{"id":321,"date":"2016-04-18T18:20:29","date_gmt":"2016-04-18T18:20:29","guid":{"rendered":"http:\/\/alectos.com\/content\/?p=321"},"modified":"2016-04-18T18:20:29","modified_gmt":"2016-04-18T18:20:29","slug":"discovery-mk-6240-pet-nfts","status":"publish","type":"post","link":"https:\/\/alectos.com\/alectos-content\/index.php\/2016\/04\/18\/discovery-mk-6240-pet-nfts\/","title":{"rendered":"Discovery of [18F]-MK-6240: A Positron Emission Tomography (PET) Imaging Agent for Quantification of Neurofibrillary Tangles (NFTs)"},"content":{"rendered":"<p>Neurofibrillary tangles (NFTs) made up of aggregated tau protein have been identified as the pathologic hallmark of several neurodegenerative diseases including Alzheimer&#8217;s disease. In vivo detection of NFTs using PET imaging represents a unique opportunity to develop a pharmacodynamic tool to accelerate discovery of new disease modifying therapeutics targeting tau pathology. Herein we present the discovery of 6-(fluoro-<sup>18<\/sup>F)-3-(1H-pyrrolo[2,3-c]pyridin-1-yl)isoquinolin-5-amine, <strong>6<\/strong> ([<sup>18<\/sup>F]-<span class=\"highlight\">MK-6240<\/span>), as a novel PET tracer for detecting NFTs. <strong>6<\/strong> exhibits high specificity and selectivity for binding to NFTs, with suitable physicochemical properties and in vivo pharmacokinetics.<\/p>\n<p><a href=\"http:\/\/alectos.com\/content\/wp-content\/uploads\/2016\/04\/MK6240.jpg\"><img decoding=\"async\" class=\"alignnone wp-image-326 size-medium\" src=\"http:\/\/alectos.com\/content\/wp-content\/uploads\/2016\/04\/MK6240-300x83.jpg\" alt=\"MK-6240\" width=\"300\" height=\"83\" \/><\/a><\/p>\n<p>Source: <a href=\"http:\/\/www.ncbi.nlm.nih.gov\/pubmed\/27088900\">Walji, A.M. et al. <em>J Med Chem<\/em> (2016). <\/a><\/p>\n","protected":false},"excerpt":{"rendered":"<p>Neurofibrillary tangles (NFTs) made up of aggregated tau protein have  [&#8230;]<\/p>\n","protected":false},"author":3,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"_monsterinsights_skip_tracking":false,"_monsterinsights_sitenote_active":false,"_monsterinsights_sitenote_note":"","_monsterinsights_sitenote_category":0,"footnotes":""},"categories":[19],"tags":[22,29,60,39,24,61],"class_list":["post-321","post","type-post","status-publish","format-standard","hentry","category-publications","tag-alzheimers","tag-merck","tag-mk-6240","tag-nfts","tag-tau","tag-tau-pet"],"_links":{"self":[{"href":"https:\/\/alectos.com\/alectos-content\/index.php\/wp-json\/wp\/v2\/posts\/321","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/alectos.com\/alectos-content\/index.php\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/alectos.com\/alectos-content\/index.php\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/alectos.com\/alectos-content\/index.php\/wp-json\/wp\/v2\/users\/3"}],"replies":[{"embeddable":true,"href":"https:\/\/alectos.com\/alectos-content\/index.php\/wp-json\/wp\/v2\/comments?post=321"}],"version-history":[{"count":0,"href":"https:\/\/alectos.com\/alectos-content\/index.php\/wp-json\/wp\/v2\/posts\/321\/revisions"}],"wp:attachment":[{"href":"https:\/\/alectos.com\/alectos-content\/index.php\/wp-json\/wp\/v2\/media?parent=321"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/alectos.com\/alectos-content\/index.php\/wp-json\/wp\/v2\/categories?post=321"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/alectos.com\/alectos-content\/index.php\/wp-json\/wp\/v2\/tags?post=321"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}