Selective, non-competitive AMPA antagonist (IC50
= 25 nM in rat cortical neurons) that displays potent anticonvulsant activity. Also significantly blocks the persistent component of Nav
1.6 channel activity. Brain penetrant and orally active.
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Functional characterization of CP-465,022, a selective, noncompetitive AMPA receptor antagonist.
Lazaro et al.
CP-465,022, a selective noncompetitive AMPA receptor antagonist, blocks AMPA receptors but is not neuroprotective in vivo.
Menniti et al.
Traditional AMPA receptor antagonists partially block Nav1.6-mediated persistent current.
Welch et al.