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.

Items 1-25 of 69

  • Creatinine
    Cat. No.
    A11842

    Creatinine

    Synonyms: NSC13123

    Creatinine acts as a GABAA and NMDA receptor modulator, demonstrating antioxidant properties and metabolic regulation. It is produced through the non-enzymatic conversion of creatine and phosphocreatine in muscle, making its serum levels an important biomarker for renal function, muscle mass, and clinical outcomes. Creatinine is utilized in evaluating perioperative renal risk and has applications in research on neurodegenerative diseases, psychiatric disorders, acute and chronic kidney injury, and renal failure. Additionally, it can induce specific Cryptococcus species to produce creatinine deiminase, highlighting its role in metabolic studies.

    500 mg
    $35.00
    1 g
    $40.00
    All 3 sizes
  • GNE 0723
    Cat. No.
    A12757

    GNE 0723

    GNE 0723 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 21 nM for GluN2A, 7.4 and 6.2 μM for GluN2C and GluN2D, respectively.

    1 mg
    $315.00
    5 mg
    $955.00
    All 6 sizes
  • Ibotenic Acid
    Cat. No.
    A14006

    Ibotenic Acid

    Synonyms: NSC 204850

    Ibotenic acid is a neuroexcitatory amino acid originally isolated from Amanita species that functions as a NMDA and metabotropic glutamate receptor agonist.

    1 mg
    $35.00
    5 mg
    $85.00
    All 6 sizes
  • (S)-Glutamic acid
    Cat. No.
    A15458

    (S)-Glutamic acid

    Synonyms: (+)-L-Glutamic acid

    (S)-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA).

    1 g
    $25.00
    5 g
    $35.00
    All 2 sizes
  • CIQ
    Cat. No.
    A15523

    CIQ

    CIQ is a subunit-selective potentiator of NMDA receptors containing the NR2C or NR2D subunit.

    2 mg
    $20.00
    5 mg
    $40.00
    All 7 sizes
  • L-Glutamic acid monosodium salt
    Cat. No.
    A16591

    L-Glutamic acid monosodium salt

    Synonyms: Monosodium glutamate

    L-Glutamic acid monosodium salt acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). (S)-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.

    50 mg
    $25.00
    100 mg
    $40.00
    All 3 sizes
  • Piracetam
    Cat. No.
    A16672

    Piracetam

    Synonyms: UCB-6215

    Piracetam is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA) that functions as an iGluR modulator. It exhibits significant neuroprotective and cognitive-enhancing properties, making it valuable in the study of various cognitive disorders. Piracetam is widely used in research to investigate mechanisms underlying memory enhancement, learning processes, and neuroplasticity.

    500 mg
    $20.00
    1 g
    $25.00
    All 4 sizes
  • (R)-Serine
    Cat. No.
    A17978

    (R)-Serine

    (R)-Serine, an endogenous amino acid involved in glia-synapse interactions that has unique neurotransmitter characteristics, is a potent co-agonist at the NMDA glutamate receptor.

    500 mg
    $40.00
    1 g
    $50.00
    All 3 sizes
  • BMS-986163
    Cat. No.
    A19770

    BMS-986163

    BMS-986163 is a negative allosteric modulator of GluN2B. The prodrug BMS-986163 rapidly converts to its active parent molecule BMS-986169 (Ki=4 nM, IC50=24 nM).

    1 mg
    $315.00
    5 mg
    $955.00
    All 6 sizes
  • GNE 5729
    Cat. No.
    A20295

    GNE 5729

    GNE 5729 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 37 nM for GluN2A, 4.7 and 9.5 μM for GluN2C and GluN2D, respectively.

    1 mg
    $315.00
    5 mg
    $775.00
    All 6 sizes
  • SYM 2081
    Cat. No.
    A20332

    SYM 2081

    SYM 2081 is a high-affinity ligand and potent, selective agonist of kainate receptors, inhibits [3H]-kainate binding with an IC50 of 35 nM, almost 3000- and 200-fold selectivity for kainate receptors over AMPA and NMDA receptors respectively.

    1 mg
    $80.00
    5 mg
    $180.00
    All 7 sizes
  • Quinolinic acid
    Cat. No.
    A20575

    Quinolinic acid

    Quinolinic acid is an endogenous N-methyl-D-aspartate (NMDA) receptor agonist synthesized from L-tryptophan via the kynurenine pathway and thereby has the potential of mediating N-methyl-D-aspartate neuronal damage and dysfunction.

    500 mg
    $20.00
    1 g
    $30.00
    All 4 sizes
  • (-)-Aspartic acid
    Cat. No.
    A20810

    (-)-Aspartic acid

    Synonyms: (R)-Aspartic acid; D-(-)-Aspartic acid

    (-)-Aspartic acid is an endogenous NMDA receptor agonist.

    500 mg
    $35.00
    5 g
    $55.00
    All 4 sizes
  • DQP-1105
    Cat. No.
    A22610

    DQP-1105

    DQP-1105 is a negative allosteric modulator of the GluN2C/D NMDA receptor inhibiting receptor function more potently when glutamate is present .

    2 mg
    $20.00
    5 mg
    $40.00
    All 6 sizes
  • SBI-810
    Cat. No.
    A36677

    SBI-810

    SBI-810 is a selective modulator of the neurotensin receptor 1 (NTSR1), characterized by its ability to penetrate the blood-brain barrier. This compound promotes β-arrestin-2 recruitment to NTSR1 while antagonizing Gq-mediated signaling pathways. SBI-810 effectively inhibits NMDA receptor activity and ERK signaling in spinal nociceptive neurons, leading to a reduction in excitatory synaptic transmission, surface expression of Nav1.7, and action potential firing in primary sensory neurons. Its profound effects on C-fiber responses demonstrate its potential in alleviating acute and chronic pain, making it a valuable tool for research into various pain disorders.

