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<script type="text/javascript" src="/corehtml/pmc/jatsreader/ptpmc_3.22/js/jr.boots.min.js"> </script><title>[99mTc-N40-1-bzlg0,D-Phe6,Leu-NHEt13,des-Met14]Bombesin(6–14) - Molecular Imaging and Contrast Agent Database (MICAD) - NCBI Bookshelf</title>
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<meta name="citation_author" content="Liang Shan">
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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="_NBK23306_"><span class="title" itemprop="name">[<sup>99m</sup>Tc-N<sub>4</sub><sup>0-1</sup>-bzlg<sup>0</sup>,D-Phe<sup>6</sup>,Leu-NHEt<sup>13</sup>,<i>des</i>-Met<sup>14</sup>]Bombesin(6–14)</span></h1><div itemprop="alternativeHeadline" class="subtitle whole_rhythm">[<sup>99m</sup>Tc]Demobesin 1</div><p class="contribs">Shan L.</p><p class="fm-aai"><a href="#_NBK23306_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="figDemobesin199mTcT1"><a href="/books/NBK23306/table/Demobesin1-99mTc.T1/?report=objectonly" target="object" title="Table" class="img_link icnblk_img figpopup" rid-figpopup="figDemobesin199mTcT1" rid-ob="figobDemobesin199mTcT1"><img class="small-thumb" src="/books/NBK23306/table/Demobesin1-99mTc.T1/?report=thumb" src-large="/books/NBK23306/table/Demobesin1-99mTc.T1/?report=previmg" alt="Image " /></a><div class="icnblk_cntnt"><h4 id="Demobesin1-99mTc.T1"><a href="/books/NBK23306/table/Demobesin1-99mTc.T1/?report=objectonly" target="object" rid-ob="figobDemobesin199mTcT1">Table</a></h4><p class="float-caption no_bottom_margin">
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<i>In vitro</i>
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Rodents
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</p></div></div><div id="Demobesin1-99mTc.Background"><h2 id="_Demobesin1-99mTc_Background_">Background</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=%22bombesin%22%25GRPR%20imaging" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>[<sup>99m</sup>Tc-N<sub>4</sub><sup>0-1</sup>-bzlg<sup>0</sup>,D-Phe<sup>6</sup>,Leu-NHEt<sup>13</sup>,<i>des</i>-Met<sup>14</sup>]Bombesin (<a class="bibr" href="#Demobesin1-99mTc.REF.6" rid="Demobesin1-99mTc.REF.6 Demobesin1-99mTc.REF.7 Demobesin1-99mTc.REF.8 Demobesin1-99mTc.REF.9 Demobesin1-99mTc.REF.10 Demobesin1-99mTc.REF.11 Demobesin1-99mTc.REF.12 Demobesin1-99mTc.REF.13 Demobesin1-99mTc.REF.14">6-14</a>) ([<sup>99m</sup>Tc]Demobesin 1) is a bombesin (BN) derivative that was synthesized and labeled with <sup>99m</sup>Tc by Nock et al. for molecular imaging of tumors expressing gastrin-releasing peptide receptor (GRPR) (<a class="bibr" href="#Demobesin1-99mTc.REF.1" rid="Demobesin1-99mTc.REF.1">1</a>).</p><p>BN is an amphibian neuropeptide consisting of 14 amino acids (pGlu-Gln-Arg-Leu-Gly-Asn-Gln-Trp-Ala-Val-Gly-His-Leu-Met-NH<sub>2</sub>) (<a class="bibr" href="#Demobesin1-99mTc.REF.2" rid="Demobesin1-99mTc.REF.2">2</a><a class="bibr" href="#Demobesin1-99mTc.REF.3" rid="Demobesin1-99mTc.REF.3">3</a>), which was first isolated from frog skin in 1970 (<a class="bibr" href="#Demobesin1-99mTc.REF.4" rid="Demobesin1-99mTc.REF.4">4</a>). The search for its mammalian counterpart led to the discovery of gastrin-releasing peptide (GRP), which consists of 27 amino acids. GRP and BN share an identical C-terminal region (-Trp-Ala-Val-Gly-His-Leu-Met-NH<sub>2</sub>) which is necessary for receptor binding and signal transduction (<a class="bibr" href="#Demobesin1-99mTc.REF.5" rid="Demobesin1-99mTc.REF.5">5</a><a class="bibr" href="#Demobesin1-99mTc.REF.6" rid="Demobesin1-99mTc.REF.6">6</a>). In addition to the release of gastrin, GRP and BN-like peptides also produce a wide range of other biological responses in diverse tissues, such as secretion of