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-107512
    Kynurenic acid sodium
    Antagonist 99.82%
    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-101165
    Cyclothiazide
    Agonist 98.29%
    Cyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABAA receptors. Cyclothiazide is frequently used to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Cyclothiazide can potentiate responses to kainate in hippocampal neurons. Cyclothiazide has effects on glutamatergic neurotransmission. Cyclothiazide also induces epileptiform EEG activity accompanying behavioral seizures.
    Cyclothiazide
  • HY-107602
    UBP310
    Antagonist 99.94%
    UBP310 is a selective GluR5 antagonist, with a Kd of 130 nM.
    UBP310
  • HY-I0096
    Indole-2-carboxylic acid
    Antagonist 99.86%
    Indole-2-carboxylic acid (I2CA) is a competitive antagonist of the glycine site of the NMDA receptor (Ki=15 μM, 5-fluoro-I2CA) and an inhibitor of HIV-1 integrase. Indole-2-carboxylic acid is selective for the glycine site of the NMDA receptor and blocks the enhancement of NMDA receptor by competitively inhibiting the binding of glycine to the NMDA receptor. Indole-2-carboxylic acid can also inhibit the strand transfer activity of HIV-1 integrase by chelating Mg2+ at the active site of integrase and interacting with the hydrophobic cavity. Indole-2-carboxylic acid can be used in the study of neurological diseases (such as stroke, epilepsy) and HIV-1 infection.
    Indole-2-carboxylic acid
  • HY-Y0511
    N,N-Dimethylglycine
    Agonist ≥98.0%
    N,N-Dimethylglycine (Dimethylglycine), a natural N-methylated glycine, is a nutrient supplement and acts as an NMDAR glycine site partial agonist. N,N-Dimethylglycine is a methyl donor that can improve immunity, act as an antioxidant to prevent oxidative stress, and scavenge excess free radicals. N,N-Dimethylglycine has antidepressant-like and surfactant effects.
    N,N-Dimethylglycine
  • HY-16312
    MDL-29951
    Antagonist 99.17%
    MDL-29951 is a novel glycine antagonist of NMDA receptor activation, with Ki of 0.14 μM for [3H]glycine binding in vitro and in vivo.
    MDL-29951
  • HY-17555
    Meclofenoxate hydrochloride
    Activator 98.33%
    Meclofenoxate (Centrophenoxine) hydrochloride is an ester synthesized from DMAE and pCPA, capable of crossing the blood-brain barrier, and can stimulate memory and enhance cognition.
    Meclofenoxate hydrochloride
  • HY-103228
    GYKI 53655 hydrochloride
    Antagonist 98.37%
    GYKI 53655 (LY300168) hydrochloride is an α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) antagonist.
    GYKI 53655 hydrochloride
  • HY-100806R
    Kynurenic acid (Standard)
    Antagonist
    Kynurenic acid (Standard) is the analytical standard of Kynurenic acid. This product is intended for research and analytical applications. 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.
    Kynurenic acid (Standard)
  • HY-15085
    MDL 105519
    Inhibitor 99.67%
    MDL 105519 is a potent and selective antagonist of glycine binding to the NMDA receptor.
    MDL 105519
  • HY-B0585
    Piracetam
    Modulator 99.92%
    Piracetam (UCB-6215) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.
    Piracetam
  • HY-14608S7
    L-Glutamic acid-d5
    Agonist 99.84%
    L-Glutamic acid-d5 is the deuterium 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-d<sub>5</sub>
  • HY-N1916
    Coniferyl ferulate
    Inhibitor 98.73%
    Coniferyl ferulate is an orally active phenolic acid compound. Coniferyl ferulate is a potent inhibitor of glutathione S-transferase (GST) (IC50 = 0.3 μM), which downregulates P-gp expression, induces apoptosis in B-MD-C1 (ADR+/+) cells, and reverses multidrug resistance. Coniferyl ferulate blocks the NMDAR/NR2B-CaMKII-MAPKs signaling pathway, inhibits ROS production and mitochondrial apoptosis, while reshapes the intestinal microbiota and microbial metabolism, ameliorates colonic inflammation and alleviates depressive symptoms in mice. Coniferyl ferulate can alleviate the toxicity of xylene to hematopoietic stem and progenitor cells by targeting Mgst2. Coniferyl ferulate exhibits antibacterial activity against the Gram-positive Bacillus subtilis and Staphylococcus aureus.
    Coniferyl ferulate
  • HY-107409
    GNE 5729
    Agonist 99.05%
    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.
    GNE 5729
  • HY-17030
    Acamprosate calcium
    Antagonist 98.30%
    Acamprosate calcium(Campral EC) is a GABA receptor agonist and modulator of glutamatergic systems; reduces alcohol consumption in animal models of alcohol addiction.
    Acamprosate calcium
  • HY-100807R
    Quinolinic acid (Standard)
    Agonist
    Quinolinic acid (Standard) is the analytical standard of Quinolinic acid. This product is intended for research and analytical applications. 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.
    Quinolinic acid (Standard)
  • HY-15068A
    NBQX disodium
    Antagonist 98.00%
    NBQX disodium (FG9202 disodium) is a highly selective and competitive AMPA receptor antagonist. NBQX disodium has neuroprotective and anticonvulsant activity.
    NBQX disodium
  • HY-N0215S8
    L-Phenylalanine-13C6
    Antagonist 99.8%
    L-Phenylalanine-13C6 is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine 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 is widely used in the production of food flavors and pharmaceuticals.
    L-Phenylalanine-<sup>13</sup>C<sub>6</sub>
  • HY-Y0966S8
    Glycine-d5
    98.0%
    Glycine-d5 is the deuterium 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-d<sub>5</sub>
  • HY-106467B
    Caroverine hydrochloride
    Antagonist
    Caroverine hydrochloride is a potent, competitive and reversible antagonist of NMDA and AMPA glutamate receptor. Caroverine hydrochloride is also an antioxidant and calcium-blocking agent that exhibits vasorelaxant action. Caroverine hydrochloride can be used for the research of inner ear tinnitus.
    Caroverine hydrochloride
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