CP-465022 (maleate) |
Catalog No.GC12742 |
Le maléate CP-465022 est un antagoniste puissant et sélectif non compétitif des récepteurs AMPA avec une activité anticonvulsivante.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 199656-46-7
Sample solution is provided at 25 µL, 10mM.
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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