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<meta name="ncbi_pagename" content="68Ga-Labeled 2-[3-(1-carboxy-5-{7-[5-carboxy-5-(3-phenyl-2-{3-phenyl-2-[2-(4,7,10-tris-carboxymethyl-1,4,7,10-tetraazacyclododec-1-l)acetylamino]propionylamino}propionylamino)pentylcarbamoyl]heptanoylamino}pentyl)ureido]pentanedioic acid - Molecular Imaging and Contrast Agent Database (MICAD) - NCBI Bookshelf">
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<script type="text/javascript" src="/corehtml/pmc/jatsreader/ptpmc_3.22/js/jr.boots.min.js"> </script><title>68Ga-Labeled 2-[3-(1-carboxy-5-{7-[5-carboxy-5-(3-phenyl-2-{3-phenyl-2-[2-(4,7,10-tris-carboxymethyl-1,4,7,10-tetraazacyclododec-1-l)acetylamino]propionylamino}propionylamino)pentylcarbamoyl]heptanoylamino}pentyl)ureido]pentanedioic acid - Molecular Imaging and Contrast Agent Database (MICAD) - NCBI Bookshelf</title>
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<meta name="citation_inbook_title" content="Molecular Imaging and Contrast Agent Database (MICAD) [Internet]">
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<meta name="citation_title" content="68Ga-Labeled 2-[3-(1-carboxy-5-{7-[5-carboxy-5-(3-phenyl-2-{3-phenyl-2-[2-(4,7,10-tris-carboxymethyl-1,4,7,10-tetraazacyclododec-1-l)acetylamino]propionylamino}propionylamino)pentylcarbamoyl]heptanoylamino}pentyl)ureido]pentanedioic acid">
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<meta name="citation_publisher" content="National Center for Biotechnology Information (US)">
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<meta name="citation_date" content="2010/12/28">
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<meta name="citation_author" content="Arvind Chopra">
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<meta name="citation_pmid" content="21249764">
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<meta name="DC.Title" content="68Ga-Labeled 2-[3-(1-carboxy-5-{7-[5-carboxy-5-(3-phenyl-2-{3-phenyl-2-[2-(4,7,10-tris-carboxymethyl-1,4,7,10-tetraazacyclododec-1-l)acetylamino]propionylamino}propionylamino)pentylcarbamoyl]heptanoylamino}pentyl)ureido]pentanedioic acid">
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<meta name="description" content="The prostate-specific membrane antigen (PSMA) is a type II membrane glycoprotein that is present primarily in the prostate and is overexpressed during all stages of the androgen-insensitive or the metastatic cancer of this organ (1). In addition, PSMA is expressed at lower levels (compared to the prostate) in the neovasculature of some solid tumors (for details, see Elsasser-Beile et al. (1)). Because of its high expression during the development and progression of a malignancy, PSMA is considered to be a good target for the imaging and treatment of prostate cancer (2). Several investigators have reported the use of radio-halogenated (e.g., 18F, 125I, etc.) and 99mTc-labeled small molecule inhibitors for the imaging of PSMA (3). Among these radionuclides, 18F is the most frequently used to label diverse positron emission tomography (PET) agents for diagnostic imaging because its addition to a molecule (usually by the replacement of a hydrogen atom) does not alter its chemical properties; however, due to its short half-life (~110 min), an on-site cyclotron is needed to produce this radio-halogen (4). Recently 68Ga (half-life, ~68 min) has been suggested to be a suitable alternative to the use of 18F for the production of PET imaging probes because 68Ga is easy to produce with a 68Ge/68Ga generator system that does not have to be on-site. However, it is necessary to mention that currently no 68Ge/68Ga generator system has been approved by the United States Food and Drug Administration (Eckelman: personal communication). In addition, 68Ga has been successfully used by some investigators to study cancer and tumor biology (4, 5). On the basis of these observations, and as an extension of their earlier work (Banerjee et al. developed two 68Ga-labeled, urea-based inhibitors of PSMA ([68Ga]-labeled 2-[3-(1-carboxy-5-{7-[5-carboxy-5-(3-phenyl-2-{3-phenyl-2-[2-(4,7,10-tris-carboxymethyl-1,4,7,10-tetraazacyclododec-1-l)acetylamino]propionylamino}propionylamino)pentylcarbamoyl]">
