1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. iGluR
  3. PEAQX

PEAQX (Synonyms: NVP-AAM077)

Cat. No.: HY-12294
Handling Instructions

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).

For research use only. We do not sell to patients.

PEAQX Chemical Structure

PEAQX Chemical Structure

CAS No. : 459836-30-7

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Top Publications Citing Use of Products

    PEAQX purchased from MCE. Usage Cited in: Neuroscience. 2018 Nov 1;391:1-12.

    PP2 and NVP-AAM077 pretreatment decreases the expression level of Cleaved Caspase-3 significantly.
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    Description

    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). 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 in excess 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 an ED50 value of 23 mg/kg in the MES test [1]. Sprague-Dawley rats were treated on PN7, PN9, and PN11 with PCP (10 mg/kg), PEAQX (NR2A-preferring antagonist; 10, 20, or 40 mg/kg), or ifenprodil (selective NR2B antagonist; 1, 5, or 10 mg/kg) and sacrificed for measurement of caspase-3 activity (an index of apoptosis) or allowed to age and tested for locomotor sensitization to PCP challenge on PN28-PN35. PCP or PEAQX on PN7, PN9, and PN11 markedly elevated caspase-3 activity in the cortex; ifenprodil showed no effect. Striatal apoptosis was evident only after subchronic treatment with a high dose of PEAQX (20 mg/kg). Animals treated with PCP or PEAQX on PN7, PN9, and PN11 showed a sensitized locomotor response to PCP challenge on PN28-PN35 [2].

    Molecular Weight

    454.21

    Formula

    C₁₇H₁₇BrN₃O₅P

    CAS No.

    459836-30-7

    SMILES

    O=C1C(NC2=C(C(C(P(O)(O)=O)N[[email protected]](C3=CC=C(Br)C=C3)C)=CC=C2)N1)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Solvent & Solubility
    In Vivo:
    • 1.

      PEAQX is dissolved in DMSO and diluted with sterile saline[3].

    References
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    Keywords:

    PEAQXNVP-AAM077iGluRIonotropic glutamate receptorsInhibitorinhibitorinhibit

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