endocrine and exocrine glands, maintenance of circadian rhythm, regulation of satiety, and contraction of smooth muscles (<a class="bibr" href="#Demobesin1-99mTc.REF.7" rid="Demobesin1-99mTc.REF.7">7</a>). They also act as potential growth factors for both normal and cancer cells (<a class="bibr" href="#Demobesin1-99mTc.REF.3" rid="Demobesin1-99mTc.REF.3 Demobesin1-99mTc.REF.5 Demobesin1-99mTc.REF.6">3, 5, 6</a>). There are four members of the BN receptor family, including three mammalian receptors: GRPR (BB<sub>2</sub> or BRS2; 384 amino acids), neuromedin B receptor (NMBR, BB<sub>1</sub>, or BRS1; 390 amino acids), and BN-like receptor 3 (BB<sub>3</sub>, BRS3, or orphan; 399 amino acids) (<a class="bibr" href="#Demobesin1-99mTc.REF.5" rid="Demobesin1-99mTc.REF.5 Demobesin1-99mTc.REF.7 Demobesin1-99mTc.REF.8">5, 7, 8</a>); the fourth receptor (BB<sub>4</sub>) has only been found in amphibians. GRPR is the only well characterized receptor of this family. GRPR is a glycosylated, 7-transmembrane, G-protein–coupled receptor that, upon binding with its ligands, gives rise to a complex cascade of intracellular reactions. It is normally found in non-neuroendocrine tissues of the breast and pancreas and in neuroendocrine cells of the brain, gastrointestinal tract, lung, and prostate (<a class="bibr" href="#Demobesin1-99mTc.REF.9" rid="Demobesin1-99mTc.REF.9">9</a>). Interestingly, GRPR is overexpressed in prostate cancer as well as in tumors of the breast, lung, pancreas, ovary, kidney, and gastrointestinal tract. It has been reported that GRPR is expressed at a high density in the intraepithelial neoplasia and primary carcinoma of the prostate, whereas normal prostate tissue and, in most cases, benign prostate hyperplasia are predominantly negative for GRPR (<a class="bibr" href="#Demobesin1-99mTc.REF.10" rid="Demobesin1-99mTc.REF.10 Demobesin1-99mTc.REF.11 Demobesin1-99mTc.REF.12 Demobesin1-99mTc.REF.13">10-13</a>).</p><p>GRPR has attracted significant interest as a target for tumor detection, tumor staging, and evaluation of tumor response to therapy (<a class="bibr" href="#Demobesin1-99mTc.REF.5" rid="Demobesin1-99mTc.REF.5 Demobesin1-99mTc.REF.6 Demobesin1-99mTc.REF.8 Demobesin1-99mTc.REF.11">5, 6, 8, 11</a>). A large number of BN derivatives have been developed, and they have been labeled with <sup>99m</sup>Tc, <sup>177</sup>Lu, <sup>67</sup>Ga, and <sup>111</sup>In for single-photon emission computed tomography and with <sup>64</sup>Cu, <sup>68</sup>Ga, and <sup>18</sup>F for positron emission tomography. The published BN derivatives can be generally classified as truncated BN (6–14 or 7–14) or full-length BN (<a class="bibr" href="#Demobesin1-99mTc.REF.1" rid="Demobesin1-99mTc.REF.1 Demobesin1-99mTc.REF.2 Demobesin1-99mTc.REF.3 Demobesin1-99mTc.REF.4 Demobesin1-99mTc.REF.5 Demobesin1-99mTc.REF.6 Demobesin1-99mTc.REF.7 Demobesin1-99mTc.REF.8 Demobesin1-99mTc.REF.9 Demobesin1-99mTc.REF.10 Demobesin1-99mTc.REF.11 Demobesin1-99mTc.REF.12 Demobesin1-99mTc.REF.13 Demobesin1-99mTc.REF.14">1-14</a>) analogs (<a class="bibr" href="#Demobesin1-99mTc.REF.10" rid="Demobesin1-99mTc.REF.10 Demobesin1-99mTc.REF.12 Demobesin1-99mTc.REF.13 Demobesin1-99mTc.REF.14 Demobesin1-99mTc.REF.15 Demobesin1-99mTc.REF.16 Demobesin1-99mTc.REF.17 Demobesin1-99mTc.REF.18">10, 12-18</a>). The truncated BN analogs seem to be favorable for <i>in vivo</i> applications because they are usually more stable than the full-length tetradecapeptides and still bind to the GRPR adequately. However, the full-length peptides offer different labeling methods by attachment of functional groups to the amino acid 1 to 6. In many cases, the amino acids on positions 13 (Leu) and 14 (Met) have been replaced by unnatural amino acids (cyclohexylalanine (CyHAla) and norleucine (Nle)), and Lys has been placed on position 3 for attachment of radiolabels with reactive esters. Spacers, chelators, or radiometals have also been widely used for conjugation and for favorable kinetics (<a class="bibr" href="#Demobesin1-99mTc.REF.19" rid="Demobesin1-99mTc.REF.19">19</a>). The BN derivatives can also be divided into agonists and antagonists (<a class="bibr" href="#Demobesin1-99mTc.REF.1" rid="Demobesin1-99mTc.REF.1 Demobesin1-99mTc.REF.20 Demobesin1-99mTc.REF.21">1, 20, 21</a>). By far, most BN derivatives are agonists. Agonists are internalized into and accumulate within cells, and it has been assumed that they exhibit higher uptake by cancer cells than antagonists. However, some reports have shown that uptake of antagonists is much higher than that of agonists because antagonists may have stronger binding for the GRPR than agonists (<a class="bibr" href="#Demobesin1-99mTc.REF.1" rid="Demobesin1-99mTc.REF.1 Demobesin1-99mTc.REF.20">1, 20</a>).</p><p>An optimal BN-like radiotracer needs to meet several requirements: high affinity for GRPR, with rapid and specific tumor uptake; high hydrophilicity, with preferred renal excretion and low hepatobiliary excretion; and high stability but relatively rapid clearance from blood (<a class="bibr" href="#Demobesin1-99mTc.REF.6" rid="Demobesin1-99mTc.REF.6">6</a>). Despite a large number of published derivatives, a valid comparison among them for the feasibility of tumor imaging is difficult because standardization between studies is lacking. Generally speaking, the majority of the radiotracers have relatively high renal and hepatic uptake, resulting in low tumor/liver and tumor/kidney ratios. Nock et al. developed a GRPR antagonist, [<sup>99m</sup>Tc]Demobesin 1, and further tested its biodistribution and feasibility of imaging GRPR-expressing tumors (<a class="bibr" href="#Demobesin1-99mTc.REF.1" rid="Demobesin1-99mTc.REF.1">1</a>).</p></div><div id="Demobesin1-99mTc.Synthesis"><h2 id="_Demobesin1-99mTc_Synthesis_">Synthesis</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=demobesin" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Demobesin 1 peptide was synthesized in two consecutive steps: coupling and deprotection (<a class="bibr" href="#Demobesin1-99mTc.REF.1" rid="Demobesin1-99mTc.REF.1">1</a>). The tetraamine chelator precursor <i>N</i>,<i>N</i>’,<i>N</i>’’,<i>N</i>’’’-tetrakis-(<i>tert</i>-butoxycarbonyl)-6-{<i>p</i>-[(carboxymethoxy)acetyl]aminobenzyl}-1,4,8,11-tetraazaundecane (N<sub>4</sub>(Boc)<sub>4</sub>-bzlg) was first coupled to the N-terminal of the BN antagonist [D-Phe<sup>6</sup>,Leu-NHEt<sup>13</sup>,<i>des</i>-Met<sup>14</sup>]BN(6–14) through the coupling agent <i>O</i>-(7-azabenzotriazolyl-1,1,3,3-tetramethylammonium hexafluorophosphate. The Boc groups were then removed with trifluoroacetic acid treatment. The peptide conjugate, Demobesin 1, was purified with semipreparative reverse-phase high-performance liquid chromatography (RP-HPLC). The overall yield of Demobesin 1 was ~70%. For radiolabeling, the lyophilized peptide was dissolved in acetic acid/EtOH (8/2 v/v), followed by addition of sodium citrate, pertechnetate generator eluate, and freshly prepared ethanolic SnCl<sub>2</sub> solution. The mixture was left to react for 30 min at ambient temperature and was then brought to pH 7 by addition of HCl before RP-HPLC purification of the [<sup>99m</sup>Tc]Demobesin 1. Radiochemical analysis showed that the specific activity and radiochemical yield of [<sup>99m</sup>Tc]Demobesin 1 were 37 GBq/μmol (1 Ci/μmol) and >96%, respectively. [<sup>99m</sup>Tc]Demobesin 1 was stable in the open reaction vial for at least 6 h after labeling. The [<sup>99g</sup>Tc]Demobesin 1 was prepared with similar protocol to that for its [<sup>99m</sup>Tc]Demobesin 1 counterpart at tracer level.