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

iGluR

Ionotropic glutamate receptors

iGluR

Related Products

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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.

iGluR Isoform Specific Products:

iGluR Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-19435
    GYKI-47261
    		Antagonist
    GYKI-47261 is a competitive, orally active, and selective AMPA receptor antagonist with an IC50 of 2.5 μM. GYKI-47261 has broad spectrum anticonvulsive activity and neuroprotective effects. GYKI-47261 is also a potent inducer of CYP2E1.
    GYKI-47261
  • HY-N0215S6
    DL-Phenylalanine-d5 hydrochloride
    		Antagonist
    DL-Phenylalanine-d5 (hydrochloride) is the deuterium labeled DL-Phenylalanine hydrochloride. L-Phenylalanine hydrochloride is an essential amino acid isolated from Escherichia coli. L-Phenylalanine hydrochloride is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine hydrochloride is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine hydrochloride is widely used in the production of food flavors and pharmaceuticals.
    DL-Phenylalanine-d<sub>5</sub> hydrochloride
  • HY-B0369AS
    Orphenadrine-d3 citrate
    		Antagonist
    Orphenadrine-d3 (citrate) is the deuterium labeled Orphenadrine citrate. Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker.
    Orphenadrine-d<sub>3</sub> citrate
  • HY-168494
    GluN2A Allosteric modulator 1
    		Antagonist
    GluN2A Allosteric modulator 1 (Compound 11) is an orally active, BBB-penetrable and highly selective GluN2A negative allosteric modulator. GluN2A Allosteric modulator 1 has IC50 values of 0.042 μM and 13 μM for GluN2A and GluN2B, respectively. GluN2A Allosteric modulator 1 can be used for the research of nervous system diseases.
    GluN2A Allosteric modulator 1
  • HY-110230
    Flupirtine-d4 hydrochloride
    		Antagonist 99.87%
    Flupirtine-d4 (D 9998-d4) hydrochloride is the deuterium labeled Flupirtine hydrochloride (HY-W709349). Flupirtine hydrochloride is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine hydrochloride is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine hydrochloride stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine hydrochloride exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine hydrochloride functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine hydrochloride can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis.
    Flupirtine-d4 hydrochloride
  • HY-159584
    LBG20304
    		Inhibitor
    LBG20304 (compound 2s) is a ligand for the homologous GluK5 receptor (IC50: 432 nM), more than 40-fold selective over the homologous GluK1-3 isoforms. Low doses of LBG20304 (<10 μM) have no agonist or antagonist functional response at heterologous GluK2/5 receptors, and at high doses (>10 μM), it exhibits low agonist activity in neuronal slices (rat).
    LBG20304
  • HY-183201
    NMDA receptor antagonist 11
    		Antagonist
    NMDA receptor antagonist 11 is a NMDA receptor antagonist with an IC50 of 65 μM. NMDA receptor antagonist 11 inhibits glycine action at the NMDA receptor glycine site. NMDA receptor antagonist 11 can be used for research on neurological diseases.
    NMDA receptor antagonist 11
  • HY-107519
    (R)-3,4-DCPG
    		Antagonist
    (R)-3,4-DCPG is an AMPA and NMDA antagonist with a Kd of 77 μM for AMPA. (R)-3,4-DCPG complete antagonizes the NMDA-induced depolarization at a concentration of 500 μM. (R)-3,4-DCPG exhibits a weak antagonistic effect on kainate-induced depolarizations.
    (R)-3,4-DCPG
  • HY-P1059
    Pep2-AVKI
    		Inhibitor
    Pep2-AVKI is a selective peptide inhibitor of the binding of the AMPA receptor subunit (GluR2) at the C-terminal PDZ site to C-kinase (PICK1). Pep2-AVKI does not affect the binding of (AMPA-type glutamate receptor) GluA2 to GRIP or ABP. Pep2-AVKI does not increase the amplitude of AMPA currents. pep2-AVKI can be used to study neurological diseases.
    Pep2-AVKI
  • HY-149975
    AMPA receptor modulator-4
    		Activator
    AMPA receptor modulator-4, a 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide (BTD), is an orally active positive allosteric modulator of the AMPA receptors (AMPAR PAMs). AMPA receptor modulator-4 can cross the blood-brain barrier. AMPA receptor modulator-4 increases the cognition performance and improves working memory performance in mice.
