199656-46-7

199656-46-7 structure
199656-46-7 structure
  • Name: CP-465022 Maleate
  • Chemical Name: 3-(2-Chlorophenyl)-2-[(E)-2-{6-[(diethylamino)methyl]-2-pyridinyl}vinyl]-6-fluoro-4(3H)-quinazolinone (2Z)-2-butenedioate (1:1)
  • CAS Number: 199656-46-7
  • Molecular Formula: C30H28ClFN4O5
  • Molecular Weight: 579.02
  • Catalog: Signaling Pathways Membrane Transporter/Ion Channel iGluR
  • Create Date: 2018-06-07 09:50:15
  • Modify Date: 2025-08-26 09:18:33
  • 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].

Name 3-(2-Chlorophenyl)-2-[(E)-2-{6-[(diethylamino)methyl]-2-pyridinyl}vinyl]-6-fluoro-4(3H)-quinazolinone (2Z)-2-butenedioate (1:1)
Synonyms 4(3H)-Quinazolinone, 3-(2-chlorophenyl)-2-[(E)-2-[6-[(diethylamino)methyl]-2-pyridinyl]ethenyl]-6-fluoro-, (2Z)-2-butenedioate (1:1)
3-(2-Chlorophenyl)-2-[(E)-2-{6-[(diethylamino)methyl]-2-pyridinyl}vinyl]-6-fluoro-4(3H)-quinazolinone (2Z)-2-butenedioate (1:1)
Description 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].
Related Catalog
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].
References

[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.

Molecular Formula C30H28ClFN4O5
Molecular Weight 579.02
Exact Mass 578.173218
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