</p></div><div id="Demobesin1-99mTc.In_Vitro_Studies_Tes"><h2 id="_Demobesin1-99mTc_In_Vitro_Studies_Tes_"><i>In Vitro</i> Studies: Testing in Cells and Tissues</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=demobesin" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>The metabolic stability of [<sup>99m</sup>Tc]Demobesin 1 was evaluated in mouse plasma and kidney homogenates (<a class="bibr" href="#Demobesin1-99mTc.REF.1" rid="Demobesin1-99mTc.REF.1">1</a>). After incubation in mouse plasma at 37°C, >85% of the [<sup>99m</sup>Tc]Demobesin 1 remained intact after 1 h. During the first 15 min of incubation, the intact peptide fraction exceeded 90%. Rapid degradation was observed in the kidney preparation, with <5% intact peptide detected after just 5 min of incubation. This result was consistent with the analysis of urine collected 30 min after injection of [<sup>99m</sup>Tc]Demobesin 1 in mice, which showed complete degradation of the original peptide. Two major hydrophilic metabolites were detected in the urine; these were, however, unrelated to <sup>99m</sup>TcO<sub>4</sub><sup>-</sup>.</p><p>The binding capability and internalization of [<sup>99m</sup>Tc]Demobesin 1 for GRPR were investigated with PC-3 cell membrane homogenates, human tumor biopsy specimens, and PC-3 culture cells (<a class="bibr" href="#Demobesin1-99mTc.REF.1" rid="Demobesin1-99mTc.REF.1">1</a>). [Tyr<sup>4</sup>]BN peptide served as the positive control and [<sup>125</sup>I-Tyr<sup>4</sup>]BN served as the specific radioligand, where [Tyr<sup>4</sup>]BN was Pyr-Gln-Arg-Tyr-Gly-Asn-Gln-Trp-Ala-Val-Gly-His-Leu-Met-NH<sub>2</sub>. Competitive binding assays in PC-3 membrane preparations demonstrated that [<sup>125</sup>I-Tyr<sup>4</sup>]BN was displaced by Demobesin 1 from BN binding sites in a monophasic and dose-dependent manner. The 50% inhibitory concentration (IC<sub>50</sub>) value was 0.7 ± 0.08 nmol, comparable to the IC<sub>50</sub> value of [Tyr<sup>4</sup>]BN (1.5 ± 0.20 nmol). The equilibrium dissociation constant and maximal binding value of [<sup>99m</sup>Tc/<sup>99g</sup>Tc]Demobesin 1 were 0.67 ± 0.10 nmol and 262 ± 13 fmol/mg, respectively. Competition binding experiments in human tumor biopsy specimens showed that Demobesin 1 had high binding affinity in the GRPR-expressing prostate cancer, but not in the NMBR-expressing (gut carcinoid) and BB<sub>3</sub>-expressing (lung carcinoid) tumors. The IC<sub>50</sub> values were 2.6 ± 0.2 nmol in prostate cancer (<i>n</i> = 5) and >1,000 nmol in BB<sub>3</sub>- or NMBR-expressing tumors (<i>n</i> = 3). Internalization was rapid, but only a small portion (~25% radioactivity) of the [<sup>99m</sup>Tc]Demobesin 1 was detected within the cells after 120 min of incubation with PC-3 culture cells.</p></div><div id="Demobesin1-99mTc.Animal_Studies"><h2 id="_Demobesin1-99mTc_Animal_Studies_">Animal Studies</h2><div id="Demobesin1-99mTc.Rodents"><h3>Rodents</h3><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=demobesin" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Nock et al. investigated the biodistribution of [<sup>99m</sup>Tc]Demobesin 1 in healthy, male, Swiss albino mice (<i>n</i> = 30) and in female, Swiss, <i>nu</i>/<i>nu</i> mice bearing subcutaneous human PC-3 xenografts (<i>n</i> = 4–6/time point) (<a class="bibr" href="#Demobesin1-99mTc.REF.1" rid="Demobesin1-99mTc.REF.1">1</a>). Each animal was given 148–185 kBq (4–5 μCi) [<sup>99m</sup>Tc]Demobesin 1 (10 pmol of total peptide) <i>via</i> the tail vein. In healthy mice, rapid clearance of the [<sup>99m</sup>Tc]Demobesin 1 was observed <i>via</i> the kidneys, with a small portion of liver uptake. High accumulation in the GRPR-expressing pancreas was detected up to 58.7 ± 