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<meta name="og:description" content="The prostate-specific membrane antigen (PSMA) is a type II membrane glycoprotein that is present primarily in the prostate and is overexpressed during all stages of the androgen-insensitive or the metastatic cancer of this organ (1). In addition, PSMA is expressed at lower levels (compared to the prostate) in the neovasculature of some solid tumors (for details, see Elsasser-Beile et al. (1)). Because of its high expression during the development and progression of a malignancy, PSMA is considered to be a good target for the imaging and treatment of prostate cancer (2). Several investigators have reported the use of radio-halogenated (e.g., 18F, 125I, etc.) and 99mTc-labeled small molecule inhibitors for the imaging of PSMA (3). Among these radionuclides, 18F is the most frequently used to label diverse positron emission tomography (PET) agents for diagnostic imaging because its addition to a molecule (usually by the replacement of a hydrogen atom) does not alter its chemical properties; however, due to its short half-life (~110 min), an on-site cyclotron is needed to produce this radio-halogen (4). Recently 68Ga (half-life, ~68 min) has been suggested to be a suitable alternative to the use of 18F for the production of PET imaging probes because 68Ga is easy to produce with a 68Ge/68Ga generator system that does not have to be on-site. However, it is necessary to mention that currently no 68Ge/68Ga generator system has been approved by the United States Food and Drug Administration (Eckelman: personal communication). In addition, 68Ga has been successfully used by some investigators to study cancer and tumor biology (4, 5). On the basis of these observations, and as an extension of their earlier work (Banerjee et al. developed two 68Ga-labeled, urea-based inhibitors of PSMA ([68Ga]-labeled 2-[3-(1-carboxy-5-{7-[5-carboxy-5-(3-phenyl-2-{3-phenyl-2-[2-(4,7,10-tris-carboxymethyl-1,4,7,10-tetraazacyclododec-1-l)acetylamino]propionylamino}propionylamino)pentylcarbamoyl]">
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preserveAspectRatio="none"><path fill="none" stroke="#000" stroke-width="36" stroke-linecap="round" style="fill:#FFF" d="m320,350a153,153 0 1,0-2,2l170,170m-91-117 110,110-26,26-110-110"></path></svg></a><a id="jr-fip-done" class="wsprkl btn" title="Dismiss find">✘</a></nav><nav id="jr-fip-info-p"><a id="jr-fip-prev" class="wsprkl btn" title="Jump to previuos match">◀</a><button id="jr-fip-matches">no matches yet</button><a id="jr-fip-next" class="wsprkl btn" title="Jump to next match">▶</a></nav></nav></div><div id="jr-epub-interstitial" class="hidden"></div><div id="jr-content"><article data-type="main"><div class="main-content lit-style" itemscope="itemscope" itemtype="http://schema.org/CreativeWork"><div class="meta-content fm-sec"><div class="fm-sec"><h1 id="_NBK51314_"><span class="title" itemprop="name"><sup>68</sup>Ga-Labeled 2-[3-(1-carboxy-5-{7-[5-carboxy-5-(3-phenyl-2-{3-phenyl-2-[2-(4,7,10-tris-carboxymethyl-1,4,7,10-tetraazacyclododec-1-l)acetylamino]propionylamino}propionylamino)pentylcarbamoyl]heptanoylamino}pentyl)ureido]pentanedioic acid</span></h1><div itemprop="alternativeHeadline" class="subtitle whole_rhythm">[<sup>68</sup>Ga]6</div><p class="contribs">Chopra A.