151 lines
46 KiB
Text
151 lines
46 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="NBK133249">
|
|
<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="/NBK133249/?report=reader">
|
|
<meta name="ncbi_pagename" content="N-(4-(6-(Isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl)-4-[11C]methoxy-N-methylbenzamide - 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>N-(4-(6-(Isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl)-4-[11C]methoxy-N-methylbenzamide - 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/DAA1106-11C/?report=reader">
|
|
<meta name="jr-next-unit" content="/books/n/micad/ITDM-11C/?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="N-(4-(6-(Isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl)-4-[11C]methoxy-N-methylbenzamide">
|
|
<meta name="citation_publisher" content="National Center for Biotechnology Information (US)">
|
|
<meta name="citation_date" content="2013/05/02">
|
|
<meta name="citation_author" content="Kam Leung">
|
|
<meta name="citation_pmid" content="23638488">
|
|
<meta name="citation_fulltext_html_url" content="https://www.ncbi.nlm.nih.gov/books/NBK133249/">
|
|
<link rel="schema.DC" href="http://purl.org/DC/elements/1.0/">
|
|
<meta name="DC.Title" content="N-(4-(6-(Isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl)-4-[11C]methoxy-N-methylbenzamide">
|
|
<meta name="DC.Type" content="Text">
|
|
<meta name="DC.Publisher" content="National Center for Biotechnology Information (US)">
|
|
<meta name="DC.Contributor" content="Kam Leung">
|
|
<meta name="DC.Date" content="2013/05/02">
|
|
<meta name="DC.Identifier" content="https://www.ncbi.nlm.nih.gov/books/NBK133249/">
|
|
<meta name="description" content="Glutamate is a major excitatory neurotransmitter at neuronal synapses in the central nervous system (CNS) (1, 2). Glutamate produces excitatory effects by acting on cell-surface ionotropic glutamate or metabotropic glutamate receptors (mGluRs). The mGluRs are GTP-binding protein (G-protein)–coupled receptors that play important roles in regulating the activity of many synapses in the CNS, and many neuronal projection pathways contain mGluRs. There are eight mGluR subtypes, which are further subdivided into groups I, II, and III. The group I receptors include mGluR1 and mGluR5, and they are found predominantly in postsynaptic locations. mGluR1 is found in moderate to high density in the cerebellum, caudate, putamen, thalamus, cingulate cortex, and hippocampus, with low density in the pons. mGluR5 is usually found in moderate to high density in the frontal cortex, caudate, putamen, nucleus accumbens, olfactory tubercle, and hippocampus, with low density in the cerebellum. mGluR1 and mGluR5 are positively coupled to phospholipase C in the regulation of neuronal excitability (3). Dysfunction of mGluR1 and mGluR5 is implicated in a variety of diseases in the CNS, including anxiety, depression, schizophrenia, Parkinson’s disease, and drug addiction or withdrawal (2, 4).">
|
|
<meta name="og:title" content="N-(4-(6-(Isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl)-4-[11C]methoxy-N-methylbenzamide">
|
|
<meta name="og:type" content="book">
|
|
<meta name="og:description" content="Glutamate is a major excitatory neurotransmitter at neuronal synapses in the central nervous system (CNS) (1, 2). Glutamate produces excitatory effects by acting on cell-surface ionotropic glutamate or metabotropic glutamate receptors (mGluRs). The mGluRs are GTP-binding protein (G-protein)–coupled receptors that play important roles in regulating the activity of many synapses in the CNS, and many neuronal projection pathways contain mGluRs. There are eight mGluR subtypes, which are further subdivided into groups I, II, and III. The group I receptors include mGluR1 and mGluR5, and they are found predominantly in postsynaptic locations. mGluR1 is found in moderate to high