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Updated: Aug 16, 2026

High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels
Published on: January 27, 2013
A potassium channel, the M-channel, as a therapeutic target
1Graduate Group in Biophysics, University of California-San Francisco, San Francisco, CA 94143-0725, USA.
Abstract:
Compounds that stimulate or inhibit M-channels (ie, voltage-gated potassium channels formed by KCNQ2, KCNQ3 and KCNQ5) have been evaluated in clinical trials for epilepsy, stroke and Alzheimer's disease. The importance of M-channel function in reducing neuronal excitability is underscored by the finding that KCNQ2/3 mutations causing mild reduction of M-channel activity are linked to neonatal epilepsy. M-channel openers decrease the hyperexcitability responsible for epileptic seizures, neuropathic pain and migraine. Conversely, M-channel blockers may enhance cognitive functions. The M-channel has thus emerged as a promising target for treating epilepsy, stroke, migraine, pain, dementia, anxiety and bipolar disorder.
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