Ontology highlight
ABSTRACT:
SUBMITTER: Alexandrou AJ
PROVIDER: S-EPMC4822888 | biostudies-literature | 2016
REPOSITORIES: biostudies-literature
Alexandrou Aristos J AJ Brown Adam R AR Chapman Mark L ML Estacion Mark M Turner Jamie J Mis Malgorzata A MA Wilbrey Anna A Payne Elizabeth C EC Gutteridge Alex A Cox Peter J PJ Doyle Rachel R Printzenhoff David D Lin Zhixin Z Marron Brian E BE West Christopher C Swain Nigel A NA Storer R Ian RI Stupple Paul A PA Castle Neil A NA Hounshell James A JA Rivara Mirko M Randall Andrew A Dib-Hajj Sulayman D SD Krafte Douglas D Waxman Stephen G SG Patel Manoj K MK Butt Richard P RP Stevens Edward B EB
PloS one 20160406 4
Human genetic studies show that the voltage gated sodium channel 1.7 (Nav1.7) is a key molecular determinant of pain sensation. However, defining the Nav1.7 contribution to nociceptive signalling has been hampered by a lack of selective inhibitors. Here we report two potent and selective arylsulfonamide Nav1.7 inhibitors; PF-05198007 and PF-05089771, which we have used to directly interrogate Nav1.7's role in nociceptor physiology. We report that Nav1.7 is the predominant functional TTX-sensitiv ...[more]