NMDA Receptors

N-methyl-D-aspartate (NMDA) receptor antagonists and modulators act on glutamate-gated ion channels in neurons. NMDA receptors take part in excitatory synaptic transmission, synaptic plasticity and excitotoxicity. The first NMDA receptor subunit was cloned from rat brain in 1991. Extracellular magnesium blocks the channel in a voltage-dependent manner, so activation requires both agonist binding and membrane depolarization. The category includes the agonist NMDA itself, the channel blocker memantine hydrochloride and the competitive antagonist SDZ 220-581. Subunit-selective tools include TCN 201, a negative allosteric modulator of GluN2A-containing receptors, and GNE 0723, a positive allosteric modulator of the same receptors.

6 Items

  • Ro 25-6981
    Cat. No.
    A13144

    Ro 25-6981

    Ro 25-6981 is a high-affinity, potent and selective blocker of N-methyl- D-aspartate (NMDA) receptors.

    1 mg
    $40.00
    2 mg
    $60.00
    All 8 sizes
  • RO 25-6981 maleate
    Cat. No.
    A16083

    RO 25-6981 maleate

    Synonyms: Ro25-6981

    Ro 25-6981 Maleate is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit. IC50 values are 0.009 and 52 uM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively.

    1 mg
    $40.00
    5 mg
    $65.00
    All 7 sizes
  • Lanicemine
    Cat. No.
    A19339

    Lanicemine

    Synonyms: AZD6765

    Lanicemine (AZD6765) is a low-trapping NMDA channel blocker with a binding (Ki) of 0.56-2.1 μM.

    5 mg
    $90.00
    10 mg
    $165.00
    All 5 sizes
  • Ensaculin
    Cat. No.
    A67269

    Ensaculin

    Synonyms: KA-672 hydrochloride; Anseculin hydrochloride

    Ensaculin is an NMDA receptor channel blocker that exhibits neuroprotective properties in models of NMDA toxicity. This compound promotes neuronal growth in primary cultures of rat brain cells, suggesting its potential for application in neurodegenerative research. Furthermore, Ensaculin holds promise as a candidate for anti-dementia therapies by modulating various neurotransmitter systems.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • NMDAR blocker 1
    Cat. No.
    A67366

    NMDAR blocker 1

    NMDAR blocker 1 is an NMDA receptor channel blocker with an IC50 of 5.0 μM, characterized by rapid on-off kinetics and strong voltage dependence, without competing with glutamate or glycine. This reagent effectively prevents glutamate/NMDA-induced intracellular Ca2+ overload and modulates the glutamate-nitric oxide-cGMP signaling pathway. NMDAR blocker 1 has been demonstrated to impede excitotoxic neurodegeneration in cultured cerebellar and hippocampal neurons, as well as mitigate excitotoxic effects in a mouse model of hyperammonemia-induced toxicity. It serves as a valuable tool for research into neurodegenerative diseases.

    Out of stock

    All 3 sizes
  • Caged MK801
    Cat. No.
    A67406

    Caged MK801

    Caged MK801 is a selective, non-competitive, irreversible blocker of the NMDA receptor, targeting the open-channel state. It is designed to release MK801 upon photolysis, providing a tool for precise temporal control in neuronal studies. This compound is compatible with neuropharmacological applications, enabling exploration of synaptic plasticity and neurodegeneration mechanisms.

    25 mg
    $1,780.00
    50 mg
    $2,280.00
    All 3 sizes

6 Items

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