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.
产品描述
A Potent, State-Dependent Blocker of Neuronal NaV Channels
产品形式
Voltage-gated Na+ channels play key roles in determining neuronal excitability1. 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.