QO-83, Retigabine analogue, is a voltage-gated potassium channel KCNQ2 (Kv7.2) activator with an EC 50 of 0.56 μM. QO-83 binds to a single hydrophobic pocket of KCNQ2-CaM complex in closed conformation. QO-83 induces a negative shift in the voltage-dependent activation curve of KCNQ2 channels, increasing the channel's voltage sensitivity. QO-83 can be used for the research of epilepsies [1].
In Vitro, QO-83 (20 μM; 1 h) binds to a single hydrophobic pocket in the PD (S5-S6 interface) of human KCNQ2-CaM complex in closed conformation, inducing conformational rearrangements of the PD and VSD (S3-S4 interface)[1]. QO-83 (10 μM) shifts the voltage-dependent activation curve negatively[1].
References:
[1]. Zhao Y, et al. Structure basis for the activation of KCNQ2 by endogenous and exogenous ligands. Cell Rep. 2026;45(1):116771.
In Vitro, QO-83 (20 μM; 1 h) binds to a single hydrophobic pocket in the PD (S5-S6 interface) of human KCNQ2-CaM complex in closed conformation, inducing conformational rearrangements of the PD and VSD (S3-S4 interface)[1]. QO-83 (10 μM) shifts the voltage-dependent activation curve negatively[1].
References:
[1]. Zhao Y, et al. Structure basis for the activation of KCNQ2 by endogenous and exogenous ligands. Cell Rep. 2026;45(1):116771.