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<script type="text/javascript" src="/corehtml/pmc/jatsreader/ptpmc_3.22/js/jr.boots.min.js"> </script><title>99mTc-Hydrazinonicotinic acid-Glu-{Glu-[cyclo(Arg-Gly-Asp-D-Phe-Lys)]2}2 - Molecular Imaging and Contrast Agent Database (MICAD) - NCBI Bookshelf</title>
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<meta name="citation_author" content="Kam Leung">
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find">&#10008;</a></nav><nav id="jr-fip-info-p"><a id="jr-fip-prev" class="wsprkl btn" title="Jump to previuos match">&#9664;</a><button id="jr-fip-matches">no matches yet</button><a id="jr-fip-next" class="wsprkl btn" title="Jump to next match">&#9654;</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="_NBK23471_"><span class="title" itemprop="name"><sup>99m</sup>Tc-Hydrazinonicotinic acid-Glu-{Glu-[cyclo(Arg-Gly-Asp-<span class="small-caps">D</span>-Phe-Lys)]<sub>2</sub>}<sub>2</sub></span></h1><div itemprop="alternativeHeadline" class="subtitle whole_rhythm"><sup>99m</sup>Tc-HYNIC-E{E[c(RGDfK)]<sub>2</sub>}<sub>2</sub></div><p class="contribs">Leung K.</p><p class="fm-aai"><a href="#_NBK23471_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="figRGDfK4HYNIC99mTcT1"><a href="/books/NBK23471/table/RGDfK4-HYNIC-99mTc.T1/?report=objectonly" target="object" title="Table" class="img_link icnblk_img" rid-ob="figobRGDfK4HYNIC99mTcT1"><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="RGDfK4-HYNIC-99mTc.T1"><a href="/books/NBK23471/table/RGDfK4-HYNIC-99mTc.T1/?report=objectonly" target="object" rid-ob="figobRGDfK4HYNIC99mTcT1">Table</a></h4><p class="float-caption no_bottom_margin">
<i>In vitro</i>
Rodents
</p></div></div><div id="RGDfK4-HYNIC-99mTc.Background"><h2 id="_RGDfK4-HYNIC-99mTc_Background_">Background</h2><p>[<a href="/sites/entrez?Db=pubmed&#x00026;Cmd=DetailsSearch&#x00026;Term=99mTc+RGD" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">PubMed</a>]</p><p>Integrins are a family of heterodimeric glycoproteins on cell surfaces that mediate diverse biological events involving cell-cell and cell-matrix interactions (<a class="bibr" href="#RGDfK4-HYNIC-99mTc.EXTYLES.1" rid="RGDfK4-HYNIC-99mTc.EXTYLES.1">1</a>). Integrins consist of an &#x003b1; and a &#x003b2; subunit and are important for cell adhesion and signal transduction. &#x003b1;<sub>v</sub>&#x003b2;<sub>3</sub> integrin is the most prominent receptor affecting tumor growth, tumor invasiveness, metastasis, tumor-induced angiogenesis, inflammation, osteoporosis, and rheumatoid arthritis (<a href="#RGDfK4-HYNIC-99mTc.EXTYLES.2">2-7</a>). Expression of &#x003b1;<sub>v</sub>&#x003b2;<sub>3</sub> integrin is strong on tumor cells and activated endothelial cells, whereas expression is weak on resting endothelial cells and most normal tissues. &#x003b1;<sub>v</sub>&#x003b2;<sub>3</sub> antagonists are being studied as antitumor and antiangiogenic agents and the agonists as angiogenic agents for coronary angiogenesis (<a class="bibr" href="#RGDfK4-HYNIC-99mTc.EXTYLES.6" rid="RGDfK4-HYNIC-99mTc.EXTYLES.6">6</a>, <a class="bibr" href="#RGDfK4-HYNIC-99mTc.EXTYLES.8" rid="RGDfK4-HYNIC-99mTc.EXTYLES.8">8</a>, <a class="bibr" href="#RGDfK4-HYNIC-99mTc.EXTYLES.9" rid="RGDfK4-HYNIC-99mTc.EXTYLES.9">9</a>). Extracellular matrix proteins (vitronectin, fibrinogen, laminin, and collagen) contain a tripeptide sequence consisting of Arg-Gly-Asp (RGD), which binds to a variety of integrins, including &#x003b1;<sub>v</sub>&#x003b2;<sub>3</sub>. Various radiolabeled antagonists have been introduced for imaging of tumors and tumor angiogenesis (<a class="bibr" href="#RGDfK4-HYNIC-99mTc.EXTYLES.10" rid="RGDfK4-HYNIC-99mTc.EXTYLES.10">10</a>).