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-90003
    Tianeptine
    		Agonist 99.84%
    Tianeptine is an atypical antidepressant. Tianeptine is a moderate-intensity agonist of the μ-opioid receptor (MOR), and to a lesser extent, is an agonist of the δ-opioid receptor (DOR). Tianeptine is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. tianeptine increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects.
    Tianeptine
  • HY-107701
    CGP 78608 hydrochloride
    		Antagonist 99.56%
    CGP 78608 hydrochloride is a highly potent and selective antagonist at the glycine-binding site of the NMDA receptor, with an IC50 of 6 nM. CGP 78608 hydrochloride acts as a potentiator of GluN1/GluN3A-mediated glycine currents, with an estimated EC50 in the low nM range (26.3 nM). Anticonvulsant activity.
    CGP 78608 hydrochloride
  • HY-Y0966S4
    Glycine-1-13C
    		99.73%
    Glycine-1-13C is the 13C-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
  • HY-161137
    LQFM215
    		Inhibitor 99.80%
    LQFM215 is a proline transporter (PROT) inhibitor. LQFM215 inhibits proline transport by competitively binding to the active site of PROT. LQFM215 effectively reduces hyperlocomotion and enhances social interaction.
    LQFM215
  • HY-164795A
    SBI-810 hydrochloride
    		Inhibitor 99.55%
    SBI-810 hydrochloride is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 hydrochloride promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 hydrochloride inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 hydrochloride effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 hydrochloride is applicable to research related to multiple pain disorders.
    SBI-810 hydrochloride
  • HY-W419700
    L-Glutamic acid ammonium
    		Agonist 98.0%
    L-Glutamic acid ammonium 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 ammonium has an agonist effect on the release of DA from dopaminergic nerve endings. L-Glutamic acid can be used in the study of neurological diseases. L-Glutamic acid ammonium acts at ionotropic and?metabotropic glutamate receptors.
    L-Glutamic acid ammonium
  • HY-148825
    NP10679
    		Inhibitor 98.40%
    NP10679 is a selective, pH dependent GluN2B subunit-specific N-methyl-D-aspartate (NMDA) receptor inhibitor with high oral bioavailability and good brain penetration. NP10679 inhibits GluN2B with IC50s of 23 and 142 nM at pH 6.9 and 7.6, respectively. NP10679 is a histamine H1 antagonist and a hERG channel inhibitor with IC50s of 73 and 620 nM, respectively. NP10679 is a reversible inhibitor of human liver CYP enzymes.
    NP10679
  • HY-129086
    BPAM344
    		Agonist 99.66%
    BPAM344 is a kainate receptor (KAR) subunits GluK1b, GluK2a, and GluK3a positive allosteric modulator (PAM).
    BPAM344
  • HY-W001158S
    N,N-Dimethylglycine-d6 hydrochloride
    		Agonist 99.46%
    N,N-Dimethylglycine-d6 (Dimethylglycine-d6) hydrochloride is the deuterium labeled N,N-Dimethylglycine hydrochloride (HY-W001158). N,N-Dimethylglycine (Dimethylglycine) hydrochloride, a natural N-methylated glycine, is a nutrient supplement and acts as an NMDAR glycine site partial agonist. N,N-Dimethylglycine hydrochloride is a methyl donor that can improve immunity, act as an antioxidant to prevent oxidative stress, and scavenge excess free radicals. N,N-Dimethylglycine hydrochloride has antidepressant-like and surfactant effects.
    N,N-Dimethylglycine-d<sub>6</sub> hydrochloride
  • HY-102053
    Apimostinel
    		Agonist 98.69%
    Apimostinel (NRX-1074; AGN-241660) is an orally active NMDA receptor partial agonist.
    Apimostinel
  • HY-N0215S11
    L-Phenylalanine-13C9,15N
    		Antagonist 99.42%
    L-Phenylalanine-13C9,15N is the 13C- and 15N-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals.
    L-Phenylalanine-<sup>13</sup>C<sub>9</sub>,<sup>15</sup>N
  • HY-100811
    7-Chlorokynurenic acid
    		Antagonist 99.86%
    7-Chlorokynurenic acid (7-CKA) is a potent and selective antagonist of the glycine B coagonist site of the N-methyl-D-aspartate (NMDA) receptor (IC50=0.56 μM). 7-Chlorokynurenic acid is also a potent inhibitor of the reuptake of glutamate into synaptic vesicles with a Ki of 0.59 μM. 7-Chlorokynurenic acid has potent antinociceptive actions after neuraxial delivery.
    7-Chlorokynurenic acid
  • HY-117772
    FSC231
    		Inhibitor 99.51%
    FSC231 is a PSD‐95/DLG/ZO‐1 (PDZ) domain inhibitor of PICK1. FSC231 has analgesic effects.
    FSC231
  • HY-107606A
    UBP301 hydrochloride
    		Antagonist
    UBP301 hydrochloride is a potent and selective antagonist of kainate receptor with IC50 and KD of 164 μM and 5.94 μM, respectively. UBP301 hydrochloride has ～30-fold selectivity of kainate receptor over AMPA receptor. UBP301 hydrochloride is the derivative of willardiine.
    UBP301 hydrochloride
  • HY-W742957
    Pregnanolone sulfate (pyridinium)
    		Inhibitor 99.78%
    Pregnanolone sulfate pyridinium is an endogenous neurosteroid that inhibits NMDA receptors and is neuroprotective.
    Pregnanolone sulfate (pyridinium)
  • HY-139192
    Brophenexin
    		Inhibitor 98.74%
    Brophenexin (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. Brophenexin shows neuroprotective activity. Brophenexin prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. Brophenexin protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss.
    Brophenexin
  • HY-129527
    GNE-9278
    		Modulator 99.91%
    GNE-9278 is a highly selective positive allosteric modulator of NMDAR that acts at the GluN1 transmembrane domain (TMD). GNE-9278 acts on activated NMDARs to increase peak current and agonist affinity.
    GNE-9278
  • HY-N0215S5
    L-Phenylalanine-15N
    		Antagonist 98.38%
    L-Phenylalanine-15N is the 15N-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals.
    L-Phenylalanine-<sup>15</sup>N
  • HY-122742
    HBT1
    		99.73%
    HBT1 is an effective AMPA receptor AMPA-R potentiator. HBT1 specifically binds to the ligand-binding domain (LBD) of AMPAR and enhances receptor activity only when AMPA is present., HBT1 has almost no agonistic effect (i.e., reaching the optimal concentration, and then the efficacy decreases as the concentration continues to increase) compared with traditional AMPA-R potentiator, avoiding the bell-shaped reaction of brain-derived neurotrophic factor (BDNF) production in primary neurons. HBT1 can be applicable to a wider range of neurological and psychiatric diseases (such as depression, Alzheimer's disease, etc.).
    HBT1
  • HY-13456
    LY-404187
    		Modulator 98.27%
    LY-404187 is a potent, selective and centrally active positive allosteric modulator of AMPA receptors, with the EC50s of 5.65, 0.15, 1.44, 1.66 and 0.21 µM for GluR1i, GluR2i, GluR2o, GluR3i and GluR4i, respectively. LY-404187 has therapeutic potential in a number of psychiatric disorders and neurodegenerative diseases.
    LY-404187
Cat. No. Product Name / Synonyms Application Reactivity
iGluR Isoform Comparison

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