CP-465022 (maleate)

CP-465022 Maleate is a potent, and selective noncompetitive AMPA receptor antagonist with anticonvulsant activity. CP-465022 is against Kainate-induced response with an IC₅₀?of 25 nM in rat cortical neurons. CP-465022 provides a new tool to investigate the role of AMPA receptors in physiological and pathophysiological processes^[1][2]. IC50 & Target: IC50: 25 nM (rat cortical neurons)^[1] In Vitro: CP-465022 (0.0001 μM-10 μM) inhibits kainate-induced response in relatively slow manner and dependents on compound concentration, exhibiting a calculated IC₅₀ of 25 nM and essentially complete inhibition at 3.2 μM^[1].
CP-465022 1 μM for 10 min has little effect on peak NMDA-induced currents but reduces current measured at 8 s during NMDA application by 26%.CP-465,022 at 10 μM inhibits peak NMDA-induced currents in cortical neurons by 36% and currents measured at 8 s by 70% d in primary cultures of cortical and cerebellar granule neurons^[1].
CP-465022 1 μM for 10 min inhibits peak NMDA currents in cultured rat cerebellar granule neurons with mean inhibition of 19% and NMDA currents measured at 8 s by 45%, similar to what is observed in the cortical neurons^[1].
CP-465022 (100 nM -10 μM) has inhibitory effects on Kainate-induced whole-cell currents in voltage-clamped rat hippocampal, 100 nM CP465,022 inhibits kainate currents developed over the course of 200s, 500 nM and 1 μM CP-465,022 nearly complete inhibits this time frame (99.3%)^[1].