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<script type="text/javascript" src="/corehtml/pmc/jatsreader/ptpmc_3.22/js/jr.boots.min.js"> </script><title>99mTc-ethylenediamine N,N&rsquo;-diacetic acid/hydrazinonicotinamide-Tyr3-octreotide - Molecular Imaging and Contrast Agent Database (MICAD) - NCBI Bookshelf</title>
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<meta name="citation_title" content="99mTc-ethylenediamine N,N&rsquo;-diacetic acid/hydrazinonicotinamide-Tyr3-octreotide">
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<meta name="citation_date" content="2007/11/07">
<meta name="citation_author" content="Arvind Chopra">
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<meta name="description" content="Somatostatin (SS) is a cyclic peptide that is primarily expressed in the central nervous system and some peripheral tissues (1). Receptors for SS have been identified in the central nervous system, cells of neuroendocrine origin, the gastrointestinal tract, and even in lymphocytes (2). The SS receptor has a seven-transmembrane domain structure and belongs to the G-protein&ndash;coupled receptor family. Five subtypes of the SS receptor have been identified, and each subtype is produced from a single gene located on a different chromosome. This indicates tissue-specific regulation of SS receptor expression and suggests that each subtype has a distinct function in the various organs (2). Because of its several physiological functions, SS is considered to be a neurotransmitter or a hormone that acts through the autocrine and paracrine processes (3). In general, SS inhibits the production of hormones from various glands. SS has been evaluated for the treatment of various diseases, including cancers of endocrine origin as a result of hyperactive glands. However, SS has a short plasma half-life because of rapid enzymatic degradation and has been observed to be ineffective for such therapy (2). The development of SS analogs resistant to enzymatic degradation, but with a biological activity similar to SS, led to the application of these analogs for the treatment of cancerous tumors (4, 5).">
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<meta name="og:description" content="Somatostatin (SS) is a cyclic peptide that is primarily expressed in the central nervous system and some peripheral tissues (1). Receptors for SS have been identified in the central nervous system, cells of neuroendocrine origin, the gastrointestinal tract, and even in lymphocytes (2). The SS receptor has a seven-transmembrane domain structure and belongs to the G-protein&ndash;coupled receptor family. Five subtypes of the SS receptor have been identified, and each subtype is produced from a single gene located on a different chromosome. This indicates tissue-specific regulation of SS receptor expression and suggests that each subtype has a distinct function in the various organs (2). Because of its several physiological functions, SS is considered to be a neurotransmitter or a hormone that acts through the autocrine and paracrine processes (3). In general, SS inhibits the production of hormones from various glands. SS has been evaluated for the treatment of various diseases, including cancers of endocrine origin as a result of hyperactive glands. However, SS has a short plasma half-life because of rapid enzymatic degradation and has been observed to be ineffective for such therapy (2). The development of SS analogs resistant to enzymatic degradation, but with a biological activity similar to SS, led to the application of these analogs for the treatment of cancerous tumors (4, 5).">
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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="_NBK23551_"><span class="title" itemprop="name"><sup>99m</sup>Tc-ethylenediamine <i>N,N&#x02019;</i>-diacetic acid/hydrazinonicotinamide-Tyr<sup>3</sup>-octreotide</span></h1><div itemprop="alternativeHeadline" class="subtitle whole_rhythm"><sup>99m</sup>Tc-HYNIC-TOC</div><p class="contribs">Chopra A.</p><p class="fm-aai"><a href="#_NBK23551_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="figHYNICTOC99mTcT1"><a href="/books/NBK23551/table/HYNICTOC99mTc.T1/?report=objectonly" target="object" title="Table" class="img_link icnblk_img" rid-ob="figobHYNICTOC99mTcT1"><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="HYNICTOC99mTc.T1"><a href="/books/NBK23551/table/HYNICTOC99mTc.T1/?report=objectonly" target="object" rid-ob="figobHYNICTOC99mTcT1">Table</a></h4><p class="float-caption no_bottom_margin">
<i>In vitro</i>
Rodents
