Retigabine

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Description

Retigabine (Ezogabine, D-23129) is an anticonvulsant for KCNQ2/3 currents with EC50 of 3.6 μM. Retigabine is a KCNQ/Kv7 potassium channel activator which functions by enhancing potassium currents via stabilizing the open conformation of the Kv7.2-7.3 channels. Studies indicate that the agonist binds in between two subunits of the channel which allows it to stabilize the channels open conformation. In addition, KCNQ3, a type of KCNQ channel, includes a hydrophobic pocket which contains a Leu338 region which is the binding site for retigabine. Furthermore, Retigabine has been shown to accelerate the activation of neuronal resting potentials while slowing deactivation of these currents. Secondly, Retigabine selectively activates the KCNQ2-5 isoforms, which results in an increased open channel probability. Studies also indicate that this compound can act as a GABA enhancer via amplifying the production of GABA in cortical neurons.

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