{"id":6683,"date":"2025-12-08T16:12:41","date_gmt":"2025-12-08T16:12:41","guid":{"rendered":"https:\/\/www.sygnaturediscovery.com\/?post_type=case-study&#038;p=6683"},"modified":"2026-02-02T18:09:37","modified_gmt":"2026-02-02T18:09:37","slug":"subtype-selective-gabaa-modulation","status":"publish","type":"case-study","link":"https:\/\/www.sygnaturediscovery.com\/fr\/case-study\/subtype-selective-gabaa-modulation\/","title":{"rendered":"Subtype selective GABA<sub>A<\/sub> modulation"},"content":{"rendered":"\n<h2 class=\"wp-block-heading has-dark-blue-500-color has-text-color has-link-color has-text-3-xl-font-size wp-elements-75a67b9cdcef53efdc911f07eba6f2f5\">GABA<sub>A<\/sub>&nbsp;receptor screening enables detailed evaluation of subtype-selective modulation using automated electrophysiology. Sygnature Discovery supports CNS drug discovery with robust assay platforms for characterizing GABA<sub>A<\/sub>&nbsp;receptor activity and pharmacology.<br><\/h2>\n\n\n\n<h2 class=\"wp-block-heading has-dark-blue-500-color has-text-color has-link-color has-text-2-xl-font-size wp-elements-2b89604eec9622da1f25f2bdaf07021c\">Introduction<\/h2>\n\n\n\n<p>The majority of inhibitory neurotransmission in the brain is mediated by the binding of \u03b3-aminobutyric acid (GABA) to the GABA<sub>A<\/sub> receptor. These receptors mainly consist of two \u03b1 subunits, two \u03b2 subunits, and either a \u03b3 or \u03b4 subunit with the varying subunit compositions determining the biophysical and pharmacological properties of the receptor. Dysregulation of GABAergic neurotransmission is associated with many neurological diseases and psychiatric disorders, making these receptors attractive targets for drug discovery programs.<\/p>\n\n\n\n<p>Developments in automated patch clamp technologies have allowed for rapid testing of large numbers of compounds against ion channel targets, however until now, the lack of an expansive panel of GABA<sub>A<\/sub> cell lines has limited the identification and characterization of subtype-selective GABA<sub>A<\/sub> compounds. To help overcome this, Sygnature Discovery has developed a GABA<sub>A<\/sub> receptor discovery platform comprising a comprehensive panel of 20 human GABA<sub>A<\/sub> recombinant cell lines stably expressing each \u03b1 subunit in combination with one of three \u03b2 subunits and \u03b32L. In addition this panel also includes the extra-synaptic \u03b14\u03b23\u03b4 and \u03b16\u03b23\u03b4 receptor subtypes, creating opportunities to improve subtype-specific drug efficacy, safety and tolerability.<\/p>\n\n\n\n<div class=\"wp-block-group alignfull is-style-default has-ivory-000-color has-text-color has-background is-layout-flow wp-block-group-is-layout-flow\" style=\"border-radius:1.5em;background:linear-gradient(90deg,rgb(0,60,97) 0%,rgb(4,30,46) 100%);margin-top:var(--wp--preset--spacing--40);margin-bottom:var(--wp--preset--spacing--40);padding-right:var(--wp--preset--spacing--60);padding-left:var(--wp--preset--spacing--60)\" allowchildrentofillwidth=\"\" overflow=\"\" flexwrap=\"\">\n<div style=\"height:64px\" aria-hidden=\"true\" class=\"wp-block-spacer\"><\/div>\n\n\n\n<p class=\"has-text-align-center has-small-font-size\" style=\"line-height:.9\"><strong>CASE STUDY<\/strong><\/p>\n\n\n\n<h2 class=\"wp-block-heading has-text-align-center\" id=\"schedule-a-visit\" style=\"font-size:clamp(20px, 1.25rem + ((1vw - 3.2px) * 0.938), 32px);line-height:1.15\"><strong>Download the PDF: Subtype selective GABA<sub>A<\/sub> modulation<\/strong><\/h2>\n\n\n\n<div class=\"wp-block-buttons is-content-justification-center is-layout-flex wp-container-core-buttons-is-layout-a89b3969 wp-block-buttons-is-layout-flex\">\n<div class=\"wp-block-button has-custom-width wp-block-button__width-50\" modaltype=\"\"><a class=\"wp-block-button__link wp-element-button\" href=\"https:\/\/www.sygnaturediscovery.com\/wp-content\/uploads\/2025\/12\/Subtype-selective-GABAA-modulation.pdf\" target=\"_blank\" rel=\"noreferrer noopener\">Download<\/a><\/div>\n<\/div>\n\n\n\n<div style=\"height:64px\" aria-hidden=\"true\" class=\"wp-block-spacer\"><\/div>\n<\/div>\n","protected":false},"excerpt":{"rendered":"","protected":false},"featured_media":0,"template":"","category":[707,773,746,687],"resource_tag":[],"class_list":["post-6683","case-study","type-case-study","status-publish","hentry","category-electrophysiology","category-gabaa-receptors","category-ion-channels","category-target-classes"],"acf":[],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v27.4 - 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