6.1% injected dose per gram of tissue (ID/g) at 30 min after injection. The intestine, another GRPR-expressing organ, also had a relatively high accumulation level (7.53 ± 0.85% ID/g at 30 min after injection). Pretreatment of the mice with intraperitoneal administration of 1 mg [Tyr<sup>4</sup>]BN 35 min before injection strongly blocked uptake of [<sup>99m</sup>Tc]Demobesin 1 in both organs, showing uptake levels of only 2.7 ± 1.1% ID/g in the pancreas and 2.26 ± 0.56% ID/g in the intestine at 30 min after injection (<i>n</i> = 4–6 animals). In mice with PC-3 xenografts (<i>n</i> = 4–6/time point), the uptake of [<sup>99m</sup>Tc]Demobesin 1 was already evident at 1 h after injection in both pancreas (79.5 ± 0.8% ID/g) and tumor (16.2 ± 3.1% ID/g). The high tumor uptake remained at this level (15.61 ± 1.19% ID/g) up to 4 h after injection. Rapid clearance of the [<sup>99m</sup>Tc]Demobesin 1, predominantly <i>via</i> the kidneys, resulted in increased high tumor/background ratios over time. The tumor/nontarget tissue ratios were 12.9 ± 3.3 for the blood, 67.6 ± 13.7 for the muscle, 2.0 ± 0.5 for the liver, and 2.0 ± 0.5 for the kidneys at 1 h after injection, and 23.1 ± 3.6 for the blood, 206.0 ± 21.1 for the muscle, 2.2 ± 0.3 for the liver, and 2.7 ± 0.4 for the kidneys at 4 h after injection.</p><p>Blocking studies were performed with intravenous administration of 250 μg [Tyr<sup>4</sup>]BN along with [<sup>99m</sup>Tc]Demobesin 1 or intraperitoneal administration of 1 mg [Tyr<sup>4</sup>]BN 35 min before the administration of [<sup>99m</sup>Tc]Demobesin 1 (<i>n</i> = 4–6 mice/group) (<a class="bibr" href="#Demobesin1-99mTc.REF.1" rid="Demobesin1-99mTc.REF.1">1</a>). The uptake of [<sup>99m</sup>Tc]Demobesin 1 in both pancreas and tumor was blocked by the [Tyr<sup>4</sup>]BN. The uptake level was only 3.26 ± 0.71% ID/g in the pancreas and 2.34 ± 0.33% ID/g in the tumor at 1 h after injection. The tumor/blocked tumor ratios were 6.9 ± 1.3 and 7.7 ± 1.2% ID/g at 1 h and 4 h, respectively.</p><p>Static imaging studies were performed in two mice bearing PC-3 tumors with administration of the [<sup>99m</sup>Tc]Demobesin 1 alone in one mouse (unblocked mouse) and together with 250 μg [Tyr<sup>4</sup>]BN in another mouse (blocked mouse) (<a class="bibr" href="#Demobesin1-99mTc.REF.1" rid="Demobesin1-99mTc.REF.1">1</a>). The images obtained at 1.5 h after injection clearly delineated the tumor in the unblocked mouse. In contrast, the tumor was not visualized in the blocked mouse.</p></div><div id="Demobesin1-99mTc.Other_NonPrimate_Mam"><h3>Other Non-Primate Mammals</h3><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=%22%20SUBSTANCENAME%22%5BSubstance%20Name%5D%20AND%20%28dog%20OR%20rabbit%20OR%20pig%20OR%20sheep%29" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>No references are currently available.</p></div><div id="Demobesin1-99mTc.NonHuman_Primates"><h3>Non-Human Primates</h3><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=%22SUBSTANCENAME%22%5BSubstance%20Name%5D%20AND%20%28primate%20NOT%20human%29" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>No references are currently available.</p></div></div><div id="Demobesin1-99mTc.Human_Studies"><h2 id="_Demobesin1-99mTc_Human_Studies_">Human Studies</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=%22SUBSTANCENAME%22%5BSubstance%20Name%5D%20AND%20human" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>No references are currently available.</p></div><div id="Demobesin1-99mTc.References"><h2 id="_Demobesin1-99mTc_References_">References</h2><dl class="temp-labeled-list"><dl class="bkr_refwrap"><dt>1.</dt><dd><div class="bk_ref" id="Demobesin1-99mTc.REF.1">Nock B., Nikolopoulou A., Chiotellis E., Loudos G., Maintas D., Reubi J.C., Maina T.
