ABT-639 is a novel, peripherally acting, selective T-type Ca2+ channel blocker. It effectively blocks recombinant human T-type (Cav3.2) Ca2+ channels and attenuates low voltage-activated currents in rat DRG neurons. With high oral bioavailability and low brain:plasma ratio, it demonstrates dose-dependent antinociception in models of knee joint pain and increases tactile allodynia thresholds in neuropathic pain models.
- Selective T-type Ca2+ channel blocker
- High oral bioavailability
- Low protein binding
- Low brain:plasma ratio
- Produces antinociception in knee joint pain models
- Increases tactile allodynia thresholds in neuropathic pain models
- Does not significantly alter hemodynamic or psychomotor function at higher doses