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-15786
    SGE-201
    		Modulator
    SGE-201 is an allosteric modulator of N-methyl-D-aspartate receptors (NMDARs), demonstrating significant neuroprotective effects by enhancing NMDAR-mediated responses while differing in action among various blockers in neuronal networks.
    SGE-201
  • HY-119781
    Kaitocephalin
    		Antagonist
    Kaitocephalin (PF1191) is an ionotropic glutamate receptor (NMDAR) antagonist with Ki values of 7.8, 590, and 14000 nM for NMDAR, AMPAR, and KAR, respectively. Kaitocephalin protects neurons by inhibiting excitotoxicity, exhibiting neuroprotective effects. Kaitocephalin can be used in research on neurological diseases such as Alzheimer's disease.
    Kaitocephalin
  • HY-P3340
    Leptin (116-130)
    		Activator
    Leptin (116-130) is a bioactive leptin fragment. Leptin (116-130) promotes AMPA receptor trafficking to synapses and facilitate activity-dependent hippocampal synaptic plasticity. Leptin (116-130) prevents hippocampal synaptic disruption and neuronal cell death in models of amyloid toxicity. Leptin (116-130) has the potential for the research of Alzheimer's disease (AD).
    Leptin (116-130)
  • HY-B0585S1
    Piracetam-d6
    		Modulator
    Piracetam-d6 is deuterium labeled Piracetam. 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-d<sub>6</sub>
  • HY-136844
    LY-300168
    		Antagonist
    LY 300168 (GYKI 53655) is a non-competitive, blood-brain-barrier permeable AMPA receptor antagonist. LY 300168 attenuates hippocampal injury. LY 300168 blocks the sound-induced clonic and tonic convulsions.
    LY-300168
  • HY-P1057
    Pep4c
    		Control
    Pep4c is an inactive control peptide for Pep2m (HY-P1058). Pep4c lacks functional activity to disrupt Protein Interacting with C Kinase 1 (PICK1)-AMPA receptor (GluA2) or N-ethylmaleimide-sensitive factor (NSF)-GluA2 interactions. Pep4c is used as a negative control in experiments to validate the specificity of Pep2m's effects on AMPA receptor trafficking and synaptic plasticity[1][2][3][4][5][6].
    Pep4c
  • HY-169951
    Lu AF90103
    Lu AF90103 (Compound 42e) is a methyl ester prodrug of compound 42d capable of penetrating the blood-brain barrier. Compound 42d acts as a partial agonist of the GluN1/GluN2B complex, exhibiting 24% efficacy, and has an EC50 value of 78 nM. Lu AF90103 plays an important role in neuropsychiatric diseases research.
    Lu AF90103
  • HY-100837
    5-Iodowillardiine
    		Agonist
    5-Iodowillardiine is a potent and selective kainate receptor agonist. 5-Iodowillardiine is selective for kainate receptors composed of hGluR5 subunits.
    5-Iodowillardiine
  • HY-105353
    CEB-1604
    		Antagonist
    CEB-1604 is an NMDA receptor antagonist. CEB-1604 inhibits NMDA-induced currents in oocytes transfected with NMDA receptor isoforms (NR1/NR2A, NR1/NR2B, NR1/NR2C, NR1/NR2D) with IC50 values ranging from 5 to 12 μM. CEB-1604 abolishes NMDA-dependent epileptiform discharges in rat cortical wedge preparations and reduces the depolarizing effects of NMDA. CEB-1604 can be used in the research field of neurological damage diseases.
    CEB-1604
  • HY-103233
    DNQX disodium salt
    		Antagonist 98.07%
    DNQX (FG 9041) disodium salt, a quinoxaline derivative, is a selective, potent competitive non-NMDA glutamate receptor antagonist (IC50s = 0.5, 2 and 40 μM for AMPA, kainate and NMDA receptors, respectively).