</p><p class="fm-aai"><a href="#_NBK51314_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="figPSMA68Ga6Tncchemicalname68galabeled"><a href="/books/NBK51314/table/PSMA68Ga6.T.nc_chemical_name68galabeled_/?report=objectonly" target="object" title="Table" class="img_link icnblk_img" rid-ob="figobPSMA68Ga6Tncchemicalname68galabeled"><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="PSMA68Ga6.T.nc_chemical_name68galabeled_"><a href="/books/NBK51314/table/PSMA68Ga6.T.nc_chemical_name68galabeled_/?report=objectonly" target="object" rid-ob="figobPSMA68Ga6Tncchemicalname68galabeled">Table</a></h4><p class="float-caption no_bottom_margin">
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</p></div></div><div id="PSMA68Ga6.Background"><h2 id="_PSMA68Ga6_Background_">Background</h2><p>[<a href="/pubmed?term=psma%20and%20prostate%20cancer&cmd=DetailsSearch" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>The prostate-specific membrane antigen (PSMA) is a type II membrane glycoprotein that is present primarily in the prostate and is overexpressed during all stages of the androgen-insensitive or the metastatic cancer of this organ (<a class="bibr" href="#PSMA68Ga6.REF.1" rid="PSMA68Ga6.REF.1">1</a>). In addition, PSMA is expressed at lower levels (compared to the prostate) in the neovasculature of some solid tumors (for details, see Elsasser-Beile et al. (<a class="bibr" href="#PSMA68Ga6.REF.1" rid="PSMA68Ga6.REF.1">1</a>)). Because of its high expression during the development and progression of a malignancy, PSMA is considered to be a good target for the imaging and treatment of prostate cancer (<a class="bibr" href="#PSMA68Ga6.REF.2" rid="PSMA68Ga6.REF.2">2</a>). Several investigators have reported the use of radio-halogenated (e.g., <sup>18</sup>F, <sup>125</sup>I, etc.) and <sup>99m</sup>Tc-labeled small molecule inhibitors for the imaging of PSMA (<a class="bibr" href="#PSMA68Ga6.REF.3" rid="PSMA68Ga6.REF.3">3</a>). Among these radionuclides, <sup>18</sup>F is the most frequently used to label diverse positron emission tomography (PET) agents for diagnostic imaging because its addition to a molecule (usually by the replacement of a hydrogen atom) does not alter its chemical properties; however, due to its short half-life (~110 min), an on-site cyclotron is needed to produce this radio-halogen (<a class="bibr" href="#PSMA68Ga6.REF.4" rid="PSMA68Ga6.REF.4">4</a>). Recently <sup>68</sup>Ga (half-life, ~68 min) has been suggested to be a suitable alternative to the use of <sup>18</sup>F for the production of PET imaging probes because <sup>68</sup>Ga is easy to produce with a <sup>68</sup>Ge/<sup>68</sup>Ga generator system that does not have to be on-site. However, it is necessary to mention that currently no <sup>68</sup>Ge/<sup>68</sup>Ga generator system has been approved by the United States Food and Drug Administration (Eckelman: personal communication). In addition, <sup>68</sup>Ga has been successfully used by some investigators to study cancer and tumor biology (<a class="bibr" href="#PSMA68Ga6.REF.4" rid="PSMA68Ga6.REF.4 PSMA68Ga6.REF.5">4, 5</a>). On the basis of these observations, and as an extension of their earlier work (Banerjee et al. developed two <sup>68</sup>Ga-labeled, urea-based inhibitors of PSMA ([<sup>68</sup>Ga]-labeled 2-[3-(1-carboxy-5-{7-[5-carboxy-5-(3-phenyl-2-{3-phenyl-2-[2-(4,7,10-tris-carboxymethyl-1,4,7,10-tetraazacyclododec-1-l)acetylamino]propionylamino}propionylamino)pentylcarbamoyl]</p><p>heptanoylamino}pentyl)ureido]pentanedioic acid ([<sup>68</sup>Ga]<b>6</b>)) and [<sup>68</sup>Ga]-labeled 2-{3-[5-(7-{1-benzyloxycarbonyl-5-[2-(4,7,10-tris-carboxymethyl-1,4,7,10-tetraazacyclododec-1-l)acetylamino]pentylcarbamoyl}-heptanoylamino)-1-carboxypentyl]ureido}pentanedioic acid ([<sup>68</sup>Ga]<b>3</b>)) and evaluated them for biodistribution and the imaging of PSMA-expressing tumors in nude mice (<a class="bibr" href="#PSMA68Ga6.REF.3" rid="PSMA68Ga6.REF.3">3</a>). This chapter details the results obtained with [<sup>68</sup>Ga]<b>6</b>. Results obtained with [<sup>68</sup>Ga]<b>3</b> are presented in a separate chapter of MICAD (<a href="http://www.micad.nih.gov/" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">www.micad.nih.gov</a>) (<a class="bibr" href="#PSMA68Ga6.REF.6" rid="PSMA68Ga6.REF.6">6</a>).</p><div id="PSMA68Ga6.Other_Sources_of_Information"><h3>Other Sources of Information</h3><p>PSMA-related chapters in <a href="/sites/entrez?db=Books&cmd=Search&term=PSMA+AND+micad%5bbook%5d&doptcmdl=TOCView&log%24=booksrch&bname=micad" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">MICAD</a>.</p><p>Alternate names and other information regarding PSMA in the <a href="http://www.hprd.org/alternate?hprd_id=02961&isoform_id=02961_1&isoform_name=Isoform_1" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">Human Protein Reference Database</a>.</p><p><a href="http://clinicaltrials.gov/ct2/results?term=PSMA" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">Clinical trials</a> involving PSMA and PSMA inhibitors.</p><p>Gene information (Gene ID: 2346) for human PSMA in <a href="/protein?Db=gene&Cmd=retrieve&dopt=full_report&list_uids=2346" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">Entrez Gene</a>.</p><p>PSMA1 variant 3 <a href="/nuccore/NM_001193471.1" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">Protein and mRNA sequence</a>.</p><p>Information on PSMA in Online Mendelian Inheritance in Man <a href="/omim/600934" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">(OMIM)</a>.</p></div></div><div id="PSMA68Ga6.Synthesis"><h2 id="_PSMA68Ga6_Synthesis_">Synthesis</h2><p>[<a href="/pubmed?term=%5B68Ga%5D3%20synthesis&cmd=DetailsSearch" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>The synthesis of [<sup>68</sup>Ga]<b>6</b> has been described in detail by Banerjee et al. (<a class="bibr" href="#PSMA68Ga6.REF.3" rid="PSMA68Ga6.REF.3">3</a>). The radiochemical yield and purity of the labeled compound were reported to be 70.0% and >99.0%, respectively. The retention time of [<sup>68</sup>Ga]<b>6</b> on analytical high-performance liquid chromatography (HPLC) was 22.5 min compared with a retention time of 25.0 min for [<sup>68</sup>Ga]<b>3</b>. The specific activity of [<sup>68</sup>Ga]<b>6</b> was reported to be between 3.0 and 6.0 MBq/nmol (81 and 162 μCi/nmol), which was similar to that of [<sup>68</sup>Ga]<b>3</b>. After purification, the radiochemical was dried under vacuum and diluted in 0.9% saline to the desired tracer concentration and used in biodistribution and imaging studies. The stability of [<sup>68</sup>Ga]<b>6</b> under <i>in vitro</i> or <i>in vivo</i> conditions was not reported.</p></div><div id="PSMA68Ga6.In_Vitro_Studies_Testing_in_Ce"><h2 id="_PSMA68Ga6_In_Vitro_Studies_Testing_in_Ce_"><i>In Vitro</i> Studies: Testing in Cells and Tissues</h2><p>[<a href="/pubmed?term=68Ga-3%20in%20vitro&cmd=DetailsSearch" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Using unlabeled <b>6</b> and [<sup>68</sup>Ga]<b>6</b> in a fluorescence-based PSMA inhibition assay, the inhibitory concentrations of these compounds were reported to be 1.23 and 0.44 nM, respectively (<a class="bibr" href="#PSMA68Ga6.REF.3" rid="PSMA68Ga6.REF.3">3</a>). In comparison, the PSMA inhibitory concentrations for unlabeled <b>3</b> and [<sup>68</sup>Ga]<b>3</b> were 2.9 and 29.0 nM, respectively.