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-148611
    NSC339614 potassium
    NSC339614 potassium is a selective GluN1/GluN2C and GluN1/GluN2D receptor enhancer with the activity of enhancing neuronal responses to specific NMDA receptors. NSC339614 potassium can selectively enhance the signaling of GluN1/GluN2C and GluN1/GluN2D receptors without affecting other NMDA receptors. The mechanism of action of NSC339614 potassium does not compete with agonists of L-glutamate or glycine, nor does it depend on membrane potential. The activity of NSC339614 potassium depends on the specific structure of the agonist ligand binding domain, showing its potential as a novel pharmacological agent for studying the function of NMDA receptor subtypes and providing new lead compounds for a variety of neurological diseases.
    NSC339614 potassium
  • HY-P1058
    Pep2m
    		Inhibitor
    Pep2m is a peptide receptor inhibitor. Pep2m inhibits the interaction between the C-terminus of the AMPA-type glutamate receptor (GluA2) subunit and N-ethylmaleimide-sensitive fusion protein (NSF). Pep2m prevents synaptic long-term depression (LTD). Pep2m can reduce postsynaptic currents in neurons, AMPA-mediated currents in cultured hippocampal neurons, and AMPA receptor surface expression[1][2][3][4][5].
    Pep2m
  • HY-137049
    Co 101244
    Co-101244 (PD 174494) is an NMDA receptor blocker that specifically targets the NR2B subunit.
    Co 101244
  • HY-15078
    NS1219
    NS1219 ((R)-SPD502) is the isomer of NS 1209 HY-15074. NS1209 is a selective AMPA receptor antagonist with neuroprotective activity. NS1209 can be used for the research of stroke, neuropathic pain and epilepsy.
    NS1219
  • HY-100356
    Aptiganel
    		Antagonist
    Aptiganel (CNS 1102 (free base)), peptide, is a noncompetitive NMDA antagonist with cerebroprotective effects. Aptiganel can be used for the research of stroke.
    Aptiganel
  • HY-P11263
    AVLX-144
    		Inhibitor
    AVLX-144 is a highly potent inhibitor of postsynaptic density protein 95 (PSD-95). AVLX-144 can be used as a template to develop imaging probes for postsynaptic density (PSD) molecules, and can be labeled with fluorine-18 (¹⁸F) or tritium (³H) to visualize PSD-95 in vivo. AVLX-144 can be utilized for the study of Parkinson's disease.
    AVLX-144
  • HY-143397
    NMDA receptor modulator 6
    		Modulator
    NMDA receptor modulator 6 (Compound 183) is a potent NMDA receptor modulator. NMDA receptor modulator 6 can be used for neurological disorder research.
    NMDA receptor modulator 6
  • HY-136905
    AMPA receptor antagonist-2
    		Inhibitor
    AMPA receptor antagonist-2 (example 23) is an AMPA receptor antagonist.
    AMPA receptor antagonist-2
  • HY-W274652
    Benzylaspartic acid
    		Agonist
    Benzylaspartic acid (IEM-1770), a derivative of aspartic acid, is a NMDA agonist. Benzylaspartic acid has antidepressant activity. Benzylaspartic acid blocks alcohol-abstinence syndrome (AAS) development in chronic alcohol drinking rat models. Benzylaspartic acid can be used for depression research.
    Benzylaspartic acid
  • HY-116244
    Ro 48-8587
    		Antagonist
    Ro 48-8587 is a selective AMPA receptor antagonist with an IC50 of 8 nM. Ro 48-8587 functionally inhibits AMPA receptor activity, blocks AMPA-induced depolarization of rat cortical wedges. Ro 48-8587 can be used for the research of ischaemia and seizures.
