| CAS NO: | 199656-46-7 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| Storage | Store at RT |
| M.Wt | 579 |
| Cas No. | 199656-46-7 |
| Formula | C26H24ClFN4O·C4H4O4 |
| Solubility | Soluble in DMSO |
| Chemical Name | 3-(2-chlorophenyl)-2-[2-[6-[(diethylamino)methyl]-2-pyridinyl]ethenyl]-6-fluoro-4(3H)-quinazolinone-(2Z)-2-butenedioate |
| Canonical SMILES | FC1=CC=C2C(C(N(C3=C(Cl)C=CC=C3)C(/C=C/C4=CC=CC(CN(CC)CC)=N4)=N2)=O)=C1.OC(/C=C\C(O)=O)=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
IC50: 25 nM for AMPA receptor-mediated currents in rat cortical neurons
CP-465022 is an AMPA antagonist.
The inhibition of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor has been hypothesized to lead to neuroprotective efficacy after cerebral ischemia on the basis of the activity in ischemia models of a variety of compounds with varying selectivity for AMPA over other glutamate receptor subtypes.
In vitro: CP-465022 inhibited AMPA receptor-mediated currents in rat cortical neurons and such inhibition was found to be noncompetitive with agonist concentration. CP-465022 was selective for AMPA over kainate and N-methyl-D-aspartate receptors. However, CP-465022 was found to be equipotent for AMPA receptors composed of different AMPA receptor subunit combinations, which indicated that CP-465022 is equivalently potent for inhibition of AMPA receptor-mediated responses in different types of neurons expressing different AMPA receptor subunits [1].
In vivo: Animal study showed that CP-465022 could potently and efficaciously inhibit AMPA receptor-mediated hippocampal synaptic transmission and the induction of seizures. However, at comparable doses, CP-465022 failed to prevent CA1 neuron loss after brief global ischemia or to reduce infarct volume after temporary middle cerebral artery occlusion [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Lazzaro JT, Paternain AV, Lerma J, Chenard BL, Ewing FE, Huang J, Welch WM, Ganong AH, Menniti FS. Functional characterization of CP-465,022, a selective, noncompetitive AMPA receptor antagonist. Neuropharmacology. 2002 Feb;42(2):143-53.
[2] Menniti FS, Buchan AM, Chenard BL, Critchett DJ, Ganong AH, Guanowsky V, Seymour PA, Welch WM. CP-465,022, a selective noncompetitive AMPA receptor antagonist, blocks AMPA receptors but is not neuroprotective in vivo. Stroke. 2003 Jan;34(1):171-6.
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