199656-46-7
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: 2024-03-03 10:38:06
-
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 |
| Molecular Formula | C30H28ClFN4O5 |
|---|---|
| Molecular Weight | 579.02 |
| Exact Mass | 578.173218 |