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Nav1.7 blocker 52 is an inhibitor of voltage-gated sodium channel 1.7 (Nav1.7; IC50 = 0.17 µM).1 It is selective for Nav1.7 over human-ether-a-go-go (hERG), also known as Kv11.1, Nav1.5, and Nav1.8 (IC50s = >10, 1.1, and 2.2 µM, respectively) but does inhibit Nav1.3 and Nav1.4 (IC50s = 0.3 and 0.4 µM, respectively). Nav1.7 blocker 52 (20 and 30 mg/kg) inhibits formalin-induced flinching in a rat model of persistent pain. It also increases the latency to paw withdrawal in a hot plate test in a mouse model of inflammatory pain induced by complete Freund’s adjuvant (CFA).2
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1. Identification of a potent, state-
2. Inhibition of inactive states of tetrodotoxin-