</p></div></div><div id="HYNICTOC99mTc.Background"><h2 id="_HYNICTOC99mTc_Background_">Background</h2><p>[<a href="/sites/entrez?Db=pubmed&#x00026;Cmd=DetailsSearch&#x00026;Term=99mTc-HYNIC-TOC" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">PubMed</a>]</p><p>Somatostatin (SS) is a cyclic peptide that is primarily expressed in the central nervous system and some peripheral tissues (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.1" rid="HYNICTOC99mTc.EXTYLES.1">1</a>). Receptors for SS have been identified in the central nervous system, cells of neuroendocrine origin, the gastrointestinal tract, and even in lymphocytes (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.2" rid="HYNICTOC99mTc.EXTYLES.2">2</a>). The SS receptor has a seven-transmembrane domain structure and belongs to the G-protein&#x02013;coupled receptor family. Five subtypes of the SS receptor have been identified, and each subtype is produced from a single gene located on a different chromosome. This indicates tissue-specific regulation of SS receptor expression and suggests that each subtype has a distinct function in the various organs (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.2" rid="HYNICTOC99mTc.EXTYLES.2">2</a>). Because of its several physiological functions, SS is considered to be a neurotransmitter or a hormone that acts through the autocrine and paracrine processes (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.3" rid="HYNICTOC99mTc.EXTYLES.3">3</a>). In general, SS inhibits the production of hormones from various glands. SS has been evaluated for the treatment of various diseases, including cancers of endocrine origin as a result of hyperactive glands. However, SS has a short plasma half-life because of rapid enzymatic degradation and has been observed to be ineffective for such therapy (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.2" rid="HYNICTOC99mTc.EXTYLES.2">2</a>). The development of SS analogs resistant to enzymatic degradation, but with a biological activity similar to SS, led to the application of these analogs for the treatment of cancerous tumors (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.4" rid="HYNICTOC99mTc.EXTYLES.4">4</a>, <a class="bibr" href="#HYNICTOC99mTc.EXTYLES.5" rid="HYNICTOC99mTc.EXTYLES.5">5</a>).</p><p>The mechanism by which SS and its analogs inhibit tumor growth was detailed by Moody et al. (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.6" rid="HYNICTOC99mTc.EXTYLES.6">6</a>). A cyclic octapeptide SS analog, octreotide, was synthesized and conjugated with diethylenetriamine pentaacetic acid (DTPA) for chelating radioactive indium (<sup>111</sup>In) to obtain <sup>111</sup>In-DPTA-octreotide (<sup>111</sup>In-DPTA-OCT). On binding to the SS receptor, <sup>111</sup>In-DPTA-OCT is rapidly internalized and results in accumulation of the radiochemical in the tumor cells. Subsequently, the tumors can be detected by scintigraphy and treated with radiolabeled peptides (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.6" rid="HYNICTOC99mTc.EXTYLES.6">6</a>). Although <sup>111</sup>In-DPTA-OCT is considered suitable for the detection and diagnosis of tumors bearing SS receptors, the use of <sup>111</sup>In as a radionuclide has some limitations. This radioelement has limited availability, a long physical half-life (67 h), high gamma energy that results in increased radiation exposure of the patient, and suboptimal image characteristics (7, 8). Therefore, Decristoforo et al. used radioactive technetium (<sup>99m</sup>Tc) with a half-life of 6 h to generate <sup>99m</sup>Tc-labeled hydrazinonicotinamide-Tyr<sup>3</sup>-octreotide (<sup>99m</sup>Tc-HYNIC-TOC), a radiochemical with superior imaging properties compared to <sup>111</sup>In-DPTA-octreotide (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.9" rid="HYNICTOC99mTc.EXTYLES.9">9</a>). This chapter describes the synthesis, <i>in vitro</i> and <i>in vivo</i>, and clinical studies performed with <sup>99m</sup>Tc-HYNIC-TOC.</p></div><div id="HYNICTOC99mTc.Synthesis"><h2 id="_HYNICTOC99mTc_Synthesis_">Synthesis</h2><p>[<a href="/sites/entrez?Db=pubmed&#x00026;Cmd=DetailsSearch&#x00026;Term=99mTc+HYNIC+TOC+synthesis" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">PubMed</a>]</p><p>The synthesis of Tyr<sup>3</sup>-octreotide (TOC) has been described elsewhere (<a href="#HYNICTOC99mTc.EXTYLES.9">9-11</a>). TOC and Lys<sup>5</sup>(butoxycarbonyl)-TOC (Lys<sup>5</sup>(BOC)-TOC) were purchased commercially. For the synthesis of HYNIC-TOC, 6-butoxycarbonyl-HYNIC, O-(7-azabenzotriazolyl)-1,1,3,3-tetramethyl-uronium hexafluorophosphate, and diisopropylethylamine dissolved in dimethylformamide (DMF) were allowed to react for 15 min at room temperature. This mixture was added to a solution of Lys<sup>5</sup>(BOC)-TOC in DMF and water, and the reaction was allowed to proceed for 1 h. The products of this reaction were purified on a SepPak column, and the derivative peptide was deprotected with trifluoroacetic acid containing thioanisole. The deprotected HYNIC-TOC was then purified by high-performance liquid chromatography (HPLC) (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.9" rid="HYNICTOC99mTc.EXTYLES.9">9</a>, <a class="bibr" href="#HYNICTOC99mTc.EXTYLES.10" rid="HYNICTOC99mTc.EXTYLES.10">10</a>).