synthesis</a></li><li><a href="#FDOPA.In_Vitro_Studies_Testing_in_Cells" ref="log$=inpage&link_id=inpage"><i>In Vitro</i> Studies: Testing in Cells and Tissues</a></li><li><a href="#FDOPA.Animal_Studies" ref="log$=inpage&link_id=inpage">Animal Studies</a></li><li><a href="#FDOPA.Human_Studies" ref="log$=inpage&link_id=inpage">Human Studies</a></li><li><a href="#FDOPA.References" ref="log$=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=1512088" ref="log$=recordlinks">PMC</a><div class="brieflinkpop offscreen_noflow">PubMed Central citations</div></li><li class="brieflinkpopper"><a class="brieflinkpopperctrl" href="/books/?Db=pcsubstance&DbFrom=books&Cmd=Link&LinkName=books_pcsubstance&IdsFromResult=1512088" ref="log$=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=1512088" ref="log$=recordlinks">PubMed</a><div class="brieflinkpop offscreen_noflow">Links to PubMed</div></li></ul></div></div><div class="portlet"><div class="portlet_head"><div class="portlet_title"><h3><span>Similar articles in PubMed</span></h3></div><a name="Shutter" sid="1" href="#" class="portlet_shutter" title="Show/hide content" remembercollapsed="true" pgsec_name="PBooksDiscovery_RA" id="Shutter"></a></div><div class="portlet_content"><ul><li class="brieflinkpopper two_line"><a class="brieflinkpopperctrl" href="/pubmed/20641715" ref="ordinalpos=1&linkpos=1&log$=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> 6-[(18)F]Fluorodopamine.</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> 6-[(18)F]Fluorodopamine.<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/20641693" ref="ordinalpos=1&linkpos=2&log$=relatedreviews&logdbfrom=pubmed"><span xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="invert">Review</span> 6-[(18)F]Fluoro-l-m-tyrosine.</a><span class="source">[Molecular Imaging and Contrast...]</span><div class="brieflinkpop offscreen_noflow"><span xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="invert">Review</span> 6-[(18)F]Fluoro-l-m-tyrosine.<div class="brieflinkpopdesc"><em xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="author">The MICAD Research Team. </em><em xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="cit">Molecular Imaging and Contrast Agent Database (MICAD). 2004</em></div></div></li><li class="brieflinkpopper two_line"><a class="brieflinkpopperctrl" href="/pubmed/20641732" ref="ordinalpos=1&linkpos=3&log$=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> 4-[(18)F]Fluoro-l-m-tyrosine.</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> 4-[(18)F]Fluoro-l-m-tyrosine.<div class="brieflinkpopdesc"><em xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="author">The MICAD Research Team. </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/26564319" ref="ordinalpos=1&linkpos=4&log$=relatedarticles&logdbfrom=pubmed">Evaluation of 6-11C-Methyl-m-Tyrosine as a PET Probe for Presynaptic Dopaminergic Activity: A Comparison PET Study with β-11C-l-DOPA and 18F-FDOPA in Parkinson Disease Monkeys.</a><span class="source">[J Nucl Med. 2016]</span><div class="brieflinkpop offscreen_noflow">Evaluation of 6-11C-Methyl-m-Tyrosine as a PET Probe for Presynaptic Dopaminergic Activity: A Comparison PET Study with β-11C-l-DOPA and 18F-FDOPA in Parkinson Disease Monkeys.<div class="brieflinkpopdesc"><em xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="author">Kanazawa M, Ohba H, Harada N, Kakiuchi T, Muramatsu S, Tsukada H. </em><em xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="cit">J Nucl Med. 2016 Feb; 57(2):303-8. Epub 2015 Nov 12.</em></div></div></li><li class="brieflinkpopper two_line"><a class="brieflinkpopperctrl" href="/pubmed/9365014" ref="ordinalpos=1&linkpos=5&log$=relatedarticles&logdbfrom=pubmed">Cerebral 6-[18F]fluoro-L-DOPA uptake in rhesus monkey: pharmacological influence of aromatic amino acid decarboxylase (AAAD) and catechol-O-methyltransferase (COMT) inhibition.