175 lines
51 KiB
Text
175 lines
51 KiB
Text
<!DOCTYPE html>
|
|
<html xmlns="http://www.w3.org/1999/xhtml" xml:lang="en" class="no-js no-jr">
|
|
<head>
|
|
<!-- For pinger, set start time and add meta elements. -->
|
|
<script type="text/javascript">var ncbi_startTime = new Date();</script>
|
|
|
|
<!-- Logger begin -->
|
|
<meta name="ncbi_db" content="books">
|
|
<meta name="ncbi_pdid" content="book-part">
|
|
<meta name="ncbi_acc" content="NBK51670">
|
|
<meta name="ncbi_domain" content="micad">
|
|
<meta name="ncbi_report" content="reader">
|
|
<meta name="ncbi_type" content="fulltext">
|
|
<meta name="ncbi_objectid" content="">
|
|
<meta name="ncbi_pcid" content="/NBK51670/?report=reader">
|
|
<meta name="ncbi_pagename" content="68Ga-Labeled 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-Tyr-cyclo(DAB-Arg-cyclo(Cys-Phe-d-Trp-Lys-Thr-Cys)) - Molecular Imaging and Contrast Agent Database (MICAD) - NCBI Bookshelf">
|
|
<meta name="ncbi_bookparttype" content="chapter">
|
|
<meta name="ncbi_app" content="bookshelf">
|
|
<!-- Logger end -->
|
|
|
|
<!--component id="Page" label="meta"/-->
|
|
<script type="text/javascript" src="/corehtml/pmc/jatsreader/ptpmc_3.22/js/jr.boots.min.js"> </script><title>68Ga-Labeled 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-Tyr-cyclo(DAB-Arg-cyclo(Cys-Phe-d-Trp-Lys-Thr-Cys)) - Molecular Imaging and Contrast Agent Database (MICAD) - NCBI Bookshelf</title>
|
|
<meta charset="utf-8">
|
|
<meta name="apple-mobile-web-app-capable" content="no">
|
|
<meta name="viewport" content="initial-scale=1,minimum-scale=1,maximum-scale=1,user-scalable=no">
|
|
<meta name="jr-col-layout" content="auto">
|
|
<meta name="jr-prev-unit" content="/books/n/micad/BPAMD68Ga/?report=reader">
|
|
<meta name="jr-next-unit" content="/books/n/micad/Ga68-MUT-DS/?report=reader">
|
|
<meta name="bk-toc-url" content="/books/n/micad/?report=toc">
|
|
<meta name="robots" content="INDEX,FOLLOW,NOARCHIVE">
|
|
<meta name="citation_inbook_title" content="Molecular Imaging and Contrast Agent Database (MICAD) [Internet]">
|
|
<meta name="citation_title" content="68Ga-Labeled 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-Tyr-cyclo(DAB-Arg-cyclo(Cys-Phe-d-Trp-Lys-Thr-Cys))">
|
|
<meta name="citation_publisher" content="National Center for Biotechnology Information (US)">
|
|
<meta name="citation_date" content="2011/01/18">
|
|
<meta name="citation_author" content="Liang Shan">
|
|
<meta name="citation_pmid" content="21290628">
|
|
<meta name="citation_fulltext_html_url" content="https://www.ncbi.nlm.nih.gov/books/NBK51670/">
|
|
<link rel="schema.DC" href="http://purl.org/DC/elements/1.0/">
|
|
<meta name="DC.Title" content="68Ga-Labeled 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-Tyr-cyclo(DAB-Arg-cyclo(Cys-Phe-d-Trp-Lys-Thr-Cys))">
|
|
<meta name="DC.Type" content="Text">
|
|
<meta name="DC.Publisher" content="National Center for Biotechnology Information (US)">
|
|
<meta name="DC.Contributor" content="Liang Shan">
|
|
<meta name="DC.Date" content="2011/01/18">
|
|
<meta name="DC.Identifier" content="https://www.ncbi.nlm.nih.gov/books/NBK51670/">
|
|
<meta name="description" content="The 68Ga-labeled 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)-Tyr-cyclo(DAB-Arg-cyclo(Cys-Phe-d-Trp-Lys-Thr-Cys)), abbreviated as 68Ga-AM3, is a somatostatin (SST)-based, bicyclic peptide conjugate developed by Fani et al. for SST receptor (SSTR)–targeted imaging of neuroendocrine tumors (1).">
|
|
<meta name="og:title" content="68Ga-Labeled 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-Tyr-cyclo(DAB-Arg-cyclo(Cys-Phe-d-Trp-Lys-Thr-Cys))">
|
|
<meta name="og:type" content="book">
|
|
<meta name="og:description" content="The 68Ga-labeled 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)-Tyr-cyclo(DAB-Arg-cyclo(Cys-Phe-d-Trp-Lys-Thr-Cys)), abbreviated as 68Ga-AM3, is a somatostatin (SST)-based, bicyclic peptide conjugate developed by Fani et al. for SST receptor (SSTR)–targeted imaging of neuroendocrine tumors (1).">
|
|
<meta name="og:url" content="https://www.ncbi.nlm.nih.gov/books/NBK51670/">
|
|
<meta name="og:site_name" content="NCBI Bookshelf">
|
|
<meta name="og:image" content="https://www.ncbi.nlm.nih.gov/corehtml/pmc/pmcgifs/bookshelf/thumbs/th-micad-lrg.png">
|
|
<meta name="twitter:card" content="summary">
|
|
<meta name="twitter:site" content="@ncbibooks">
|
|
<meta name="bk-non-canon-loc" content="/books/n/micad/Ga68-AM3/?report=reader">
|
|
<link rel="canonical" href="https://www.ncbi.nlm.nih.gov/books/NBK51670/">
|
|
<link href="https://fonts.googleapis.com/css?family=Archivo+Narrow:400,700,400italic,700italic&subset=latin" rel="stylesheet" type="text/css">
|
|
<link rel="stylesheet" href="/corehtml/pmc/jatsreader/ptpmc_3.22/css/libs.min.css">
|
|
<link rel="stylesheet" href="/corehtml/pmc/jatsreader/ptpmc_3.22/css/jr.min.css">
|
|
<meta name="format-detection" content="telephone=no">
|
|
<link rel="stylesheet" href="/corehtml/pmc/css/bookshelf/2.26/css/books.min.css" type="text/css">
|
|
<link rel="stylesheet" href="/corehtml/pmc/css/bookshelf/2.26/css//books_print.min.css" type="text/css" media="print">
|
|
<link rel="stylesheet" href="/corehtml/pmc/css/bookshelf/2.26/css/books_reader.min.css" type="text/css">
|
|
