Overview
- Catterall, W.A. (1992) Physiol. Rev. 72, S15.
- Ilyin, V.I. et al. (2005) Br. J. Pharmacol. 144, 801.
- Carter, R.B. et al. (1997) Soc. Neurosci. Absrt. 23, 2163.
Alomone Labs Co 102862 inhibits NaV1.7 channel currents in HEK293 cells.A. Time course of current reversible inhibition by 50 µM Co 102862 (#C-160). Currents were elicited by a voltage ramp from a holding potential of -100 mV to 60 mV (30 ms) delivered every 10 seconds. B. Example traces of current response to voltage ramp stimulation before and during application of 50 µM Co 102862.
Voltage-gated Na+ channels play key roles in determining neuronal excitability1,2. Voltage- and use-dependent blockage of voltage-gated Na+ channels appear to be important in the mechanism of action of many anticonvulsants (e.g. phenytoin (PHT), carbamazepine (CBZ) and lamotrigine (LTG)), local anesthetics (e.g. lidocaine and bupivacaine) and Class I antiarrhythmics3-10.
Co 102862 is a potent, broad spectrum and state-dependent blocker of neuronal voltage-gated Na+ channels that interacts selectively with inactivated states as opposed to resting states of the channel11. IC50 values are 0.28-15.9 
μM in rat hippocampal neurons11.
Co 102862 is an anticonvulsant, demonstrating potent activity in rodent models of tonic/clonic and partial-complex seizures12.
