{"id":3163,"date":"2021-02-16T13:16:39","date_gmt":"2021-02-16T13:16:39","guid":{"rendered":"https:\/\/www.sygnaturediscovery.com\/technical-note\/receptor-binding\/"},"modified":"2025-11-26T14:18:58","modified_gmt":"2025-11-26T14:18:58","slug":"receptor-binding","status":"publish","type":"technical-note","link":"https:\/\/www.sygnaturediscovery.com\/fr\/technical-note\/receptor-binding\/","title":{"rendered":"Receptor Binding"},"content":{"rendered":"<p><strong><em>Ex vivo<\/em><\/strong><strong>\u00a0Receptor Occupancy and\u00a0<em>In Vitro<\/em>\u00a0Radioligand Binding <\/strong><\/p>\n<p><em>Ex vivo<\/em>\u00a0receptor occupancy is a powerful technique utilised in drug discovery to demonstrate target engagement of centrally penetrant compounds. In addition, it can be used to profile binding sites associated with adverse side-effects.<\/p>\n<p>At Sygnature\u00a0<em>ex vivo<\/em>\u00a0receptor occupancy studies can be undertaken with DMPK and\/or behavioural profiling thus providing an invaluable link between\u00a0<em>in vitro<\/em>\u00a0activity, drug exposure at the site of interest, and\u00a0<em>in vivo<\/em> efficacy.\u00a0 These studies can be used to determine:<\/p>\n<ul>\n<li>Central receptor occupancy for a range of drug doses.<\/li>\n<li>Occupancy in different brain regions in the same animal.<\/li>\n<li>Occupancy at a range of targets in the same animal.<\/li>\n<li>Time-course of occupancy.<\/li>\n<\/ul>\n<p><strong>[3H]DAMGO Ex Vivo Autoradiography in Various Rat Brain Regions 60 Minutes<\/strong><\/p>\n<p><img decoding=\"async\" class=\"aligncenter size-full wp-image-10342\" src=\"https:\/\/www.sygnaturediscovery.com\/wp-content\/uploads\/2025\/11\/3HDAMGO-Ex-Vivo-Autoradiography-in-Various-Rat-Brain-Regions-60-Minutes-Following-Administration-of-Morphine-.png\" alt=\"\"><\/p>\n<p>Our dedicated team of experts have been conducting\u00a0<em>in vitro<\/em>\u00a0receptor binding assays and\u00a0<em>ex vivo<\/em>\u00a0occupancy studies for more than 20 years. We have the expertise to design bespoke studies to meet clients\u2019 precise needs by developing novel assays using custom-synthesised radioligands. Alternatively, we can provide off the shelf assays using commercially available radioligands ([<sup>3<\/sup>H] and [<sup>125<\/sup>I]) for well-characterised neurotransmitter receptors and uptake sites including:<\/p>\n<p><img decoding=\"async\" class=\"aligncenter size-full wp-image-10343\" src=\"https:\/\/www.sygnaturediscovery.com\/wp-content\/uploads\/2025\/11\/Table.png\" alt=\"\"><\/p>\n<p><strong><em>In vitro<\/em><\/strong><strong>\u00a0Receptor Binding Assays<\/strong><\/p>\n<p>Radioligand receptor binding assays are extremely powerful tools for studying receptors and to characterize the binding of a drug to its target receptor, providing an important contribution to drug screening and development programmes. There are three types of\u00a0<em>in vitro<\/em>\u00a0radioligand binding assays: competition, saturation and kinetic, all of which can be performed at Sygnature either in recombinant cell lines or using native tissue from rat and mouse brains (either in membrane preparations or in tissue slices).<\/p>\n<p><strong>Competition Studies: Affinity of morphine and buprenorphine for <\/strong><strong>\u00b5<\/strong><strong>-opioid Receptors<\/strong><\/p>\n<p><img decoding=\"async\" class=\"aligncenter size-full wp-image-10344\" src=\"https:\/\/www.sygnaturediscovery.com\/wp-content\/uploads\/2025\/11\/Screen-Shot-2021-02-16-at-13.15.42.png\" alt=\"\"><\/p>\n<p><strong>Saturation Analysis: Kd and Bmax<\/strong><\/p>\n<p>Saturation analysis can be performed to understand receptor density (Bmax) and the equilibrium dissociation constant (Kd), and their relationship to a pharmacodynamic endpoint. For example, binge-eating is associated with decreased D<sub>1<\/sub>\u00a0receptor density and increased \u03bc-opioid receptor density in the striatum.<\/p>\n<p><img decoding=\"async\" class=\"aligncenter size-full wp-image-10345\" src=\"https:\/\/www.sygnaturediscovery.com\/wp-content\/uploads\/2025\/11\/Screen-Shot-2021-02-16-at-13.16.10.png\" alt=\"\"><\/p>\n<p><strong>Functional Studies<\/strong><\/p>\n<p>Sygnature also has the expertise to undertake functional pharmacological activity assays by assessing receptor function using [<sup>35<\/sup>S] GTPgammaS binding or by measuring uptake into rat and mouse synaptosomes.<\/p>\n","protected":false},"excerpt":{"rendered":"<p>Elevate drug discovery with ex vivo receptor binding at Sygnature Discovery. Uncover target engagement &#038; receptor insights for effective compounds.<\/p>\n","protected":false},"featured_media":3164,"template":"","category":[1],"resource_tag":[],"class_list":["post-3163","technical-note","type-technical-note","status-publish","has-post-thumbnail","hentry","category-uncategorized"],"acf":[],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v28.0 - https:\/\/yoast.com\/product\/yoast-seo-wordpress\/ -->\n<title>Receptor Binding - Technical Notes - Sygnature Discovery<\/title>\n<meta name=\"description\" content=\"Elevate drug discovery with ex vivo receptor binding at Sygnature. 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