Cannabidiol interactions with voltage-gated sodium channels

eLife logo “Voltage-gated sodium channels are targets for a range of pharmaceutical drugs developed for treatment of neurological diseases.

Cannabidiol (CBD), the non-psychoactive compound isolated from cannabis plants, was recently approved for treatment of two types of epilepsy associated with sodium channel mutations.

This study used high resolution X-ray crystallography to demonstrate the detailed nature of the interactions between CBD and the NavMs voltage-gated sodium channel, and electrophysiology to show the functional effects of binding CBD to these channels.

CBD binds at a novel site at the interface of the fenestrations and the central hydrophobic cavity of the channel. Binding at this site blocks the transmembrane-spanning sodium ion translocation pathway, providing a molecular mechanism for channel inhibition. Modelling studies suggest why the closely-related psychoactive compound tetrahydrocannabinol may not have the same effects on these channels. Finally, comparisons are made with the TRPV2 channel, also recently proposed as a target site for CBD.

In summary, this study provides novel insight into a possible mechanism for CBD interactions with sodium channels.”

https://pubmed.ncbi.nlm.nih.gov/33089780/

https://elifesciences.org/articles/58593

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