    DNQX disodium salt
  • HY-100714B
    L-AP5
    		Antagonist
    L-AP5 (L-APV; L-2-Amino-5-phosphonovaleric acid) is an NMDA antagonist and is the isomer of D-AP5 (HY-100714A). L-AP5 shows a relatively weak amino acid and synaptic blocking activity.
    L-AP5
  • HY-101809A
    CNS 5161
    		Antagonist
    CNS-5161 is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.
    CNS 5161
  • HY-145761
    AMPA-IN-1
    		Inhibitor
    AMPA-IN-1 is a potent inhibitor of AMPA receptor. AMPA receptors are receptors that are widely expressed in the brain, and play a central role in the regulation of fast excitatory synaptic transmission and synaptic plasticity. AMPA-IN-1 has the potential for the research of various central diseases including epilepsy (extracted from patent WO2017082288A1, compound 14).
    AMPA-IN-1
  • HY-155628
    AMPA receptor modulator-6
    		Modulator
    AMPA receptor modulator-6 is an AMPA receptor positive allosteric modulator (PAM). AMPA receptor modulator-6 can be used in the study of neurological diseases.
    AMPA receptor modulator-6
  • HY-105450
    GPI-3000
    		Antagonist
    GPI-3000 is a NMDA receptor antagonist. GPI-3000 can ameliorate metabolic injury and shows neuroprotective effect. GPI-3000 can be used for the researches of metabolic and neurological disease.
    GPI-3000
  • HY-175824
    PSD-95/nNOS PPI-IN-1
    		Inhibitor
    PSD-95/nNOS PPI-IN-1 is a inhibitor targeting the PSD-95/nNOS interaction with potential blood-brain barrier penetration. PSD-95/nNOS PPI-IN-1 binds to the PSD-95 PDZ2 domain with high affinity (Ki = 19.45 μM). PSD-95/nNOS PPI-IN-1 inhibits glutamate-induced excitotoxicity by reducing intracellular ROS levels and inhibiting apoptosis. PSD-95/nNOS PPI-IN-1 significantly reduces cerebral infarct volume in rat tMCAO models. PSD-95/nNOS PPI-IN-1 can be used for the study of acute ischemic stroke.
    PSD-95/nNOS PPI-IN-1
  • HY-W015309S2
    Decanoic acid-d2
    		Inhibitor
    Decanoic acid-d2 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects.
    Decanoic acid-d<sub>2</sub>
  • HY-B1585
    Caramiphen
    Parpanil is an anticholinergic agent with NMDA receptor antagonist activity. Parpanil can be used to inhibit diseases related to cholinergic neurotransmission. Parpanil exerts its pharmacological effects by blocking cholinergic effects.
    Caramiphen
  • HY-P4110
    TAT-NSF222 Fusion Peptide
    		Inhibitor
    TAT-NSF222 Fusion Peptide is a fusion polypeptide with two domains, a TAT domain, which enters cells through macropinocytosis, and an NSF domain that inhibits N-ethylmaleimide-sensitive factor (NSF). TAT-NSF222 Fusion Peptide is an exocytosis inhibitor.
    TAT-NSF222 Fusion Peptide
  • HY-16728A
    Rapastinel acetate
    		Modulator
    Rapastinel (GLYX-13) acetate is a potent NMDAR modulator capable of crossing the blood-brain barrier, and it exhibits extremely high affinity for human NMDAR (EC50=0.0017-9.9 nM). Rapastinel acetate enhances ERK signaling and activates the mTOR pathway, thereby upregulating the expression of BDNF and VGF, and inducing significant neuroplastic changes such as enhanced LTP and increased mature dendritic spine density in the hippocampus. Rapastinel acetate moderately elevates the efflux of dopamine, norepinephrine and 5-HT in the prefrontal cortex, and uniquely avoids side effects of traditional antidepressants such as dissociation, addiction or sedation. Rapastinel acetate is applicable to the research of major depressive disorder and hepatocellular carcinoma.
    Rapastinel acetate
Cat. No. Product Name / Synonyms Application Reactivity
iGluR Isoform Comparison

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