Raxatrigine is an inhibitor of voltage-gated sodium channels (Nav; IC50s = 22, 13, 23, 10, 84, 15, 32, and 6 ?M for Nav1.1-Nav1.8 channels in a FLIPR membrane potential assay using HEK293 cells).1 Its activity is state-dependent at the Nav1.7 channel, with a nine-fold increase in potency for the open/inactivated state (IC50 = 6.3 ?M) compared to the closed/resting state (IC50 = 54 ?M). Raxatrigine (30 mg/kg, i.p.) decreases spontaneous pain behavior in an OD1 mouse pain model.
1.Deuis, J.R., Wingerd, J.S., Winter, Z., et al.Analgesic effects of GpTx-1, PF-04856264 and CNV1014802 in a mouse model of NaV1.7-mediated painToxins (Basel)8(3)78(2016)