{"id":257349,"date":"2025-07-28T14:43:38","date_gmt":"2025-07-28T14:43:38","guid":{"rendered":"https:\/\/project.uniurb.it\/vitality\/?p=257349"},"modified":"2025-10-08T08:32:23","modified_gmt":"2025-10-08T08:32:23","slug":"industrial-and-academic-approaches","status":"publish","type":"post","link":"https:\/\/project.uniurb.it\/vitality\/industrial-and-academic-approaches\/","title":{"rendered":"Industrial and academic approaches to the search for alternative melatonin receptor ligands: An historical survey"},"content":{"rendered":"<p>[et_pb_section fb_built=&#8221;1&#8243; _builder_version=&#8221;4.27.4&#8243; _module_preset=&#8221;default&#8221; custom_padding=&#8221;2px|||||&#8221; global_colors_info=&#8221;{}&#8221;][et_pb_row _builder_version=&#8221;4.27.4&#8243; _module_preset=&#8221;default&#8221; custom_padding=&#8221;50px|||||&#8221; locked=&#8221;off&#8221; global_colors_info=&#8221;{}&#8221;][et_pb_column type=&#8221;4_4&#8243; _builder_version=&#8221;4.27.4&#8243; _module_preset=&#8221;default&#8221; global_colors_info=&#8221;{}&#8221;][et_pb_text _builder_version=&#8221;4.27.4&#8243; _module_preset=&#8221;default&#8221; text_font_size=&#8221;16px&#8221; custom_margin=&#8221;||60px||false|false&#8221; global_colors_info=&#8221;{}&#8221;]<span style=\"font-weight: 400;\">Prof. Gilberto Spadoni<\/span><br \/>\n[\/et_pb_text][et_pb_text _builder_version=&#8221;4.27.4&#8243; _module_preset=&#8221;default&#8221; locked=&#8221;on&#8221; global_colors_info=&#8221;{}&#8221;]<\/p>\n<h3>Abstract<\/h3>\n<p>[\/et_pb_text][et_pb_text _builder_version=&#8221;4.27.4&#8243; _module_preset=&#8221;default&#8221; global_colors_info=&#8221;{}&#8221;]<span style=\"font-weight: 400;\">The search for melatonin receptor agonists formed the main part of melatonin <\/span><span style=\"font-weight: 400;\">medicinal chemistry programs for the last three decades. In this short review, we summarize the two main aspects of these programs: the development of all the necessary tools to characterize the newly synthesized ligands at the two melatonin receptors MT1 and MT2, and the medicinal chemist&#8217;s approaches to find chemically diverse ligands at these receptors. Both strategies are described. It turns out that the main source of tools were industrial laboratories, while the medicinal chemistry was mainly carried out in academia. Such complete accounts are interesting, as they delineate the spirits in which the teams were working demonstrating their strength and innovative character. Most of the programs were focused on nonselective <\/span><span style=\"font-weight: 400;\">agonists and few of them reached the market. In contrast, discovery of MT1<\/span><span style=\"font-weight: 400;\">\u2010<\/span><span style=\"font-weight: 400;\"> selective agonists and melatonergic antagonists with proven in vivo activity and MT1 or MT2<\/span><span style=\"font-weight: 400;\">\u2010<\/span><span style=\"font-weight: 400;\">selectivity is still in its infancy, despite the considerable interest that subtype selective compounds may bring in the domain, as the physiological respective roles of the two subtypes of melatonin receptors, is still poorly understood. Poly<\/span><span style=\"font-weight: 400;\">\u2010<\/span><span style=\"font-weight: 400;\">pharmacology applications and multitarget ligands have also been considered.<\/span><br \/>\n[\/et_pb_text][et_pb_text _builder_version=&#8221;4.27.4&#8243; _module_preset=&#8221;default&#8221; custom_margin=&#8221;||0px|||&#8221; locked=&#8221;on&#8221; global_colors_info=&#8221;{}&#8221;]<\/p>\n<h4>Keyword<\/h4>\n<p>[\/et_pb_text][et_pb_text _builder_version=&#8221;4.27.4&#8243; _module_preset=&#8221;default&#8221; global_colors_info=&#8221;{}&#8221;]<span style=\"font-weight: 400;\">Agonists, chemical approach, ligands, melatonin, receptor<\/span><br \/>\n[\/et_pb_text][et_pb_text _builder_version=&#8221;4.27.4&#8243; _module_preset=&#8221;default&#8221; custom_margin=&#8221;||0px|||&#8221; locked=&#8221;on&#8221; global_colors_info=&#8221;{}&#8221;]<\/p>\n<h4>Link<\/h4>\n<p>[\/et_pb_text][et_pb_text _builder_version=&#8221;4.27.4&#8243; _module_preset=&#8221;default&#8221; link_option_url_new_window=&#8221;on&#8221; global_colors_info=&#8221;{}&#8221;]<a title=\"Industrial and academic approaches to the search for alternative melatonin receptor ligands: An historical survey\" href=\"https:\/\/hdl.handle.net\/11576\/2734151\" target=\"_blank\" rel=\"noopener\">https:\/\/hdl.handle.net\/11576\/2734151<\/a><br \/>\n[\/et_pb_text][\/et_pb_column][\/et_pb_row][\/et_pb_section]<\/p>\n","protected":false},"excerpt":{"rendered":"<p>Prof. Gilberto Spadoni Abstract The search for melatonin receptor agonists formed the main part of melatonin medicinal chemistry programs for the last three decades. In this short review, we summarize the two main aspects of these programs: the development of all the necessary tools to characterize the newly synthesized ligands at the two melatonin receptors [&hellip;]<\/p>\n","protected":false},"author":4,"featured_media":0,"comment_status":"open","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"_et_pb_use_builder":"on","_et_pb_old_content":"","_et_gb_content_width":"","footnotes":""},"categories":[19],"tags":[],"class_list":["post-257349","post","type-post","status-publish","format-standard","hentry","category-wp1"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v25.5 - https:\/\/yoast.com\/wordpress\/plugins\/seo\/ -->\n<title>Industrial and academic approaches to the search for alternative melatonin receptor ligands: An historical survey - Vitality<\/title>\n<meta name=\"description\" content=\"Historical review of industrial and academic approaches to discover new ligands for MT1\/MT2 melatonin receptors.\" \/>\n<meta name=\"robots\" content=\"index, follow, max-snippet:-1, max-image-preview:large, max-video-preview:-1\" \/>\n<link rel=\"canonical\" href=\"https:\/\/project.uniurb.it\/vitality\/industrial-and-academic-approaches\/\" \/>\n<meta property=\"og:locale\" content=\"it_IT\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Industrial and academic approaches to the search for alternative melatonin receptor ligands: An historical survey - 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