Cannabidiol activates neuronal Kv7 channels.
basic_science · Level V
Where this comes from
- Record sourced from PubMed, PMID 35179483.
- Also identified by DOI 10.7554/eLife.73246 and PMC identifier 8856652.
- Licence recorded as CC BY.
- The licence permits redistribution, so the abstract is shown in full and the full text is available from the publisher.
Abstract
Cannabidiol (CBD), a chemical found in the <i>Cannabis sativa</i> plant, is a clinically effective antiepileptic drug whose mechanism of action is unknown. Using a fluorescence-based thallium flux assay, we performed a large-scale screen and found enhancement of flux through heterologously expressed human Kv7.2/7.3 channels by CBD. Patch-clamp recordings showed that CBD acts at submicromolar concentrations to shift the voltage dependence of Kv7.2/7.3 channels in the hyperpolarizing direction, producing a dramatic enhancement of current at voltages near -50 mV. CBD enhanced native M-current in mouse superior cervical ganglion starting at concentrations of 30 nM and also enhanced M-current in rat hippocampal neurons. The potent enhancement of Kv2/7.3 channels by CBD may contribute to its effectiveness as an antiepileptic drug by reducing neuronal hyperexcitability.
Medical subject headings
- Cannabidiol
- KCNQ2 Potassium Channel
- KCNQ3 Potassium Channel
- Neurons