Retigabine is a positive allosteric modulator of KCNQ2-5 (KV7.2-7.5) ion channels, with EC50 values being 1.4, 1.6 and 5.2 μM for KCNQ3/5, KCNQ2/3 and KCNQ4, respectively. Retigabine is the first neuronal potassium channel opener used for the treatment of epilepsy. KCNQ2-5 channels, predominantly expressed in neurons, are important determinants of cellular excitability. The occurrence of human genetic mutations in KCNQ2/3 channels are associated with the syndrome of benign familial neonatal convulsions.
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