In vitro and in vivo properties of aminotriazines used in this study.

Shown for each compound are IC50 on non-inactivated human Nav1.7, IC50 on 20%-inactivated human Nav1.7, and IC50 on 20%-inactivated rat Nav1.7, all taken with patch-clamp electrophysiology; in vitro plasma protein binding; the ratio of brain to plasma concentrations in vivo; whether the compound produced analgesic efficacy in the rat formalin model of pain; and the plasma concentration corresponding to the lowest dose that produced efficacy. IC50s on hNav1.7 were measured with manual patch-clamp electrophysiology; IC50s on rNav1.7 were measured with the PatchXpress® automated electrophysiology platform. Brain to plasma ratios were calculated from concentrations experimentally measured following the formalin test. ND = no data. Analgesic efficacy was determined by a statistically significant (p In vitro and in vivo properties of aminotriazines used in this study.