</p><p>Radiolabeling of HYNIC-TOC was performed in an ethylenediamine diacetic acid (EDDA) solution (pH 7.0). The HYNIC-TOC was mixed with a solution of pertechnetate (<sup>99m</sup>TcO<sub>4</sub><sup>-</sup>) containing tin in 0.1 N nitrogen-purged hydrochloric acid (HCl). The reaction was carried out at room temperature for 60 min, and the radiolabeled HYNIC-TOC was separated from free pertechnetate by HPLC (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.9" rid="HYNICTOC99mTc.EXTYLES.9">9</a>, <a class="bibr" href="#HYNICTOC99mTc.EXTYLES.10" rid="HYNICTOC99mTc.EXTYLES.10">10</a>). The mean radiochemical yield of the reaction was 63.6% and the radiochemical purity (RCP) of the product was &#x0003e;98% (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.9" rid="HYNICTOC99mTc.EXTYLES.9">9</a>, <a class="bibr" href="#HYNICTOC99mTc.EXTYLES.10" rid="HYNICTOC99mTc.EXTYLES.10">10</a>). The specific activity of <sup>99m</sup>Tc-HYNIC-TOC was reported by the investigators to be ~37 GBq/&#x003bc;mol (1 Ci/&#x003bc;mol) (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.9" rid="HYNICTOC99mTc.EXTYLES.9">9</a>). The labeled HYNIC-TOC was stable as an aqueous solution for at least 24 h and in human plasma for at least 4 h. In human plasma, some of the labeled peptide (amount not provided by the investigators) bound to the plasma proteins that were precipitated by acetonitrile (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.9" rid="HYNICTOC99mTc.EXTYLES.9">9</a>).</p><p><sup>99m</sup>Tc-HYNIC-TOC has also been prepared by the coligand exchange of EDDA and tricine as detailed by von Guggenberg et al. (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.12" rid="HYNICTOC99mTc.EXTYLES.12">12</a>). For this, HYNIC-TOC was incubated with EDDA (dissolved in 0.1 N HCl), tricine (in 2.0 M phosphate buffer (pH 6.0)) and tin (dissolved in nitrogen-purged 0.1 N HCl). Pertechnetate was added to the solution and the mixture was boiled for 10 min. The RCP of the product was &#x0003e;90%. Specific activity of the radiochemical generated by this method was not provided by the investigators (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.12" rid="HYNICTOC99mTc.EXTYLES.12">12</a>).</p><p>HYNIC-TOC is also available as a freeze-dried kit for labeling with <sup>99m</sup>TcO<sub>4</sub><sup>-</sup> (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.8" rid="HYNICTOC99mTc.EXTYLES.8">8</a><a class="bibr" href="#HYNICTOC99mTc.EXTYLES.11" rid="HYNICTOC99mTc.EXTYLES.11">11</a>). To generate the kit, HYNIC-TOC was dissolved in ethanol and tin chloride in 0.1 N nitrogen-purged HCl just before use. These solutions were dispensed in a solution containing EDDA, tricine, and mannitol. The solution mixture was dispensed into glass vials and frozen immediately to &#x0003c;&#x02013;50&#x000b0;C. The freeze-drying was then initiated as detailed by von Guggenberg et al. (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.8" rid="HYNICTOC99mTc.EXTYLES.8">8</a>). Upon completion of the freeze-drying procedure, the vials were capped under vacuum and stored at 2&#x02013;8&#x000b0;C. To radiolabel the peptide, the freeze-dried formulation was reconstituted in 0.2 M phosphate buffer in the vial (pH 6&#x02013;7) and pertechnetate was added to it immediately. The mixture was then boiled for 10 min. The labeled product was analyzed by HPLC and thin-layer chromatography (TLC). A number of batches (<i>n</i> = 10) were prepared and evaluated for labeling over 1 year (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.8" rid="HYNICTOC99mTc.EXTYLES.8">8</a>). All preparations yielded a product with &#x0003e;90% RCP as determined by HPLC and TLC. The reconstituted product labeled over a 24-h period had a RCP of &#x0003e;90%.