{"id":17878,"date":"2025-08-22T11:18:48","date_gmt":"2025-08-22T09:18:48","guid":{"rendered":"https:\/\/www.nanion.de\/?post_type=news&#038;p=17878"},"modified":"2025-08-22T11:19:19","modified_gmt":"2025-08-22T09:19:19","slug":"nav1-7-channels-advancing-preclinical-models-for-pain-drug-discovery","status":"publish","type":"news","link":"https:\/\/nanion.com\/ja\/news\/nav1-7-channels-advancing-preclinical-models-for-pain-drug-discovery\/","title":{"rendered":"Na<sub>v<\/sub>1.7 channels: advancing preclinical models for pain drug discovery"},"content":{"rendered":"<p data-start=\"1368\" data-end=\"1599\">The voltage-gated sodium channel <strong data-start=\"1401\" data-end=\"1411\">Na<sub>v<\/sub>1.7<\/strong> is a key regulator of pain signaling. Mutations in this channel can cause severe inherited pain syndromes or complete insensitivity to pain, making it a target for new analgesics.<\/p>\n<p data-start=\"1601\" data-end=\"1811\">Despite years of research, no selective Na<sub>v<\/sub>1.7 modulator has reached the clinic. One major challenge is the lack of reliable preclinical assays that capture the <strong data-start=\"1762\" data-end=\"1790\">state-dependent behavior<\/strong> of these channels.<\/p>\n<p data-start=\"1813\" data-end=\"2027\">In a new study, researchers from the University of Bari tested the effect of <strong data-start=\"1914\" data-end=\"1928\">mexiletine<\/strong>, a non-selective sodium channel blocker used in neuropathic pain, on Na<sub>v<\/sub>1.7 in two cell systems:<\/p>\n<ul data-start=\"2029\" data-end=\"2135\">\n<li data-start=\"2029\" data-end=\"2081\"><strong data-start=\"959\" data-end=\"974\">TE671 cells<\/strong> (endogenously expressing Na<sub>v<\/sub>1.7 )<\/li>\n<\/ul>\n<ul data-start=\"957\" data-end=\"1063\">\n<li data-start=\"1010\" data-end=\"1063\">\n<p data-start=\"1012\" data-end=\"1063\"><strong data-start=\"1012\" data-end=\"1028\">HEK293 cells<\/strong> (stably expressing human Na<sub>v<\/sub>1.7 )<\/p>\n<\/li>\n<\/ul>\n<p data-start=\"1065\" data-end=\"1238\">Using an automated patch clamp system (Patchliner), the team compared drug effects under voltage-, tonic-, and use-dependent conditions.<\/p>\n<p data-start=\"2282\" data-end=\"2301\">\n<p data-start=\"2282\" data-end=\"2301\">\n<p data-start=\"2282\" data-end=\"2301\">Key findings:<\/p>\n<ul data-start=\"2302\" data-end=\"2672\">\n<li data-start=\"2302\" data-end=\"2386\">\n<p data-start=\"2304\" data-end=\"2386\">Mexiletine blocked Na<sub>v<\/sub>1.7 currents with almost identical potency in both models.<\/p>\n<\/li>\n<li data-start=\"2387\" data-end=\"2513\">\n<p data-start=\"2389\" data-end=\"2513\">The drug showed stronger effects when channels were inactivated (at depolarized potentials or high-frequency stimulation).<\/p>\n<\/li>\n<li data-start=\"2514\" data-end=\"2585\">\n<p data-start=\"2516\" data-end=\"2585\">Both cell lines had similar activation and inactivation properties.<\/p>\n<\/li>\n<li data-start=\"2586\" data-end=\"2672\">\n<p data-start=\"2588\" data-end=\"2672\">Mexiletine shifted inactivation to more negative voltages in a dose-dependent way.<\/p>\n<\/li>\n<\/ul>\n<p data-start=\"2674\" data-end=\"2867\">Importantly, <strong data-start=\"2687\" data-end=\"2736\">TE671 cells proved to be a robust alternative<\/strong> to engineered HEK293 systems. They are easier to handle and provide consistent results, making them valuable for drug screening.<\/p>\n<p data-start=\"2869\" data-end=\"3074\">This study confirms the utility of automated patch clamp for Na<sub>v<\/sub>1.7 pharmacology and establishes <strong data-start=\"2966\" data-end=\"3004\">mexiletine as a reference compound<\/strong> for future efforts to design selective modulators for pain therapy.<\/p>\n<p data-start=\"2507\" data-end=\"2510\">\u2014<\/p>\n<p data-start=\"2512\" data-end=\"2726\">\ud83d\udcd6 Read the full article: <a href=\"https:\/\/www.sciencedirect.com\/science\/article\/pii\/S0753332225006444?via%3Dihub\"><em data-start=\"2538\" data-end=\"2686\">Towards development of Nav1.7 channel modulators for pain treatment: A comparison of mexiletine effect in two cell models by automated patch clamp<\/em> (Biomedicine &amp; Pharmacotherapy, 2025)<\/a><\/p>\n<p data-start=\"2728\" data-end=\"2804\">\ud83d\udd2c Learn about the <a href=\"\/products\/patchliner\/\">Patchliner<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"<p>The voltage-gated sodium channel Nav1.7 is a key regulator of pain signaling. Mutations in this channel can ca [&hellip;]<\/p>\n","protected":false},"featured_media":17912,"template":"","news_categories":[528,15],"class_list":["post-17878","news","type-news","status-publish","has-post-thumbnail","hentry","news_categories-front-page-news","news_categories-blogs"],"acf":[],"_links":{"self":[{"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/news\/17878","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/news"}],"about":[{"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/types\/news"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/media\/17912"}],"wp:attachment":[{"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/media?parent=17878"}],"wp:term":[{"taxonomy":"news_categories","embeddable":true,"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/news_categories?post=17878"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}