density in the cerebellum, caudate, putamen, thalamus, cingulate cortex, and hippocampus, with low density in the pons. mGluR5 is usually found in moderate to high density in the frontal cortex, caudate, putamen, nucleus accumbens, olfactory tubercle, and hippocampus, with low density in the cerebellum. mGluR1 and mGluR5 are positively coupled to phospholipase C in the regulation of neuronal excitability (3). Dysfunction of mGluR1 and mGluR5 is implicated in a variety of diseases in the CNS, including anxiety, depression, schizophrenia, Parkinson’s disease, and drug addiction or withdrawal (2, 4).">
|
|
<meta name="og:url" content="https://www.ncbi.nlm.nih.gov/books/NBK133249/">
|
|
<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/ITMM-11C/?report=reader">
|
|
<link rel="canonical" href="https://www.ncbi.nlm.nih.gov/books/NBK133249/">
|
|
<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="CE8D8A127D648D31000000000031002C.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/NBK133249/?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/DAA1106-11C/?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">N-(4-(6-(Isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl)-4-[11C]methoxy-N-methylbenzamide</div><div class="j">Molecular Imaging and Contrast Agent Database (MICAD) [Internet]</div></div><div class="tail"><a href="/books/n/micad/ITDM-11C/?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/NBK133249/"><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/NBK133249/&text=N-(4-(6-(Isopropylamino)pyrimidin-4-yl)-1%2C3-thiazol-2-yl)-4-%5B11C%5Dmethoxy-N-methylbenzamide"><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/NBK133249/?report=classic">Switch to classic view</a><a href="/books/NBK133249/pdf/Bookshelf_NBK133249.pdf">PDF (146K)</a><a href="/books/NBK133249/?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%20NBK133249%20%2F%20sid%3ACE8B5AF87C7FFCB1_0191SID%20%2F%20phid%3ACE8D8A127D648D31000000000031002C.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="_NBK133249_"><span class="title" itemprop="name"><i>N</i>-(4-(6-(Isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl)-4-[<sup>11</sup>C]methoxy-<i>N</i>-methylbenzamide</span></h1><div itemprop="alternativeHeadline" class="subtitle whole_rhythm">[<sup>11</sup>C]ITMM</div><p class="contribs">Leung K.</p><p class="fm-aai"><a href="#_NBK133249_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="figITMM11CTncchemicalnamen46isopropyla"><a href="/books/NBK133249/table/ITMM-11C.T.nc_chemical_namen46isopropyla/?report=objectonly" target="object" title="Table" class="img_link icnblk_img" rid-ob="figobITMM11CTncchemicalnamen46isopropyla"><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="ITMM-11C.T.nc_chemical_namen46isopropyla"><a href="/books/NBK133249/table/ITMM-11C.T.nc_chemical_namen46isopropyla/?report=objectonly" target="object" rid-ob="figobITMM11CTncchemicalnamen46isopropyla">Table</a></h4><p class="float-caption no_bottom_margin">
|
|
|
|
<i>In vitro</i>
|
|
|
|
|
|
Rodents
|
|
</p></div></div><div id="ITMM-11C.Background"><h2 id="_ITMM-11C_Background_">Background</h2><p>[<a href="/sites/entrez?Db=pubmed&Cmd=DetailsSearch&Term=ITMM" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Glutamate is a major excitatory neurotransmitter at neuronal synapses in the central nervous system (CNS) (<a class="bibr" href="#ITMM-11C.REF.1" rid="ITMM-11C.REF.1 ITMM-11C.REF.2">1, 2</a>). Glutamate produces excitatory effects by acting on cell-surface ionotropic glutamate or metabotropic glutamate receptors (mGluRs). The mGluRs are GTP-binding protein (G-protein)–coupled receptors that play important roles in regulating the activity of many synapses in the CNS, and many neuronal projection pathways contain mGluRs. There are eight mGluR subtypes, which are further subdivided into groups I, II, and III. The group I receptors include mGluR1 and