Effect of retigabine
(RET), RL-81, and compound 60 on Kv7.2/Kv7.3 currents.
(A) Representative macroscopic current
traces recorded from CHO cell expressing Kv7.2/Kv7.3 channels in response
to the indicated voltage protocol before (left) and after (right)
application of 1 μM RET, RL-81 and compound 60,
as indicated. Current scale, 200 pA; time scale, 200 ms. (B,C) Dose–response
curves reporting the effects of the 3 indicated compounds on the V1/2 shift (ΔV1/2) in mV (B) and on maximal current density (Idrug/Icontrol; C) calculated at
+20 mV for Kv7.2/Kv7.3 channels. (D,E) Current density of the indicated
homomeric Kv7.2 channels (D) and the effect of 10 μM RET or
1 μM 60 on the indicated homomeric Kv7.2 mutant
channels. * indicates values significantly different (p < 0.05) from respective controls.