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Journal: Pain
Article Title: Analgesia and peripheral c-fiber modulation by selective Na v 1.8 inhibition in rhesus
doi: 10.1097/j.pain.0000000000003404
Figure Lengend Snippet: Na v channel compound profile assessed on the Qube or Qpatch*. Ten-point titrations in the Qube automated patch-clamp assay determined MSD199 to be a potent and selective compound (IC 50 = 4.7 ± 0.8 nM, mean ± SD). MSD199 potency was too weak to calculate for all other Na v isoforms except Na v 1.4, which was 1781-fold shifted to 8370 nM mean IC 50 ± 1429.
Article Snippet: We characterized the potent, selective Na v 1.8 inhibitor 2-(4,4-difluoroazepan-1-yl)-6-methyl-N-(2-sulfamoylpyridin-4-yl)nicotinamide (C 18 H 22 N 5 O 3 S Cl, MSD199, Fig. ) using the automated
Techniques: Patch Clamp