CP-465022 hydrochloride 

CP-465022 hydrochloride 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: 25 nM (rat cortical neurons)^[1]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

499.41

C₂₆H₂₅Cl₂FN₄O

1785666-59-2

O=C1N(C2=CC=CC=C2Cl)C(/C=C/C3=NC(CN(CC)CC)=CC=C3)=NC4=C1C=C(F)C=C4.[H]Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. J T Lazzaro, et al. Functional characterization of CP-465,022, a selective, noncompetitive AMPA receptor antagonist. Neuropharmacology. 2002 Feb;42(2):143-53.  [Content Brief]