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-179108
    NMDAR modulator 1
    		Modulator
    NMDAR modulator 1 (Compound 12) is a positive, allosteric GluN1/GluN2B receptor modulator. NMDAR modulator 1 enhances NMDAR current. NMDAR modulator 1 can be used in the research of psychiatric disorders.
    NMDAR modulator 1
  • HY-139708
    NMDA receptor antagonist-3
    		Antagonist
    NMDA receptor antagonist-3, a NMDA receptor antagonist, stands out with a remarkable percentage of recovery (40.0%, at 100 μM) and safe toxicological profile in SH-SY5Y and human adipose mesenchymal stem cells.
    NMDA receptor antagonist-3
  • HY-19391
    UK-240455
    		Antagonist
    UK-240455 is a potent and selective N-methyl D-aspartate (NMDA) glycine site antagonist.
    UK-240455
  • HY-155185A
    NMDA receptor antagonist 8
    		Antagonist
    NMDA receptor antagonist 8 (Compound (R)-10a) is GluN2B subunit-selective NMDA Receptor antagonist, with an Ki of 265 nM and an IC50 of 62 nM. NMDA receptor antagonist 8 can be used for research of neurodegenerative diseases.
    NMDA receptor antagonist 8
  • HY-171979
    Fluorolintane
    		Inhibitor
    Fluorolintane exhibits high affinity for N-methyl-D-aspartate (NMDA) receptors with a Ki of 87.92 nM. Fluorolintane inhibits prepulse inhibition in rats. Fluorolintane also inhibits NMDA receptor-induced field excitatory postsynaptic potentials in rat hippocampal slices.
    Fluorolintane
  • HY-100159A
    Ipenoxazone hydrochloride
    		Antagonist
    Ipenoxazone (MLV-6976) hydrochloride is a potent and centrally acting muscle relaxant.
    Ipenoxazone hydrochloride
  • HY-119950
    ADCI
    		Antagonist
    ADCI, a noncompetitive NMDA antagonist, is a broad-spectrum anticonvulsant agent.
    ADCI
  • HY-19432
    UBP-282
    		Antagonist
    UBP-282 is a potent, selective and competitive AMPA and kainate receptor antagonist. UBP-282 inhibits the fast component of the dorsal root-evoked ventral root potential (fDR-VRP) with an IC50 value of 10.3 μM. UBP-282 antagonizes kainate-induced depolarisations of dorsal roots with a pA2 value of 4.96.
    UBP-282
  • HY-N11061
    Withaphysalin D
    		Antagonist
    Withaphysalin D is a selective antagonist against the N-methyl-D-aspartate receptor (NMDAR) containing GluN2B. Withaphysalin D can be isolated from water lilies and has neuroprotective properties. Withaphysalin D is able to cross the blood-brain barrier.
    Withaphysalin D
  • HY-100834A
    5,7-Dichlorokynurenic acid sodium
    		Antagonist
    5,7-Dichlorokynurenic acid (5,7-DCKA) sodium is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid sodium reduces NMDA-induced neuron injury. 5,7-Dichlorokynurenic acid sodium increases social interaction time, increases open arm exploration time, disinhibits suppressed conflict responding in rodent models. 5,7-Dichlorokynurenic acid sodium exhibits anxiolytic-like activity in rodent models and supports exploration of glycine’s role in NMDA receptor-mediated synaptic transmission.
    5,7-Dichlorokynurenic acid sodium
  • HY-117176
    KRP-199
    		Antagonist
    KRP-199 (compound 14h) is an α-amino-3-hydroxy-5-methylisoxazolepropionic acid receptor (AMPA-R) antagonist (Ki=16 nM) with high potency and selectivity for AMPA-R in vitro and good neuroprotective effects in vivo. KRP-199 can be used in the study of neurodegenerative diseases.
    KRP-199
  • HY-185027
    Memagal
    		Antagonist
    Memagal is an AchE inhibitor (IC50 = 1.16 nM) and a NMDAR antagonist (Ki = 4.6 μM). Memagal inhibits the neurotoxicity induced by NMDA (HY-17551), with its IC50 value being 0.28 nM. Memagal can be used for research on Alzheimer's disease.
    Memagal
  • HY-165474
    TDPAM01
    		Agonist
    TDPAM01 is a positive allosteric modulator of AMPA receptor GluA2. TDPAM01 can specifically bind to the ligand-binding domain (LBD) of GluA2 and shows an IC50 of 13.4 nM for the GluA2 flop subtype. TDPAM01 can stabilize the activated conformation of GluA2 receptors, delay the receptor deactivation or desensitization process, maintaining the rapid excitatory synaptic transmission in the central nervous system.
    TDPAM01
  • HY-180197
    PICK1 PDZ-IN-1
    PICK1 PDZ-IN-1 (Compound 6b) is a selective and brain-penetrant protein interacting with C kinase 1 (PICK1) PDZ domain inhibitor with a Ki of 27.73 μM. PICK1 PDZ-IN-1 can competitively inhibit the interaction between PICK1 and the GluA2 subunit of AMPA receptors. PICK1 PDZ-IN-1 can increase the survival rate of HT22 cells and primary cortical neuron cells induced by glutamate and inhibit ROS production. PICK1 PDZ-IN-1 exhibits neuroprotective effect and reduces the area of cerebral infarction. PICK1 PDZ-IN-1 can be used for the research of ischemic stroke.
    PICK1 PDZ-IN-1
  • HY-107701A
    CGP-78608
    		Antagonist
    CGP 78608 is a highly potent and selective antagonist at the glycine-binding site of the NMDA receptor, with an IC50 of 6 nM. CGP 78608 acts as a potentiator of GluN1/GluN3A-mediated glycine currents, with an estimated EC50 in the low nM range (26.3 nM). CGP 78608 has anticonvulsant activities.
    CGP-78608
  • HY-P1293A
    Conantokin G TFA
    		Antagonist
    Conantokin G TFA, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G TFA inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G TFA has neuroprotective properties.
    Conantokin G TFA
  • HY-12294B
    (Rac)-PEAQX
    		Antagonist
    (Rac)-PEAQX is a NMDA receptor agonist. (Rac)-PEAQX can promote the activation of caspase-3 and induce cell apoptosis in cortical striatal slice cultures .
    (Rac)-PEAQX
  • HY-W016145S
    L-Glutamic acid-13C5 hydrate salt
    		Agonist
    L-Glutamic acid-13C5 hydrate salt is the 13C labeled L-Glutamic acid hydrate salt. L-Glutamic acid monosodium hydrate is an excitatory amino acid neurotransmitter that acts as an agonist for all subtypes of glutamate receptors (metabolic rhodophylline, NMDA, and AMPA). L-Glutamic acid monosodium hydrate has an agonist effect on the release of DA from dopaminergic nerve endings. L-Glutamic acid monosodium hydrate can be used in the study of neurological diseases. L-Glutamic acid monosodium hydrate acts at ionotropic and?metabotropic glutamate receptors.
    L-Glutamic acid-<sup>13</sup>C<sub>5</sub> hydrate salt
  • HY-120074
    UBP512
    		Modulator
    UBP512 is an NMDA receptor modulator with the activity to regulate NMDA receptor activity. UBP512 is a GluN2A-selective enhancer and GluN2C and GluN2D inhibitor, belonging to a new generation of NMDA receptor modulators, which may have potential effects on the study and inhibition of related neurological diseases.
    UBP512
  • HY-W709349
    Flupirtine hydrochloride
    		Antagonist
    Flupirtine (D 9998) 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 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
iGluR Isoform Comparison

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