mGluR5, and they are found predominantly in postsynaptic locations. mGluR1 is found in moderate to high density in the cerebellum, caudate, putamen, thalamus, cingulate cortex, and hippocampus, with low density in the pons. mGluR5 is usually found in moderate to high density in the frontal cortex, caudate, putamen, nucleus accumbens, olfactory tubercle, and hippocampus, with low density in the cerebellum. mGluR1 and mGluR5 are positively coupled to phospholipase C in the regulation of neuronal excitability (<a class="bibr" href="#ITMM-11C.REF.3" rid="ITMM-11C.REF.3">3</a>). Dysfunction of mGluR1 and mGluR5 is implicated in a variety of diseases in the CNS, including anxiety, depression, schizophrenia, Parkinson’s disease, and drug addiction or withdrawal (<a class="bibr" href="#ITMM-11C.REF.2" rid="ITMM-11C.REF.2 ITMM-11C.REF.4">2, 4</a>).</p><p>Positron emission tomography (PET) radioligands targeting mGluR5 can visualize and analyze mGluR5 expression in normal physiological and pathological conditions (<a class="bibr" href="#ITMM-11C.REF.4" rid="ITMM-11C.REF.4 ITMM-11C.REF.5 ITMM-11C.REF.6 ITMM-11C.REF.7 ITMM-11C.REF.8">4-8</a>). However, only a few mGluR1 ligands have been studied. <i>N</i>-(4-(6-(Isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl)-4-methoxy-<i>N</i>-methylbenzamide (ITMM) was shown to be a selective mGluR1 antagonist with nanomolar affinity (<i>K</i><sub>i</sub> = 12.6 nM), with little inhibition of mGluR5. Fujinaga et al. (<a class="bibr" href="#ITMM-11C.REF.9" rid="ITMM-11C.REF.9">9</a>) labeled ITMM with <sup>11</sup>C to prepare <i>N</i>-(4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl)-4-[<sup>11</sup>C]methoxy-<i>N</i>-methylbenzamide ([<sup>11</sup>C]ITMM) for use with <i>in vivo</i> PET imaging of mGluR1 distribution in rat brains. Toyohara et al. (<a class="bibr" href="#ITMM-11C.REF.10" rid="ITMM-11C.REF.10">10</a>) evaluated [<sup>11</sup>C]ITMM in mouse and human brains. [<sup>11</sup>C]ITMM was shown to be a suitable PET radioligand for mapping mGluR1 in the human brain.</p><div id="ITMM-11C.Related_Resource_Links"><h3>Related Resource Links:</h3><ul><li class="half_rhythm"><div>Chapters in MICAD (<a href="/books?Db=books&Cmd=DetailsSearch&Term=mGluR1+AND+micad%5Bbook%5D" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">mGluR1</a>, <a href="/books?term=mGluR5%20AND%20micad%5Bbook%5D" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">mGluR5</a>)</div></li><li class="half_rhythm"><div>Gene information in NCBI (<a href="/gene/2911" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">mGluR1</a>, <a href="/gene/2915" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">mGluR5</a>)</div></li><li class="half_rhythm"><div>Articles in Online Mendelian Inheritance in Man (OMIM) (<a href="http://omim.org/entry/604473" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">mGluR1</a>, <a href="/omim/604102" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">mGluR5</a>)</div></li><li class="half_rhythm"><div>Clinical trials (<a href="http://www.clinicaltrials.gov/ct2/results?term=mGluR1" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">mGluR1</a>, <a href="http://www.clinicaltrials.gov/ct2/results?term=mglur5" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">mGluR5</a>)</div></li></ul></div></div><div id="ITMM-11C.Synthesis"><h2 id="_ITMM-11C_Synthesis_">Synthesis</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=ITMM%20and%20synthesis" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Fujinaga et al. (<a class="bibr" href="#ITMM-11C.REF.9" rid="ITMM-11C.REF.9">9</a>) synthesized [<sup>11</sup>C]ITMM by methylation of the hydroxyl precursor with [<sup>11</sup>C]MeI (prepared with [<sup>11</sup>C]CO<sub>2</sub>) for 5 min at 70°C. Subsequent separation with high-performance liquid chromatography (HPLC) produced a radiochemical purity >99%. Average radiochemical yield was 