Cannabidiol activates neuronal Kv7 channels
Year: 2022
Type: article
Abstract: 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.
Source: eLife
DOI: 10.7554/elife.73246
Institutions: Harvard University, Boston Children's Hospital
Language: English
Subfield: Molecular Biology
Domain: Life Sciences
Open Access status: gold
Estimated APC paid: $2,500
Awards: Voltage-dependent ion channels controlling firing patterns of central neurons, G1197465562, G2515541506, G5187253962, State-dependent interaction of antiepileptic drugs with voltage-dependent sodium channels and differential regulation of excitatory and inhibitory central neurons, Boston Intellectual and Developmental Disabilities Research Center, Voltage-dependent ion channels in Purkinje neurons, G7760141445, G786101262, Boston Children's Hospital/HMS Intellectual and Developmental Disabilities Research Center, Unravelling Mechanisms and Novel Therapeutic Targets for Peripheral Neuropathy and Neuropathic Pain
OpenAlex ID: W4212875674