AMG 8379 (AMG-8379, AMG8379) is a potent and selective voltage-gated sodium channel Nav1.7 antaognist with IC50 of 8.5 nM.
AMG 8379 potently blocks endogenous tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglion (DRG) neurons with IC50 of 3.1 nM in whole-cell patch clamp electrophysiology assays.
AMG 8379 displays100- to 1000-fold selectivity over other NaV family members, including NaV1.4 and NaV1.5.
AMG 8379 blocks mechanically induced action potential firing in C-fibers, reduces the frequency of thermally induced C-fiber spiking.
AMG 8379 exhibits pharmacodynamic effects in translatable models of both itch and pain.
