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Retigabine, a KV7 channel opener and novel
anticonvulsant compound
Retigabine (RTG), initially derived from flupirtine, a
substance used for therapy of acute and chronic pain,
enhances the activity of KV7.2–5 channels (Rundfeldt &
Netzer, 2000; Tatulian et al. 2001; Dupuis et al. 2002).
Since none of the clinically used anticonvulsants exhibits a
similar mechanism of action,RTGrepresents a new class of
anticonvulsant compounds the effectiveness of which has
been demonstrated in many seizure models (summarized
in Wuttke & Lerche, 2006). It is currently undergoing
phase III clinical testing for pharmacoresistent focal
epilepsies. Since augmentation of theMcurrent mediated
by RTG-activated KV7.2 and KV7.3 channels will lead to a
stabilization of the resting and subthreshold membrane
potential towards the K+ equilibrium potential, thus
generally reducing membrane excitability, M channels
are an attractive pharmacological target to treat any
disease going along with neuronal hyperexcitability, such
as epilepsy, PNH, neuropathic pain, migraine and stroke.
It is important to note that RTG does not enhance the
activity of the cardiac KV7.1 channel (Fig. 5A) rendering
cardiac side-effects unlikely.
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