Figure 5.

CBD block of F1763A mutant, NaChBac, and Kv2.1. A, TTC block of hNav1.1 (hNav1.1, IC₅₀ = 1.6 ± 0.1 μm, slope = 0.7 ± 0.03; Phe¹⁷⁶³, IC₅₀ ∼ 44.1 μm) with and without the F1763A mutation. B, F1763A causes a slight decrease in CBD potency in hNav1.1 (hNav1.1: IC₅₀ = 2.5 ± 0.2 μm, slope = 2.0 ± 0.2, n = 2–6; F1763A: IC₅₀ = 4.8 ± 0.2 μm, slope = 4.1 ± 0.6, n = 3–811 cells exposed at each concentration). C, shows a comparison of the CBD inhibition of hNav1.6, NaChBac, and Kv2.1 (hNav1.6: IC₅₀ = 3.0 ± 0.1 μm, slope = 3.1 ± 0.2, n = 2–6; NaChBac: IC₅₀ = 1.5 ± 0.2 μm, slope = 2.8 ± 0.9, n = 1–4; Kv2.1: IC₅₀ = 3.7 ± 0.8 μm, slope = 1.1 ± 0.2, n = 1–5 11 cells exposed at each concentration). D, shows the state-dependent block of NaChBac tested at −55 and −100 mV (−100 mV: IC₅₀ = 1.5 ± 0.2 μm, slope = 2.8 ± 0.9, n = 1–4; −55 mV: IC₅₀ = 0.24 ± 0.05 μm, slope = 2.8 ± 0.9, n = 1–311 cells exposed at each concentration). E, current traces associated with the channels shown in C.