    Ro 48-8587
  • HY-183324
    AMPA receptor modulator-12
    		Modulator
    AMPA receptor modulator-12 is an orally acrive AMPA receptor positive allosteric modulator. AMPA receptor modulator-12 also exhibits moderate binding affinity for the human dopamine transporter with a Kd of 1.57 μM. AMPA receptor modulator-12 enhances AMPA receptor-mediated ion currents, delays channel deactivation. AMPA receptor modulator-12 prolongs sleep latency, reduces sleep duration, extends forced swimming time, improves rotarod endurance, and alleviates acute sleep deprivation-related behavioral deficits. AMPA receptor modulator-12 does not increase spontaneous locomotion. AMPA receptor modulator-12 can be used for the research of narcolepsy and fatigue-related conditions.
    AMPA receptor modulator-12
  • HY-178153
    BPAM363
    		Modulator
    BPAM363 is an orally active, selective positive allosteric modulator (PAM) of AMPARs with blood-brain barrier penetration. BPAM363 selectively potentiates AMPAR activity in human and rat models, with an EC2x value of 0.96 μM in rat embryonic cortex primary neurons. BPAM363 upregulates BDNF protein expression in rat primary cortical neuronal cultures. BPAM363 enhances AMPA-mediated excitatory postsynaptic responses in rat and mice. BPAM363 can be used for the study of cognitive disorders.
    BPAM363
  • HY-100842
    (R)-3C4HPG
    		Inhibitor
    (R)-3C4HPG is an NMDA receptor antagonist.
    (R)-3C4HPG
  • HY-169950
    NMDA agonist 1
    		Agonist
    NMDA agonist 1 (compound 42d) is a potent NMDA agonist with a Ki value of 96 nM. NMDA agonist 1 acts as a partial agonist of the GluN1/GluN2B complex with an EC50 value of 78 nM.
    NMDA agonist 1
  • HY-183101
    AMPAR modulator-12
    		Modulator
    AMPAR modulator-12 is a blood-brain barrier-permeable AMPAR positive allosteric modulator. AMPAR modulator-12 reduces NOX-1 expression, enhances AMPAR-mediated currents, promotes excitatory postsynaptic transmission and restores AMPAR function. AMPAR modulator-12 enhances excitatory and inhibitory synaptic transmission, reduces burst firing in the lateral habenula after withdrawal, and produces rapid and sustained antidepressant-like effects. AMPAR modulator-12 is applicable for the research of depression.
    AMPAR modulator-12
  • HY-167885
    SN-35210 free base
    		Inhibitor
    SN-35210 free base, an ester analogue, is designed for rapid offset via esterase-mediated hydrolysis.
    SN-35210 free base
  • HY-111528
    CGP 43487
    		Antagonist
    CGP 43487 is a NMDA receptor antagonist. CGP 43487 significantly affects the gross structural characteristics of the developing dentate gyrus.
    CGP 43487
  • HY-112095
    EVT-101 free base
    		Antagonist
    EVT-101 free base is a GluN2B antagonist. EVT-101 free base binds at the same GluN1/GluN2B dimer interface as Ifenprodil (HY-12882). EVT-101 free base inhibits calcium influx in chicken-derived cells, with an EC50 of 22 nM. EVT-101 can be used in the research of brain disorders.
    EVT-101 free base
  • HY-105476
    TAN 950A
    		Inhibitor
    TAN 950A is antifungal amino acid antibiotic. TAN 950A has affinity for three excitatory amino acid (EAA) receptor and can inhibit [3H]AMPA, [3H]kainite and [3H]CPP binding competitively. TAN 950A can be used for the researches of infection and neurological disease.
    TAN 950A
  • HY-101440
    Indantadol
    		Antagonist
    Indantadol (the free base of CHF-3381) is an orally active, non-selective NMDA antagonist and MAO inhibitor. Indantadol blocks the binding of [³H]-MK-801 to NMDA receptors in a non-competitive manner, with an IC50 of 8.1 μM. Indantadol completely inhibits dopamine release caused by NMDA. Indantadol protects neurons, with an ED₅₀ of 35 μM. Indantadol has anticonvulsant and anti-high pain hypersensitivity activities.
    Indantadol
Cat. No. Product Name / Synonyms Application Reactivity
iGluR Isoform Comparison

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