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. 2012 Sep;140(3):307–324. doi: 10.1085/jgp.201210826

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© 2012 Garg et al.

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Figure 2. — Voltage-dependent hEAG1 channel block by astemizole. (A) Control hEAG1 currents (bottom) elicited with voltage-pulse protocol shown in the top. V_h was −100 mV, and V_pre was 10 s in duration and ranged from −130 to +35 mV, applied in 15-mV increments. (B) Currents recorded from the same oocyte after steady-state block by 2 µM astemizole. (C) Voltage dependence of hEAG1 activation (◆) and inactivation (■) in control, and inhibition by 2 µM astemizole (□). For inactivation and inhibition curves, normalized I_max was plotted as a function of V_pre. For the activation curve, I_pre normalized for electrical driving force was plotted as a function of V_pre. Data (n = 5) were fitted with a Boltzmann function (curves). For control inactivation, V_0.5 = −88.5 ± 2.4 mV and z = 2.84 ± 0.62; for control activation, V_0.5 = −17.8 ± 1.4 mV and z = 1.84 ± 0.01. For inactivation in the presence of astemizole, V_0.5 = −15.7 ± 3.3 mV and z = 1.51 ± 0.07. (D) Comparison of the voltage dependence of hEAG1 activation (dashed curve) and block by 2 µM astemizole (□).