</p><p>Gonz&#x000e1;lez-V&#x000e1;zquez et al. determined the RCP of the labeled product from the reconstituted freeze-dried kit by instant TLC on silica gel and HPLC (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.11" rid="HYNICTOC99mTc.EXTYLES.11">11</a>). Three different mobile phases were used to determine the purity by instant TLC: 2-butanone for <sup>99m</sup>TcO<sub>4</sub><sup>-</sup> (Rf = 1), 0.1 M sodium citrate (pH 5.0) for the <sup>99m</sup>Tc-coligand and <sup>99m</sup>TcO<sub>4</sub><sup>-</sup> (Rf = 1), and methanol:1 M ammonium acetate (1:1 v/v) for <sup>99m</sup>Tc-colloid (Rf = 0). The radiolabeled peptide had Rf values of 0.0, 0.0, and 0.7&#x02013;1.0, respectively, in the three mobile phases. The specific activity of the labeled product was not provided by the investigators (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.11" rid="HYNICTOC99mTc.EXTYLES.11">11</a>). In one study, <sup>111</sup>In-DPTA-OCT, prepared from a commercial kit, was used for comparison (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.10" rid="HYNICTOC99mTc.EXTYLES.10">10</a>).</p></div><div id="HYNICTOC99mTc.In_Vitro_Studies_Tes"><h2 id="_HYNICTOC99mTc_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+HYNIC-TOC+in+vitro" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">PubMed</a>]</p><p>The <i>in vitro</i> properties of <sup>99m</sup>Tc-HYNIC-TOC were investigated with AR42J cells, a rat pancreatic cell line (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.9" rid="HYNICTOC99mTc.EXTYLES.9">9</a>, <a class="bibr" href="#HYNICTOC99mTc.EXTYLES.10" rid="HYNICTOC99mTc.EXTYLES.10">10</a>). The labeled peptide had a dissociation constant of 2.6 nmol/L for the receptor. Rapid internalization of the labeled compound, which increased with time (5% per milligram protein at 80 min), was observed in receptor binding studies with intact cells (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.10" rid="HYNICTOC99mTc.EXTYLES.10">10</a>). During the same period, the surface-bound activity remained at &#x0003c;1% per milligram protein during the same period.</p></div><div id="HYNICTOC99mTc.Animal_Studies"><h2 id="_HYNICTOC99mTc_Animal_Studies_">Animal Studies</h2><div id="HYNICTOC99mTc.Rodents"><h3>Rodents</h3><p>[<a href="/sites/entrez?Db=pubmed&#x00026;Cmd=DetailsSearch&#x00026;Term=99mTc+HYNIC-TOC+rodentia" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">PubMed</a>]</p><p>The biodistribution of <sup>99m</sup>Tc-HYNIC-TOC was investigated in nude mice bearing AR42J or HepG2 (a human hepatocellular carcinoma cell line) cell tumors (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.10" rid="HYNICTOC99mTc.EXTYLES.10">10</a>, <a class="bibr" href="#HYNICTOC99mTc.EXTYLES.13" rid="HYNICTOC99mTc.EXTYLES.13">13</a>). Mice with the AR42J pancreatic cell tumors (<i>n</i> = 8) were studied for <sup>99m</sup>Tc-HYNIC-TOC uptake between 10 and 30 days after the growth of tumors (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.10" rid="HYNICTOC99mTc.EXTYLES.10">10</a>). Eight animals were injected with the radiolabeled peptide through the tail vein. Among these, four animals had been treated with cold HYNIC-TOC 30 min before administration of the radiochemical. A significant difference in the uptake (<i>P</i> &#x0003c; 0.05) was observed between the blocked and unblocked animals. Approximately 9.6% of the injected dose per gram tissue (% ID/g) of the label accumulated in the tumors of the unblocked animals. This value was ~1.8% ID/g for the blocked animals. Residual activity was also found in the blood (~0.28% ID/g), liver (~1.06% ID/g), gut (~1.58% ID/g), pancreas (~0.45% ID/g), and kidneys (~4.7% ID/g) of the unblocked animals. The tumor/organ ratios for the accumulation of radioactivity were 33.97, 9.11, 31.29, and 2.05 for the blood, liver, muscle, and kidneys, respectively. Compared to <sup>111</sup>In-DPTA-OCT, the accumulation was comparable in the liver and the gut, approximately half in the blood and muscles, and approximately 10-fold higher in the kidneys (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.10" rid="HYNICTOC99mTc.EXTYLES.10">10</a>).</p><p>In the second study, groups of nude mice (a subcutaneous group and an intra-liver group) (<i>n</i> = 3 in each group) bearing HepG2 cell tumors were injected with <sup>99m</sup>Tc-HYNIC-TOC through the caudal vein and imaged at 2 h and 4.5 h after the injection (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.13" rid="HYNICTOC99mTc.EXTYLES.13">13</a>). Accumulation of radioactivity in the tumor xenografts in both animal groups was observed. The label was retained in the kidneys and excreted through the bladder. The investigators suggested that accumulation of label in the kidneys was probably because of nonspecific uptake by the tubulus cells. This can lead to nephrotoxicity, and the investigators recommended that <sup>99m</sup>Tc-HYNIC-TOC should be carefully evaluated further before use in humans (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.13" rid="HYNICTOC99mTc.EXTYLES.13">13</a>).