Key result
Retigabine inhibited KV2.1 channels with an IC50 of 22.0 μM and significantly reduced KV2.1 current density at clinically relevant concentrations upon prolonged exposure.
Effect estimate: IC50 22.0 μM
Retigabine, a KV7 channel opener, also inhibits KV2.1 channels at clinically relevant concentrations, which may explain its neuroprotective properties and potential off-target effects.
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Retigabine's KV2.1 inhibition at clinical concentrations warrants monitoring; leaves open whether this mediates neuroprotection or off-target effects in humans.
Stas et al. (2016) studied this question. Retigabine vs. Control (vehicle/DMSO) was evaluated on Inhibition of KV2.1 currents (IC50 22.0 μM). Retigabine inhibited KV2.1 channels with an IC50 of 22.0 μM and significantly reduced KV2.1 current density at clinically relevant concentrations upon prolonged exposure.
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