22 ± 5% (<i>n</i> = 21) based on [<sup>11</sup>C]CO<sub>2</sub>. The specific activity of [<sup>11</sup>C]ITMM was 95–140 GBq/µmol (2.56–3.78 Ci/µmol) at the end of synthesis (EOS). The total synthesis time was 25 ± 3 min from the end of bombardment (EOB). For higher specific activity, [<sup>11</sup>C]ITMM was prepared <i>via</i> methylation of the hydroxyl precursor with [<sup>11</sup>C]MeI (prepared with [<sup>11</sup>C]CH<sub>4</sub>) for 5 min at 70°C. Average radiochemical yield was 6 ± 1% (<i>n</i> = 3) based on [<sup>11</sup>C]CH<sub>4</sub>. The specific activity of [<sup>11</sup>C]ITMM was 4,370–7,840 GBq/µmol (118–212 Ci/µmol) at EOS. The total synthesis time was 29 ± 1 min.</p><p>Toyohara et al. (<a class="bibr" href="#ITMM-11C.REF.10" rid="ITMM-11C.REF.10">10</a>) prepared [<sup>11</sup>C]ITMM by methylation of the hydroxyl precursor with [<sup>11</sup>C]methyl triflate under NaOH as a base using an automated synthesizer for 1 min at room temperature. Subsequent separation with HPLC produced a radiochemical purity >98%. Average radiochemical yield was 66.0 ± 27.4% (<i>n</i> = 4) based on [<sup>11</sup>C]methyl triflate. The specific activity of [<sup>11</sup>C]ITMM was 97.9–351.1 GBq/µmol (2.64–9.49 Ci/µmol) at EOS. The total synthesis time was <25 min from the EOB.</p></div><div id="ITMM-11C.In_Vitro_Studies_Testing_in_Cel"><h2 id="_ITMM-11C_In_Vitro_Studies_Testing_in_Cel_"><i>In Vitro</i> Studies: Testing in Cells and Tissues</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=ITMM%20and%20in%20vitro" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p><i>In vitro</i> binding affinity of ITMM was determined with rat brain homogenates using [<sup>18</sup>F]fluoro-<i>N</i>-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-<i>N</i>-methylbenzamide ([<sup>18</sup>F]FITM) as the mGluR1 radioligand (<a class="bibr" href="#ITMM-11C.REF.9" rid="ITMM-11C.REF.9">9</a>). The <i>K</i><sub>i</sub> values were 12.6 ± 1.2 nM and 5.4 ± 1.2 nM for ITMM and FITM, respectively. Both agents showed IC<sub>50</sub> values >10,000 nM for mGluR5. ITMM (LogD 2.57) was found to be more lipophilic than FITM (LogD 1.45).</p><p><i>In vitro</i> [<sup>11</sup>C]ITMM autoradiographic imaging studies were performed on rat brain sections (<a class="bibr" href="#ITMM-11C.REF.9" rid="ITMM-11C.REF.9">9</a>). [<sup>11</sup>C]ITMM bound heterogeneously to the brain sections, with the highest accumulation of radioactivity in the mGluR1-rich cerebellum, followed by the thalamus and striatum, with the lowest radioactivity in the pons. JNJ-16259685 (1,000 nM), another mGluR1 antagonist, blocked radioactivity signals by >70% in the cerebellum, thalamus, and striatum.</p></div><div id="ITMM-11C.Animal_Studies"><h2 id="_ITMM-11C_Animal_Studies_">Animal Studies</h2><div id="ITMM-11C.Rodents"><h3>Rodents</h3><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=ITMM%20and%20rodentia" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Fujinaga et al. (<a class="bibr" href="#ITMM-11C.REF.9" rid="ITMM-11C.REF.9">9</a>) performed <i>ex vivo</i> biodistribution studies in mice (<i>n</i> = 4/group) at 1–60 min after intravenous injection of 4.8 MBq (0.13 mCi) [<sup>11</sup>C]ITMM (0.04 nmol). The radioactivity levels in most tissues were highest at 1–5 min and decreased gradually thereafter. The highest accumulation at 5 min was observed in the liver (8.34% injected dose/gram (ID/g)), followed by the kidney (5.64% ID/g), small intestine (4.55% ID/g), brain (3.21% ID/g), lung (2.90% ID/g), heart (2.09% ID/g), spleen (1.96% ID/g), blood (1.95% ID/g), and muscle (1.22% ID/g). The accumulation in the brain remained high at 2.38% ID/g and 1.85% ID/g at 30 min and 60 min, respectively.