<style type="text/css">p a.figpopup{display:inline !important} .bk_tt {font-family: monospace} .first-line-outdent .bk_ref {display: inline} .body-content h2, .body-content .h2 {border-bottom: 1px solid #97B0C8} .body-content h2.inline {border-bottom: none} a.page-toc-label , .jig-ncbismoothscroll a {text-decoration:none;border:0 !important} .temp-labeled-list .graphic {display:inline-block !important} .temp-labeled-list img{width:100%}</style>
|
|
|
|
<link rel="shortcut icon" href="//www.ncbi.nlm.nih.gov/favicon.ico">
|
|
<meta name="ncbi_phid" content="CE8C009A7D6450B1000000000071005D.m_5">
|
|
<meta name='referrer' content='origin-when-cross-origin'/><link type="text/css" rel="stylesheet" href="//static.pubmed.gov/portal/portal3rc.fcgi/4216699/css/3852956/3849091.css"></head>
|
|
<body>
|
|
<!-- Book content! -->
|
|
|
|
|
|
<div id="jr" data-jr-path="/corehtml/pmc/jatsreader/ptpmc_3.22/"><div class="jr-unsupported"><table class="modal"><tr><td><span class="attn inline-block"></span><br />Your browser does not support the NLM PubReader view.<br />Go to <a href="/pmc/about/pr-browsers/">this page</a> to see a list of supported browsers<br />or return to the <br /><a href="/books/NBK51670/?report=classic">regular view</a>.</td></tr></table></div><div id="jr-ui" class="hidden"><nav id="jr-head"><div class="flexh tb"><div id="jr-tb1"><a id="jr-links-sw" class="hidden" title="Links"><svg xmlns="http://www.w3.org/2000/svg" version="1.1" x="0px" y="0px" viewBox="0 0 70.6 85.3" style="enable-background:new 0 0 70.6 85.3;vertical-align:middle" xml:space="preserve" width="24" height="24">
|
|
<style type="text/css">.st0{fill:#939598;}</style>
|
|
<g>
|
|
<path class="st0" d="M36,0C12.8,2.2-22.4,14.6,19.6,32.5C40.7,41.4-30.6,14,35.9,9.8"></path>
|
|
<path class="st0" d="M34.5,85.3c23.2-2.2,58.4-14.6,16.4-32.5c-21.1-8.9,50.2,18.5-16.3,22.7"></path>
|
|
<path class="st0" d="M34.7,37.1c66.5-4.2-4.8-31.6,16.3-22.7c42.1,17.9,6.9,30.3-16.4,32.5h1.7c-66.2,4.4,4.8,31.6-16.3,22.7 c-42.1-17.9-6.9-30.3,16.4-32.5"></path>
|
|
</g>
|
|
</svg> Books</a></div><div class="jr-rhead f1 flexh"><div class="head"><a href="/books/n/micad/BPAMD68Ga/?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="body"><div class="t">68Ga-Labeled 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-Tyr-cyclo(DAB-Arg-cyclo(Cys-Phe-d-Trp-Lys-Thr-Cys))</div><div class="j">Molecular Imaging and Contrast Agent Database (MICAD) [Internet]</div></div><div class="tail"><a href="/books/n/micad/Ga68-MUT-DS/?report=reader"><svg xmlns="http://www.w3.org/2000/svg" viewBox="0 0 100 100" preserveAspectRatio="none"><path d="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></div><div id="jr-tb2"><a id="jr-bkhelp-sw" class="btn wsprkl hidden" title="Help with NLM PubReader">?</a><a id="jr-help-sw" class="btn wsprkl hidden" title="Settings and typography in NLM PubReader"><svg xmlns="http://www.w3.org/2000/svg" viewBox="0 0 512 512" preserveAspectRatio="none"><path d="M462,283.742v-55.485l-29.981-10.662c-11.431-4.065-20.628-12.794-25.274-24.001 c-0.002-0.004-0.004-0.009-0.006-0.013c-4.659-11.235-4.333-23.918,0.889-34.903l13.653-28.724l-39.234-39.234l-28.72,13.652 c-10.979,5.219-23.68,5.546-34.908,0.889c-0.005-0.002-0.01-0.003-0.014-0.005c-11.215-4.65-19.933-13.834-24-25.273L283.741,50 h-55.484l-10.662,29.981c-4.065,11.431-12.794,20.627-24.001,25.274c-0.005,0.002-0.009,0.004-0.014,0.005 c-11.235,4.66-23.919,4.333-34.905-0.889l-28.723-13.653l-39.234,39.234l13.653,28.721c5.219,10.979,5.545,23.681,0.889,34.91 c-0.002,0.004-0.004,0.009-0.006,0.013c-4.649,11.214-13.834,19.931-25.271,23.998L50,228.257v55.485l29.98,10.661 c11.431,4.065,20.627,12.794,25.274,24c0.002,0.005,0.003,0.01,0.005,0.014c4.66,11.236,4.334,23.921-0.888,34.906l-13.654,28.723 l39.234,39.234l28.721-13.652c10.979-5.219,23.681-5.546,34.909-0.889c0.005,0.002,0.01,0.004,0.014,0.006 c11.214,4.649,19.93,13.833,23.998,25.271L228.257,462h55.484l10.595-29.79c4.103-11.538,12.908-20.824,24.216-25.525 c0.005-0.002,0.009-0.004,0.014-0.006c11.127-4.628,23.694-4.311,34.578,0.863l28.902,13.738l39.234-39.234l-13.66-28.737 c-5.214-10.969-5.539-23.659-0.886-34.877c0.002-0.005,0.004-0.009,0.006-0.014c4.654-11.225,13.848-19.949,25.297-24.021 L462,283.742z M256,331.546c-41.724,0-75.548-33.823-75.548-75.546s33.824-75.547,75.548-75.547 c41.723,0,75.546,33.824,75.546,75.547S297.723,331.546,256,331.546z"></path></svg></a><a id="jr-fip-sw" class="btn wsprkl hidden" title="Find"><svg xmlns="http://www.w3.org/2000/svg" viewBox="0 0 550 600" preserveAspectRatio="none"><path fill="none" stroke="#000" stroke-width="36" stroke-linecap="round" style="fill:#FFF" d="m320,350a153,153 0 1,0-2,2l170,170m-91-117 110,110-26,26-110-110"></path></svg></a><a id="jr-rtoc-sw" class="btn wsprkl hidden" title="Table of Contents"><svg xmlns="http://www.w3.org/2000/svg" viewBox="0 0 100 100" preserveAspectRatio="none"><path d="M20,20h10v8H20V20zM36,20h44v8H36V20zM20,37.33h10v8H20V37.33zM36,37.33h44v8H36V37.33zM20,54.66h10v8H20V54.66zM36,54.66h44v8H36V54.66zM20,72h10v8 H20V72zM36,72h44v8H36V72z"></path></svg></a></div></div></nav><nav id="jr-dash" class="noselect"><nav id="jr-dash" class="noselect"><div id="jr-pi" class="hidden"><a id="jr-pi-prev" class="hidden" title="Previous page"><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 class="pginfo">Page <i class="jr-pg-pn">0</i> of <i class="jr-pg-lp">0</i></div><a id="jr-pi-next" class="hidden" title="Next page"><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><div id="jr-is-tb"><a id="jr-is-sw" class="btn