PEAQX_459836-30-7_DataSheet_MedChemExpress

Product Data Sheet

Product Name:

CAS No.:

Cat. No.:

MWt:

Formula:

Purity :PEAQX459836-30-7HY-12294454.21C17H17BrN3O5P>98%

Solubility:DMSO

Mechanisms: Pathways:Membrane Tranporter/Ion Channel; Target:NMDA Receptor

Pathways:Neuronal Signaling; Target:NMDA Receptor

Biological Activity:

PEAQX(NVP-AAM 077) is a potent and orally active NMDA antagonist with a 15-fold preference for humanNMDA receptors with the 1A/2A(IC50=270 nM), rather than 1A/2B(29,600 nM).

IC50 value: 270 nM(hNMDA A1/A2) [1]

Target: NR2A antagonist

in vitro: PEAQX has a high binding affinity for NMDA receptors (IC50=8 nM), and a functional preference inexcess of 100-fold for hNMDA 1A/2A (IC50=of 270 nM) over 1A/2B receptors (IC50=29,600 nM) [1].

in vivo: PEAQX is practically inactive in Xenopus oocytes expressing hNMDA 1A/2B receptors, displays anED50 value of 23 mg/kg in the MES test [1]. Sprague-Dawley rats were treated on PN7, PN9, and PN11 withPCP (10 mg/kg), PEAQX (NR2A-preferring antagonist; 10, 20, or 40 mg/kg), or ifenprodil (selective NR2Bantagonist; 1, 5, or 10 mg/kg) and sacrificed for measurement of caspase-3 activity (an index of apoptosis) orallowed to age and t...

References:

[1]. Auberson YP, et al. 5-Phosphonomethylquinoxalinediones as competitive NMDA receptor antagonistswith a preference for the human 1A/2A, rather than 1A/2B receptor composition. Bioorg Med Chem Lett. 2002Apr 8;12(7):1099-102.

[2]. Anastasio NC, et al. Differential role of N-methyl-D-aspartate receptor subunits 2A and 2B in mediatingphencyclidine-induced perinatal neuronal apoptosis and behavioral deficits. Neuroscience. 2009 Nov10;163(4):1181-91.

Caution: Not fully tested. For research purposes only

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