{"id":15923,"date":"2025-02-20T01:00:00","date_gmt":"2025-02-20T01:00:00","guid":{"rendered":"https:\/\/onhee.com\/?p=15923"},"modified":"2025-04-18T14:31:35","modified_gmt":"2025-04-18T14:31:35","slug":"99mtcdemomedin-c-a-radioligand-based-on-human-gastrin-releasi","status":"publish","type":"post","link":"https:\/\/onhee.com\/?p=15923","title":{"rendered":"[99mTc]Demomedin C, a Radioligand Based on Human Gastrin Releasi"},"content":{"rendered":"<div style=\"padding: 10px 0;text-align: center\"><\/div>\n<p><strong>[99mTc]Demomedin C, a Radioligand Based on Human Gastrin Releasing Peptide(18-27): Synthesis and Preclinical Evaluation in Gastrin Releasing Peptide Receptor-Expressing Models<\/strong><br \/> Berthold Artur Nock , Renzo Cescato , Eleni Ketani , B. Waser , J. C. Reubi , T. Maina, <em>J. Med. Chem.<\/em>, Just Accepted Manuscript<br \/> DOI: 10.1021\/jm300741f<br \/> Publication Date (Web): September 11, 2012<br \/> Copyright \u00a9 2012 American Chemical Society<\/p>\n<p>The synthesis and preclinical evaluation of [99mTc]Demomedin C in gastrin releasing peptide receptor(GRPR)-expressing models are reported. Demomedin C resulted by coupling a Boc-protected N4-chelator to neuromedin C (human GRP(18-27)) and after 99mTc-labeling afforded [99mTc]Demomedin C. Demomedin C showed high affinity and selectivity for the GRPR during receptor autoradiography on human cancer samples (IC50 in nM: GRPR, 1.4\u00b10.2; NMBR, 106\u00b118; and BB3R, &gt;1000). It triggered GRPR internalization in HEK-GRPR cells and Ca2+ release in PC-3 cells (EC50= 1.3 nM). [99mTc]Demomedin C rapidly and specifically internalized at 37oC in PC-3 cells and was stable in mouse plasma. [99mTc]Demomedin C efficiently and specifically localized in human PC-3 implants in mice (9.84\u00b10.81%ID\/g at 1 h pi; 6.36\u00b10.85%ID\/g at 4 h pi and 0.41\u00b10.07%ID\/g at 4 h pi block). Thus, human GRP-based radioligands, such as [99mTc]Demomedin C, can successfully target GRPR-expressing human tumors in vivo while displaying attractive biological features \u00e2\u20ac\u201c e.g. higher GRPR-selectivity \u00e2\u20ac\u201c vs. their frog-homologs.<\/p>\n","protected":false},"excerpt":{"rendered":"<p>[99mTc]Demomedin C, a Radioligand Based on Human Gastrin Releasing Peptide(18-27): Synthesis and Preclinical Evaluation in Gastrin Releasing Peptide Receptor-Expressing Models Berthold Artur Nock , Renzo Cescato , Eleni Ketani , B. Waser , J. C. Reubi , T. Maina, J. Med. Chem., Just Accepted Manuscript DOI: 10.1021\/jm300741f Publication Date (Web): September 11, 2012 Copyright \u00a9 &hellip; <\/p>\n<p class=\"link-more\"><a href=\"https:\/\/onhee.com\/?p=15923\" class=\"more-link\">Read more<span class=\"screen-reader-text\"> &#8220;[99mTc]Demomedin C, a Radioligand Based on Human Gastrin Releasi&#8221;<\/span><\/a><\/p>\n","protected":false},"author":0,"featured_media":0,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[1],"tags":[],"class_list":["post-15923","post","type-post","status-publish","format-standard","hentry","category-news"],"_links":{"self":[{"href":"https:\/\/onhee.com\/index.php?rest_route=\/wp\/v2\/posts\/15923","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/onhee.com\/index.php?rest_route=\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/onhee.com\/index.php?rest_route=\/wp\/v2\/types\/post"}],"replies":[{"embeddable":true,"href":"https:\/\/onhee.com\/index.php?rest_route=%2Fwp%2Fv2%2Fcomments&post=15923"}],"version-history":[{"count":1,"href":"https:\/\/onhee.com\/index.php?rest_route=\/wp\/v2\/posts\/15923\/revisions"}],"predecessor-version":[{"id":16272,"href":"https:\/\/onhee.com\/index.php?rest_route=\/wp\/v2\/posts\/15923\/revisions\/16272"}],"wp:attachment":[{"href":"https:\/\/onhee.com\/index.php?rest_route=%2Fwp%2Fv2%2Fmedia&parent=15923"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/onhee.com\/index.php?rest_route=%2Fwp%2Fv2%2Fcategories&post=15923"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/onhee.com\/index.php?rest_route=%2Fwp%2Fv2%2Ftags&post=15923"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}