1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. iGluR
  3. Dizocilpine free base

Dizocilpine free base (Synonyms: MK-801 free base)

Cat. No.: HY-15084B
Handling Instructions

Dizocilpine, 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.

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Dizocilpine free base Chemical Structure

Dizocilpine free base Chemical Structure

CAS No. : 77086-21-6

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Top Publications Citing Use of Products

    Dizocilpine free base purchased from MCE. Usage Cited in: Neuroreport. 2017 May 24;28(8):444-450.

    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, 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

    Ki: 37.2 nM (NMDA receptor, in rat brain membrane)[1]

    In Vitro

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

    In Vivo

    Dizocilpine (MK 801) (1 mg/kg) treatment before each METH injection reduces the extent of DA depletion by 55% in striatal of mice. Dizocilpine (MK 801) (1 mg/kg) also attenuates the effects of METH on microglial activation in striatal of mice[4].
    Dizocilpine ((+)-MK 801) (0.05, 0.2 mg/kg, i.p.) attenuates subsequent cocaine-primed reinstatement without disruption in rats. Dizocilpine (MK 801) (0.2 mg/kg, i.p.) prior to two reactivation sessions in the home cage shows no suppression on subsequent cocaine-primed reinstatement[5].
    Dizocilpine (0.03, 0.1, 0.3 and 1 mg/kg, i.p.) significantly increases the ambulation of mice at 0.3 and 1 mg/kg, but not at 0.03 and 0.1 mg/kg[6].

    Molecular Weight

    221.30

    Formula

    C₁₆H₁₅N

    CAS No.

    77086-21-6

    SMILES

    C[[email protected]]1(N2)C3=CC=CC=C3C[[email protected]]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.

    References
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    Keywords:

    DizocilpineMK-801MK801MK 801iGluRIonotropic glutamate receptorsnoncompetitiveambulationhyperlocomotionanticonvulsantneurotransmitteranestheticvoltageInhibitorinhibitorinhibit

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