</p><p>Fujinaga et al. (<a class="bibr" href="#ITMM-11C.REF.9" rid="ITMM-11C.REF.9">9</a>) performed dynamic PET imaging studies for 90 min in rats (<i>n</i> = 4) after intravenous injection of 37–55 MBq (1.0–1.5 mCi) [<sup>11</sup>C]ITMM (0.3–0.5 nmol). Blocking studies were performed with injection of excess ITMM (1 mg/kg) or mGluR1 antagonist JNJ-16259685 (3 mg/kg) just before injection of the tracer. Baseline tissue time-activity curves revealed high accumulation of radioactivity that peaked at 30–45 min in the cerebellum, with moderate radioactivity in the thalamus and striatum and low radioactivity in the pons. The cerebellum/pons, thalamus/pons, and striatum/pons maximum ratios were 6.98, 5.05, and 4.32, respectively. Both ITMM and JNJ-16259685 showed >85% inhibition of radioactivity in the cerebellum, thalamus, and striatum. PET imaging studies with wild-type and mGluR1-knockout mice showed high radioactivity in the cerebellum and thalamus in the wild-type mouse brain and only a low, homogeneous distribution of radioactivity in the knockout mouse brain. Toyohara et al. (<a class="bibr" href="#ITMM-11C.REF.10" rid="ITMM-11C.REF.10">10</a>) showed that the maximum standard uptake values in the cerebellum, cerebral cortex, and striatum were 1.7, 0.9, and 0.8, respectively, at 15 min after injection of [<sup>11</sup>C]ITMM in mice (<i>n</i> = 4).</p></div><div id="ITMM-11C.Other_NonPrimate_Mammals"><h3>Other Non-Primate Mammals</h3><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=ITMM%20and%20%28dog%20or%20pig%20or%20sheep%20or%20rabbit%29" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>No publication is currently available.</p></div><div id="ITMM-11C.NonHuman_Primates"><h3>Non-Human Primates</h3><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=ITMM%20and%20%28primate%20not%20human%29" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>No publication is currently available.</p></div></div><div id="ITMM-11C.Human_Studies"><h2 id="_ITMM-11C_Human_Studies_">Human Studies</h2><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=ITMM%20and%20human" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Toyohara et al. (<a class="bibr" href="#ITMM-11C.REF.10" rid="ITMM-11C.REF.10">10</a>) performed dynamic PET imaging scans for 90 min with a normal male subject (27 years old) after injection of 565 MBq (15.3 mCi) [<sup>11</sup>C]ITMM (8 nmol). Radioactivity in the cerebellum reached a plateau at 40 min. The volume of distribution (V<sub>T</sub>) values were 2.7, 1.1, 0.9, 0.8, 0.7, 0.6, 0.5, and 0.5 for the cerebellum, thalamus, temporal cortex, parietal cortex, frontal cortex, occipital cortex, caudate, and putamen, respectively. [<sup>11</sup>C]ITMM remained 84.7% intact in the blood at 10 min and declined to 60.5% intact at 60 min. Plasma radioactivity decreased rapidly and exhibited a three-phase clearance pattern with half-lives of 1, 4, and 29 min.</p></div><div id="ITMM-11C.References"><h2 id="_ITMM-11C_References_">References</h2><dl class="temp-labeled-list"><dl class="bkr_refwrap"><dt>1.</dt><dd><div class="bk_ref" id="ITMM-11C.REF.1">Pin J.P., Duvoisin R.
|
|
<em>The metabotropic glutamate receptors: structure and functions.</em>
|
|
<span><span class="ref-journal">Neuropharmacology. </span>1995;<span class="ref-vol">34</span>(1):1–26.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/7623957" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 7623957</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>2.</dt><dd><div class="bk_ref" id="ITMM-11C.REF.2">Ferraguti F., Crepaldi L., Nicoletti F.
|
|
<em>Metabotropic glutamate 1 receptor: current concepts and perspectives.</em>
|
|
<span><span class="ref-journal">Pharmacol Rev. </span>2008;<span class="ref-vol">60</span>(4):536–81.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/19112153" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 19112153</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>3.</dt><dd><div class="bk_ref" id="ITMM-11C.REF.3">Abe T., Sugihara H., Nawa H., Shigemoto R., Mizuno N., Nakanishi S.
