Co 102862. Voltage-gated Na+ channels play key roles in determining neuronal excitability. Voltage- and use-dependent block 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 antiarrhythmics.
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 channel. IC50 values are 0.28-15.9 μM in rat hippocampal neurons.
Co 102862 is an anticonvulsant, demonstrating potent activity in rodent models of tonic/clonic and partial-complex seizures.
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