wsprkl hidden" title="Switch between Figures/Tables strip and Progress bar"><svg xmlns="http://www.w3.org/2000/svg" viewBox="0 0 100 100" preserveAspectRatio="none"><rect x="10" y="40" width="20" height="20"></rect><rect x="40" y="40" width="20" height="20"></rect><rect x="70" y="40" width="20" height="20"></rect></svg></a></div><nav id="jr-istrip" class="istrip hidden"><a id="jr-is-prev" href="#" class="hidden" title="Previous"><svg xmlns="http://www.w3.org/2000/svg" viewBox="0 0 100 100" preserveAspectRatio="none"><path d="M80,40 60,65 80,90 70,90 50,65 70,40z M50,40 30,65 50,90 40,90 20,65 40,40z"></path><text x="35" y="25" textLength="60" style="font-size:25px">Prev</text></svg></a><a id="jr-is-next" href="#" class="hidden" title="Next"><svg xmlns="http://www.w3.org/2000/svg" viewBox="0 0 100 100" preserveAspectRatio="none"><path d="M20,40 40,65 20,90 30,90 50,65 30,40z M50,40 70,65 50,90 60,90 80,65 60,40z"></path><text x="15" y="25" textLength="60" style="font-size:25px">Next</text></svg></a></nav><nav id="jr-progress"></nav></nav></nav><aside id="jr-links-p" class="hidden flexv"><div class="tb sk-htbar flexh"><div><a class="jr-p-close btn wsprkl">Done</a></div><div class="title-text f1">NCBI Bookshelf</div></div><div class="cnt lol f1"><a href="/books/">Home</a><a href="/books/browse/">Browse All Titles</a><a class="btn share" target="_blank" rel="noopener noreferrer" href="https://www.facebook.com/sharer/sharer.php?u=https://www.ncbi.nlm.nih.gov/books/NBK51670/"><svg xmlns="http://www.w3.org/2000/svg" viewBox="0 0 33 33" style="vertical-align:middle" width="24" height="24" preserveAspectRatio="none"><g><path d="M 17.996,32L 12,32 L 12,16 l-4,0 l0-5.514 l 4-0.002l-0.006-3.248C 11.993,2.737, 13.213,0, 18.512,0l 4.412,0 l0,5.515 l-2.757,0 c-2.063,0-2.163,0.77-2.163,2.209l-0.008,2.76l 4.959,0 l-0.585,5.514L 18,16L 17.996,32z"></path></g></svg> Share on Facebook</a><a class="btn share" target="_blank" rel="noopener noreferrer" href="https://twitter.com/intent/tweet?url=https://www.ncbi.nlm.nih.gov/books/NBK51670/&text=68Ga-Labeled%201%2C4%2C7%2C10-tetraazacyclododecane-1%2C4%2C7%2C10-tetraacetic%20acid-Tyr-cyclo(DAB-Arg-cyclo(Cys-Phe-d-Trp-Ly..."><svg xmlns="http://www.w3.org/2000/svg" viewBox="0 0 33 33" style="vertical-align:middle" width="24" height="24"><g><path d="M 32,6.076c-1.177,0.522-2.443,0.875-3.771,1.034c 1.355-0.813, 2.396-2.099, 2.887-3.632 c-1.269,0.752-2.674,1.299-4.169,1.593c-1.198-1.276-2.904-2.073-4.792-2.073c-3.626,0-6.565,2.939-6.565,6.565 c0,0.515, 0.058,1.016, 0.17,1.496c-5.456-0.274-10.294-2.888-13.532-6.86c-0.565,0.97-0.889,2.097-0.889,3.301 c0,2.278, 1.159,4.287, 2.921,5.465c-1.076-0.034-2.088-0.329-2.974-0.821c-0.001,0.027-0.001,0.055-0.001,0.083 c0,3.181, 2.263,5.834, 5.266,6.438c-0.551,0.15-1.131,0.23-1.73,0.23c-0.423,0-0.834-0.041-1.235-0.118 c 0.836,2.608, 3.26,4.506, 6.133,4.559c-2.247,1.761-5.078,2.81-8.154,2.81c-0.53,0-1.052-0.031-1.566-0.092 c 2.905,1.863, 6.356,2.95, 10.064,2.95c 12.076,0, 18.679-10.004, 18.679-18.68c0-0.285-0.006-0.568-0.019-0.849 C 30.007,8.548, 31.12,7.392, 32,6.076z"></path></g></svg> Share on Twitter</a></div></aside><aside id="jr-rtoc-p" class="hidden flexv"><div class="tb sk-htbar flexh"><div><a class="jr-p-close btn wsprkl">Done</a></div><div class="title-text f1">Table of Content</div></div><div class="cnt lol f1"><a href="/books/n/micad/?report=reader">Title Information</a><a href="/books/n/micad/toc/?report=reader">Table of Contents Page</a></div></aside><aside id="jr-help-p" class="hidden flexv"><div class="tb sk-htbar flexh"><div><a class="jr-p-close btn wsprkl">Done</a></div><div class="title-text f1">Settings</div></div><div class="cnt f1"><div id="jr-typo-p" class="typo"><div><a class="sf btn wsprkl">A-</a><a class="lf btn wsprkl">A+</a></div><div><a class="bcol-auto btn wsprkl"><svg xmlns="http://www.w3.org/2000/svg" viewBox="0 0 200 100" preserveAspectRatio="none"><text x="10" y="70" style="font-size:60px;font-family: Trebuchet MS, ArialMT, Arial, sans-serif" textLength="180">AUTO</text></svg></a><a class="bcol-1 btn wsprkl"><svg xmlns="http://www.w3.org/2000/svg" viewBox="0 0 100 100" preserveAspectRatio="none"><path d="M15,25 85,25zM15,40 85,40zM15,55 85,55zM15,70 85,70z"></path></svg></a><a class="bcol-2 btn wsprkl"><svg xmlns="http://www.w3.org/2000/svg" viewBox="0 0 100 100" preserveAspectRatio="none"><path d="M5,25 45,25z M55,25 95,25zM5,40 45,40z M55,40 95,40zM5,55 45,55z M55,55 95,55zM5,70 45,70z M55,70 95,70z"></path></svg></a></div></div><div class="lol"><a class="" href="/books/NBK51670/?report=classic">Switch to classic view</a><a href="/books/NBK51670/pdf/Bookshelf_NBK51670.pdf">PDF (152K)</a><a href="/books/NBK51670/?report=printable">Print View</a></div></div></aside><aside id="jr-bkhelp-p" class="hidden flexv"><div class="tb sk-htbar flexh"><div><a class="jr-p-close btn wsprkl">Done</a></div><div class="title-text f1">Help</div></div><div class="cnt f1 lol"><a id="jr-helpobj-sw" data-path="/corehtml/pmc/jatsreader/ptpmc_3.22/" data-href="/corehtml/pmc/jatsreader/ptpmc_3.22/img/bookshelf/help.xml" href="">Help</a><a href="mailto:info@ncbi.nlm.nih.gov?subject=PubReader%20feedback%20%2F%20NBK51670%20%2F%20sid%3ACE8B5AF87C7FFCB1_0191SID%20%2F%20phid%3ACE8C009A7D6450B1000000000071005D.4">Send us feedback</a><a id="jr-about-sw" data-path="/corehtml/pmc/jatsreader/ptpmc_3.22/" data-href="/corehtml/pmc/jatsreader/ptpmc_3.22/img/bookshelf/about.xml" href="">About