</p><p>The accumulation of <sup>99m</sup>Tc-<a href="http://www.chemocare.com/bio/octreotide_acetate.asp" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">octreotide</a> (commercially available) and <sup>99m</sup>Tc-HYNIC-TOC in rat kidneys was investigated and compared by Kopecky et al. (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.14" rid="HYNICTOC99mTc.EXTYLES.14">14</a>). In rat kidney perfusion experiments, the investigators observed that <sup>99m</sup>Tc-octreotide had a three-fold lower clearance value compared to <sup>99m</sup>Tc-HYNIC-TOC. The accumulation of <sup>99m</sup>Tc-HYNIC-TOC for up to 48 h in the kidneys was suggested to be primarily responsible for the renal excretion of this radiopharmaceutical. The investigators also suggested that the presence of SS receptors, differences in the tonicity levels of the kidneys, and other mechanisms were probably responsible for accumulation of the SS analogs in these organs (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.14" rid="HYNICTOC99mTc.EXTYLES.14">14</a>).</p></div><div id="HYNICTOC99mTc.Other_NonPrimate_Mam"><h3>Other Non-Primate Mammals</h3><p>[<a href="/sites/entrez?Db=pubmed&#x00026;Cmd=DetailsSearch&#x00026;Term=99mTc-HYNIC-TOC+non-primate+mammals" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">PubMed</a>]</p><p>No publications are currently available.</p></div><div id="HYNICTOC99mTc.NonHuman_Primates"><h3>Non-Human Primates</h3><p>[<a href="/sites/entrez?Db=pubmed&#x00026;Cmd=DetailsSearch&#x00026;Term=99mTc-HYNIC-TOC+non-human+primates" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">PubMed</a>]</p><p>No publications are currently available.</p></div></div><div id="HYNICTOC99mTc.Human_Studies"><h2 id="_HYNICTOC99mTc_Human_Studies_">Human Studies</h2><p>[<a href="/sites/entrez?Db=pubmed&#x00026;Cmd=DetailsSearch&#x00026;Term=99mTc-HYNIC-TOC+humans" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">PubMed</a>]</p><p>Li et al. evaluated the use and biodistribution of <sup>99m</sup>Tc-HYNIC-TOC to image endocrine, non-endocrine, and benign tumors in humans (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.15" rid="HYNICTOC99mTc.EXTYLES.15">15</a>). In this study, imaging with <sup>99m</sup>Tc-HYNIC-TOC was also compared to <sup>111</sup>In-pentetreotide and radioiodinated meta-[radioiodinated]iodobenzylguanidine (<sup>131</sup>I-MIBG) tumor imaging of the patients. The <i>in vivo</i> biodistribution of <sup>99m</sup>Tc-HYNIC-TOC was observed to be similar to that of <sup>111</sup>In-pentetreotide, with uptake primarily in the liver, spleen, and kidneys. <sup>99m</sup>Tc-HYNIC-TOC imaging demonstrated intense tumor uptake at 1 hour after injection and revealed more lesions compared to <sup>131</sup>I-MIBG. The investigators concluded that <sup>99m</sup>Tc-HYNIC-TOC was a suitable agent for the detection of SS-positive tumors in humans (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.15" rid="HYNICTOC99mTc.EXTYLES.15">15</a>).</p><p>In another study, the sensitivity, specificity, and accuracy of <sup>99m</sup>Tc-HYNIC-TOC scintigraphy was observed to be 86.4%, 75.0%, and 84.6%, respectively, for imaging in patients with medullary thyroid carcinoma (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.16" rid="HYNICTOC99mTc.EXTYLES.16">16</a>).</p><p>A study to compare the diagnostic efficacy of <a href="http://www.rxlist.com/cgi/generic/neotect.htm" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri"><sup>99m</sup>Tc-depreotide</a> and <sup>99m</sup>Tc-HYNIC-TOC to differentiate between malignant and benign causes of solitary pulmonary nodules was performed in human patients (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.17" rid="HYNICTOC99mTc.EXTYLES.17">17</a>). The investigators reported that <sup>99m</sup>Tc-depreotide accumulated primarily in the spine, sternum, ribs, and lungs (mean lung/heart ratio = 2.2), but no such accumulation was observed with <sup>99m</sup>Tc-EDDA/HYNIC-TOC (mean lung/heart ratio = 0.7). A comparison of scintigrams revealed <sup>99m</sup>Tc-depreotide provided higher-quality images compared to <sup>99m</sup>Tc-EDDA/HYNIC-TOC. In addition, <sup>99m</sup>Tc-depreotide showed a higher accumulation than <sup>99m</sup>Tc-EDDA/HYNIC-TOC in lung tumors compared to blood pool (heart): 4.5 &#x000b1; 1.05 and 1.8 &#x000b1; 0.29, respectively (<i>P</i> &#x0003c; 0.05). However, the mean tumor/lung background ratios were similar for both radiotracers (2.2 in malignant and 1.4 in benign lesions, respectively). A significantly higher non-uniformity of counts was observed with <sup>99m</sup>Tc-EDDA/HYNIC-TOC compared to <sup>99m</sup>Tc-depreotide (16.4% <i>versus</i> 11.4%; <i>P</i> &#x0003c; 0.01) in the lung background region (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.17" rid="HYNICTOC99mTc.EXTYLES.17">17</a>).