</p><p>Using a 1-octanol/water mixture with the shake flask method, the partition coefficient of [<sup>68</sup>Ga]<b>6</b> was determined to be −3.9, which was similar to that of [<sup>68</sup>Ga]<b>3</b> (<a class="bibr" href="#PSMA68Ga6.REF.3" rid="PSMA68Ga6.REF.3">3</a>). This indicated that both radiolabeled compounds had a lipophilic nature (<a class="bibr" href="#PSMA68Ga6.REF.3" rid="PSMA68Ga6.REF.3">3</a>). On the basis of the HPLC analysis reported above, [<sup>68</sup>Ga]<b>6</b> appeared to have a slightly higher lipophilicity than [<sup>68</sup>Ga]<b>3</b>.</p></div><div id="PSMA68Ga6.Animal_Studies"><h2 id="_PSMA68Ga6_Animal_Studies_">Animal Studies</h2><div id="PSMA68Ga6.Rodents"><h3>Rodents</h3><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=%22SUBSTANCENAME%22%5BSubstance%20Name%5D%20AND%20rodentia" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>The biodistribution of [<sup>68</sup>Ga]<b>6</b> was studied in severe-combined immunodeficient (SCID) mice bearing <a href="http://www.atcc.org/ATCCAdvancedCatalogSearch/ProductDetails/tabid/452/Default.aspx?ATCCNum=CRL-1435&Template=cellBiology" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PC-3</a>-PIP (transfected with the PSMA gene and expressing high levels of the antigen) and PC-3-FLU (does not express PSMA) cell xenograft tumors (<a class="bibr" href="#PSMA68Ga6.REF.3" rid="PSMA68Ga6.REF.3">3</a>). The mice were injected with the tracer through the tail vein and euthanized 5, 60, 120, and 180 min after the injection (<i>n</i> = 4 mice/time point) to determine the amount of radioactivity accumulated in the tumors and major organs. Results obtained from this study were presented as percent of injected dose per gram tissue (% ID/g). At 5 min post-injection (p.i.), the PSMA-expressing tumor had an uptake of 6.61 ± 0.55% ID/g that decreased to 1.80 ± 0.16% ID/g by 3 h p.i. Non-targeted organs such as kidneys, spleen, and lungs that contain high levels of PSMA showed a high uptake of 64.75 ± 12.00% ID/g, 5.17 ± 2.22% ID/g, and 4.59 ± 0.68% ID/g, respectively, at 5 min p.i. The radioactivity in these organs dropped to 10.04 ± 1.22% ID/g, 0.34 ± 0.09% ID/g, and 0.14 ± 0.03% ID/g, respectively, at 3 h p.i. Similar to [<sup>68</sup>Ga]<b>3</b>, (see below for details), the clearance of radioactivity with [<sup>68</sup>Ga]<b>6</b> from the kidneys was faster than from the PSMA-expressing tumors. In mice injected with [<sup>68</sup>Ga]<b>6</b> PC-3-PIP, the tumor/muscle uptake ratio (T/M) increased from 4.17 at 30 min p.i. to 436.29 at 3 h p.i.; during the same time, the PC-3-FLU tumor T/M ratio increased from 1.67 at 30 min p.i. to 28.70 at 3 h p.i.</p><p>A biodistribution study was also performed with [<sup>68</sup>Ga]<b>3</b> in SCID mice bearing the same tumors as described above (<a class="bibr" href="#PSMA68Ga6.REF.3" rid="PSMA68Ga6.REF.3">3</a>). At 30 min p.i., the [<sup>68</sup>Ga]<b>3</b> uptake of the PC-3-PIP tumors decreased gradually from 3.78 ± 0.09% ID/g to 1.10 ± 0.19% ID/g by 3 h p.i. (uptake in the PC-3-FLU tumors was 0.82 ± 0.20% ID/g at 30 min p.i. and 0.39 ± 0.02% ID/g at 3 h p.i.). During the same period, the label cleared rapidly from the kidneys, decreasing from 97.19 ± 16.07% ID/g at 30 min p.i. to 2.13 ± 0.11% ID/g at 3 h p.i. Except for the bladder, all other organs had <1.0% ID/g incorporation of radioactivity by 3 h p.i. The accumulation of radioactivity in the bladder was 8.96 ± 5.30% ID/g at 30 min p.i.; accumulation increased to 25.29 ± 8.63% ID/g at 60 min p.i. and decreased to 5.39 ± 2.98 at 3 h p.i. This indicated that the tracer was excreted mainly through the urinary route. With [<sup>68</sup>Ga]<b>3</b>, the PC-3-PIP T/M increased from 8.30 at 30 min p.i. to 20.37 at 3 h p.i. In comparison, the T/M for the PC-3-FLU tumors was 1.80 at 30 min p.i. and increased to 7.34 at 3 h p.i.