PubReader</a></div></aside><aside id="jr-objectbox" class="thidden hidden"><div class="jr-objectbox-close wsprkl">✘</div><div class="jr-objectbox-inner cnt"><div class="jr-objectbox-drawer"></div></div></aside><nav id="jr-pm-left" class="hidden"><svg xmlns="http://www.w3.org/2000/svg" viewBox="0 0 40 800" preserveAspectRatio="none"><text font-stretch="ultra-condensed" x="800" y="-15" text-anchor="end" transform="rotate(90)" font-size="18" letter-spacing=".1em">Previous Page</text></svg></nav><nav id="jr-pm-right" class="hidden"><svg xmlns="http://www.w3.org/2000/svg" viewBox="0 0 40 800" preserveAspectRatio="none"><text font-stretch="ultra-condensed" x="800" y="-15" text-anchor="end" transform="rotate(90)" font-size="18" letter-spacing=".1em">Next Page</text></svg></nav><nav id="jr-fip" class="hidden"><nav id="jr-fip-term-p"><input type="search" placeholder="search this page" id="jr-fip-term" autocorrect="off" autocomplete="off" /><a id="jr-fip-mg" class="wsprkl btn" title="Find"><svg xmlns="http://www.w3.org/2000/svg" viewBox="0 0 550 600" preserveAspectRatio="none"><path fill="none" stroke="#000" stroke-width="36" stroke-linecap="round" style="fill:#FFF" d="m320,350a153,153 0 1,0-2,2l170,170m-91-117 110,110-26,26-110-110"></path></svg></a><a id="jr-fip-done" class="wsprkl btn" title="Dismiss find">✘</a></nav><nav id="jr-fip-info-p"><a id="jr-fip-prev" class="wsprkl btn" title="Jump to previuos match">◀</a><button id="jr-fip-matches">no matches yet</button><a id="jr-fip-next" class="wsprkl btn" title="Jump to next match">▶</a></nav></nav></div><div id="jr-epub-interstitial" class="hidden"></div><div id="jr-content"><article data-type="main"><div class="main-content lit-style" itemscope="itemscope" itemtype="http://schema.org/CreativeWork"><div class="meta-content fm-sec"><div class="fm-sec"><h1 id="_NBK51670_"><span class="title" itemprop="name"><sup>68</sup>Ga-Labeled 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-Tyr-cyclo(DAB-Arg-cyclo(Cys-Phe-<span class="small-caps">d</span>-Trp-Lys-Thr-Cys))</span></h1><div itemprop="alternativeHeadline" class="subtitle whole_rhythm"><sup>68</sup>Ga-AM3</div><p class="contribs">Shan L.</p><p class="fm-aai"><a href="#_NBK51670_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="figGa68AM3Tncchemicalname68galabeled1"><a href="/books/NBK51670/table/Ga68-AM3.T.nc_chemical_name68galabeled_1/?report=objectonly" target="object" title="Table" class="img_link icnblk_img" rid-ob="figobGa68AM3Tncchemicalname68galabeled1"><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="Ga68-AM3.T.nc_chemical_name68galabeled_1"><a href="/books/NBK51670/table/Ga68-AM3.T.nc_chemical_name68galabeled_1/?report=objectonly" target="object" rid-ob="figobGa68AM3Tncchemicalname68galabeled1">Table</a></h4><p class="float-caption no_bottom_margin">
|
|
|
|
<i>In vitro</i>
|
|
|
|
|
|
Rodents
|
|
</p></div></div><div id="Ga68-AM3.Background"><h2 id="_Ga68-AM3_Background_">Background</h2><p>[<a href="/pubmed/?term=somatostatin+receptor+and+targeted" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>The <sup>68</sup>Ga-labeled 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)-Tyr-cyclo(DAB-Arg-cyclo(Cys-Phe-<span class="small-caps">d</span>-Trp-Lys-Thr-Cys)), abbreviated as <sup>68</sup>Ga-AM3, is a somatostatin (SST)-based, bicyclic peptide conjugate developed by Fani et al. for SST receptor (SSTR)–targeted imaging of neuroendocrine tumors (<a class="bibr" href="#Ga68-AM3.REF.1" rid="Ga68-AM3.REF.1">1</a>).</p><p>The human SSTR family is a group of G-protein–coupled receptors with five members (SSTR1–SSTR5). All receptor members have seven α-helical transmembrane domains and possess a highly conserved sequence motif (YANSCANPI/VLY) in the seventh topology, which serves as a signature sequence for this family (<a class="bibr" href="#Ga68-AM3.REF.2" rid="Ga68-AM3.REF.2 Ga68-AM3.REF.3 Ga68-AM3.REF.4">2-4</a>). Overall, there is 39%–57% sequence identity among the members, with the highest homology between SSTR1 and SSTR4, and among SSTR2, SSTR3, and SSTR5, respectively. The two groups of receptors also differ in their interactions with SST and its analogs (<a class="bibr" href="#Ga68-AM3.REF.3" rid="Ga68-AM3.REF.3 Ga68-AM3.REF.4 Ga68-AM3.REF.5 Ga68-AM3.REF.6">3-6</a>). SSTR2, SSTR3, and SSTR5 have a high affinity for octreotide and seglitide, whereas SSTR1 and SSTR4 exhibit a very low affinity for them. With the exception of SSTR2, the precise contributions of other members remain to be elucidated. This is largely due to the lack of highly selective ligands and the co-expression of different members in single cells. SSTRs are distributed widely in cells both in the nervous system and periphery, and they have been shown to be overexpressed in a large number of malignancies, with particularly high density in neuroendocrine tumors (<a class="bibr" href="#Ga68-AM3.REF.2" rid="Ga68-AM3.REF.2 Ga68-AM3.REF.7 Ga68-AM3.REF.8">2, 7, 8</a>).