    5 mg
    $145.00
    10 mg
    $235.00
    All 4 sizes
  • cis-ACPD
    Cat. No.
    A61891

    cis-ACPD

    Cis-ACPD is a potent agonist of the NMDA receptor, exhibiting an IC50 of 3.3 µM. Additionally, it selectively activates group II metabotropic glutamate receptors, with EC50 values of 13 µM for mGluR2 and 50 µM for mGluR4. The compound is widely used in neuropharmacological research to study excitatory neurotransmission and the role of glutamate receptors in various neurological disorders.

    Out of stock

    All 3 sizes
  • UCM-A86
    Cat. No.
    A67060

    UCM-A86

    UCM-A86 is a selective positive allosteric modulator of the GluN1/GluN3 NMDA receptors, exhibiting EC50 values of 21 µM and 19 µM for GluN1/GluN3A and GluN1/GluN3B receptors, respectively. This compound preferentially enhances signaling through GluN1/GluN3A/B receptors while displaying minimal activity at GluN1/GluN2A-D receptors. UCM-A86 serves as a valuable tool for research focused on central nervous system disorders and the modulation of NMDA receptor activity.

    Out of stock

    All 3 sizes
  • Simufilam hydrochloride
    Cat. No.
    A67082

    Simufilam hydrochloride

    Synonyms: PTI-125 hydrochloride

    Simufilam hydrochloride is an orally active modulator of filamin A (FLNA) that targets neuronal signaling pathways. This compound restores NMDAR signaling and Arc expression while inhibiting dysregulated mTOR activity. Additionally, it enhances insulin sensitivity and mitigates Aβ42-induced neuroinflammation and tau protein hyperphosphorylation. Simufilam hydrochloride is applicable in research related to Alzheimer's disease, particularly in understanding the underlying mechanisms of neurodegeneration.

    1 mg
    $80.00
    2 mg
    $110.00
    All 7 sizes
  • L-Homocysteic acid
    Cat. No.
    A67089

    L-Homocysteic acid

    Synonyms: L-HCA

    L-Homocysteic acid is an endogenous excitatory amino acid functioning as a NMDA receptor agonist, with an effective concentration (EC50) of 14 μM. Its neurotoxic properties make it a valuable tool in the investigation of neurological disorders. L-Homocysteic acid enables researchers to explore the roles of excitatory neurotransmission and contribute to the understanding of related pathophysiological conditions.

    5 mg
    $35.00
    10 mg
    $60.00
    All 2 sizes
  • Plazinemdor
    Cat. No.
    A67094

    Plazinemdor

    Synonyms: CAD-9303

    Plazinemdor is a positive allosteric modulator of the N-methyl-D-aspartate (NMDA) receptor. This compound enhances NMDA receptor activity, making it a valuable tool for investigating its role in psychiatric, neurological, and neurodevelopmental disorders. Plazinemdor is suitable for research applications focused on understanding the underlying mechanisms of various nervous system diseases.

    5 mg
    $285.00
    10 mg
    $505.00
    All 5 sizes
  • Rapastinel Trifluoroacetate
    Cat. No.
    A67098

    Rapastinel Trifluoroacetate

    Synonyms: GLYX-13 Trifluoroacetate

    Rapastinel Trifluoroacetate is a modulator of the NMDA receptor, functioning as a partial agonist at the glycine site. This compound has shown potential for the treatment of major depressive disorder, contributing to neuroplasticity and synaptic function. It is utilized in research exploring depression and related neurological conditions, providing insights into the therapeutic effects of NMDA receptor modulation.

    1 mg
    $25.00
    5 mg
    $65.00
    All 6 sizes
  • GNE-9278
    Cat. No.
    A67103

    GNE-9278

    GNE-9278 is a selective positive allosteric modulator of the N-methyl-D-aspartate receptor (NMDAR), targeting the GluN1 transmembrane domain. It enhances peak current and agonist affinity in activated NMDARs, offering potential insights into synaptic transmission and plasticity. This compound is valuable for research investigating NMDAR-related neurological disorders and synaptic function.

    5 mg
    $100.00
    10 mg
    $170.00
    All 5 sizes
  • Simufilam
    Cat. No.
    A67113

    Simufilam

    Synonyms: PTI-125

    Simufilam is an orally active modulator of filamin A (FLNA) that restores NMDA receptor (NMDAR) signaling and Arc expression. It effectively inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, which results in improved insulin sensitivity and a reduction in Aβ42-induced neuroinflammation and tau protein hyperphosphorylation. This compound is particularly valuable for research applications focused on Alzheimer's disease and related neurodegenerative disorders.

    5 mg
    $165.00
    10 mg
    $250.00
    All 4 sizes
  • DQP-997-74
    Cat. No.
    A67120

    DQP-997-74

    DQP-997-74 is a selective negative allosteric modulator of the N-methyl-D-aspartate receptor (NMDAR), specifically targeting the GluN2C and GluN2D subunits with IC50 values of 0.069 μM and 0.035 μM, respectively. This compound exhibits blood-brain barrier penetrability and demonstrates synergistic effects with glutamate, resulting in enhanced inhibition of hypersynchronous neural activity under high-frequency excitatory synaptic transmission. DQP-997-74 has shown potential to reduce epileptogenesis in murine models of tuberous sclerosis complex (TSC)-induced epilepsy, making it a valuable tool for research on NMDAR-related neurological disorders.

    5 mg
    $515.00
    10 mg
    $845.00
    All 5 sizes

Items 1-25 of 69

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