</p><p>For the PET imaging study, a single animal bearing <a href="http://www.atcc.org/ATCCAdvancedCatalogSearch/ProductDetails/tabid/452/Default.aspx?ATCCNum=CRL-1740&Template=cellBiology" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">LNCaP</a> cell (expressing PSMA) tumors was injected intravenously with either [<sup>68</sup>Ga]<b>3</b> or [<sup>68</sup>Ga]<b>6</b> as described by Banerjee et al. (<a class="bibr" href="#PSMA68Ga6.REF.3" rid="PSMA68Ga6.REF.3">3</a>). From the PET images it was clear that both tracers accumulated primarily in the PSMA-positive tumors and the kidneys (the kidneys are known to express PSMA in the proximal renal tubules), similar to the observations made during the biodistribution study. In a blocking study, the tumor-bearing mice (the number of animals used per timepoint was not reported) were injected with 2-(phosphonomethyl)pentanedioic acid (2-PMPA) (50 mg/kg body weight), a known selective ligand of PSMA, and later the animals were injected with the respective tracers (time elapsed between the pretreatment with 2-PMPA and injection of the tracer was not reported). PET images of the animals were acquired at 30 and 60 min p.i., and it was observed that the PSMA-expressing tumors and the kidneys did not accumulate either tracer, suggesting that both radiochemicals bound specifically to the membrane antigen.</p><p>From these studies, the investigators concluded that both [<sup>68</sup>Ga]<b>3</b> and [<sup>68</sup>Ga]<b>6</b> bind specifically to PSMA and could be used for the imaging of PSMA-positive tumors in rodents (<a class="bibr" href="#PSMA68Ga6.REF.3" rid="PSMA68Ga6.REF.3">3</a>). They also mentioned that more animal studies are necessary before these radiochemicals can be evaluated in the clinic.</p></div><div id="PSMA68Ga6.Other_NonPrimate_Mammals"><h3>Other Non-Primate Mammals</h3><p>[<a href="/pubmed?term=68Ga-3%20Non-Primate%20Mammals&cmd=DetailsSearch" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>No references are currently available.</p></div><div id="PSMA68Ga6.NonHuman_Primates"><h3>Non-Human Primates</h3><p>[<a href="/pubmed?term=68Ga-3%20Non-Human%20Primates&cmd=DetailsSearch" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>No references are currently available.</p></div></div><div id="PSMA68Ga6.Human_Studies"><h2 id="_PSMA68Ga6_Human_Studies_">Human Studies</h2><p>[<a href="/pubmed?term=68Ga-3%20Human%20Studies&cmd=DetailsSearch" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>No references are currently available.</p></div><div id="PSMA68Ga6.Supplemental_Information"><h2 id="_PSMA68Ga6_Supplemental_Information_">Supplemental Information</h2><p>[<a href="/books/n/micad/disclaimer/?report=reader">Disclaimers</a>]</p><p>No information is currently available.</p></div><div id="PSMA68Ga6.NIH_Support"><h2 id="_PSMA68Ga6_NIH_Support_">NIH Support</h2><p>These studies were funded by National Institutes of Health grants R01CA134675 and U24 CA92871.</p></div><div id="PSMA68Ga6.References"><h2 id="_PSMA68Ga6_References_">References</h2><dl class="temp-labeled-list"><dl class="bkr_refwrap"><dt>1.</dt><dd><div class="bk_ref" id="PSMA68Ga6.REF.1">Elsasser-Beile U., Buhler P., Wolf P. Targeted therapies for prostate cancer against the prostate specific membrane antigen. <span><span class="ref-journal">Curr Drug Targets. </span>2009;<span class="ref-vol">10</span>(2):118–25.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/19199907" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 19199907</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>2.