</p><p>As the targets of SST radiopharmaceuticals, SSTRs are of considerable clinical relevance for tumor imaging and radionuclide therapy (<a class="bibr" href="#Ga68-AM3.REF.2" rid="Ga68-AM3.REF.2 Ga68-AM3.REF.9 Ga68-AM3.REF.10">2, 9, 10</a>). Because the native SST has a very short biological half-life (<2 min), various analogs have been synthesized, including a group of bicyclic peptides. Bicyclic peptides were first synthesized to understand the bioactive conformation and pharmacophoric amino acid sequence, and to increase the metabolic stability of the natural peptide SST-14 (also known as somatotropin release-inhibiting factor (SRIF)-14) by increasing the rigidity of bicyclic peptides (<a class="bibr" href="#Ga68-AM3.REF.11" rid="Ga68-AM3.REF.11 Ga68-AM3.REF.12">11, 12</a>). Thereafter, various modified bicyclic peptides have been synthesized and have exhibited higher potency and longer duration of biological activity than SRIF-14 (<a class="bibr" href="#Ga68-AM3.REF.1" rid="Ga68-AM3.REF.1 Ga68-AM3.REF.11 Ga68-AM3.REF.12">1, 11, 12</a>). As seen in the structure of the lead peptide cyclo(Aha,cyclo(Cys-Phe-<span class="small-caps">d</span>-Trp-Lys-Thr-Cys)), conformational constraints are introduced by head-to-tail coupling of a 16-atom ring with 7-aminoheptanoic acid (Aha) to the N- and C-terminally amino acid–deleted octreotide. To identify metabolically stable pansomatostatin analogs, a group of investigators from Switzerland have generated a set of bicyclic peptides by forming a second 16-atom ring with Arg and γ-aminobutyric acid (GABA) while keeping the octreotide 20-atom sequence as an inner circle (<a class="bibr" href="#Ga68-AM3.REF.13" rid="Ga68-AM3.REF.13 Ga68-AM3.REF.14 Ga68-AM3.REF.15">13-15</a>). These modifications led to the development of another lead peptide, cyclo(Arg-cyclo(Cys-Phe-<span class="small-caps">d</span>-Trp-Lys-Thr-Cys)-GABA), which is named HR3005 (<a class="bibr" href="#Ga68-AM3.REF.1" rid="Ga68-AM3.REF.1">1</a>). Arg has been shown to be important for broad binding to SSTR subtypes, and GABA can be exchanged with diaminobutyric acid (DAB) for chelator coupling. Based on the HR3005 sequence, four bicyclic analogs have been further synthesized by Fani et al. from the same group (<a class="bibr" href="#Ga68-AM3.REF.1" rid="Ga68-AM3.REF.1">1</a>). The influence of the conformational constraints on receptor binding profiles and the pharmacokinetics of the respective radiopeptides have been investigated. Studies by Fani et al. have shown that the high rigidity of these bicyclic radiopeptides leads to agonistic ligands with good affinity for all five SSTRs (<a class="bibr" href="#Ga68-AM3.REF.1" rid="Ga68-AM3.REF.1">1</a>). The pharmacokinetic data of the DOTA-conjugated bicyclic peptide AM3 (DOTA-Tyr-cyclo(DAB-Arg-cyclo(Cys-Phe-<span class="small-caps">d</span>-Trp-Lys-Thr-Cys))) make it an excellent candidate for use as an imaging radiotracer (<a class="bibr" href="#Ga68-AM3.REF.1" rid="Ga68-AM3.REF.1">1</a>).</p><div id="Ga68-AM3.Related_Resource_Links"><h3>Related Resource Links:</h3><ul><li class="half_rhythm"><div>
|
|
<a href="/sites/entrez?db=Books&cmd=Search&term=somatostatin+receptor+AND+micad%5bbook%5d&doptcmdl=TOCView&log%24=booksrch&bname=micad" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">MICAD chapters on SSTR imaging</a>
|
|
</div></li><li class="half_rhythm"><div>
|
|
<a href="/gene/?term=somatostatin+receptors" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">Gene information on SSTRs</a>
|
|
</div></li><li class="half_rhythm"><div><a href="/omim?term=somatostatin%20receptors" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">Articles on SSTRs in Online Mendelian Inheritance in Man (OMIM</a>)</div></li><li class="half_rhythm"><div>
|
|
<a href="/sites/entrez?db=pccompound&term=somatostatin" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">Somatostatin analogs in PubChem</a>
|
|
</div></li><li class="half_rhythm"><div>
|
|
<a href="/pcassay?term=somatostatin%20receptors" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">Bioassays of SSTRs in PubChem</a>
|
|
</div></li><li class="half_rhythm"><div>
|
|
<a href="http://clinicaltrials.gov/ct2/results?term=somatostatin+receptors" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">SSTR-related clinical trials in ClinicalTrial.gov</a>
|
|
</div></li></ul></div></div><div id="Ga68-AM3.Synthesis"><h2 id="_Ga68-AM3_Synthesis_">Synthesis</h2><p>[<a href="/pubmed/?term=20956465" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Fani et al. synthesized AM3 on the basis of the lead peptide of HR3005 (<a class="bibr" href="#Ga68-AM3.REF.1" rid="Ga68-AM3.REF.1">1</a>). The GABA in HR3005 was replaced with DAB, followed by coupling of the peptide with DOTA through Tyr as a spacer. The <sup>68</sup>Ga-labeled AM3 (<sup>68</sup>Ga-AM3) was prepared according to the method of Zhernosekov et al. (<a class="bibr" href="#Ga68-AM3.REF.16" rid="Ga68-AM3.REF.16">16</a>). The radiotracer solution was prepared by dilution with 0.9% NaCl containing 0.1% bovine serum albumin. The overall yield was ~30%. The <sup>68</sup>Ga-labeling yield was >97% with a specific activity of 35 GBq/µmol (0.95 Ci/µmol). The radiochemical purity of <sup>68</sup>Ga-AM3 was >95%.</p></div><div id="Ga68-AM3.In_Vitro_Studies_Testing_in_Cel"><h2 id="_Ga68-AM3_In_Vitro_Studies_Testing_in_Cel_"><i>In Vitro</i> Studies: Testing in Cells and Tissues</h2><p>[<a href="/pubmed/?term=20956465" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Fani et al. characterized AM3 and <sup>68</sup>Ga-AM3 for their binding affinity, cell internalization, and effect on intracellular Ca<sup>2+</sup> release (<a class="bibr" href="#Ga68-AM3.REF.1" rid="Ga68-AM3.REF.1">1</a>).