{"id":2692,"date":"2023-01-12T11:39:43","date_gmt":"2023-01-12T02:39:43","guid":{"rendered":"https:\/\/misterx95.myds.me\/wordpress\/?p=2692"},"modified":"2023-01-12T11:39:44","modified_gmt":"2023-01-12T02:39:44","slug":"berbamine-reduces-chloroquine-induced-itch-in-mice-through-inhibition-of-mrgprx1","status":"publish","type":"post","link":"https:\/\/misterx95.myds.me\/wordpress\/?p=2692","title":{"rendered":"Berbamine Reduces Chloroquine-Induced Itch in Mice through Inhibition of MrgprX1"},"content":{"rendered":"\n<p><a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/?term=Ryu+K&amp;cauthor_id=36430803\">Kunhi Ryu<\/a><sup>\u00a0<\/sup>,\u00a0<a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/?term=Heo+Y&amp;cauthor_id=36430803\">Yunkyung Heo<\/a><sup>\u00a0<\/sup>,\u00a0<a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/?term=Lee+Y&amp;cauthor_id=36430803\">Yechan Lee<\/a><sup>\u00a0<\/sup>,\u00a0<a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/?term=Jeon+H&amp;cauthor_id=36430803\">Hyejin Jeon<\/a><sup>\u00a0<\/sup>,\u00a0<a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/?term=Namkung+W&amp;cauthor_id=36430803\">Wan Namkung<\/a><sup>\u00a0<\/sup><\/p>\n\n\n\n<p><\/p>\n\n\n\n<h2>Abstract<\/h2>\n\n\n\n<p>Chloroquine (CQ) is an antimalaria drug that has been widely used for decades. However, CQ-induced pruritus remains one of the major obstacles in CQ treatment for uncomplicated malaria. Recent studies have revealed that MrgprX1 plays an essential role in CQ-induced itch. To date, a few MrgprX1 antagonists have been discovered, but they are clinically unavailable or lack selectivity. Here, a cell-based high-throughput screening was performed to identify novel antagonists of MrgprX1, and the screening of 2543 compounds revealed two novel MrgprX1 inhibitors, berbamine and closantel. Notably, berbamine potently inhibited CQ-mediated MrgprX1 activation (IC<sub>50<\/sub>&nbsp;= 1.6 \u03bcM) but did not alter the activity of other pruritogenic GPCRs. In addition, berbamine suppressed the CQ-mediated phosphorylation of ERK1\/2. Interestingly, CQ-induced pruritus was significantly reduced by berbamine in a dose-dependent manner, but berbamine had no effect on histamine-induced, protease-activated receptors 2-activating peptide-induced, and deoxycholic acid-induced itch in mice. These results suggest that berbamine is a novel, potent, and selective antagonist of MrgprX1 and may be a potential drug candidate for the development of therapeutic agents to treat CQ-induced pruritus.<\/p>\n\n\n\n<p><strong>Keywords:\u00a0<\/strong>Chloroquine; MrgprA3; MrgprX1; antagonist; berbamine; itch.<\/p>\n\n\n\n<p><\/p>\n\n\n\n<div class=\"wp-block-file\"><a href=\"https:\/\/misterx95.myds.me\/wordpress\/wp-content\/uploads\/2023\/01\/Berbamine-Reduces-Chloroquine-Induced-Itch-in-Mice-through-Inhibition-of-MrgprX1-copy.pdf\">Berbamine Reduces Chloroquine Induced Itch in Mice through Inhibition of MrgprX1<\/a><a href=\"https:\/\/misterx95.myds.me\/wordpress\/wp-content\/uploads\/2023\/01\/Berbamine-Reduces-Chloroquine-Induced-Itch-in-Mice-through-Inhibition-of-MrgprX1-copy.pdf\" class=\"wp-block-file__button\" download>Download<\/a><\/div>\n\n\n\n<p><\/p>\n\n\n\n<p>Presenter: Hye In Kim<\/p>\n","protected":false},"excerpt":{"rendered":"<p>Kunhi Ryu\u00a0,\u00a0Yunkyung Heo\u00a0,\u00a0Yechan Lee\u00a0,\u00a0Hyejin Jeon\u00a0,\u00a0Wan Namkung\u00a0 Abstract Chloroquine (CQ) is an antimalaria drug that has been widely used for decades. However, CQ-induced pruritus remains one of the major obstacles in CQ treatment for uncomplicated malaria. Recent studies have revealed that MrgprX1 plays an essential role in CQ-induced itch. To date, a few MrgprX1 antagonists have [&hellip;]<\/p>\n","protected":false},"author":7,"featured_media":0,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"site-sidebar-layout":"default","site-content-layout":"","ast-site-content-layout":"","site-content-style":"default","site-sidebar-style":"default","ast-global-header-display":"","ast-banner-title-visibility":"","ast-main-header-display":"","ast-hfb-above-header-display":"","ast-hfb-below-header-display":"","ast-hfb-mobile-header-display":"","site-post-title":"","ast-breadcrumbs-content":"","ast-featured-img":"","footer-sml-layout":"","theme-transparent-header-meta":"","adv-header-id-meta":"","stick-header-meta":"","header-above-stick-meta":"","header-main-stick-meta":"","header-below-stick-meta":"","astra-migrate-meta-layouts":"default","ast-page-background-enabled":"default","ast-page-background-meta":{"desktop":{"background-color":"var(--ast-global-color-4)","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""},"tablet":{"background-color":"","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""},"mobile":{"background-color":"","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""}},"ast-content-background-meta":{"desktop":{"background-color":"var(--ast-global-color-5)","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""},"tablet":{"background-color":"var(--ast-global-color-5)","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""},"mobile":{"background-color":"var(--ast-global-color-5)","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""}}},"categories":[1],"tags":[],"_links":{"self":[{"href":"https:\/\/misterx95.myds.me\/wordpress\/index.php?rest_route=\/wp\/v2\/posts\/2692"}],"collection":[{"href":"https:\/\/misterx95.myds.me\/wordpress\/index.php?rest_route=\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/misterx95.myds.me\/wordpress\/index.php?rest_route=\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/misterx95.myds.me\/wordpress\/index.php?rest_route=\/wp\/v2\/users\/7"}],"replies":[{"embeddable":true,"href":"https:\/\/misterx95.myds.me\/wordpress\/index.php?rest_route=%2Fwp%2Fv2%2Fcomments&post=2692"}],"version-history":[{"count":2,"href":"https:\/\/misterx95.myds.me\/wordpress\/index.php?rest_route=\/wp\/v2\/posts\/2692\/revisions"}],"predecessor-version":[{"id":2695,"href":"https:\/\/misterx95.myds.me\/wordpress\/index.php?rest_route=\/wp\/v2\/posts\/2692\/revisions\/2695"}],"wp:attachment":[{"href":"https:\/\/misterx95.myds.me\/wordpress\/index.php?rest_route=%2Fwp%2Fv2%2Fmedia&parent=2692"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/misterx95.myds.me\/wordpress\/index.php?rest_route=%2Fwp%2Fv2%2Fcategories&post=2692"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/misterx95.myds.me\/wordpress\/index.php?rest_route=%2Fwp%2Fv2%2Ftags&post=2692"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}