CP-465022 Maleate is a potent, selective, noncompetitive AMPA receptor antagonist with anticonvulsant activity. It effectively counters the Kainate-induced response in rat cortical neurons, exhibiting an IC 50 of 25 nM. As such, CP-465022 Maleate presents a valuable instrument for studying the involvement of AMPA receptors in various physiological and pathophysiological processes [1] [2].

CP-465022 (0.0001 μM-10 μM) progressively inhibits kainate-induced responses based on its concentration, achieving a 50% inhibition concentration (IC50) of 25 nM, with near-total inhibition at 3.2 μM [1]. At a concentration of 1 μM for 10 minutes, CP-465022 marginally affects peak NMDA-induced currents but decreases the currents measured at 8 seconds by 26%. When increased to 10 μM, CP-465022 reduces peak NMDA-induced currents by 36% and significantly diminishes currents measured at the same time interval by 70% in primary cortical and cerebellar granule neuron cultures [1]. Similarly, a 10-minute exposure to 1 μM CP-465022 impedes peak NMDA currents by 19% and reduces subsequent currents at 8 seconds by 45% in rat cerebellar granule neuron cultures, aligning with effects observed in cortical neurons [1]. Furthermore, CP-465022 (100 nM-10 μM) demonstrates inhibitory actions on kainate-induced currents in rat hippocampal cells, with 100 nM CP-465022 suppressing the development of kainate currents over 200 seconds. Concentrations of 500 nM and 1 μM achieve almost complete inhibition (99.3%) within this timeframe [1].