</dt><dd><div class="bk_ref" id="PSMA68Ga6.REF.2">Dijkgraaf I., Boerman O.C. Radionuclide imaging of tumor angiogenesis. <span><span class="ref-journal">Cancer Biother Radiopharm. </span>2009;<span class="ref-vol">24</span>(6):637–47.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/20025543" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 20025543</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>3.</dt><dd><div class="bk_ref" id="PSMA68Ga6.REF.3">Banerjee S.R., Pullambhatla M., Byun Y., Nimmagadda S., Green G., Fox J.J., Horti A., Mease R.C., Pomper M.G. 68Ga-labeled inhibitors of prostate-specific membrane antigen (PSMA) for imaging prostate cancer. <span><span class="ref-journal">J Med Chem. </span>2010;<span class="ref-vol">53</span>(14):5333–41.</span> [<a href="/pmc/articles/PMC3341619/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC3341619</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/20568777" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 20568777</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>4.</dt><dd><div class="bk_ref" id="PSMA68Ga6.REF.4">Fani M., Andre J.P., Maecke H.R. 68Ga-PET: a powerful generator-based alternative to cyclotron-based PET radiopharmaceuticals. <span><span class="ref-journal">Contrast Media Mol Imaging. </span>2008;<span class="ref-vol">3</span>(2):67–77.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/18383558" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 18383558</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>5.</dt><dd><div class="bk_ref" id="PSMA68Ga6.REF.5">Holland J.P., Williamson M.J., Lewis J.S. Unconventional nuclides for radiopharmaceuticals. <span><span class="ref-journal">Mol Imaging. </span>2010;<span class="ref-vol">9</span>(1):1–20.</span> [<a href="/pmc/articles/PMC4962336/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC4962336</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/20128994" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 20128994</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>6.</dt><dd><div class="bk_ref" id="PSMA68Ga6.REF.6">Chopra, A., [68Ga]-Labeled 2-{3-[5-(7-{1-Benzyloxycarbonyl-5-[2-(4,7,10-tris-carboxymethyl-1,4,7,10-tetraazacyclododec-1-l)acetylamino] [<a href="https://pubmed.ncbi.nlm.nih.gov/21290633" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 21290633</span></a>]</div></dd></dl><li><div class="bk_ref" id="PSMA68Ga6.REF.7">pentylcarbamoyl}-heptanoylamino)-1-carboxypentyl]ureido}pentanedioic acid. Molecular Imaging and Contrast agent Database (MICAD) [database online]. National Library of Medicine, NCBI, Bethesda, MD, USA. Available from <a href="http://www.micad.nih.gov/" ref="pagearea=cite-ref&targetsite=external&targetcat=link&targettype=uri">www<wbr style="display:inline-block"></wbr>​.micad.nih.gov</a>, 2004 -to current.</div></li></dl></div><div id="bk_toc_contnr"></div></div></div><div class="fm-sec"><h2 id="_NBK51314_pubdet_">Publication Details</h2><h3>Author Information and Affiliations</h3><div class="contrib half_rhythm"><span itemprop="author">Arvind Chopra</span>, PhD<div class="affiliation small">National Center for Biotechnology Information, NLM, NIH, Bethesda, MD 20894<div><span class="email-label">Email: </span><a href="mailto:dev@null" data-email="vog.hin.mln.ibcn@dacim" class="oemail">vog.hin.mln.ibcn@dacim</a></div></div></div><h3>Publication History</h3><p class="small">Created: <span itemprop="datePublished">September 27, 2010</span>; Last Update: <span itemprop="dateModified">December 28, 2010</span>.