</p><p><a href="/sites/entrez?Db=pubmed&#x00026;Cmd=Search&#x00026;Term=%22Gonz%C3%A1lez-V%C3%A1zquez%20A%22%5BAuthor%5D&#x00026;itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsPanel.Pubmed_RVAbstractPlus" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri"><u>Gonz&#x000e1;lez-V&#x000e1;zquez </u></a>et al. studied the biokinetic model for <sup>99m</sup>Tc-HYNIC-TOC prepared from lyophilized kits and evaluated its dosimetry as a tumor-imaging agent in patients with histologically confirmed neuroendocrine tumors (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.11" rid="HYNICTOC99mTc.EXTYLES.11">11</a>). Whole-body images from patients were acquired between 5 min and 24 h after administration of <sup>99m</sup>Tc-HYNIC-TOC. The images showed an average tumor/blood (heart) ratio of 4.3 &#x000b1; 0.7 in receptor-positive tumors at 1 h. The mean absorbed radiation doses calculated for this study with the use of 740 MBq (20 mCi) of <sup>99m</sup>Tc-HYNIC-TOC were 24, 21.5, 5.5, and 1.0 mSv (2.4, 2.15, 0.55, and 0.1 rem) for spleen, kidneys, liver, and bone marrow, respectively; the radiochemical had an effective dose of 4.4 mSv (0.44 rem) (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.11" rid="HYNICTOC99mTc.EXTYLES.11">11</a>).</p><p><sup>99m</sup>Tc-HYNIC-TOC scintigraphy was used to assess the retrobulbar irradiation response in Graves' ophthalmopathy (GO) patients (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.7" rid="HYNICTOC99mTc.EXTYLES.7">7</a>). Patients were treated with <a href="http://www.drugs.com/pro/octreoscan.html" ref="pagearea=body&amp;targetsite=external&amp;targetcat=link&amp;targettype=uri">octreoscan</a> followed by retrobulbar irradiation therapy. The response to therapy was then assessed 3 months after start of the treatment. Of the 14 GO patients enrolled in the study, 8 (57.1%) patients responded to retrobulbar radiotherapy and 6 (42.9%) patients were non-responders. Using the orbital/occipital ratio, the 8 responders were compared to the 6 non-responders for the orbital uptake of <sup>99m</sup>Tc-HYNIC-TOC. At 4 h after administration, <sup>99m</sup>Tc-HYNIC-TOC scintigraphy showed that the responders had a higher (<i>P</i> = 0.001) orbital/occipital uptake ratio than the non-responders, and a significant correlation (<i>P</i> = 0.034) was observed between the orbital/occipital ratio and the clinical activity score of the study. It was also observed that the 8 patients who responded to therapy were also positive for scintigraphy, but 5 of the 6 non-responding patients were negative for scintigraphy. The investigators concluded that orbital <sup>99m</sup>Tc-HYNIC-TOC scintigraphy was useful for the estimation of disease activity and for the prediction of the response to subsequent radiotherapy in GO patient, and that patients who were positive for octreoscan were more likely to respond to irradiation therapy (<a class="bibr" href="#HYNICTOC99mTc.EXTYLES.7" rid="HYNICTOC99mTc.EXTYLES.7">7</a>).</p></div><div id="HYNICTOC99mTc.references"><h2 id="_HYNICTOC99mTc_references_">References</h2><dl class="temp-labeled-list"><dl class="bkr_refwrap"><dt>1.</dt><dd><div class="bk_ref" id="HYNICTOC99mTc.EXTYLES.1">Hofland L.J. , Lamberts S.W.
The pathophysiological consequences of somatostatin receptor internalization and resistance. <span><span class="ref-journal">Endocr Rev. </span>2003;<span class="ref-vol">
<strong>24</strong>
</span>(1):28&ndash;47.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/12588807" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 12588807</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>2.</dt><dd><div class="bk_ref" id="HYNICTOC99mTc.EXTYLES.2">Breeman W.A. , Kwekkeboom D.J. , de Blois E. , de Jong M. , Visser T.J. , Krenning E.P.
Radiolabelled regulatory peptides for imaging and therapy. <span><span class="ref-journal">Anticancer Agents Med Chem. </span>2007;<span class="ref-vol">
<strong>7</strong>
</span>(3):345&ndash;57.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/17504160" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 17504160</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>3.</dt><dd><div class="bk_ref" id="HYNICTOC99mTc.EXTYLES.3">Reubi J.C.
Peptide receptors as molecular targets for cancer diagnosis and therapy. <span><span class="ref-journal">Endocr Rev. </span>2003;<span class="ref-vol">
<strong>24</strong>
</span>(4):389&ndash;427.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/12920149" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 12920149</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>4.</dt><dd><div class="bk_ref" id="HYNICTOC99mTc.EXTYLES.4">Forrer F. , Waldherr C. , Maecke H.R. , Mueller-Brand J.
