1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
    Neuronal Signaling
  3. iGluR

iGluR

Ionotropic glutamate receptors

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-107718
    Midafotel
    Antagonist 99.00%
    Midafotel (SDZ-EAA 494) is a potent and comprtitive NMDA antagonist with an ED50 value of 39 nM. Midafotel causes intense stereotyped behaviors. Midafotel shows neuroprotective effects.
    Midafotel
  • HY-177127
    Satoprodil
    Inhibitor
    Satoprodil (example 2) is a potent N-methyl-D-aspartate (NMDA) receptor negative allosteric modulator with an IC50 value of 123 nM for NR2B.
    Satoprodil
  • HY-148250
    TP-050
    Agonist
    TP-050, a chemical probe, is a potent, orally active and selective NMDAR agonist with an EC50 value of 0.51 μM and 9.6 μM for GluN2A and GluN2D, respecticely. TP-050 can cross the blood-brain barrier (BBB). TP-050 induces hippocampal long-term (LPT) potentiation enhancemen and enhances neuronal signal transmission.
    TP-050
  • HY-124160
    JNJ-56022486
    Modulator
    JNJ-56022486 is an orally active and potent negative AMPA receptor modulator (Ki=19 nM) selective for?TARP-γ8. JNJ-56022486 is also a TARP-γ8 receptor antagonist, with blood?brain?barrier (BBB) permeability. JNJ-56022486 can be used for research of Epilepsy.
    JNJ-56022486
  • HY-100998
    Metaphit
    Antagonist
    Metaphit is a specific PCPantagonist and site-directed acylating agent of the [3H]phencyclidine binding site in rat brain homogenates. Metaphit prevents PCP-induced locomotor behavior through presynaptic mechanisms.
    Metaphit
  • HY-B0122A
    Topiramate lithium
    Antagonist
    Topiramate (McN 4853) lithium is a broad-spectrum antiepileptic agent. Topiramate lithium 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 lithium
  • HY-18663B
    CP-465022 hydrochloride
    Antagonist
    CP-465022 hydrochloride is a potent, and selective noncompetitive AMPA receptor antagonist with anticonvulsant activity. CP-465022 is against Kainate-induced response with an IC50 of 25 nM in rat cortical neurons. CP-465022 provides a new tool to investigate the role of AMPA receptors in physiological and pathophysiological processes.
    CP-465022 hydrochloride
  • HY-118574
    UBP141
    Antagonist
    UBP141 is a GluN2C/2D (NR2C/2D)-preferring receptor antagonist, with Kds of 2.8, 4.2, 14.2, and 19.3 μM for NMDA receptor subtypes: GluN2C, 2D, 2A, and 2B, respectively. UBP141 can induce potent motor impairment in WT mice.
    UBP141
  • HY-138940
    3-Methoxy PCE hydrochloride
    Antagonist
    3-Methoxy PCE (3-MEO PCE) hydrochloride is structurally classified as an arylcyclohexylamine and is an /b>NMDA receptor antagonist with a pKi value of 7.22.
    3-Methoxy PCE hydrochloride
  • HY-143390
    NMDA receptor modulator 2
    Modulator
    NMDA receptor modulator 2 (Compound 1) is a potent NMDA receptor modulator. NMDA receptor modulator 2 can be used for neurological disorder research.
    NMDA receptor modulator 2
  • HY-176297
    Tezampanel etibutil
    Antagonist
    Tezampanel etibutil is an orally active AMPA/GluR antagonist. Tezampanel etibutil can be used in the research of pain, migraine, and neurological disorders.
    Tezampanel etibutil
  • HY-W736861
    N-Phthaloylglutamic acid
    Agonist
    N-Phthaloylglutamic acid is a partial agonist NMDA receptor with a Ki of 13 μM targeting Glu binding-site.
    N-Phthaloylglutamic acid
  • HY-105627A
    Profadol hydrochloride
    Inhibitor
    Profadol (CI-572) hydrochloride is a potent analgesic agent. Profadol is a µ-opioid receptor (MOR) agonist. Profadol hydrochloride activates the γ-aminobutyric acid (GABA) receptors and inhibits the N-methyl-D-aspartate (NMDA) receptor. Profadol increases the mRNA and protein expression of MOR.
    Profadol hydrochloride
  • HY-146588
    NMDA receptor antagonist 4
    Antagonist 99.64%
    NMDA receptor antagonist 4 (IIc) is a uncompetitive, voltage-dependent, orally active NMDAR blocker, with an IC50 of 1.93 μM. NMDA receptor antagonist 4 shows a positive predicted blood-brain-barrier (BBB) permeability, and can be studied in Alzheimer's disease.
    NMDA receptor antagonist 4
  • HY-106397
    Delucemine
    Antagonist
    Delucemine is a selective serotonin reuptake inhibitor (SSRI) and NMDAR antagonist. Delucemine can be used as an antidepressant.
    Delucemine
  • HY-107695
    Remacemide hydrochloride
    Antagonist
    Remacemide hydrochloride (FPL 12924AA), a moderate inhibitor of the Na+ channel, is a weak uncompetitive NMDA receptor antagonist with IC50s of 68 μM and 76 μM for MK-801 binding and NMDA currents, respectively. Remacemide hydrochloride is an anticonvulsant agent.
    Remacemide hydrochloride
  • HY-14608AR
    L-Glutamic acid monosodium salt (Standard)
    Agonist
    L-Glutamic acid (monosodium salt) (Standard) is the analytical standard of L-Glutamic acid (monosodium salt). This product is intended for research and analytical applications. L-Glutamic acid monosodium salt 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 salt has an agonist effect on the release of DA from dopaminergic nerve endings. L-Glutamic acid monosodium salt can be used in the study of neurological diseases.
    L-Glutamic acid monosodium salt (Standard)
  • HY-124779
    (S)-Alaproclate
    Inhibitor
    (S)-Alaproclate ((S)-GEA 654) is more potent than the R-(+)-enantiomer both in blocking the NMDA receptor currents in vitro and in antagonizing the cGMP increase in vivo.
    (S)-Alaproclate
  • HY-108235C
    (R)-Lanicemine
    Antagonist
    (R)-Lanicemine ((R)-AZD6765) is the less active R-enantiomer of Lanicemine. Lanicemine (AZD6765) is a low-trapping NMDA channel blocker (Ki of 0.56-2.1 μM for NMDA receptor; IC50s of 4-7 μM and 6.4 μM in CHO and Xenopus oocyte cells, respectively). Antidepressant effects.
    (R)-Lanicemine
  • HY-172419A
    Blixeprodil hydrochloride
    Antagonist
    Blixeprodil hydrochloride (GM-1020 hydrochloride) is an orally active, blood-brain barrier-penetrant NMDA receptor inhibitor with a Ki of 3.25 µM in rat cortical tissues. Blixeprodil hydrochloride binds to the MK-801 ion channel site and blocks NMDA receptor-mediated currents in hyperpolarized states in a voltage-dependent manner. Blixeprodil hydrochloride modulates the power of cortical EEG frequency bands, alters spontaneous motor activity, and induces ataxia at high doses. Blixeprodil hydrochloride can be used in the research of depression.
    Blixeprodil hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity

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