</p><p>Most of the cyclic RGD peptides are composed of five amino acids. Haubner et al. (<a class="bibr" href="#RGDfK4-HYNIC-99mTc.EXTYLES.11" rid="RGDfK4-HYNIC-99mTc.EXTYLES.11">11</a>) reported that various cyclic RGD peptides exhibit selective inhibition of binding to &#x003b1;<sub>v</sub>&#x003b2;<sub>3</sub> (IC<sub>50</sub>, 7-40 nM) but not to &#x003b1;<sub>v</sub>&#x003b2;<sub>5</sub> (IC<sub>50</sub>, 600-4,000 nM) or &#x003b1;<sub>IIb</sub>&#x003b2;<sub>3</sub> (IC<sub>50</sub>, 700-5,000 nM) integrins. Various radiolabeled cyclic RGD peptides have been found to have high accumulation in tumors in nude mice (<a class="bibr" href="#RGDfK4-HYNIC-99mTc.EXTYLES.12" rid="RGDfK4-HYNIC-99mTc.EXTYLES.12">12</a>). Hydrazinonicotinic acid (HYNIC) is a coupling agent for <sup>99m</sup>Tc labeling of peptides that can achieve high specific activities without affecting receptor-binding ability of the amino acid sequence. Liu et al. (<a class="bibr" href="#RGDfK4-HYNIC-99mTc.EXTYLES.13" rid="RGDfK4-HYNIC-99mTc.EXTYLES.13">13</a>) reported the success of radiolabeling cylco(Arg-Gly-Asp-<span class="small-caps">D</span>-Phe-Lys) (c(RGDfK)) tetramer linked by glutamic acid that was conjugated with HYNIC. Trisodium triphenylphosphine-3,3&#x02019;,3&#x02019;&#x02019;-trisulfonate (TPPTS) and tris(hydroxymethyl)-methylglycine (tricine) were used as coligands. <sup>99m</sup>Tc-HYNIC-E{E[c(RGDfK)]<sub>2</sub>}<sub>2</sub>(tricine)(TPPTS) showed high tumor accumulation in nude mice bearing human tumor xenografts.</p></div><div id="RGDfK4-HYNIC-99mTc.Synthesis"><h2 id="_RGDfK4-HYNIC-99mTc_Synthesis_">Synthesis</h2><p>[<a href="/sites/entrez?Db=pubmed&#x00026;Cmd=DetailsSearch&#x00026;Term=99mTc+RGD+synthesis" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">PubMed</a>]</p><p>Liu et al. (<a class="bibr" href="#RGDfK4-HYNIC-99mTc.EXTYLES.13" rid="RGDfK4-HYNIC-99mTc.EXTYLES.13">13</a>) reported the synthesis of <sup>99m</sup>Tc-HYNIC-E{E[c(RGDfK)]<sub>2</sub>}<sub>2</sub>(tricine)(TPPTS) by incubation of 20 &#x003bc;g HYNIC-E{E[c(RGDfK)]<sub>2</sub>}<sub>2</sub>, 6.5 mg tricine, 5 mg TPPTS, and 1.85 GBq (50 mCi ) Na[<sup>99m</sup>TcO<sub>4</sub>] for 20-25 min at 100&#x000ba;C. Radiochemical purity was &#x0003e;95%.</p></div><div id="RGDfK4-HYNIC-99mTc.In_Vitro_Studies_Tes"><h2 id="_RGDfK4-HYNIC-99mTc_In_Vitro_Studies_Tes_"><i>In Vitro</i> Studies: Testing in Cells and Tissues</h2><p>[<a href="/sites/entrez?Db=pubmed&#x00026;Cmd=DetailsSearch&#x00026;Term=99mTc+RGD+in+vitro" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">PubMed</a>]</p><p>Using a receptor-binding assay with <sup>125</sup>I-echistatin to &#x003b1;<sub>v</sub>&#x003b2;<sub>3</sub> integrin receptors on cell surface of MDA-MB-435 human breast cancer cells, Liu et al. (<a class="bibr" href="#RGDfK4-HYNIC-99mTc.EXTYLES.13" rid="RGDfK4-HYNIC-99mTc.EXTYLES.13">13</a>) reported that E{E[c(RGDfK)]<sub>2</sub>}<sub>2</sub> and E[c(RGDfK)]<sub>2</sub> had IC<sub>50</sub> values of 51 &#x000b1; 11 and 78 &#x000b1; 27 nM, respectively. IC<sub>50</sub> values for HYNIC-E{E[c(RGDfK)]<sub>2</sub>}<sub>2</sub> and HYNIC-E[c(RGDfK)]<sub>2</sub> were 55 &#x000b1; 11 and 52 &#x000b1; 9 nM, respectively. The <i>in vitro</i> solution stability of <sup>99m</sup>Tc-HYNIC-E{E[c(RGDfK)]<sub>2</sub>}<sub>2</sub>(tricine)(TPPTS) was tested by incubating the radiolabeled peptide in buffer solution that contained 1.0 mg/ml cysteine at 37&#x000ba;C for up to 12 h. No significant degradation of <sup>99</sup>Tc-HYNIC-E{E[c(RGDfK)]<sub>2</sub>}<sub>2</sub>(tricine)(TPPTS) was observed under this condition.