Targeted radionuclide therapy with 90Y-DOTATOC in patients with neuroendocrine tumors. <span><span class="ref-journal">Anticancer Res. </span>2006;<span class="ref-vol">
<strong>26</strong>
</span>(1B):703&ndash;7.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/16739341" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 16739341</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>5.</dt><dd><div class="bk_ref" id="HYNICTOC99mTc.EXTYLES.5">Koukouraki S. , Strauss L.G. , Georgoulias V. , Schuhmacher J. , Haberkorn U. , Karkavitsas N. , Dimitrakopoulou-Strauss A.
Evaluation of the pharmacokinetics of 68Ga-DOTATOC in patients with metastatic neuroendocrine tumours scheduled for 90Y-DOTATOC therapy. <span><span class="ref-journal">Eur J Nucl Med Mol Imaging. </span>2006;<span class="ref-vol">
<strong>33</strong>
</span>(4):460&ndash;6.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/16437218" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 16437218</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>6.</dt><dd><div class="bk_ref" id="HYNICTOC99mTc.EXTYLES.6">Moody T.W. , Chan D. , Fahrenkrug J. , Jensen R.T.
Neuropeptides as autocrine growth factors in cancer cells. <span><span class="ref-journal">Curr Pharm Des. </span>2003;<span class="ref-vol">
<strong>9</strong>
</span>(6):495&ndash;509.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/12570813" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 12570813</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>7.</dt><dd><div class="bk_ref" id="HYNICTOC99mTc.EXTYLES.7">Sun H. , Jiang X.F. , Wang S. , Chen H.Y. , Sun J. , Li P.Y. , Ning G. , Zhao Y.J.
99mTc-HYNIC-TOC scintigraphy in evaluation of active Graves' ophthalmopathy (GO). <span><span class="ref-journal">Endocrine. </span>2007;<span class="ref-vol">
<strong>31</strong>
</span>(3):305&ndash;310.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/17906380" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 17906380</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>8.</dt><dd><div class="bk_ref" id="HYNICTOC99mTc.EXTYLES.8">von Guggenberg E. , Mikolajczak R. , Janota B. , Riccabona G. , Decristoforo C.
Radiopharmaceutical development of a freeze-dried kit formulation for the preparation of [99mTc-EDDA-HYNIC-D-phe1, Tyr3]-octreotide, a somatostatin analog for tumor diagnosis. <span><span class="ref-journal">Journal of Pharmaceutical Sciences. </span>2004;<span class="ref-vol">
<strong>93</strong>
</span>(10):2497&ndash;2506.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/15349959" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 15349959</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>9.</dt><dd><div class="bk_ref" id="HYNICTOC99mTc.EXTYLES.9">Decristoforo C. , Mather S.J.
Preparation, 99mTc-labeling, and in vitro characterization of HYNIC and N3S modified RC-160 and [Tyr3]octreotide. <span><span class="ref-journal">Bioconjug Chem. </span>1999;<span class="ref-vol">
<strong>10</strong>
</span>(3):431&ndash;8.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/10346875" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 10346875</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>10.</dt><dd><div class="bk_ref" id="HYNICTOC99mTc.EXTYLES.10">Decristoforo C. , Melendez-Alafort L. , Sosabowski J.K. , Mather S.J.
99mTc-HYNIC-[Tyr3]-octreotide for imaging somatostatin-receptor-positive tumors: preclinical evaluation and comparison with 111In-octreotide. <span><span class="ref-journal">J Nucl Med. </span>2000;<span class="ref-vol">
<strong>41</strong>
</span>(6):1114&ndash;9.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/10855644" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 10855644</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>11.</dt><dd><div class="bk_ref" id="HYNICTOC99mTc.EXTYLES.11">Gonzalez-Vazquez A. , Ferro-Flores G. , Arteaga de Murphy C. , Gutierrez-Garcia Z.
Biokinetics and dosimetry in patients of 99mTc-EDDA/HYNIC-Tyr3-octreotide prepared from lyophilized kits. <span><span class="ref-journal">Appl Radiat Isot. </span>2006;<span class="ref-vol">
<strong>64</strong>
</span>(7):792&ndash;7.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/16542847" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 16542847</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>12.</dt><dd><div class="bk_ref" id="HYNICTOC99mTc.EXTYLES.12">Von Guggenberg E. , Sarg B. , Lindner H. , Alafort L.M. , Mather S.J. , Moncayo R. , Decristoforo C.
Preparation via coligand exchange and characterization of [99mTc-EDDA-HYNIC-D-Phen1, Tyr3]octereotide(99mTc-EDDA/HYNIC-TOC). <span><span class="ref-journal">Journal of Labelled Compounds and Radiopharmaceuticals. </span>2003;<span class="ref-vol">
<strong>46</strong>
</span>:307&ndash;318.</span></div></dd></dl><dl class="bkr_refwrap"><dt>13.</dt><dd><div class="bk_ref" id="HYNICTOC99mTc.EXTYLES.13">Li Y. , Si J.M. , Zhang J. , Du J. , Wang F. , Jia B.