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<em>[99mTc]Demobesin 1, a novel potent bombesin analogue for GRP receptor-targeted tumour imaging.</em>
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<span><span class="ref-journal">Eur J Nucl Med Mol Imaging. </span>2003;<span class="ref-vol">30</span>(2):247–58.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/12552343" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 12552343</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>2.</dt><dd><div class="bk_ref" id="Demobesin1-99mTc.REF.2">Maina T., Nock B.A., Zhang H., Nikolopoulou A., Waser B., Reubi J.C., Maecke H.R.
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<em>Species differences of bombesin analog interactions with GRP-R define the choice of animal models in the development of GRP-R-targeting drugs.</em>
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<span><span class="ref-journal">J Nucl Med. </span>2005;<span class="ref-vol">46</span>(5):823–30.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/15872357" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 15872357</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>3.</dt><dd><div class="bk_ref" id="Demobesin1-99mTc.REF.3">Smith C.J., Volkert W.A., Hoffman T.J.
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<em>Gastrin releasing peptide (GRP) receptor targeted radiopharmaceuticals: a concise update.</em>
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<span><span class="ref-journal">Nucl Med Biol. </span>2003;<span class="ref-vol">30</span>(8):861–8.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/14698790" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 14698790</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>4.</dt><dd><div class="bk_ref" id="Demobesin1-99mTc.REF.4">Erspamer V., Erpamer G.F., Inselvini M.
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<em>Some pharmacological actions of alytesin and bombesin.</em>
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<span><span class="ref-journal">J Pharm Pharmacol. </span>1970;<span class="ref-vol">22</span>(11):875–6.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/4395815" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 4395815</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>5.</dt><dd><div class="bk_ref" id="Demobesin1-99mTc.REF.5">Smith C.J., Volkert W.A., Hoffman T.J.
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<em>Radiolabeled peptide conjugates for targeting of the bombesin receptor superfamily subtypes.</em>
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<span><span class="ref-journal">Nucl Med Biol. </span>2005;<span class="ref-vol">32</span>(7):733–40.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/16243649" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 16243649</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>6.</dt><dd><div class="bk_ref" id="Demobesin1-99mTc.REF.6">Ananias H.J., de Jong I.J., Dierckx R.A., van de Wiele C., Helfrich W., Elsinga P.H.
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<em>Nuclear imaging of prostate cancer with gastrin-releasing-peptide-receptor targeted radiopharmaceuticals.</em>
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<span><span class="ref-journal">Curr Pharm Des. </span>2008;<span class="ref-vol">14</span>(28):3033–47.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/18991717" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 18991717</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>7.</dt><dd><div class="bk_ref" id="Demobesin1-99mTc.REF.7">Ischia J., Patel O., Shulkes A., Baldwin G.S.
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<em>Gastrin-releasing peptide: different forms, different functions.</em>
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<span><span class="ref-journal">Biofactors. </span>2009;<span class="ref-vol">35</span>(1):69–75.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/19319848" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 19319848</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>8.</dt><dd><div class="bk_ref" id="Demobesin1-99mTc.REF.8">Maina T., Nock B., Mather S.
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<em>Targeting prostate cancer with radiolabelled bombesins.</em>
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<span><span class="ref-journal">Cancer Imaging. </span>2006;<span class="ref-vol">6</span>:153–7.</span> [<a href="/pmc/articles/PMC1693771/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC1693771</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/17098646" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 17098646</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>9.</dt><dd><div class="bk_ref" id="Demobesin1-99mTc.REF.9">Weber H.C.
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<em>Regulation and signaling of human bombesin receptors and their biological effects.</em>
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<span><span class="ref-journal">Curr Opin Endocrinol Diabetes Obes. </span>2009;<span class="ref-vol">16</span>(1):66–71.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/19115523" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 19115523</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>10.</dt><dd><div class="bk_ref" id="Demobesin1-99mTc.REF.10">Yang Y.S., Zhang X., Xiong Z., Chen X.
