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  3. PEAQX

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).

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PEAQX Chemical Structure

PEAQX Chemical Structure

CAS No. : 459836-30-7

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Top Publications Citing Use of Products

    PEAQX purchased from MedChemExpress. Usage Cited in: Neuroscience. 2018 Nov 1;391:1-12.  [Abstract]

    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.
    SMILES

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

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    Room temperature in continental US; may vary elsewhere.

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

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    In Vivo:

    The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

    • Protocol 1

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

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    PEAQX
    Cat. No.:
    HY-12294
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