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-103234
    GYKI 52466
    Antagonist
    GYKI 52466 is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 can be used in Parkinson's disease research.
    GYKI 52466
  • HY-106969A
    ZD 9379 sodium
    Antagonist
    ZD 9379 sodium is a competitive glycine/NMDA receptor antagonist, with an IC50 value of 75 nM (glutamate site). ZD 9379 sodium selectively antagonizes the glycine binding site (GlyB site) on the NMDA receptor, inhibiting the binding of glycine to the NMDA receptor and alleviating excitotoxicity. ZD 9379 sodium reduces the frequency of cortical spreading depression (SDs), alleviates energy depletion in the ischemic penumbra, and delays the expansion of infarction. ZD 9379 sodium reduces the infarct volume and improves neurological function in mouse models. ZD 9379 sodium can be used in studies of acute ischemic stroke, etc.
    ZD 9379 sodium
  • HY-Y0966S9
    Glycine-15N,d2
    Glycine-15N,d2 is the deuterium and 15N-labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
    Glycine-<sup>15</sup>N,d<sub>2</sub>
  • HY-172121
    NMDA agonist 2
    Agonist
    NMDA agonist 2 (compound 8d) is a potent agonist of NMDA receptor, with the EC50 of 0.034 μM for GluN1/2C. NMDA agonist 2 plays an important role in neurological and psychiatric disorders.
    NMDA agonist 2
  • HY-P3319
    β-Neuroprotectin
    β-Neuroprotectin is a (3H)TCP binding inhibitor with activity against NMDA-mediated neuronal cell death. β-Neuroprotectin can effectively inhibit the binding of [3H]TCP. β-Neuroprotectin provides neuroprotection at low concentrations against NMDA-induced neuronal cell death.
    β-Neuroprotectin
  • HY-107696
    Ro 04-5595 hydrochloride
    Antagonist
    Ro 04-5595 hydrochloride is a GluN2B-selective NMDA receptor antagonist (Ki: 31 nM).
    Ro 04-5595 hydrochloride
  • HY-107717
    MNI-caged-NMDA
    MNI-caged-NMDA is a light-sensitive amino acid with rapid release properties suitable for use in the study of fast synaptic receptor mechanisms. MNI-caged-NMDA shows metered release of NMDA receptors, inducing rapid and sustained receptor activation in cerebellar interneurons. MNI-caged-NMDA is able to achieve rapid transient responses and generate large inward currents by local laser photolysis. The use of MNI-caged-NMDA can effectively study neurotransmitter signaling and its inhibitory effects on GABA-A receptors.
    MNI-caged-NMDA
  • HY-170945
    Antidepressant agent 9
    Inhibitor
    Antidepressant agent 9 (Compound 24) is an orally active and BBB-penetrable NMDAR and SERT inhibitor with IC50 values of 3.50 μM and 1044 nM, respectively. Antidepressant agent 9 has good metabolic stability and plasma exposure. Antidepressant agent 9 can exert antidepressant-like activity in the mouse forced swim test.
    Antidepressant agent 9
  • HY-115860
    TAS-4
    TAS-4 is a potent and selective mGluR4 positive allosteric modulator with significant anti-Parkinson's disease activity. TAS-4 is able to show efficacy when used alone or in combination with l-DOPA. TAS-4 is able to reverse haloperidol-induced spasticity when administered alone. TAS-4 enhances the contralateral rotation behavior induced by l-DOPA in a dose-dependent manner. TAS-4 combined with low-dose l-DOPA shows anti-Parkinson's effects similar to full-dose l-DOPA without exacerbating abnormal motor side effects.
    TAS-4
  • HY-15082
    Irampanel
    Antagonist
    Irampanel (BIIR 561) is an AMPA receptor and voltage-dependent sodium channel blocker. Irampanel inhibits kainate-induced currents in rat cortical neurons.
    Irampanel
  • HY-156634
    Risevistinel
    Modulator
    Risevistinel (NYX-783) is a positive allosteric modulator of N-methyl-D-aspartate (NMDA) receptor. Nevadistinel can be used to inhibit cognitive impairment associated with neurodegenerative diseases, such as mild cognitive impairment, mild Alzheimer's disease, Parkinson's disease, Lewy body disease.
    Risevistinel
  • HY-10933S
    CX516-d10
    Modulator
    CX516-d10 is the deuterium labeled CX516. CX516 (BDP 12) is an ampakine and acts as an AMPA receptor positive allosteric modulator for the research of Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI).
    CX516-d<sub>10</sub>
  • HY-124264
    UBP710
    Modulator
    UBP710 is a selective NMDA receptor modulator. UBP710 displays greater activity in potentiating GluN2B-containing receptors than those containing GluN2A.
    UBP710
  • HY-120243
    L-Ibotenic acid
    Agonist
    L-Ibotenic acid is a psychoactive compound found in Amanita muscaria and related mushroom species. L-Ibotenic acid is a conformationally restricted analog of the neurotransmitter glutamate, which may be activated by different conformations of L-glutamate and is a non-selective glutamate receptor agonist.
    L-Ibotenic acid
  • HY-124539
    ZK 187638
    Antagonist
    ZK 187638 is an AMPA receptor antagonist. ZK 187638 antagonizes the kainate-induced currents in cultured hippocampal neurons with an IC50 of 3.4 μM in a noncompetitive fashion.
    ZK 187638
  • HY-121704
    SR 57227A free base
    SR 57227A Free base is a highly selective compound for both peripheral and central 5-HT3 receptors and acts as an inhibitor of NMDA receptor-mediated responses in rat cortical pyramidal cells, demonstrating antidepressant-like effects in rats while reducing isolation-induced aggressive behavior.
    SR 57227A free base
  • HY-172213
    (3S,6R)-NML
    Antagonist
    (3S,6R)-NML is a NMDA receptor antagonist, with pIC50s of 4.8 (GluN1-GluN2A), 4.6 (GluN1-GluN2B), 5.0 (GluN1-GluN2C), 5.0 (GluN1-GluN2D) respectively. (3S,6R)-NML can be used for depression research.
    (3S,6R)-NML
  • HY-P1287
    Conantokin-T
    Antagonist
    Conantokin-T is a γ-carboxyglutamate-containing, N-methyl-D-aspartate (NMDA) antagonist peptidewith an IC50 value of 2 μM. Conantokin-T inhibits NMDA receptor-mediated calcium influx in central nervous system neurons. Conantokin-T can be purified from the venom of the fish-hunting cone snail, Conus tulipa.
    Conantokin-T
  • HY-118814
    YM928
    Antagonist
    YM928 is an orally active and noncompetitive α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonist. YM928 inhibits AMPA receptor-mediated toxicity in primary rat hippocampal cultures with an IC50 value of 2 μM. YM928 blocks AMPA-induced intracellular calcium influx with an IC50 value of 3 μM and antagonizes AMPA-induced inward currents with an IC50 value of 1 μM. YM928 is promising for research of neurological disorders.
    YM928
  • HY-114987
    EMD 21657
    Modulator
    EMD 21657 is a derivative of Piracetam (HY-B0585). EMD 21657 inhibits LOT compound action potential, and enhances the local anesthetic effect of Hexanol (HY-W032022). EMD 21657 exhibits hemolytic effect, and can be used in research about alcoholic encephalopathy syndrome.
    EMD 21657
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