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
| Molecular Formula | C17H17BrN3O5P |
| Molecular Weight | 454.212 |
| Charge | 0 |
| Count |
|
| Stereochemistry | EPIMERIC |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
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
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.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 17:28:54 UTC 2023
by
admin
on
Sat Dec 16 17:28:54 UTC 2023
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| Record UNII |
LE8K7M4APN
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| Record Status |
Validated (UNII)
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9868551
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LE8K7M4APN
Created by
admin on Sat Dec 16 17:28:54 UTC 2023 , Edited by admin on Sat Dec 16 17:28:54 UTC 2023
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459836-30-7
Created by
admin on Sat Dec 16 17:28:54 UTC 2023 , Edited by admin on Sat Dec 16 17:28:54 UTC 2023
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PEAQX
Created by
admin on Sat Dec 16 17:28:54 UTC 2023 , Edited by admin on Sat Dec 16 17:28:54 UTC 2023
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| Related Record | Type | Details | ||
|---|---|---|---|---|
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TARGET -> INHIBITOR |
the Ki of PEAQX revealed it only shows a 5 fold difference in affinity for GluN1/GluN2A vs. GluN1/GluN2B receptors. It is also a potent anticonvulsant in animal tests.
COMPETITIVE ANTAGONIST
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TARGET -> INHIBITOR |
the Ki of PEAQX revealed it only shows a 5 fold difference in affinity for GluN1/GluN2A vs. GluN1/GluN2B receptors. It is also a potent anticonvulsant in animal tests.
COMPETITIVE ANTAGONIST
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TARGET -> INHIBITOR |
COMPETITIVE ANTAGONIST
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