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-136659
    Ro 04-5595
    Ro 04-5595 is a selective antagonist with specific activity against the NR2B subunit of the NMDA receptor. Ro 04-5595 exhibits favorable pharmacokinetic properties in in vitro and in vivo studies, with rapid uptake and clearance. Ro 04-5595 exhibits strong binding in NR2B receptor-enriched regions and low binding in the cerebellum. Ro 04-5595 is able to effectively inhibit specific binding, showing high affinity for the NR2B receptor and a clear ranking of binding affinity with a variety of other compounds.
    Ro 04-5595
  • HY-157476
    AChE-IN-53
    		Inhibitor
    AChE-IN-53 (Compound I-52) is a potent NMDAR inhibitor, which is a compound with favorable behavioral and neuroprotective effects.
    AChE-IN-53
  • HY-107699
    PPPA
    		Antagonist
    PPPA is a competitive NMDA receptor antagonist that displays moderate selectivity for NR2A-containing receptors.
    PPPA
  • HY-106968
    ZD-9379
    		Antagonist
    ZD-9379 is a potent, orally active, and brain penetrant full antagonist at the glycine site of the NMDA receptor. ZD-9379 has neuroprotective effect.
    ZD-9379
  • HY-181127
    GluN2B-NMDAR Allosteric modulator 1
    		Modulator
    GluN2B-NMDAR Allosteric modulator 1 is a selective GluN2B-NMDAR positive allosteric modulator. GluN2B-NMDAR Allosteric modulator 1 can increase glutamate- and aspartate-evoked GluN2B-NMDAR-gated currents with EC50 values of 43.7 and 18 nM. GluN2B-NMDAR Allosteric modulator 1 can reverse anxiety-like behavior and social cognition deficits in mice. GluN2B-NMDAR Allosteric modulator 1 can be used for the research of neurological disease, such as anxiety.
    GluN2B-NMDAR Allosteric modulator 1
  • HY-15076
    SPD-502 sodium
    SPD-502 sodium 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 sodium 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 sodium may be promising for studying neurodegenerative conditions associated with glutamate excitotoxicity.
    SPD-502 sodium
  • HY-168966
    JNJ-54082730
    		Modulator
    JNJ-54082730 (Compound 1) is the orally active inhibitor for phosphodiesterase (PDE) that inhibits PDE2A, PDE3B, and PDE10A2 with IC50s of 0.95 nM, 6.17 μM (pIC50=5.21) and 87.1 nM (pIC50=7.06), respectively. JNJ-54082730 modulates the activity of AMPA receptor, enhance the synaptic plasticity and promotes the learning and memory function in rats models. JNJ-54082730 can cross blood-brain barrier.
    JNJ-54082730
  • HY-15410
    Gacyclidine
    		Antagonist
    Gacyclidine, a non competitive N-methyl-D-aspartate (NMDA) antagonist, can be used in the study of spinal cord injuries.
    Gacyclidine
  • HY-120524
    CGP 31358
    CGP 31358 is an anticonvulsant agent that binds to a site on the NMDA receptor complex that is coupled to both the transmitter recognition site and to the channel domain. CGP 31358 inhibits the binding of L-Glutamate to the NMDA receptor complex with an IC50 of 53 μM.
    CGP 31358
  • HY-120155
    MS-377
    		Modulator
    MS-377 is a selective and orally active sigma-1 receptor ligand (Ki=73 nM) with weak affinity for sigma-2 receptor (Ki=6900 nM) and no affinity for any other receptors including dopamine, serotonin, PCP site, glutamate, γ-aminobutylic acid, adenosine, adrenergic receptors, etc. (Ki: >10 μM). MS-377 indirectly modulates the NMDA receptor ion-channel complex. MS-377 is a antipsychotic agent. MS-377 inhibits PCP-induced behaviors by inhibition of the increase in dopamine and serotonin release in the rat medial prefrontal cortex. MS-377 can be used for research of schizophrenia.
    MS-377
  • HY-107710
    LY 233053
    		Antagonist
    LY 233053 is a potent and competitive NMDA-receptor antagonist with anticonvulsant and antiepileptic efficacy.
    LY 233053
  • HY-P10357A
    Tat-CBD3 TFA
    		Inhibitor
    Tat-CBD3 TFA, a 15-amino acid peptide from CRMP2, fused to the TAT cell-penetrating motif of the HIV-1 protein, disrupts CRMP2-NMDAR interaction without change in NMDAR localization.
    Tat-CBD3 TFA
  • HY-118489
    L644711
    		Inhibitor
    L644711 is an anion transport inhibitor that reduces cell swelling by inhibiting potassium-activated D-aspartate release in astrocytes. L644711 can be used in the study of brain injury and neuroprotection.
    L644711
  • HY-19435A
    GYKI-47261 dihydrochloride
    		Antagonist
    GYKI-47261 dihydrochloride 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 dihydrochloride is also a potent inducer of CYP2E1.
    GYKI-47261 dihydrochloride
  • HY-P10212
    AVLX-125
    		Inhibitor
    AVLX-125 (UCCB01-125) is a PSD-95 and PDZ domain inhibitor with Kd value of 10 nM. AVLX-125 can be used in the study of inflammatory pain.
    AVLX-125
  • HY-17387S1
    (-)-Huperzine A-d4 hydrochloride
    		Antagonist
    (-)-Huperzine A-d4 hydrochloride is deuterated labeled (-)-Huperzine A (HY-17387). (-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease.
    (-)-Huperzine A-d<sub>4</sub> hydrochloride
  • HY-110234R
    Topiramate D12 (Standard)
    		Antagonist
    Topiramate D12 (Standard) is the analytical standard of Topiramate D12. This product is intended for research and analytical applications. Topiramate D12 (McN 4853 D12) is a deuterium labeled Topiramate. Topiramate is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase.
    Topiramate D12 (Standard)
  • HY-W018061A
    Traxoprodil mesylate
    		Antagonist
    Traxoprodil mesylate (CP101,606) is a potent and selective NMDA antagonist and protect hippocampal neurons with an IC50 of 10 nM.
    Traxoprodil mesylate
  • HY-182479
    MDL 100748
    		Antagonist
    MDL 100748 is an NMDA receptor glycine site antagonist. MDL 100748 modulates NMDA receptor function by acting at the strychnine-insensitive glycine site, which is required for NMDA receptor activation alongside glutamate. MDL 100748 decreases response rates in operant conditioning sessions in phencyclidin (PCP)-trained rats. MDL 100748 can be used for reserach on dementias and schizophrenia.
    MDL 100748
  • HY-107518
    (R,S)-3,4-Dicarboxyphenylglycine
    		Antagonist
    (R,S)-3,4-Dicarboxyphenylglycine ((RS)-3,4-DCPG) is an AMPA receptor antagonist. (R,S)-3,4-Dicarboxyphenylglycine antagonizes AMPA-mediated depolarization of motor neurons in neonatal rats. (R,S)-3,4-Dicarboxyphenylglycine can be used in the study of neurological diseases.
    (R,S)-3,4-Dicarboxyphenylglycine
Cat. No. Product Name / Synonyms Application Reactivity
iGluR Isoform Comparison

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