|
|
<em>Molecular characterization of a novel metabotropic glutamate receptor mGluR5 coupled to inositol phosphate/Ca2+ signal transduction.</em>
|
|
<span><span class="ref-journal">J Biol Chem. </span>1992;<span class="ref-vol">267</span>(19):13361–8.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/1320017" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 1320017</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>4.</dt><dd><div class="bk_ref" id="ITMM-11C.REF.4">Gasparini F., Lingenhohl K., Stoehr N., Flor P.J., Heinrich M., Vranesic I., Biollaz M., Allgeier H., Heckendorn R., Urwyler S., Varney M.A., Johnson E.C., Hess S.D., Rao S.P., Sacaan A.I., Santori E.M., Velicelebi G., Kuhn R.
|
|
<em>2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist.</em>
|
|
<span><span class="ref-journal">Neuropharmacology. </span>1999;<span class="ref-vol">38</span>(10):1493–503.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/10530811" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 10530811</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>5.</dt><dd><div class="bk_ref" id="ITMM-11C.REF.5">Ametamey S.M., Kessler L.J., Honer M., Wyss M.T., Buck A., Hintermann S., Auberson Y.P., Gasparini F., Schubiger P.A.
|
|
<em>Radiosynthesis and preclinical evaluation of 11C-ABP688 as a probe for imaging the metabotropic glutamate receptor subtype 5.</em>
|
|
<span><span class="ref-journal">J Nucl Med. </span>2006;<span class="ref-vol">47</span>(4):698–705.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/16595505" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 16595505</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>6.</dt><dd><div class="bk_ref" id="ITMM-11C.REF.6">Ametamey S.M., Treyer V., Streffer J., Wyss M.T., Schmidt M., Blagoev M., Hintermann S., Auberson Y., Gasparini F., Fischer U.C., Buck A.
|
|
<em>Human PET studies of metabotropic glutamate receptor subtype 5 with 11C-ABP688.</em>
|
|
<span><span class="ref-journal">J Nucl Med. </span>2007;<span class="ref-vol">48</span>(2):247–52.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/17268022" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 17268022</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>7.</dt><dd><div class="bk_ref" id="ITMM-11C.REF.7">Baumann C.A., Mu L., Johannsen S., Honer M., Schubiger P.A., Ametamey S.M.
|
|
<em>Structure-activity relationships of fluorinated (E)-3-((6-methylpyridin-2-yl)ethynyl)cyclohex-2-enone-O-methyloxime (ABP688) derivatives and the discovery of a high affinity analogue as a potential candidate for imaging metabotropic glutamate recepors subtype 5 (mGluR5) with positron emission tomography (PET).</em>
|
|
<span><span class="ref-journal">J Med Chem. </span>2010;<span class="ref-vol">53</span>(10):4009–17.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/20411954" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 20411954</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>8.</dt><dd><div class="bk_ref" id="ITMM-11C.REF.8">Honer M., Stoffel A., Kessler L.J., Schubiger P.A., Ametamey S.M.
|
|
<em>Radiolabeling and in vitro and in vivo evaluation of [(18)F]-FE-DABP688 as a PET radioligand for the metabotropic glutamate receptor subtype 5.</em>
|
|
<span><span class="ref-journal">Nucl Med Biol. </span>2007;<span class="ref-vol">34</span>(8):973–80.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/17998101" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 17998101</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>9.</dt><dd><div class="bk_ref" id="ITMM-11C.REF.9">Fujinaga M., Yamasaki T., Yui J., Hatori A., Xie L., Kawamura K., Asagawa C., Kumata K., Yoshida Y., Ogawa M., Nengaki N., Fukumura T., Zhang M.R.
