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-W008038
    NMDAR antagonist 3
    		Antagonist
    NMDAR antagonist 3 (Compound 2) is an antagonist of the NMDA receptor. NMDAR antagonist 3 has a certain but weak inhibitory activity against the NR1A/2B subtype of the NMDA receptor.
    NMDAR antagonist 3
  • HY-15073
    Becampanel
    		Antagonist ≥98.0%
    Becampanel (AMP397) is the first competitive AMPA antagonist and an antiepileptic agent.
    Becampanel
  • HY-B0122S
    Topiramate-13C6
    		Antagonist 99.67%
    Topiramate-13C6 (McN 4853-13C6) is the 13C labeled isotope of Topiramate (HY-B0122). Topiramate (McN 4853) 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-<sup>13</sup>C<sub>6</sub>
  • HY-12503
    CFM-2
    		Antagonist 98.93%
    CFM-2 is a potent and selective non-competitive AMPAR antagonist. CFM-2 possesses anticonvulsant activity in various models of seizures.
    CFM-2
  • HY-B1126
    Orphenadrine hydrochloride
    		Antagonist
    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 hydrochloride
  • HY-117734
    PYD-106
    		Modulator 98.13%
    PYD-106 is a stereoselective pyrrolidinone (PYD) positive allosteric modulator for GluN2C-containing NMDA receptors. PYD-106 increases opening frequency and open time of single channel currents activated by maximally effective concentrations of agonist but only has modest effects on glutamate and glycine EC50. PYD-106 selectively enhances the responses of diheteromeric GluN1/GluN2C receptors but not triheteromeric GluN1/GluN2A/GluN2C receptors.
    PYD-106
  • HY-107774
    BMS-986163
    		Modulator
    BMS-986163 is a negative allosteric modulator of GluN2B. The proagent BMS-986163 rapidly converts to its active parent molecule BMS-986169 (Ki=4 nM, IC50=24 nM).
    BMS-986163
  • HY-136459
    NMDA receptor antagonist 2
    		Antagonist
    NMDA receptor antagonist 2 is a potent and orally active NR2B subtype-selective NMDA antagonist with an IC50 and a Ki of 1.0 nM and 0.88 nM, respectively. NMDA receptor antagonist 2 is used for the study of neuropathic pain and Parkinson’s disease.
    NMDA receptor antagonist 2
  • HY-139142A
    Simufilam dihydrochloride
    		Activator
    Simufilam dihydrochloride (PTI-125 dihydrochloride) is an orally active FLNA modulator. Simufilam dihydrochloride restores NMDAR signaling and Arc expression. Simufilam dihydrochloride inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, improves insulin sensitivity, reduces Aβ42-induced neuroinflammation and tau protein hyperphosphorylation. Simufilam dihydrochloride can be used for research of Alzheimer's disease.
    Simufilam dihydrochloride
  • HY-B0504S5
    Creatinine-15N
    		Modulator
    Creatinine-15N (NSC13123-15N) is the 15N-labeled Creatinine (HY-B0504). Creatinine (NSC13123) is an orally active, blood-brain barrier-permeable modulator of GABAA and NMDA receptors, with activities of antioxidation and metabolic regulation. Creatinine is generated via non-enzymatic conversion of creatine and phosphocreatine in muscle. Creatinine serum levels correlate with muscle mass, glomerular filtration rate, and extrarenal clearance, serving as an evaluation biomarker for renal function, muscle mass, and clinical outcomes, and used for perioperative renal risk assessment. In addition, Creatinine can induce specific Cryptococcus species to produce creatinine deiminase and act as their nitrogen source, while it can be secreted via renal tubules. Creatinine is widely used in research related to various diseases such as neurodegenerative diseases, psychiatric disorders, acute kidney injury, chronic kidney disease, and renal failure.
    Creatinine-<sup>15</sup>N
  • HY-Y0966S5
    Glycine-1-13C,15N
    		99.5%
    Glycine-1-13C,15N is the 13C- 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-1-<sup>13</sup>C,<sup>15</sup>N
  • HY-17030S
    Acamprosate-d3 calcium
    		Antagonist 99.9%
    Acamprosate-d3 (calcium) is the deuterium labeled Acamprosate calcium. Acamprosate calcium is a GABA receptor agonist and modulator of glutamatergic systems.
    Acamprosate-d<sub>3</sub> calcium
  • HY-103234B
    GYKI 52466 hydrochloride
    		Antagonist
    GYKI 52466 hydrochloride is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 hydrochloride has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 hydrochloride can be used in Parkinson's disease research.
    GYKI 52466 hydrochloride
  • HY-112699
    AMPA receptor modulator-1
    		Inhibitor
    AMPA receptor modulator-1 is a potent, orally active and selective AMPAR regulatory protein TARP γ-8 negative modulator with a pIC50 of 9.7, more selective over GluA1/γ-2 (pIC50=5).
    AMPA receptor modulator-1
  • HY-103491
    PF-06462894
    		Modulator
    PF-06462894 is an alkyne-lacking metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator profiled in both rat and nonhuman primates.
    PF-06462894
  • HY-120681
    CGP39653
    		Antagonist
    CGP39653 is a competitive NMDA receptor antagonist that inhibits receptor function by competing with glutamate for the binding site.
    CGP39653
  • HY-107944R
    Chlorphenesin carbamate (Standard)
    		Inhibitor
    Chlorphenesin carbamate (Standard) is the analytical standard of Chlorphenesin carbamate. This product is intended for research and analytical applications. Chlorphenesin carbamate is a centrally acting skeletal muscle relaxant. Chlorphenesin carbamate can be used for the research of pain and discomfort related to skeletal muscle trauma and inflammation. Chlorphenesin carbamate is a selective blocker of polysynaptic pathways at the spinal and supra-spinal levels. Antinociceptive effect.
    Chlorphenesin carbamate (Standard)
  • HY-103235
    NPEC-caged-(S)-AMPA
    		Activator
    NPEC- caged-(S)-AMPA, a caged neurotransmitter analog, is a NPEC photoprotecting group caged the (S)-AMPA (HY-100815A) to make caged ligands specific for glutamate receptor sub-types. NPEC- caged-(S)-AMPA selectively activates AMPA receptor.
    NPEC-caged-(S)-AMPA
  • HY-17670
    AMPA receptor modulator-11
    		Modulator
    AMPA receptor modulator-11 (example 210) is a positive allosteric AMPA receptor modulator. AMPA receptor modulator-11 can be used for research on depression, schizophrenia, Alzheimer's disease or attention deficit hyperactivity disorder (ADHD).
    AMPA receptor modulator-11
  • HY-181007
    NMDA receptor antagonist 9
    		Antagonist
    NMDA receptor antagonist 9 is a selective GluN2B subunit-containing NMDA receptor antagonist with a Ki of 5.2 nM. NMDA receptor antagonist 9 exhibits 9-fold selectivity over σ1 receptors, shows poor selectivity towards σ2 receptors. NMDA receptor antagonist 9 inhibits ion flux through GluN2B subunit-containing NMDA receptors. NMDA receptor antagonist 9 can be used for the research of neurological disease, such as alzheimer’s disease and parkinson’s disease.
    NMDA receptor antagonist 9
Cat. No. Product Name / Synonyms Application Reactivity
iGluR Isoform Comparison

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