Details
| Stereochemistry | EPIMERIC |
| Molecular Formula | C17H17BrN3O5P |
| Molecular Weight | 454.212 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@H](NC(C1=C2NC(=O)C(=O)NC2=CC=C1)P(O)(O)=O)C3=CC=C(Br)C=C3
InChI
InChIKey=XXZGNAZRWCBSBK-WFVOFKTRSA-N
InChI=1S/C17H17BrN3O5P/c1-9(10-5-7-11(18)8-6-10)19-17(27(24,25)26)12-3-2-4-13-14(12)21-16(23)15(22)20-13/h2-9,17,19H,1H3,(H,20,22)(H,21,23)(H2,24,25,26)/t9-,17?/m0/s1
PEAQX (NVP-AAM 077) is a potent and orally active NMDA antagonist with a 15-fold preference for human NMDA receptors with the 1A/2A(IC50=270 nM), rather than 1A/2B (29,600 nM). Animals treated with PCP or PEAQX on PN7, PN9, and PN11 showed a sensitized locomotor response to PCP challenge on PN28-PN35. PEAQX induced social suppression in rats.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| 5-Phosphonomethylquinoxalinediones as competitive NMDA receptor antagonists with a preference for the human 1A/2A, rather than 1A/2B receptor composition. | 2002 Apr 8 |
|
| Differential role of N-methyl-D-aspartate receptor subunits 2A and 2B in mediating phencyclidine-induced perinatal neuronal apoptosis and behavioral deficits. | 2009 Nov 10 |
|
| Ifenprodil, a NR2B-selective antagonist of NMDA receptor, inhibits reverse Na+/Ca2+ exchanger in neurons. | 2012 Nov |
|
| Low doses of the NMDA receptor antagonists, MK-801, PEAQX, and ifenprodil, induces social facilitation in adolescent male rats. | 2013 Aug 1 |
|
| The effects of an acute challenge with the NMDA receptor antagonists, MK-801, PEAQX, and ifenprodil, on social inhibition in adolescent and adult male rats. | 2014 Apr |
|
| Age-dependent effects on social interaction of NMDA GluN2A receptor subtype-selective antagonism. | 2016 Jul |
Sample Use Guides
In “older” hippocampal rat neurons (13-16 DIV), ifenprodil (50uM) and PEAQX
(5uM) applied separately only partly (45-55%) inhibited NMDA-induced increases in
[Ca2+]c with IC50=0.29±0.14uM and 0.13±0.04uM, respectively. If applied simultaneously, even at lower concentrations, ifenprodil (1uM) and PEAQX
(0.1uM) practically completely inhibited NMDA-induced increases in [Ca2+]c.
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9868551
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LE8K7M4APN
Created by
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459836-30-7
Created by
admin on Sat Dec 16 17:28:54 GMT 2023 , Edited by admin on Sat Dec 16 17:28:54 GMT 2023
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PEAQX
Created by
admin on Sat Dec 16 17:28:54 GMT 2023 , Edited by admin on Sat Dec 16 17:28:54 GMT 2023
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SUBSTANCE RECORD
