CP-465022 (maleate)
Catalogue Number: C4398-APE
| Manufacturer: | Apexbio |
| Molecular Formula: | C26H24ClFN4O C4H4O4 |
| Type: | Other Inhibitors |
| Shipping Condition: | Blue Ice |
| Storage Condition: | RT |
| Unit(s): | 10 mg, 5 mg |
Description
Description: 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.
Additional Text
Solubility
Soluble in DMSO
Smile String
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=CC(O)=O)=O
Storage Note
Store at RT
C4398 Datasheet
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