</p><p>The binding profile of AM3 was determined with receptor autoradiography. The cell membrane pellets were prepared from human embryonic kidney (HEK) cells expressing different subtypes of SSTRs (<a class="bibr" href="#Ga68-AM3.REF.17" rid="Ga68-AM3.REF.17">17</a>). The binding affinity was expressed as 50% inhibitory concentration (IC<sub>50</sub>; <i>n</i> > 3). The lead peptide HR3005 showed high affinity (comparable to SRIF-28) for SSTR2 (2.4 ± 0.6 nM) and SSTR3 (3.4 ± 0.8 nM), and moderate affinity for SSTR5 (14.5 ± 4.5 nM), SSTR1 (34 ± 10 nM), and SSTR4 (68 ± 22 nM), conferring almost pansomatostatin potency to this peptide. Replacement of GABA with DAB in the HR3005 did not change the affinity profile, whereas DOTA-coupling led to marked loss of affinity for all SSTR subtypes. By introducing Tyr as a spacer between DOTA and the peptide, the affinity of generated AM3 recovered to levels comparable to those of HR3005. The IC<sub>50</sub> values of AM3 were 119 ± 6 nM for SSTR1, 2.3 ± 0.2 nM for SSTR2, 4.0 ± 0.03 nM for SSTR3, 97 ± 21 nM for SSTR4, and 27 ± 1 nM for SSTR5. The binding profile of <sup>68</sup>Ga-AM3 was not examined.</p><p>The immunofluorescence microscopy–based internalization assay for SSTR2 and SSTR3 with HEK-SSTR2 and HEK-SSTR3 cells showed that AM3 elicited a pronounced relocation of SSTR2 and SSTR3 from the plasma membrane to the cytoplasm at 30 min after it was applied to the cells, an effect similar to that of the control, SRIF-28.</p><p>The stimulating effect of AM3 on the intracellular Ca<sup>2+</sup> release was tested with HEK cells expressing SSTR2, SSTR3, and SSTR5. Intracellular Ca<sup>2+</sup> release is a part of the signaling pathway regulated by native SST. On SSTR3 and SSTR5, no signal was found. On SSTR2, a large, concentration-dependent increase of the signal was observed. This indicates that AM3 is an agonist because of its stimulating effect on the Ca<sup>2+</sup> release and high potencies similar to those of SRIF-14. The agonist-elicited response in terms of the half maximal effective concentration value was 21.5 ± 3.5 nM.</p><p>The internalization rate and efflux of <sup>177</sup>Lu-AM3 were studied in HEK-SSTR2 and HEK-SSTR3 cells (for details, refer to the chapter on <sup>177</sup>Lu-AM3 in <a href="/books/NBK5330/" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">MICAD</a>). Similar experiments were not performed for <sup>68</sup>Ga-AM3. <sup>177</sup>Lu-AM3 was extremely stable in human blood and serum at 37°C. However, the stability of <sup>68</sup>Ga-AM3 was not tested.</p></div><div id="Ga68-AM3.Animal_Studies"><h2 id="_Ga68-AM3_Animal_Studies_">Animal Studies</h2><div id="Ga68-AM3.Rodents"><h3>Rodents</h3><p>[<a href="/pubmed/?term=20956465" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Five-week-old athymic female Swiss nude mice with HEK-SSTR2 tumors (<i>n</i> = 4–7 mice/group) were used for biodistribution studies after injection of <sup>68</sup>Ga-AM3 (100 µl/10 pmol per 0.4 MBq (0.011 mCi)) into the tail vein (<a class="bibr" href="#Ga68-AM3.REF.1" rid="Ga68-AM3.REF.1">1</a>). Nonspecific uptake was determined with co-injection of 2,000-fold excess DOTANOC (<a class="bibr" href="#Ga68-AM3.REF.18" rid="Ga68-AM3.REF.18 Ga68-AM3.REF.19">18, 19</a>). One group of mice was pre-injected with lysine 10 min before the injection of <sup>68</sup>Ga-AM3 to study kidney blocking. The results were expressed as percentage of injected dose per gram of tissue (% ID/g).</p><p>The biodistribution profile of <sup>68</sup>Ga-AM3 at early times was similar to that of <sup>177</sup>Lu-AM3, showing fast blood clearance, fast nontarget clearance, and high receptor-mediated uptake in the tumors. At 1 h after injection, the SSTR2 tumors accumulated the highest <sup>68</sup>Ga-AM3, with an uptake value of 11.92 ± 1.22% ID/g and a tumor/kidney ratio of 1.2. Blocking experiments with DOTANOC (high affinities for SSTR2, SSTR3, and SSTR5) confirmed the receptor-mediated uptake. Pre-injection of lysine (20 mg/100 µl) resulted in ~50% reduction of the kidney uptake with no significant impact on the tumor uptake.<br />For PET/CT studies, the mice bearing HEK-SSTR2 tumors were injected with <sup>68</sup>Ga-AM3, including a group preinjected with lysine and a group co-injected with DOTANOC (<a class="bibr" href="#Ga68-AM3.REF.1" rid="Ga68-AM3.REF.1">1</a>). The mice were euthanized at 1 h after injection and scanned for 60 min using a routine combined PET/CT scanner. The images clearly showed high tumor and kidney uptake but negligible background. Preinjection of lysine resulted in a significant reduction of the kidney uptake. The specific uptake of <sup>68</sup>Ga-AM3 was also confirmed using DOTANOC as a blocking agent, with which only the kidneys were visualized. The imaging study results were consistent with the biodistribution data.</p></div><div id="Ga68-AM3.Other_NonPrimate_Mammals"><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="Ga68-AM3.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="Ga68-AM3.Human_Studies"><h2 id="_Ga68-AM3_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="Ga68-AM3.References"><h2 id="_Ga68-AM3_References_">References</h2><dl class="temp-labeled-list"><dl class="bkr_refwrap"><dt>1.</dt><dd><div class="bk_ref" id="Ga68-AM3.REF.1">Fani M., Mueller A., Tamma M.L., Nicolas G., Rink H.R., Cescato R., Reubi J.C., Maecke H.R.
