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Co 102862 is a state-dependent inhibitor of voltage-gated sodium channels (Nav).1 It selectively binds to inactivated Nav channels over resting Nav channels (Kis = 0.6 and >15 µM, respectively). Co 102862 (1 µM) inhibits sodium currents (INa) in primary rat acutely dissociated hippocampal neurons. In vivo, Co 102862 inhibits early- and late-phase nociceptive responses in the formalin test in mice (ED50s = 10.6 and 5.2 mg/kg, respectively).2 It also reduces the number of tonic seizures induced by maximum electroshock (MES) in mice and rats.
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1. V102862 (Co 102862): A potent, broad-
2. In vivo metabolism and mass balance of 4-