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<em>Comparative in vitro and in vivo evaluation of two 64Cu-labeled bombesin analogs in a mouse model of human prostate adenocarcinoma.</em>
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<span><span class="ref-journal">Nucl Med Biol. </span>2006;<span class="ref-vol">33</span>(3):371–80.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/16631086" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 16631086</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>11.</dt><dd><div class="bk_ref" id="Demobesin1-99mTc.REF.11">Liu S., Edwards D.S., Barrett J.A.
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<em>99mTc labeling of highly potent small peptides.</em>
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<span><span class="ref-journal">Bioconjug Chem. </span>1997;<span class="ref-vol">8</span>(5):621–36.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/9327124" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 9327124</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>12.</dt><dd><div class="bk_ref" id="Demobesin1-99mTc.REF.12">Zhang X., Cai W., Cao F., Schreibmann E., Wu Y., Wu J.C., Xing L., Chen X.
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<em>18F-labeled bombesin analogs for targeting GRP receptor-expressing prostate cancer.</em>
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<span><span class="ref-journal">J Nucl Med. </span>2006;<span class="ref-vol">47</span>(3):492–501.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/16513619" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 16513619</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>13.</dt><dd><div class="bk_ref" id="Demobesin1-99mTc.REF.13">Schroeder R.P., van Weerden W.M., Bangma C., Krenning E.P., de Jong M.
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<em>Peptide receptor imaging of prostate cancer with radiolabelled bombesin analogues.</em>
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<span><span class="ref-journal">Methods. </span>2009;<span class="ref-vol">48</span>(2):200–4.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/19398012" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 19398012</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>14.</dt><dd><div class="bk_ref" id="Demobesin1-99mTc.REF.14">Chen X., Park R., Hou Y., Tohme M., Shahinian A.H., Bading J.R., Conti P.S.
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<em>microPET and autoradiographic imaging of GRP receptor expression with 64Cu-DOTA-[Lys3]bombesin in human prostate adenocarcinoma xenografts.</em>
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<span><span class="ref-journal">J Nucl Med. </span>2004;<span class="ref-vol">45</span>(8):1390–7.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/15299066" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 15299066</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>15.</dt><dd><div class="bk_ref" id="Demobesin1-99mTc.REF.15">Hohne A., Mu L., Honer M., Schubiger P.A., Ametamey S.M., Graham K., Stellfeld T., Borkowski S., Berndorff D., Klar U., Voigtmann U., Cyr J.E., Friebe M., Dinkelborg L., Srinivasan A.
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<em>Synthesis, 18F-labeling, and in vitro and in vivo studies of bombesin peptides modified with silicon-based building blocks.</em>
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<span><span class="ref-journal">Bioconjug Chem. </span>2008;<span class="ref-vol">19</span>(9):1871–9.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/18754574" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 18754574</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>16.</dt><dd><div class="bk_ref" id="Demobesin1-99mTc.REF.16">Li Z.B., Wu Z., Chen K., Ryu E.K., Chen X.
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<em>18F-labeled BBN-RGD heterodimer for prostate cancer imaging.</em>
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<span><span class="ref-journal">J Nucl Med. </span>2008;<span class="ref-vol">49</span>(3):453–61.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/18287274" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 18287274</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>17.</dt><dd><div class="bk_ref" id="Demobesin1-99mTc.REF.17">Prasanphanich A.F., Retzloff L., Lane S.R., Nanda P.K., Sieckman G.L., Rold T.L., Ma L., Figueroa S.D., Sublett S.V., Hoffman T.J., Smith C.J.
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<em>In vitro and in vivo analysis of [(64)Cu-NO2A-8-Aoc-BBN(7-14)NH(2)]: a site-directed radiopharmaceutical for positron-emission tomography imaging of T-47D human breast cancer tumors.</em>
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<span><span class="ref-journal">Nucl Med Biol. </span>2009;<span class="ref-vol">36</span>(2):171–81.</span> [<a href="/pmc/articles/PMC2756974/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC2756974</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/19217529" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 19217529</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>18.</dt><dd><div class="bk_ref" id="Demobesin1-99mTc.REF.18">Santos-Cuevas C.L., Ferro-Flores G., Arteaga de Murphy C., Ramirez Fde M., Luna-Gutierrez M.A., Pedraza-Lopez M., Garcia-Becerra R., Ordaz-Rosado D.
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<em>Design, preparation, in vitro and in vivo evaluation of (99m)Tc-N2S2-Tat(49-57)-bombesin: a target-specific hybrid radiopharmaceutical.</em>
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<span><span class="ref-journal">Int J Pharm. </span>2009;<span class="ref-vol">375</span>(1-2):75–83.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/19393305" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 19393305</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>19.</dt><dd><div class="bk_ref" id="Demobesin1-99mTc.REF.19">Fragogeorgi, E.A., C. Zikos, E. Gourni, P. Bouziotis, M. Paravatou-Petsotas, G. Loudos, N. Mitsokapas, S. Xanthopoulos, M. Mavri-Vavayanni, E. Livaniou, A.D. Varvarigou, and S.C. Archimandritis, <em>Spacer Site Modifications for the Improvement of the in Vitro and in Vivo Binding Properties of (99m)Tc-N(3)S-X-Bombesin[2-14] Derivatives.</em> Bioconjug Chem, 2009. [<a href="https://pubmed.ncbi.nlm.nih.gov/19344122" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 19344122</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>20.</dt><dd><div class="bk_ref" id="Demobesin1-99mTc.REF.20">Cescato R., Maina T., Nock B., Nikolopoulou A., Charalambidis D., Piccand V., Reubi J.C.
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<em>Bombesin receptor antagonists may be preferable to agonists for tumor targeting.</em>
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<span><span class="ref-journal">J Nucl Med. </span>2008;<span class="ref-vol">49</span>(2):318–26.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/18199616" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 18199616</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>21.</dt><dd><div class="bk_ref" id="Demobesin1-99mTc.REF.21">Nock B.A., Nikolopoulou A., Galanis A., Cordopatis P., Waser B., Reubi J.C., Maina T.
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<em>Potent bombesin-like peptides for GRP-receptor targeting of tumors with 99mTc: a preclinical study.</em>
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<span><span class="ref-journal">J Med Chem. </span>2005;<span class="ref-vol">48</span>(1):100–10.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/15634004" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 15634004</span></a>]</div></dd></dl></dl></div><div id="bk_toc_contnr"></div></div></div><div class="fm-sec"><h2 id="_NBK23306_pubdet_">Publication Details</h2><h3>Author Information and Affiliations</h3><div class="contrib half_rhythm"><span itemprop="author">Liang Shan</span>, PhD<div class="affiliation small">National Center for Biotechnology Information, NLM, NIH<div><span class="email-label">Email: </span><a href="mailto:dev@null" data-email="vog.hin.mln.ibcn@dacim" class="oemail">vog.hin.mln.ibcn@dacim</a></div></div><div class="small">Corresponding author.</div></div><h3>Publication History</h3><p class="small">Created: <span itemprop="datePublished">August 30, 2009</span>; Last Update: <span itemprop="dateModified">October 28, 2009</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>Shan L. [99mTc-N40-1-bzlg0,D-Phe6,Leu-NHEt13,des-Met14]Bombesin(6–14) 2009 Aug 30 [Updated 2009 Oct 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/RGDfK-Orn3-CGG99mTc/?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/DSPL-99mTc-111In/?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="figobDemobesin199mTcT1"><div id="Demobesin1-99mTc.T1" class="table"><p class="large-table-link" style="display:none"><span class="right"><a href="/books/NBK23306/table/Demobesin1-99mTc.T1/?report=objectonly" target="object">View in own window</a></span></p><div class="large_tbl" id="__Demobesin1-99mTc.T1_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>99m</sup>Tc-N<sub>4</sub><sup>0-1</sup>-bzlg<sup>0</sup>,D-Phe<sup>6</sup>,Leu-NHEt<sup>13</sup>,<i>des</i>-Met<sup>14</sup>]Bombesin(6–14)</td><td rowspan="9" colspan="1" style="text-align:left;vertical-align:middle;">
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<span class="graphic"><img src="/books/NBK23306/bin/M99mTcDemobesin_1.jpg" alt="Image M99mTcDemobesin_1.jpg" /></span>
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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>99m</sup>Tc]Demobesin 1</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;">Peptide</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;">Gastrin-releasing peptide receptor (GRPR)</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;">Receptor</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Method of detection:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align: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;">
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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>99m</sup>Tc</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;">Structure of [<sup>99m</sup>Tc]Demobesin 1. Click on <a href="/entrez/viewer.fcgi?db=protein&id=4885361" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">protein</a>, <a href="/entrez/viewer.fcgi?db=nuccore&id=61677286" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">nucleotide</a> (RefSeq), and <a href="/entrez/query.fcgi?db=gene&cmd=Retrieve&dopt=full_report&list_uids=2925" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">gene</a> for more information about gastrin-releasing peptide receptor.</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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