Fig. 6
From: Direct neurotransmitter activation of voltage-gated potassium channels
GABA and metabolites compete for binding to KCNQ3-W265. All error bars in figure indicate SEM. a Mean effects of BHB and GABOB (10 µM) versus valeric acid (no effects at 5 mM) on KCNQ2/3 in oocytes (n = 5–6). b Mean dose response of KCNQ2/3 activation at −60 mV by GABA (from Fig. 2) and related compounds (n = 5–10). c In silico docking predicts that BHB and GABOB bind to KCNQ3-W265, the latter also H-bonding with L237 in the S4–5 linker. d, e GABOB (d), but not glutamate (e), antagonizes the effects of GABA on KCNQ2/3 activation in oocytes (n = 4–6). Upper, mean tail currents; lower, current fold-change elicited by neurotransmitter combination versus voltage. f GABOB antagonizes the effects of retigabine on KCNQ2/3 activation in oocytes (n = 10). Upper, mean tail currents; lower, current fold-change elicited versus voltage. Data are for KCNQ2/3 in the absence of retigabine (Ctrl), with retigabine (RTG), or with retigabine + GABOB (RTG + GABOB). **P < 0.01; ****P < 0.0001
