Potent and selective Nav
1.7 channel blocker (IC50
= 8, 11 and 171 nM for mouse, human and rat Nav
1.7, respectively). Exhibits selectivity for Nav
1.7 over other Nav
1 channels (IC50
values are 0.11, 0.16, 0.85, 10, 11 and 25 μ
M for Nav
1.3 and Nav
1.5, respectively). Also exhibits selectivity over a panel of 81 other ion channels, receptors, enzymes and transporters. Blocks spontaneous firing of inherited erythromelalgia (IEM)-derived iPSC sensory neurons in vitro
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Pharmacological reversal of a pain phenotype in iPSC-derived sensory neurons and patients with inherited erythromelalgia.
Cao et al.
Subtype-selective small molecule inhibitors reveal a fundamental role for Nav1.7 in nociceptor electrogenesis, axonal conduction and presynaptic release.
Alexandrou et al.
PLoS One, 2016;11:e0152405