Cannabidiol Selectively Binds to the Voltage-Gated Sodium Channel Na_v1.4 in Its Slow-Inactivated State and Inhibits Sodium Current.

ABSTRACT: Cannabidiol (CBD), one of the cannabinoids from the cannabis plant, can relieve the myotonia resulting from sodium channelopathy, which manifests as repetitive discharges of muscle membrane. We investigated the binding kinetics of CBD to Na_v1.4 channels on the muscle membrane. The binding affinity of CBD to the channel was evaluated using whole-cell recording. The CDOCKER program was employed to model CBD docking onto the Na_v1.4 channel to determine its binding sites. Our results revealed no differential inhibition of sodium current by CBD when the channels were in activation or fast inactivation status. However, differential inhibition was observed with a dose-dependent manner after a prolonged period of depolarization, leaving the channel in a slow-inactivated state

SUBMITTER: Huang CW 

PROVIDER: S-EPMC8465134 | biostudies-literature | 2021 Sep

REPOSITORIES: biostudies-literature