</p></div><div id="RGDfK4-HYNIC-99mTc.Animal_Studies"><h2 id="_RGDfK4-HYNIC-99mTc_Animal_Studies_">Animal Studies</h2><div id="RGDfK4-HYNIC-99mTc.Rodents"><h3>Rodents</h3><p>[<a href="/sites/entrez?Db=pubmed&#x00026;Cmd=DetailsSearch&#x00026;Term=99mTc+RGD+rodentia" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">PubMed</a>]</p><p>Liu et al. (<a class="bibr" href="#RGDfK4-HYNIC-99mTc.EXTYLES.13" rid="RGDfK4-HYNIC-99mTc.EXTYLES.13">13</a>) performed biodistribution studies of <sup>99m</sup>Tc-HYNIC-E{E[c(RGDfK)]<sub>2</sub>}<sub>2</sub>(tricine)(TPPTS) in nude mice bearing MDA-MB-435 tumors. Tumor uptake was 5.60 &#x000b1; 0.87% ID/g at 5 min after injection and increased to 7.30 &#x000b1; 1.32% ID/g at 120 min. The uptakes of the tetramer in the tumor were significantly higher than that of the dimer (3.50% ID/g at 5 min and 3.82% ID/g at 120 min). Tumor/blood ratios were similar at all time points with highest at 24 h with a value of 63 for both compounds. At all time points, retention of the tetramer in the kidney (33.05% ID/g at 5 min and 25.93% ID/g at 120 min) was significantly higher as compared to the dimer (24.15% ID/g at 5 min and 14.33% ID/g at 120 min). Both peptides exhibited similar accumulation in the spleen, liver and lung. The tumor/blood, tumor/liver and tumor/lung ratios were significantly better than those of the dimer at 30-120 min after injection.</p><p>Co-injection of E-[c(RGDfK)]<sub>2</sub> (30 mg/kg) with <sup>99m</sup>Tc-HYNIC-E{E[c(RGDfK)]<sub>2</sub>}<sub>2</sub>(tricine)(TPPTS) resulted in a significant reduction of radioactivity in the tumor, lung, liver, spleen, and intestine. The radioactivity in the kidney and muscle was also slightly reduced. SPECT imaging in nude mice bearing MDA-MB-435 tumors with 15 MBq (0.41 mCi) of <sup>99m</sup>Tc-HYNIC-E{E[c(RGDfK)]<sub>2</sub>}<sub>2</sub>(tricine)(TPPTS) revealed that the tumors were clearly visualized at 1, 2, and 4 h after injection with low radioactivity levels in the liver and lungs.</p></div><div id="RGDfK4-HYNIC-99mTc.Other_NonPrimate_Mam"><h3>Other Non-Primate Mammals</h3><p>[<a href="/sites/entrez?Db=pubmed&#x00026;Cmd=DetailsSearch&#x00026;Term=99mTc+RGD+(dog+or+pig+or+sheep+or+rabbit)" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">PubMed</a>]</p><p>No publication is currently available.</p></div><div id="RGDfK4-HYNIC-99mTc.NonHuman_Primates"><h3>Non-Human Primates</h3><p>[<a href="/sites/entrez?Db=pubmed&#x00026;Cmd=DetailsSearch&#x00026;Term=99mTc+RGD+(primate+not+human)" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">PubMed</a>]</p><p>No publication is currently available.</p></div></div><div id="RGDfK4-HYNIC-99mTc.Human_Studies"><h2 id="_RGDfK4-HYNIC-99mTc_Human_Studies_">Human Studies</h2><p>[<a href="/sites/entrez?Db=pubmed&#x00026;Cmd=DetailsSearch&#x00026;Term=99mTc+RGD+human" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">PubMed</a>]</p><p>No publication is currently available.</p></div><div id="RGDfK4-HYNIC-99mTc.NIH_Support"><h2 id="_RGDfK4-HYNIC-99mTc_NIH_Support_">NIH Support</h2><p>R01 CA115883-01A2</p></div><div id="RGDfK4-HYNIC-99mTc.references"><h2 id="_RGDfK4-HYNIC-99mTc_references_">References</h2><dl class="temp-labeled-list"><dl class="bkr_refwrap"><dt>1.</dt><dd><div class="bk_ref" id="RGDfK4-HYNIC-99mTc.EXTYLES.1">Hynes R.O. 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</span>(2):438&ndash;46.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/17341108" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 17341108</span></a>]</div></dd></dl></dl></div><div id="bk_toc_contnr"></div></div></div><div class="fm-sec"><h2 id="_NBK23471_pubdet_">Publication Details</h2><h3>Author Information and Affiliations</h3><div class="contrib half_rhythm"><span itemprop="author">Kam Leung</span>, PhD<div class="affiliation small">
National Center for Biotechnology Information, NLM, NIH,
