Fig. 4.

Binding of other channel blockers. (A) Comparisons of the channel-blocking effects of compounds listed in Table 1. Plots of drug concentrations versus block of the NavMs current were fit by the Hill equation. The IC₅₀s are listed in Table 1 (±SEM, n = 4–8 replicates). (B) Comparisons of channel blocker potencies, hydrophobicities, and recoveries from block for compounds listed in Table 1. (Upper) The potencies (IC₅₀) for NavMs (filled circles) and hNa_v1.1 (open circles), and octanol:water partition coefficient log P (blue squares) are plotted for each drug listed in the lower panel. (Lower) Percentage of current recovered after ≥60% sodium current block. (C) The structure of the NavMs-pore (ribbon representation with the same monomer colors as in Fig. 2) overlaid with the anomalous difference maps contoured at 5 σ for compounds PI1 to PI5 (red for PI1, cyan for PI2, magenta for PI3, yellow for PI4, green for PI5), showing the similarity of the positions of the bromine atoms.