Somatostatin receptor subtype 2-mediated scintigraphy and localization using (99m)Tc-HYNIC-Tyr(3)-octreotide in human hepatocellular carcinoma-bearing nude mice. <span><span class="ref-journal">World J Gastroenterol. </span>2005;<span class="ref-vol">
<strong>11</strong>
</span>(25):3953&ndash;7.</span> [<a href="/pmc/articles/PMC4504904/" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pmc">PMC free article<span class="bk_prnt">: PMC4504904</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/15991301" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 15991301</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>14.</dt><dd><div class="bk_ref" id="HYNICTOC99mTc.EXTYLES.14">Kopecky M. , Semecky V. , Trejtnar F. , Laznicek M. , Laznickova A. , Nachtigal P. , Decristoforo C. , Mather S.J. , Macke H.R.
Analysis of accumulation of 99mTc-octreotide and 99mTc-EDDA/HYNIC-Tyr3-octreotide in the rat kidneys. <span><span class="ref-journal">Nucl Med Biol. </span>2004;<span class="ref-vol">
<strong>31</strong>
</span>(2):231&ndash;9.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/15013489" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 15013489</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>15.</dt><dd><div class="bk_ref" id="HYNICTOC99mTc.EXTYLES.15">Li F. , Chen L.B. , Jing H.L. , Du Y.R. , Chen F. <span><span class="ref-journal">, and , <em>.</em> </span><span class="ref-journal">Zhongguo Yi Xue Ke Xue Yuan Xue Bao. </span>2003;<span class="ref-vol">
<strong>25</strong>
</span>(5):563&ndash;6.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/14650159" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 14650159</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>16.</dt><dd><div class="bk_ref" id="HYNICTOC99mTc.EXTYLES.16">Czepczynski R. , Kosowicz J. , Ziemnicka K. , Mikolajczak R. , Gryczynska M. , Sowinski J. <span><span class="ref-journal">, and , <em>.</em> </span><span class="ref-journal">Endokrynol Pol. </span>2006;<span class="ref-vol">
<strong>57</strong>
</span>(4):431&ndash;5.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/17006849" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 17006849</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>17.</dt><dd><div class="bk_ref" id="HYNICTOC99mTc.EXTYLES.17">Plachcinska A. , Mikolajczak R. , Kozak J. , Rzeszutek K. , Kusmierek J.
Comparative analysis of 99mTc-depreotide and 99mTc-EDDA/HYNIC-TOC thorax scintigrams acquired for the purpose of differential diagnosis of solitary pulmonary nodules. <span><span class="ref-journal">Nucl Med Rev Cent East Eur. </span>2006;<span class="ref-vol">
<strong>9</strong>
</span>(1):24&ndash;9.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/16791800" ref="pagearea=cite-ref&amp;targetsite=entrez&amp;targetcat=link&amp;targettype=pubmed">PubMed<span class="bk_prnt">: 16791800</span></a>]</div></dd></dl></dl></div><div id="bk_toc_contnr"></div></div></div><div class="fm-sec"><h2 id="_NBK23551_pubdet_">Publication Details</h2><h3>Author Information and Affiliations</h3><div class="contrib half_rhythm"><span itemprop="author">Arvind Chopra</span><div class="affiliation small">
National Center for Biotechnology Information, NLM, NIH, Bethesda, MD 20894,
<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">October 12, 2007</span>; Last Update: <span itemprop="dateModified">November 7, 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>Chopra A. 99mTc-ethylenediamine N,N&#x02019;-diacetic acid/hydrazinonicotinamide-Tyr3-octreotide. 2007 Oct 12 [Updated 2007 Nov 7]. 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/RGDyK-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/EC-C225-99mtc/?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="figobHYNICTOC99mTcT1"><div id="HYNICTOC99mTc.T1" class="table"><p class="large-table-link" style="display:none"><span class="right"><a href="/books/NBK23551/table/HYNICTOC99mTc.T1/?report=objectonly" target="object">View in own window</a></span></p><div class="large_tbl" id="__HYNICTOC99mTc.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-ethylenediamine <i>N,N&#x02019;</i>-diacetic acid/hydrazinonicotinamide-Tyr<sup>3</sup>-octreotide</td><td rowspan="9" colspan="1" style="text-align:left;vertical-align:middle;">
<div class="graphic"><img src="/books/NBK23551/bin/HYNICTOC99mTc.jpg" alt="Image HYNICTOC99mTc.jpg" /></div>
</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-TOC</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;"><sup>99m</sup>Tc-EDDA/HYNIC-TOC</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;">Compound</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
<b>Target:</b>
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Somatostatin receptor</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
<b>Target Category:</b>
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Receptor-ligand 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;">Single-photon emission computed tomography (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>
<ul class="simple-list"><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;">Structure of <sup>99m</sup>Tc-HYNIC-TOC.</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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