    AMPA receptor modulator-4
  • HY-B0184R
    Felbamate (Standard)
    		Inhibitor
    Felbamate (Standard) is the analytical standard of Felbamate. This product is intended for research and analytical applications. Felbamate (W-554) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA).
    Felbamate (Standard)
  • HY-15074
    SPD-502
    SPD-502 is a novel glutamate antagonist with potential neuroprotective properties, particularly in brain ischemia. It selectively targets the AMPA receptor, showing high affinity (IC50 = 0.043 μM) and competitive inhibition of AMPA-induced effects in rat cortical membranes and cultured mouse cortical neurons. In vivo, SPD-502 effectively blocks AMPA-evoked spike activity in the hippocampus after intravenous administration, significantly increasing the seizure threshold in mice and demonstrating robust protection against ischemia-induced damage to hippocampal neurons in gerbils. These findings suggest SPD-502 may be promising for studying neurodegenerative conditions associated with glutamate excitotoxicity.
    SPD-502
  • HY-P1195A
    PDZ1 Domain inhibitor peptide TFA
    PDZ1 Domain inhibitor peptide TFA, a cyclic peptide, incorporates a β-Ala lactam side chain linker and targets the PDZ1 domains of the postsynaptic density protein 95 (PSD-95). PDZ1 Domain inhibitor peptide TFA disrupts the GluR6/PSD-95 interaction and is very efficient in competing against the C terminus of GluR6 for the PDZ1 domain.
    PDZ1 Domain inhibitor peptide TFA
  • HY-14608S9
    L-Glutamic acid-15N,d5
    		Agonist
    L-Glutamic acid-15N,d5 is the deuterium and 15N-labeled L-Glutamic acid. L-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). L-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
    L-Glutamic acid-<sup>15</sup>N,d<sub>5</sub>
  • HY-U00199A
    (S)-Norzopiclone
    		Inhibitor
    (S)-Norzopiclone ((S)-N-Desmethyl zopiclone; SEP-174559) is a metabolite of Zopiclone with anxiolytic and anticonvulsant effects. (S)-Norzopiclone has benzodiazepine-like actions at γ2-bearing subtypes of the GABAA receptor and inhibits nACh and NMDA receptors.
    (S)-Norzopiclone
  • HY-101440A
    Indantadol hydrochloride
    Indantadol hydrochloride (CHF-3381) is an orally active, non-selective NMDA antagonist and MAO inhibitor. Indantadol hydrochloride blocks the binding of [³H]-MK-801 to NMDA receptors in a non-competitive manner, with an IC50 of 8.1 μM. Indantadol hydrochloride completely inhibits dopamine release caused by NMDA. Indantadol hydrochloride protects neurons, with an ED₅₀ of 35 μM. Indantadol hydrochloride has anticonvulsant and anti-high pain hypersensitivity activities.
    Indantadol hydrochloride
  • HY-B1126S
    Orphenadrine-d3 hydrochloride
    Orphenadrine-d3 (hydrochloride) is the deuterium labeled Orphenadrine hydrochloride. Orphenadrine hydrochloride is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine hydrochloride relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine hydrochloride 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-d<sub>3</sub> hydrochloride
  • HY-119886
    BMS-986169
    		Inhibitor
    BMS-986169 is an inhibitor of the glutamate N-methyl-D-aspartate 2B receptor (GluN2B). BMS-986169 has a high binding affinity for the allosteric regulatory site of the GluN2B subunit, with a Ki value of 4.03-6.3 nM. BMS-986169 can inhibit the function of GluN2B receptors in Xenopus oocytes, with an IC50 value of 24.1 nM. BMS-986169 can also inhibit the activity of the hERG channel, with an IC50 value of 28.4 μM. BMS-986169 can be used in research on treatment-resistant depression.
    BMS-986169
  • HY-124906
    JAMI1001A
    		Modulator
    JAMI1001A is a positive allosteric modulator of AMPA receptor. JAMI1001A efficaciously modulates AMPA receptor deactivation and desensitization of both flip and flop receptor isoforms.
    JAMI1001A
  • HY-120189
    LY 233536
    		Antagonist
    LY 233536 is a competitive NMDA receptor antagonist.
    LY 233536
Cat. No. Product Name / Synonyms Application Reactivity
iGluR Isoform Comparison

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