|
|
<em>Radiolabeled bicyclic somatostatin-based analogs: a novel class of potential radiotracers for SPECT/PET of neuroendocrine tumors.</em>
|
|
<span><span class="ref-journal">J Nucl Med. </span>2010;<span class="ref-vol">51</span>(11):1771–9.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/20956465" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 20956465</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>2.</dt><dd><div class="bk_ref" id="Ga68-AM3.REF.2">Froidevaux S., Eberle A.N.
|
|
<em>Somatostatin analogs and radiopeptides in cancer therapy.</em>
|
|
<span><span class="ref-journal">Biopolymers. </span>2002;<span class="ref-vol">66</span>(3):161–83.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/12385036" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 12385036</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>3.</dt><dd><div class="bk_ref" id="Ga68-AM3.REF.3">Tulipano G., Schulz S.
|
|
<em>Novel insights in somatostatin receptor physiology.</em>
|
|
<span><span class="ref-journal">Eur J Endocrinol. </span>2007;<span class="ref-vol">156</span> Suppl 1:S3–11.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/17413186" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 17413186</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>4.</dt><dd><div class="bk_ref" id="Ga68-AM3.REF.4">van der Hoek J., Hofland L.J., Lamberts S.W.
|
|
<em>Novel subtype specific and universal somatostatin analogues: clinical potential and pitfalls.</em>
|
|
<span><span class="ref-journal">Curr Pharm Des. </span>2005;<span class="ref-vol">11</span>(12):1573–92.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/15892663" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 15892663</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>5.</dt><dd><div class="bk_ref" id="Ga68-AM3.REF.5">Lesche S., Lehmann D., Nagel F., Schmid H.A., Schulz S.
|
|
<em>Differential effects of octreotide and pasireotide on somatostatin receptor internalization and trafficking in vitro.</em>
|
|
<span><span class="ref-journal">J Clin Endocrinol Metab. </span>2009;<span class="ref-vol">94</span>(2):654–61.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/19001514" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 19001514</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>6.</dt><dd><div class="bk_ref" id="Ga68-AM3.REF.6">Yim C.B., Dijkgraaf I., Merkx R., Versluis C., Eek A., Mulder G.E., Rijkers D.T., Boerman O.C., Liskamp R.M.
|
|
<em>Synthesis of DOTA-conjugated multimeric [Tyr3]octreotide peptides via a combination of Cu(I)-catalyzed "click" cycloaddition and thio acid/sulfonyl azide "sulfo-click" amidation and their in vivo evaluation.</em>
|
|
<span><span class="ref-journal">J Med Chem. </span>2010;<span class="ref-vol">53</span>(10):3944–53.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/20411957" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 20411957</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>7.</dt><dd><div class="bk_ref" id="Ga68-AM3.REF.7">Strowski M.Z., Blake A.D.
|
|
<em>Function and expression of somatostatin receptors of the endocrine pancreas.</em>
|
|
<span><span class="ref-journal">Mol Cell Endocrinol. </span>2008;<span class="ref-vol">286</span>(1-2):169–79.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/18375050" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 18375050</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>8.</dt><dd><div class="bk_ref" id="Ga68-AM3.REF.8">Kwekkeboom D.J., Kam B.L., van Essen M., Teunissen J.J., van Eijck C.H., Valkema R., de Jong M., de Herder W.W., Krenning E.P.
|
|
<em>Somatostatin-receptor-based imaging and therapy of gastroenteropancreatic neuroendocrine tumors.</em>
|
|
<span><span class="ref-journal">Endocr Relat Cancer. </span>2010;<span class="ref-vol">17</span>(1):R53–73.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/19995807" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 19995807</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>9.</dt><dd><div class="bk_ref" id="Ga68-AM3.REF.9">Bal C.S., Gupta S.K., Zaknun J.J.
|
|
<em>Radiolabeled somatostatin analogs for radionuclide imaging and therapy in patients with gastroenteropancreatic neuroendocrine tumors.</em>
|
|
<span><span class="ref-journal">Trop Gastroenterol. </span>2010;<span class="ref-vol">31</span>(2):87–95.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/20862981" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 20862981</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>10.</dt><dd><div class="bk_ref" id="Ga68-AM3.REF.10">de Jong M., Breeman W.A., Kwekkeboom D.J., Valkema R., Krenning E.P.
|
|
<em>Tumor imaging and therapy using radiolabeled somatostatin analogues.</em>
|
|
<span><span class="ref-journal">Acc Chem Res. </span>2009;<span class="ref-vol">42</span>(7):873–80.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/19445476" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 19445476</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>11.</dt><dd><div class="bk_ref" id="Ga68-AM3.REF.11">Veber D.F., Holly F.W., Paleveda W.J., Nutt R.F., Bergstrand S.J., Torchiana M., Glitzer M.S., Saperstein R., Hirschmann R.
|
|
<em>Conformationally restricted bicyclic analogs of somatostatin.</em>
|
|
<span><span class="ref-journal">Proc Natl Acad Sci U S A. </span>1978;<span class="ref-vol">75</span>(6):2636–40.</span> [<a href="/pmc/articles/PMC392617/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC392617</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/208068" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 208068</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>12.</dt><dd><div class="bk_ref" id="Ga68-AM3.REF.12">Veber D.F., Freidlinger R.M., Perlow D.S., Paleveda W.J. Jr, Holly F.W., Strachan R.G., Nutt R.F., Arison B.H., Homnick C., Randall W.C., Glitzer M.S., Saperstein R., Hirschmann R.
|
|
<em>A potent cyclic hexapeptide analogue of somatostatin.</em>
|
|
<span><span class="ref-journal">Nature. </span>1981;<span class="ref-vol">292</span>(5818):55–8.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/6116194" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 6116194</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>13.</dt><dd><div class="bk_ref" id="Ga68-AM3.REF.13">Ginj M., Hinni K., Tschumi S., Schulz S., Maecke H.R.
|
|
<em>Trifunctional somatostatin-based derivatives designed for targeted radiotherapy using auger electron emitters.</em>
|
|
<span><span class="ref-journal">J Nucl Med. </span>2005;<span class="ref-vol">46</span>(12):2097–103.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/16330576" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 16330576</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>14.</dt><dd><div class="bk_ref" id="Ga68-AM3.REF.14">Ginj M., Schmitt J.S., Chen J., Waser B., Reubi J.C., de Jong M., Schulz S., Maecke H.R.
|
|
<em>Design, synthesis, and biological evaluation of somatostatin-based radiopeptides.</em>
|
|
<span><span class="ref-journal">Chem Biol. </span>2006;<span class="ref-vol">13</span>(10):1081–90.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/17052612" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 17052612</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>15.</dt><dd><div class="bk_ref" id="Ga68-AM3.REF.15">Ginj M., Zhang H., Waser B., Cescato R., Wild D., Wang X., Erchegyi J., Rivier J., Macke H.R., Reubi J.C.
|
|
<em>Radiolabeled somatostatin receptor antagonists are preferable to agonists for in vivo peptide receptor targeting of tumors.</em>
|
|
<span><span class="ref-journal">Proc Natl Acad Sci U S A. </span>2006;<span class="ref-vol">103</span>(44):16436–41.</span> [<a href="/pmc/articles/PMC1618814/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC1618814</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/17056720" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 17056720</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>16.</dt><dd><div class="bk_ref" id="Ga68-AM3.REF.16">Zhernosekov K.P., Filosofov D.V., Baum R.P., Aschoff P., Bihl H., Razbash A.A., Jahn M., Jennewein M., Rosch F.
|
|
<em>Processing of generator-produced 68Ga for medical application.</em>
|
|
<span><span class="ref-journal">J Nucl Med. </span>2007;<span class="ref-vol">48</span>(10):1741–8.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/17873136" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 17873136</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>17.</dt><dd><div class="bk_ref" id="Ga68-AM3.REF.17">Reubi J.C., Schar J.C., Waser B., Wenger S., Heppeler A., Schmitt J.S., Macke H.R.
|
|
<em>Affinity profiles for human somatostatin receptor subtypes SST1-SST5 of somatostatin radiotracers selected for scintigraphic and radiotherapeutic use.</em>
|
|
<span><span class="ref-journal">Eur J Nucl Med. </span>2000;<span class="ref-vol">27</span>(3):273–82.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/10774879" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 10774879</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>18.</dt><dd><div class="bk_ref" id="Ga68-AM3.REF.18">Wild D., Schmitt J.S., Ginj M., Macke H.R., Bernard B.F., Krenning E., De Jong M., Wenger S., Reubi J.C.
|
|
<em>DOTA-NOC, a high-affinity ligand of somatostatin receptor subtypes 2, 3 and 5 for labelling with various radiometals.</em>
|
|
<span><span class="ref-journal">Eur J Nucl Med Mol Imaging. </span>2003;<span class="ref-vol">30</span>(10):1338–47.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/12937948" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 12937948</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>19.</dt><dd><div class="bk_ref" id="Ga68-AM3.REF.19">Wild D., Macke H.R., Waser B., Reubi J.C., Ginj M., Rasch H., Muller-Brand J., Hofmann M.
|
|
<em>68Ga-DOTANOC: a first compound for PET imaging with high affinity for somatostatin receptor subtypes 2 and 5.</em>
|
|
<span><span class="ref-journal">Eur J Nucl Med Mol Imaging. </span>2005;<span class="ref-vol">32</span>(6):724.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/15551131" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 15551131</span></a>]</div></dd></dl></dl></div><div id="bk_toc_contnr"></div></div></div><div class="fm-sec"><h2 id="_NBK51670_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">December 10, 2010</span>; Last Update: <span itemprop="dateModified">January 18, 2011</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. 68Ga-Labeled 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-Tyr-cyclo(DAB-Arg-cyclo(Cys-Phe-d-Trp-Lys-Thr-Cys)) 2010 Dec 10 [Updated 2011 Jan 18]. 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/BPAMD68Ga/?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/Ga68-MUT-DS/?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="figobGa68AM3Tncchemicalname68galabeled1"><div id="Ga68-AM3.T.nc_chemical_name68galabeled_1" class="table"><p class="large-table-link" style="display:none"><span class="right"><a href="/books/NBK51670/table/Ga68-AM3.T.nc_chemical_name68galabeled_1/?report=objectonly" target="object">View in own window</a></span></p><div class="large_tbl" id="__Ga68-AM3.T.nc_chemical_name68galabeled_1_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>68</sup>Ga-Labeled 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-Tyr-cyclo(DAB-Arg-cyclo(Cys-Phe-<span class="small-caps">d</span>-Trp-Lys-Thr-Cys))</td><td rowspan="9" colspan="1" style="text-align:center;vertical-align:middle;"></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>68</sup>Ga-AM3</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;">Peptides</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 receptors (SSTRs)</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;">Receptors</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;">Positron emission tomography (PET)</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
|
|
<b>Source of signal / contrast:</b>
|
|
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><sup>68</sup>Ga</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
|
|
<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><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;">For structures of octreotide analogues, click on <a href="/pcsubstance?term=octreotide" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubChem</a>.</td></tr></tbody></table></div></div></article></div><div id="jr-scripts"><script src="/corehtml/pmc/jatsreader/ptpmc_3.22/js/libs.min.js"> </script><script src="/corehtml/pmc/jatsreader/ptpmc_3.22/js/jr.min.js"> </script></div></div>
|
|
|
|
|
|
|
|
|
|
<!-- Book content -->
|
|
|
|
<script type="text/javascript" src="/portal/portal3rc.fcgi/rlib/js/InstrumentNCBIBaseJS/InstrumentPageStarterJS.js"> </script>
|
|
|
|
|
|
<!-- CE8B5AF87C7FFCB1_0191SID /projects/books/PBooks@9.11 portal105 v4.1.r689238 Tue, Oct 22 2024 16:10:51 -->
|
|
<span id="portal-csrf-token" style="display:none" data-token="CE8B5AF87C7FFCB1_0191SID"></span>
|
|
|
|
<script type="text/javascript" src="//static.pubmed.gov/portal/portal3rc.fcgi/4216699/js/3968615.js" snapshot="books"></script></body>
|
|
</html>
|