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CP-465022 hydrochloride

CAS No. : 1785666-59-2

MCE 站：CP-465022 hydrochloride

产品活性：CP-465022 hydrochloride 是一种强效的、选择性的、非竞争性的 AMPA受体 拮抗剂，具有抗惊厥活性。CP-465022 对 Kainate 诱导反应具有抑制作用，IC₅₀ 为 25 nM。CP-465022 是研究 AMPA 受体在生理和病理方面研究的有效工具。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：iGluR

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 ?M.
CP-465022 1 ?M 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 ?M 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.
CP-465022 1 ?M 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.
CP-465022 (100 nM -10 ?M) 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 ?M CP-465,022 nearly complete inhibits this time frame (99.3%).

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