</p><h3>Copyright</h3><div><div class="half_rhythm"><a href="/books/about/copyright/">Copyright Notice</a></div></div><h3>Publisher</h3><p><a href="http://www.ncbi.nlm.nih.gov/" ref="pagearea=page-banner&targetsite=external&targetcat=link&targettype=publisher">National Center for Biotechnology Information (US)</a>, Bethesda (MD)</p><h3>NLM Citation</h3><p>Chopra A. 68Ga-Labeled 2-[3-(1-carboxy-5-{7-[5-carboxy-5-(3-phenyl-2-{3-phenyl-2-[2-(4,7,10-tris-carboxymethyl-1,4,7,10-tetraazacyclododec-1-l)acetylamino]propionylamino}propionylamino)pentylcarbamoyl]heptanoylamino}pentyl)ureido]pentanedioic acid. 2010 Sep 27 [Updated 2010 Dec 28]. 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/Ga68-MUT-DS/?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/NOTABP68Ga/?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="figobPSMA68Ga6Tncchemicalname68galabeled"><div id="PSMA68Ga6.T.nc_chemical_name68galabeled_" class="table"><p class="large-table-link" style="display:none"><span class="right"><a href="/books/NBK51314/table/PSMA68Ga6.T.nc_chemical_name68galabeled_/?report=objectonly" target="object">View in own window</a></span></p><div class="large_tbl" id="__PSMA68Ga6.T.nc_chemical_name68galabeled__lrgtbl__"><table><tbody><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Chemical name:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><sup>68</sup>Ga-Labeled 2-[3-(1-carboxy-5-{7-[5-carboxy-5-(3-phenyl-2-{3-phenyl-2-[2-(4,7,10-tris-carboxymethyl-1,4,7,10-tetraazacyclododec-1-l)acetylamino]propionylamino}<br />propionylamino)pentylcarbamoyl]heptanoylamino}<br />pentyl)ureido]pentanedioic acid</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/99430928" 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=99430928" alt="image 99430928 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:top;">[<sup>68</sup>Ga]<b>6</b></td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Synonym:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"></td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Agent Category:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Compound</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Target:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Prostate-specific membrane antigen (PSMA)</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Target Category:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Antigen</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Method of detection:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Positron emission tomography (PET)</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Source of signal / contrast:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><sup>68</sup>Ga</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Activation:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">No</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Studies:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">
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<ul class="simple-list"><li class="half_rhythm"><div>
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<img alt="Checkbox" src="/corehtml/pmc/css/bookshelf/2.26/img/studies.checkbox.png" />
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<i>In vitro</i>
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</div></li><li class="half_rhythm"><div>
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<img alt="Checkbox" src="/corehtml/pmc/css/bookshelf/2.26/img/studies.checkbox.png" /> Rodents
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</div></li></ul>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Click on the above structure for additional information on [<sup>68</sup>Ga]<b>6</b> 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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