|
|
<em>Synthesis and evaluation of novel radioligands for positron emission tomography imaging of metabotropic glutamate receptor subtype 1 (mGluR1) in rodent brain.</em>
|
|
<span><span class="ref-journal">J Med Chem. </span>2012;<span class="ref-vol">55</span>(5):2342–52.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/22316010" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 22316010</span></a>]</div></dd></dl><dl class="bkr_refwrap"><dt>10.</dt><dd><div class="bk_ref" id="ITMM-11C.REF.10">Toyohara J., Sakata M., Fujinaga M., Yamasaki T., Oda K., Ishii K., Zhang M.R., Moriguchi Jeckel C.M., Ishiwata K.
|
|
<em>Preclinical and the first clinical studies on [(11)C]ITMM for mapping metabotropic glutamate receptor subtype 1 by positron emission tomography.</em>
|
|
<span><span class="ref-journal">Nucl Med Biol. </span>2013;<span class="ref-vol">40</span>(2):214–20.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/23265669" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 23265669</span></a>]</div></dd></dl></dl></div><div id="bk_toc_contnr"></div></div></div><div class="fm-sec"><h2 id="_NBK133249_pubdet_">Publication Details</h2><h3>Author Information and Affiliations</h3><div class="contrib half_rhythm"><span itemprop="author">Kam Leung</span>, PhD<div class="affiliation small">National Center for Biotechnology Information, NLM, NIH<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">February 14, 2013</span>; Last Update: <span itemprop="dateModified">May 2, 2013</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>Leung K. N-(4-(6-(Isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl)-4-[11C]methoxy-N-methylbenzamide. 2013 Feb 14 [Updated 2013 May 2]. 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/DAA1106-11C/?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/ITDM-11C/?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="figobITMM11CTncchemicalnamen46isopropyla"><div id="ITMM-11C.T.nc_chemical_namen46isopropyla" class="table"><p class="large-table-link" style="display:none"><span class="right"><a href="/books/NBK133249/table/ITMM-11C.T.nc_chemical_namen46isopropyla/?report=objectonly" target="object">View in own window</a></span></p><div class="large_tbl" id="__ITMM-11C.T.nc_chemical_namen46isopropyla_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;"><i>N</i>-(4-(6-(Isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl)-4-[<sup>11</sup>C]methoxy-<i>N</i>-methylbenzamide</td><td rowspan="9" colspan="1" style="text-align:center;vertical-align:middle;">
|
|
<a href="https://pubchem.ncbi.nlm.nih.gov/substance/162023992" title="View this structure in PubChem" class="img_link" ref="pagearea=body&targetsite=entrez&targetcat=link&targettype=pubchem"><img src="https://pubchem.ncbi.nlm.nih.gov/image/imgsrv.fcgi?t=l&sid=162023992" alt="image 162023992 in the ncbi pubchem database" /></a>
|
|
</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
|
|
<b>Abbreviated name:</b>
|
|
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">[<sup>11</sup>C]ITMM, [<sup>11</sup>C]6</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;">Compound</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
|
|
<b>Target:</b>
|
|
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Metabotropic glutamate receptor subtype 1 (mGluR1)</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
|
|
<b>Target category:</b>
|
|
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Receptor</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:</b>
|
|
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><sup>11</sup>C</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><li class="half_rhythm"><div>
|
|
<img alt="Checkbox" src="/corehtml/pmc/css/bookshelf/2.26/img/studies.checkbox.png" /> Humans
|
|
</div></li></ul>
|
|
</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Click on the above structure for additional information in <a href="http://pubchem.ncbi.nlm.nih.gov/" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubChem</a>.</td></tr></tbody></table></div></div></article></div><div id="jr-scripts"><script src="/corehtml/pmc/jatsreader/ptpmc_3.22/js/libs.min.js"> </script><script src="/corehtml/pmc/jatsreader/ptpmc_3.22/js/jr.min.js"> </script></div></div>
|
|
|
|
|
|
|
|
|
|
<!-- Book content -->
|
|
|
|
<script type="text/javascript" src="/portal/portal3rc.fcgi/rlib/js/InstrumentNCBIBaseJS/InstrumentPageStarterJS.js"> </script>
|
|
|
|
|
|
<!-- CE8B5AF87C7FFCB1_0191SID /projects/books/PBooks@9.11 portal106 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>
|