1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
    Neuronal Signaling
  3. iGluR

iGluR

Ionotropic glutamate receptors

iGluR (ionotropic glutamate receptor) is a ligand-gated ion channel that is activated by the neurotransmitter glutamate. iGluR are integral membrane proteins compose of four large subunits that form a central ion channel pore. Sequence similarity among all known glutamate receptor subunits, including the AMPA, kainate, NMDA, and δ receptors.

AMPA receptors are the main charge carriers during basal transmission, permitting influx of sodium ions to depolarise the postsynaptic membrane. NMDA receptors are blocked by magnesium ions and therefore only permit ion flux following prior depolarisation. This enables them to act as coincidence detectors for synaptic plasticity. Calcium influx through NMDA receptors leads to persistent modifications in the strength of synaptic transmission.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-W018061
    Traxoprodil
    Antagonist 99.88%
    Traxoprodil (CP101,606) is a potent and selective NMDA antagonist and protect hippocampal neurons with an IC50 of 10 nM.
    Traxoprodil
  • HY-12506
    Naspm
    Inhibitor
    Naspm (1-Naphthyl acetyl spermine), a synthetic analogue of Joro spider toxin, is a calcium permeable AMPA (CP-AMPA) receptors antagonist.
    Naspm
  • HY-15085
    MDL 105519
    Inhibitor 99.00%
    MDL 105519 is a potent and selective antagonist of glycine binding to the NMDA receptor.
    MDL 105519
  • HY-P0117
    Tat-NR2B9c
    Inhibitor 99.97%
    Tat-NR2B9c (Tat-NR2Bct; NA-1) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy.
    Tat-NR2B9c
  • HY-P0117A
    Tat-NR2B9c TFA
    Inhibitor 99.67%
    Tat-NR2B9c TFA (Tat-NR2Bct TFA) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c TFA disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c TFA also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy.
    Tat-NR2B9c TFA
  • HY-100808
    D-Serine
    Agonist ≥98.0%
    D-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. D-Serinee has a cardinal modulatory role in major NMDAR-dependent processes including NMDAR-mediated neurotransmission, neurotoxicity, synaptic plasticity, and cell migration.
    D-Serine
  • HY-B0405A
    Bupivacaine hydrochloride
    Inhibitor 99.89%
    Bupivacaine hydrochloride is a NMDA receptor inhibitor.Bupivacaine can block sodium, L-calcium, and potassium channels.Bupivacaine potently blocks SCN5A channels with the IC50 of 69.5 μM. Bupivacaine hydrochloride can be used for the research of chronic pain.
    Bupivacaine hydrochloride
  • HY-12505
    CX546
    Agonist 99.62%
    CX546 is a first-generation and selective benzamide-type positive AMPAR modulator. CX546 is a prototypical ampakine agent and has antipsychotic effects.
    CX546
  • HY-N0368
    Linalool
    Inhibitor 98.55%
    Linalool is a natural monoterpene which is a competitive NMDA receptor antagonist. Linalool is orally active and crosses the blood-brain barrier. Linalool has anticancer, antibacterial, anti-inflammatory, neuroprotective, anxiolytic, antidepressant, anti-stress, cardioprotective, hepatoprotective, nephroprotective and pulmonary protective activities.
    Linalool
  • HY-15084A
    (-)-Dizocilpine maleate
    99.92%
    (-)-Dizocilpine maleate ((-)-MK-801 maleate) is a less active (-)-enantiomer of Dizocilpine. (-)-Dizocilpine maleate is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with a Ki of 211.7 nM. (-)-Dizocilpine maleate has antidepressant effects.
    (-)-Dizocilpine maleate
  • HY-B0369A
    Orphenadrine citrate
    Antagonist 99.95%
    Orphenadrine citrate is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine citrate relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine citrate is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases.
    Orphenadrine citrate
  • HY-100815D
    (RS)-AMPA monohydrate
    Agonist 98.40%
    (RS)-AMPA ((±)-AMPA) monohydrate is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA monohydrate does not interfere with binding sites for kainic acid or NMDA receptors.
    (RS)-AMPA monohydrate
  • HY-100806S
    Kynurenic acid-d5
    Antagonist 98.35%
    Kynurenic acid-d5 is the deuterium labeled Kynurenic acid. Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8[1][2].
    Kynurenic acid-d<sub>5</sub>
  • HY-101165
    Cyclothiazide
    Agonist 98.78%
    Cyclothiazide, a positive allosteric modulator of AMPA receptors, is used frequently to block the desensitization of both native and heterologously expressed AMPA receptors. Cyclothiazide is known to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current.
    Cyclothiazide
  • HY-139897
    CX 717
    Agonist 99.79%
    CX 717 is a positive allosteric modulator of AMPA receptor. Antidepressant-like effect. CX 717 can be used for the research of adult attention deficit hyperactivity disorder (ADHD).
    CX 717
  • HY-103234A
    GYKI 52466 dihydrochloride
    Antagonist 99.38%
    GYKI 52466 dihydrochloride is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 dihydrochloride has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 dihydrochloride can be used in Parkinson's disease research.
    GYKI 52466 dihydrochloride
  • HY-107512
    Kynurenic acid sodium
    Antagonist 99.79%
    Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8.
    Kynurenic acid sodium
  • HY-114427
    NS-102
    Antagonist 98.23%
    NS-102 is a selective kainate (GluK2) receptor antagonist. NS-102 is a potent GluR6/7 receptor antagonist.
    NS-102
  • HY-16728B
    Rapastinel Trifluoroacetate
    Modulator ≥98.0%
    Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with glycine-site partial agonist properties. Rapastinel Trifluoroacetate has the potential for major depressive disorder treatment.
    Rapastinel Trifluoroacetate
  • HY-B1270
    Isoxsuprine hydrochloride
    Antagonist 99.87%
    Isoxsuprine hydrochloride is a beta-adrenergic receptor agonist with Kis of 13.65 μΜ and 3.48 μΜ for myometrial and placcntal beta-adrenergic receptor, respectively. Isoxsuprine hydrochloride is also a NMDA receptor antagonist.
    Isoxsuprine hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity