FIGURE 2.
Effect of Gr4b on Nav channel subtypes. (A) Representative current traces showing that Gr4b slowed the fast inactivation of Nav1.9 expressed in ND7/23 cells. The currents evoked by 100 ms depolarization to −40 mV from holding potentials of −120 mV. (B) The dose-response curves for the Gr4b-induced inhibition of the fast inactivation of Nav1.9, EC50 of 25 ± 1 nM (n = 6). (C,D) Representative current traces show that Gr4b blocked the currents of Nav1.4 and Nav1.7. Currents were elicited by 50 ms depolarizing steps to −10 mV from a holding potential of −90 mV. (E) Dose-response curves for Gr4b inhibiting Nav1.4 and Nav1.7 currents. The IC50 values were 411 ± 184 nM and 27 ± 3 nM for hNav1.4 and Nav1.7, respectively (n = 4–6). (F) Representative traces show that the Nav1.8 currents are unaffected by Gr4b (n = 4). Representative current traces from ND7/23 cells expressing Nav1.8 in the absence (black) and presence of 250 nM (red) or 2.5 μM (blue) Gr4b. Currents were elicited by 50 ms depolarizing steps to 10 mV from a holding potential of −90 mV.