</a><span class="source">[Brain Res. 1997]</span><div class="brieflinkpop offscreen_noflow">Cerebral 6-[18F]fluoro-L-DOPA uptake in rhesus monkey: pharmacological influence of aromatic amino acid decarboxylase (AAAD) and catechol-O-methyltransferase (COMT) inhibition.<div class="brieflinkpopdesc"><em xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="author">Psylla M, Günther I, Antonini A, Vontobel P, Reist HW, Zollinger A, Leenders KL. </em><em xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="cit">Brain Res. 1997 Aug 29; 767(1):45-54. </em></div></div></li></ul><a class="seemore" href="/sites/entrez?db=pubmed&cmd=link&linkname=pubmed_pubmed_reviews&uid=20641250" ref="ordinalpos=1&log$=relatedreviews_seeall&logdbfrom=pubmed">See reviews...</a><a class="seemore" href="/sites/entrez?db=pubmed&cmd=link&linkname=pubmed_pubmed&uid=20641250" ref="ordinalpos=1&log$=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 href="javascript:historyDisplayState('ClearHT')">Clear</a><a href="javascript:historyDisplayState('HTOff')" class="HTOn">Turn Off</a><a href="javascript:historyDisplayState('HTOn')" class="HTOff">Turn On</a></div><ul id="activity"><li class="ra_rcd ralinkpopper two_line"><a class="htb ralinkpopperctrl" ref="log$=activity&linkpos=1" href="/portal/utils/pageresolver.fcgi?recordid=67d6469684f3725e59ab79cd">L-3,4-Dihydroxy-6-[18F]fluorophenylalanine - Molecular Imaging and Contrast Agen...</a><div class="ralinkpop offscreen_noflow">L-3,4-Dihydroxy-6-[18F]fluorophenylalanine - Molecular Imaging and Contrast Agent Database (MICAD)<div class="brieflinkpopdesc"></div></div><div class="tertiary"></div></li><li class="ra_rcd ralinkpopper two_line"><a class="htb ralinkpopperctrl" ref="log$=activity&linkpos=2" href="/portal/utils/pageresolver.fcgi?recordid=67d6469567c23b31e031936c">ImPyβImPyβImβ-C3-18F - Molecular Imaging and Contrast Agent Database (MICAD)</a><div class="ralinkpop offscreen_noflow">ImPyβImPyβImβ-C3-18F - Molecular Imaging and Contrast Agent Database (MICAD)<div class="brieflinkpopdesc"></div></div><div class="tertiary"></div></li><li class="ra_rcd ralinkpopper two_line"><a class="htb ralinkpopperctrl" ref="log$=activity&linkpos=3" href="/portal/utils/pageresolver.fcgi?recordid=67d646932f30673f7b760d8c">Fluoro-pegylated (1E,4E)-1-(4-(dimethylamino)phenyl)-5-(4-(2-(2-(2-fluoroethoxy)...</a><div class="ralinkpop offscreen_noflow">Fluoro-pegylated (1E,4E)-1-(4-(dimethylamino)phenyl)-5-(4-(2-(2-(2-fluoroethoxy)ethoxy)ethoxy)phenyl)penta-1,4-dien-3-one and (1E,4E)-1-(4-(2-(2-(2-fluoroethoxy)ethoxy)ethoxy)phenyl)-5-(4-(methylamino)phenyl)penta-1,4-dien-3-one - Molecular Imaging and Contrast Agent Database (MICAD)<div class="brieflinkpopdesc"></div></div><div class="tertiary"></div></li><li class="ra_rcd ralinkpopper two_line"><a class="htb ralinkpopperctrl" ref="log$=activity&linkpos=4" href="/portal/utils/pageresolver.fcgi?recordid=67d64692cde49f3df75b49fc">Cys-Arg-Pro-Pro-Arg-[18F]fluorodipalmitin-liposomes - Molecular Imaging and Cont...</a><div class="ralinkpop offscreen_noflow">Cys-Arg-Pro-Pro-Arg-[18F]fluorodipalmitin-liposomes - Molecular Imaging and Contrast Agent Database (MICAD)<div class="brieflinkpopdesc"></div></div><div class="tertiary"></div></li><li class="ra_rcd ralinkpopper two_line"><a class="htb ralinkpopperctrl" ref="log$=activity&linkpos=5" href="/portal/utils/pageresolver.fcgi?recordid=67d6469067c23b31e0317d5a">Cyclo(-Arg-Gly-Asp-d-Phe-Lys(([18F]Fluoropropionyl)galacto-amino acid)-) - Molec...</a><div class="ralinkpop offscreen_noflow">Cyclo(-Arg-Gly-Asp-d-Phe-Lys(([18F]Fluoropropionyl)galacto-amino acid)-) - Molecular Imaging and Contrast Agent Database (MICAD)<div class="brieflinkpopdesc"></div></div><div class="tertiary"></div></li></ul><p class="HTOn">Your browsing activity is empty.</p><p class="HTOff">Activity recording is turned off.</p><p id="turnOn" class="HTOff"><a href="javascript:historyDisplayState('HTOn')">Turn recording back on</a></p><a class="seemore" href="/sites/myncbi/recentactivity">See more...</a></div></div></div>
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