Is reverse use-dependence physiologically relevant? We now have a follow-up testing action potential clamp 20 Hz on Nav1.8 cell line at 37C. Under these conditions, only Abbott A-887 inhibition is relieved, but Vertex compounds re-inhibit too quickly doi.org/10.1085/jgp....
Differential state-dependent Nav1.8 inhibition by suzetrigine, LTGO-33, and A-887826
Jo et al. use the Nav1.8 inhibitors suzetrigine, A-887826, and LTGO-33 to show differences in the kinetics with which the compounds unbind from depolarized
doi.org
March 31, 2025 at 9:52 PM
Is reverse use-dependence physiologically relevant? We now have a follow-up testing action potential clamp 20 Hz on Nav1.8 cell line at 37C. Under these conditions, only Abbott A-887 inhibition is relieved, but Vertex compounds re-inhibit too quickly doi.org/10.1085/jgp....