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Tranilast has long been used as a TRPV2 inhibitor, but its molecular mechanism remained unclear. The study expressed rat TRPV2 in HEK293 cells and measured whole-cell currents and calcium influx with established agonists. Tranilast up to 1 mM did not directly block TRPV2 activity, yet reduced chloramine T–dependent, oxidation-induced TRPV2 activation. Tranilast also attenuated ROS-related effects on TRPA1 and voltage-gated Na+ channel currents, and lowered phagocytosis in RBL cells, with a smaller reduction in TRPV2 knockouts, indicating indirect, redox-dependent modulation.",{"@graph":69,"@context":122},[70,84,105],{"@type":71,"itemListElement":72},"BreadcrumbList",[73,77,79,82],{"item":74,"name":75,"@type":76,"position":8},"https://docshare.wps.com","Home","ListItem",{"item":78,"name":9,"@type":76,"position":14},"https://docshare.wps.com/document/",{"item":80,"name":35,"@type":76,"position":81},"https://docshare.wps.com/document/healthcare/",3,{"item":83,"name":65,"@type":76,"position":19},"https://docshare.wps.com/document/tranilast-does-not-inhibit-trpv2/461018/",{"url":83,"name":65,"@type":85,"image":86,"author":91,"headline":65,"publisher":94,"fileFormat":97,"inLanguage":63,"description":67,"dateModified":98,"datePublished":99,"encodingFormat":97,"isAccessibleForFree":100,"interactionStatistic":101},"DigitalDocument",{"url":87,"@type":88,"width":89,"height":90},"https://docshare.wps.com/thumbnails/tranilast-does-not-inhibit-trpv2/461018.png","ImageObject",300,407,{"name":92,"@type":93},"นรินทร์","Person",{"url":74,"name":95,"@type":96},"DocShare","Organization","application/pdf","2026-10-31","2026-09-30",true,{"@type":102,"interactionType":103,"userInteractionCount":34},"InteractionCounter",{"@type":104},"ViewAction",{"@type":106,"mainEntity":107},"FAQPage",[108,114,118],{"name":109,"@type":110,"acceptedAnswer":111},"Does tranilast directly inhibit TRPV2 currents and calcium influx?","Question",{"text":112,"@type":113},"No. Tranilast up to 1 mM did not inhibit TRPV2-mediated currents or calcium influx induced by established agonists in the experimental setup described.","Answer",{"name":115,"@type":110,"acceptedAnswer":116},"How does tranilast affect TRPV2 activation under oxidative conditions?",{"text":117,"@type":113},"When co-applied with the oxidant chloramine T, tranilast diminished oxidation-induced activation of TRPV2, consistent with interference in redox signaling rather than direct channel blockade.",{"name":119,"@type":110,"acceptedAnswer":120},"What functional effects did tranilast show beyond TRPV2?",{"text":121,"@type":113},"Tranilast reduced chloramine T-induced activation of TRPA1, impaired development of non-inactivating voltage-gated Na+ channel currents, and decreased phagocytic activity in RBL cells, with less reduction in TRPV2-knockout cells.","https://schema.org",{"og:url":83,"og:type":124,"og:title":65,"og:site_name":95,"og:description":67},"article",{"robots":126,"canonical":83},"index,follow",{"doc_id":128,"site_id":62},461018,1790845412,{"code":4,"msg":5,"data":131},{"doc_id":128,"user_id":132,"nickname":92,"user_avatar":133,"doc_module":4,"category_id":34,"category_name":35,"doc_title":65,"doc_description":67,"doc_content":134,"file_id":135,"file_url":136,"file_type":137,"file_size":138,"view_count":34,"is_deleted":4,"is_public":8,"is_downloadable":8,"audit_status":8,"page_count":139,"language":140,"language_code":63,"site_id":62,"html_lang":63,"table_of_contents":141,"faqs":142,"seo_title":143,"seo_description":67,"update_tm":144,"read_time":145,"preview_page_count":4},2336475104957,"https://ap-avatar.wpscdn.com/avatar/22000c4c6bd8a5076e1?x-image-process=image/resize,m_fixed,w_180,h_180&k=1787554080175789136","Article  \nTranilast Does Not Inhibit TRPV2  \nTabea C. Fricke 1,2, *, Nele Stein 1, Christine Herzog 1, Frank G. Echtermeyer 1 and Andreas Leffler 1  \nAcademic Editors: Hiroki Kittaka and Makoto Tominaga  \nReceived: 19 November 2025  \nRevised: 5 December 2025  \nAccepted: 19 December 2025  \nPublished: 21 December 2025  \nCopyright: © 2025 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license.  \n1 Department of Anesthesiology and Intensive Care Medicine, Hannover Medical School, Carl-Neuberg Strasse 1, 30625 Hannover, Germany  \n2 PRACTIS Clinician Scientist Program, Dean’s Office for Academic Career Development, Hannover Medical School, Carl-Neuberg Strasse 1, 30625 Hannover, Germany  \n* Correspondence: [fricke.tabea@mh-hannover.de](fricke.tabea@mh-hannover.de); Tel.: +49-511-532-8494  \nHighlights  \nWhat are the main findings?  \n• Tranilast does not directly block TRPV2 currents or calcium influx induced by established agonists.  \n• Tranilast reduces oxidation-induced TRPV2 modulation rather than direct channel inhibition.  \nWhat are the implications of the main findings?  \n• The long-held view of tranilast as a TRPV2 blocker should be reconsidered; its effects are indirect and redox-dependent.  \n• This work refines the pharmacological understanding of TRPV2 modulation and guides more accurate experimental and therapeutic use of tranilast in TRPV2 channel research.  \nAbstract  \nTransient receptor potential vanilloid 2 (TRPV2) is a non-selective cation channel involved in diverse physiological and pathological processes. Tranilast has frequently been described and used as a rather specific inhibitor of TRPV2 . However, the molecular basis of this inhibition was never been studied in detail. Here, we investigated whether tranilast indeed directly inhibits TRPV2 . Rat TRPV2 was expressed in human embryonic kidney (HEK293) cells, and channel function was assessed using whole-cell electrophysiology and calcium imaging in response to established agonists. In parallel, we conducted phagocytosis assays in rat basophilic leukemia (RBL) cells, including a CRISPR/Cas9-generated TRPV2-knockout cell line. Tranilast up to 1 mM did not inhibit TRPV2-mediated currents or calcium influx induced by any agonist. However, when co-applied with the oxidant chloramine T, tranilast diminished oxidation-induced activation of TRPV2 . This effect may indicate a general interference of tranilast with redox signaling. Accordingly, tranilast also reduced chloramine T-induced activation of TRPA1 as well as the development of non-inactivating currents of voltage-gated Na+ channels. Furthermore, tranilast decreased phagocytic activity in both wildtype and TRPV2-knockout RBL cells. However, the reduction was less pronounced in TRPV2-knockout cells. These findings demonstrate that tranilast does not directly inhibit TRPV2 . Instead, tranilast seems to indirectly suppress channel activation by reducing reactive oxygen species (ROS). This refined understanding of how tranilast modulates TRPV2 has important implications for the interpretation of prior and future pharmacological studies targeting TRPV2 .  \nKeywords: TRPV2; tranilast; reactive oxygen species (ROS); ion channel modulation; channel pharmacology  \n1. Introduction  \nTransient receptor potential (TRP) channels form a superfamily of non-selective cation channels that act as cellular sensors for a broad range of chemical and physical stimuli. Among these, the vanilloid subfamily member TRPV2 is a Ca2+-permeable channel expressed in multiple tissues, including immune cells, cardiac myocytes, and sensory neurons [1–3] . TRPV2 contributes to processes such as innate immune responses, cardiac contractility, cancer cell migration, and inflammatory signaling [2,4–7] . Owing to its diverse physiological roles, TRPV2 has attracted interest as a potential therapeutic target in several patho","cbCaik86K5aKSAZc","https://ap.wps.com/l/cbCaik86K5aKSAZc","pdf",1868295,18,"English","# Highlights\n# Abstract\n# 1. Introduction","[{\"question\":\"Does tranilast directly inhibit TRPV2 currents and calcium influx?\",\"answer\":\"No. Tranilast up to 1 mM did not inhibit TRPV2-mediated currents or calcium influx induced by established agonists in the experimental setup described.\"},{\"question\":\"How does tranilast affect TRPV2 activation under oxidative conditions?\",\"answer\":\"When co-applied with the oxidant chloramine T, tranilast diminished oxidation-induced activation of TRPV2, consistent with interference in redox signaling rather than direct channel blockade.\"},{\"question\":\"What functional effects did tranilast show beyond TRPV2?\",\"answer\":\"Tranilast reduced chloramine T-induced activation of TRPA1, impaired development of non-inactivating voltage-gated Na+ channel currents, and decreased phagocytic activity in RBL cells, with less reduction in TRPV2-knockout cells.\"}]","Tranilast Does Not Inhibit TRPV2 | PDF",1790760339,45]