2. Induced Disease Models Products Membrane Transporter/Ion Channel Neuronal Signaling
  3. Nervous System Disease Models iGluR
  4. Schizophrenia Models
  5. Dizocilpine

Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca2+ flux.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Dizocilpine maleate) that retains the same biological activity.

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

Dizocilpine Chemical Structure

Dizocilpine Chemical Structure

CAS No. : 77086-21-6

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Dizocilpine Related Antibodies

Top Publications Citing Use of Products

    Dizocilpine purchased from MedChemExpress. Usage Cited in: Cell Biosci. 2023 Mar 16;13(1):57.  [Abstract]

    Dizocilpine (MK-801; 1 mg/kg; i.v.; single) suppresses RIPC-induced SIRT3 upregulation in mice.

    Dizocilpine purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2020 Aug;24(16):9287-9299.  [Abstract]

    Neurons are pre-treated with 10 μM Dizocilpine (MK801), followed by TNF-α treatment (40 ng/mL, 2 h). MK801 could attenuate TNF-α- induced intracellular calcium accumulation, phosphorylation of CAMK II and calpain-2, calpain activation and cathepsin B release as well as TrkB truncation.

    Dizocilpine purchased from MedChemExpress. Usage Cited in: Neuroreport. 2017 May 24;28(8):444-450.  [Abstract]

    Western blot analysis confirms that MK-801 inhibits the decrease in GDF10 in SNL rats. The relative expression level of GDF10 in the SNL-vehicle group is significantly decreased, but remains unchanged in the SNL-MK-801 group versus sham.

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    Description

    Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca2+ flux[1][2].

    IC50 & Target

    NMDA Receptor

     

    In Vitro

    Dizocilpine (MK-801) progressively suppresses of current induced by NMDA. Mg2+ (10 mM) prevents Dizocilpine from blocking the N-Me-D-Asp-induced current, even when Dizocilpine is applied for a long time in the presence of NMDA. Dizocilpine blocks NMDA-activated single-channel activity in outside-out patches[3].
    Dizocilpine (MK-801; <500 μM) inhibits activation of microglia induced by LPS with increased Cox-2 protein expression in BV-2 cells. Dizocilpine (<500 μM) reduces microglial TNF-α output with an EC50 of 400 μM in BV-2 cells[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Dizocilpine Related Antibodies
    In Vivo

    Dizocilpine maleate (0.2 mg/kg, i.p.) exhibits a half-time of 52.31 min, an AUC of 3185.48 nM·min and a clearance of 34 nM in Sprague-Dawley rats[2].
    Induction of Schizophrenia
    Background
    The specific mechanism of schizophrenia induction is unclear. One hypothesis is that, Dizocilpine maleateleads to dysregulation of glutamatergic system through NMDA inhibition[2].
    Specific Mmodeling Methods
    Rats: Sprague-Dawley • male • adult with weight of 250-300 g
    Administration: 0.4 mg/kg • i.p. • single dose.
    Note
    Dizocilpine maleate is dissolved in 0.9% sterile saline.


    Modeling Indicators
    Behavior: Increased spontaneous activity with obvious anxiety-like behavior, increased motor activity in longer diatance (hyperactivity), reduced time staying in central area (avoidance of central area).
    Prepulse Inhibition (PPI): Decreased PPI significantly.
    maze test:Avoided open arm entries in elevated plus maze test and reduced number of novel arm entries in Y maze test.
    Correlated Product(s): Phencyclidine
    Opposite Product(s): Clozapine (HY-14539); Haloperidol (HY-14538)

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    221.30

    Formula

    C16H15N
    CAS No.
    SMILES

    C[C@]1(N2)C3=CC=CC=C3C[C@]2([H])C4=CC=CC=C14
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Purity & Documentation
    References
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    Dizocilpine Related Classifications

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    Help & FAQs
    • 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.

    Keywords:

    Dizocilpine77086-21-6MK-801MK801MK 801iGluRIonotropic glutamate receptorsnoncompetitiveambulationhyperlocomotionanticonvulsantneurotransmittervoltageInhibitorinhibitorinhibit

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