Differential Inhibition of Human Nav1.2 Resurgent and Persistent Sodium Currents by Cannabidiol and GS967

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dc.contributor.authorMason, Emily R.
dc.contributor.authorCummins, Theodore R.
dc.contributor.departmentPharmacology and Toxicology, School of Medicineen_US
dc.date.accessioned2020-06-25T17:16:44Z
dc.date.available2020-06-25T17:16:44Z
dc.date.issued2020-04
dc.description.abstractMany epilepsy patients are refractory to conventional antiepileptic drugs. Resurgent and persistent currents can be enhanced by epilepsy mutations in the Nav1.2 channel, but conventional antiepileptic drugs inhibit normal transient currents through these channels, along with aberrant resurgent and persistent currents that are enhanced by Nav1.2 epilepsy mutations. Pharmacotherapies that specifically target aberrant resurgent and/or persistent currents would likely have fewer unwanted side effects and be effective in many patients with refractory epilepsy. This study investigated the effects of cannbidiol (CBD) and GS967 (each at 1 μM) on transient, resurgent, and persistent currents in human embryonic kidney (HEK) cells stably expressing wild-type hNav1.2 channels. We found that CBD preferentially inhibits resurgent currents over transient currents in this paradigm; and that GS967 preferentially inhibits persistent currents over transient currents. Therefore, CBD and GS967 may represent a new class of more targeted and effective antiepileptic drugs.en_US
dc.eprint.versionFinal published versionen_US
dc.identifier.citationMason, E. R., & Cummins, T. R. (2020). Differential Inhibition of Human Nav1.2 Resurgent and Persistent Sodium Currents by Cannabidiol and GS967. International journal of molecular sciences, 21(7), 2454. https://doi.org/10.3390/ijms21072454en_US
dc.identifier.urihttps://hdl.handle.net/1805/23095
dc.language.isoen_USen_US
dc.publisherMDPIen_US
dc.relation.isversionof10.3390/ijms21072454en_US
dc.relation.journalInternational Journal of Molecular Sciencesen_US
dc.rightsAttribution 4.0 International*
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/*
dc.sourcePMCen_US
dc.subjectVoltage-gated sodium channelsen_US
dc.subjectAntiepileptic drugsen_US
dc.subjectNav1.2en_US
dc.subjectCBDen_US
dc.subjectCannabidiolen_US
dc.subjectGS967en_US
dc.subjectPrax330en_US
dc.subjectResurgent currenten_US
dc.subjectPersistent currenten_US
dc.titleDifferential Inhibition of Human Nav1.2 Resurgent and Persistent Sodium Currents by Cannabidiol and GS967en_US
dc.typeArticleen_US
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