1. The slow kinetics of TREK‐1 inhibition by THexA.
The slow kinetics of TREK‐1 inhibition by THexA. (A) State‐dependent inhibition of ShakerΔ6–46 channels with 20 μM THexA indicative of open‐channel block. (B) Time course of TREK‐1 inhibition of indicated QA compounds (5 μM THexA, 50 μM TPenA and 5 mM TButA) equalized for better comparison (i.e., 5 mM TButA produced only 60% inhibition) as monitored by a fast piezo‐driven application system. (C) The blocking and unblocking time course from experiments as shown in (B) was fitted with a monoexponential function and τ values for QA inhibition (τon) and recovery from QA inhibition (τoff) are plotted (n⩾3 for each blocker). The dotted lines represent the time courses for activation/deactivation on pHi gating as illustrated in the inset (n=7).
Paula L Piechotta et al. EMBO J. 2011;30:
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