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Cannabidiol activates neuronal Kv7 channels

By Zachary Niday, Laurel Heckman, Sooyeon Jo, Han-Xiong Bear Zhang, Akie Fujita, Jaehoon Shim, Roshan Pandey, Hoor Al Jandal, Selwyn Jayakar, Jennifer A Smith, Clifford J Woolf, Bruce P. Bean

Posted 21 Aug 2021
bioRxiv DOI: 10.1101/2021.08.20.457154

Cannabidiol (CBD), a chemical found in the Cannabis sativa 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. Using patch clamp recordings, we found that CBD at low concentrations activates Kv7.2/7.3 channels at subthreshold voltages, with 100 nM CBD producing a doubling of current at -50 mV. CBD shifted the voltage-dependence of channels in the hyperpolarizing direction, producing a shift in the midpoint of activation by about ~-14 mV at 300 nM. CBD also effectively enhanced native M-current in both mouse superior cervical ganglion neurons and rat hippocampal neurons. The potent enhancement of Kv2/7.3 channels by CBD seems likely to contribute to its effectiveness as an antiepileptic drug by reducing neuronal hyperexcitability.

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