Selective blocker of human NaV
1.7 channels (IC50
values are 0.17, 0.3, 0.4 and 1.1 μ
M at hNaV
1.4 and hNaV
1.5 respectively). Also inhibits tetrodotoxin-sensitive sodium channels. Displays analgesic efficacy in the formalin pain model.
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Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain.
Bregman et al.
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