Key result
Retigabine produced a hyperpolarizing shift in the activation curves for KCNQ2/3, KCNQ2, KCNQ3, and KCNQ4 currents, as well as native M channels in rat sympathetic neurons, but did not enhance cardiac KCNQ1 currents.
Population
Chinese hamster ovary cells expressing KCNQ1, KCNQ2, KCNQ3, KCNQ4, and KCNQ2/3 channels, and primary…
Comparison
Retigabine (0.1 to 1000 mM) vs Control conditions (absence of retigabine)
Design
Preclinical
Authors
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Supports neuronal KCNQ selectivity without cardiac KCNQ1 effects in rats; leaves open human translation and safety data.
Retigabine enhances neuronal KCNQ2-4 and native M-currents by shifting their activation to more hyperpolarized potentials, but does not affect cardiac KCNQ1 channels.
Tatulian et al. (2001) studied this question. Retigabine vs. Control (absence of retigabine) was evaluated on Shift in the half-activation potential (V1/2) of KCNQ channels. Retigabine produced a hyperpolarizing shift in the activation curves for KCNQ2/3, KCNQ2, KCNQ3, and KCNQ4 currents, as well as native M channels in rat sympathetic neurons, but did not enhance cardiac KCNQ1 currents.
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