<span class="before-email-separator"></span><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><h3>Publication History</h3><p class="small">Created: <span itemprop="datePublished">July 15, 2007</span>; Last Update: <span itemprop="dateModified">August 31, 2007</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&amp;targetsite=external&amp;targetcat=link&amp;targettype=publisher">National Center for Biotechnology Information (US)</a>, Bethesda (MD)</p><h3>NLM Citation</h3><p>Leung K. 99mTc-Hydrazinonicotinic acid-Glu-{Glu-[cyclo(Arg-Gly-Asp-D-Phe-Lys)]2}2. 2007 Jul 15 [Updated 2007 Aug 31]. 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/RGDfK2-HYNIC-99mTc/?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/scVEGF-HYNIC-99mTc/?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="figobRGDfK4HYNIC99mTcT1"><div id="RGDfK4-HYNIC-99mTc.T1" class="table"><p class="large-table-link" style="display:none"><span class="right"><a href="/books/NBK23471/table/RGDfK4-HYNIC-99mTc.T1/?report=objectonly" target="object">View in own window</a></span></p><div class="large_tbl" id="__RGDfK4-HYNIC-99mTc.T1_lrgtbl__"><table><tbody><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
<b>Chemical name:</b>
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><sup>99m</sup>Tc-Hydrazinonicotinic acid-Glu-{Glu-[cyclo(Arg-Gly-Asp-<span class="small-caps">D</span>-Phe-Lys)]<sub>2</sub>}<sub>2</sub></td><td rowspan="9" colspan="1" style="text-align:left;vertical-align:middle;">
<a href="https://pubchem.ncbi.nlm.nih.gov/substance/26671687" title="View this structure in PubChem" class="img_link" ref="pagearea=body&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubchem"><img src="https://pubchem.ncbi.nlm.nih.gov/image/imgsrv.fcgi?t=l&amp;sid=26671687" alt="image 26671687 in the ncbi pubchem database" /></a>
</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
<b>Abbreviated name:</b>
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><sup>99m</sup>Tc-HYNIC-E{E[c(RGDfK)]<sub>2</sub>}<sub>2</sub></td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
<b>Synonym:</b>
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"></td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
<b>Agent Category:</b>
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Peptide</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
<b>Target:</b>
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Integrin &#x003b1;<sub>v</sub>&#x003b2;<sub>3</sub></td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
<b>Target Category:</b>
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Receptor binding</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
<b>Method of detection:</b>
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">SPECT, gamma planar imaging</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
<b>Source of signal:</b>
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><sup>99m</sup>Tc</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
<b>Activation:</b>
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">No</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
<b>Studies:</b>
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">
<ul class="simple-list"><li class="half_rhythm"><div>
<img alt="Checkbox" src="/corehtml/pmc/css/bookshelf/2.26/img/studies.checkbox.png" />
<i>In vitro</i>
</div></li></ul>
<ul class="simple-list"><li class="half_rhythm"><div>
<img alt="Checkbox" src="/corehtml/pmc/css/bookshelf/2.26/img/studies.checkbox.png" /> Rodents
</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&amp;targetsite=external&amp;targetcat=link&amp;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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