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-100806S
    Kynurenic acid-d5
    Antagonist 98.35%
    Kynurenic acid-d5 is the deuterium labeled Kynurenic acid. Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.
    Kynurenic acid-d<sub>5</sub>
  • HY-B1488
    Tacrine hydrochloride
    Inhibitor 99.95%
    Tacrine hydrochloride is a potent inhibitor of both AChE and BChE, with IC50s of 31 nM and 25.6 nM, respectively. Tacrine hydrochloride is also a NMDAR inhibitor, with an IC50 of 26 μM. Tacrine hydrochloride can be used for the research of Alzheimer’s disease.
    Tacrine hydrochloride
  • HY-Y0511
    N,N-Dimethylglycine
    Agonist ≥98.0%
    N,N-Dimethylglycine (Dimethylglycine) is a natural N-methylated glycine, is a nutrient supplement and acts as an NMDAR glycine site partial agonist. N,N-Dimethylglycine is a methyl donor, could improve immunity, function as an antioxidant to prevent oxidative stress, and scavenge excess of free radicals. N,N-Dimethylglycine exhibits antidepressant-like and surfactant effects.
    N,N-Dimethylglycine
  • HY-B0585
    Piracetam
    Modulator 99.92%
    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
  • HY-W018061
    Traxoprodil
    Antagonist 99.88%
    Traxoprodil (CP101,606) is a potent and selective NMDA antagonist and protect hippocampal neurons with an IC50 of 10 nM.
    Traxoprodil
  • HY-B0303
    Diphenhydramine
    Antagonist 99.08%
    Diphenhydramine is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) .
    Diphenhydramine
  • HY-15066A
    CNQX disodium
    Antagonist 99.95%
    CNQX disodium (FG9065 disodium) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX disodium is a competitive non-NMDA receptor antagonist. CNQX disodium blocks the expression of fear-potentiated startle in rats.
    CNQX disodium
  • HY-P0117
    Tat-NR2B9c
    Inhibitor 99.97%
    Tat-NR2B9c (Tat-NR2Bct; NA-1) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c also inhibits?neuronal nitric oxide synthase (nNOS)/PSD-95?interaction, and possesses neuroprotective efficacy.
    Tat-NR2B9c
  • HY-100456
    ZL006
    Inhibitor 99.23%
    ZL006 is a potent inhibitor of nNOS/PSD-95 interaction, and inhibits NMDA receptor-mediated NO synthesis.
    ZL006
  • HY-N0368
    Linalool
    Inhibitor 98.55%
    Linalool is a natural monoterpene which is a competitive NMDA receptor antagonist. Linalool is orally active and crosses the blood-brain barrier. Linalool has anticancer, antibacterial, anti-inflammatory, neuroprotective, anxiolytic, antidepressant, anti-stress, cardioprotective, hepatoprotective, nephroprotective and pulmonary protective activities.
    Linalool
  • HY-100815A
    (S)-AMPA
    Agonist ≥99.0%
    (S)-AMPA (L-AMPA), an active S-enantiomer of AMPA, is a potent and selective AMPA receptor agonist.
    (S)-AMPA
  • HY-16312
    MDL-29951
    Antagonist 99.17%
    MDL-29951 is a novel glycine antagonist of NMDA receptor activation, with Ki of 0.14 μM for [3H]glycine binding in vitro and in vivo.
    MDL-29951
  • HY-12506
    Naspm
    Inhibitor
    Naspm (1-Naphthyl acetyl spermine), a synthetic analogue of Joro spider toxin, is a calcium permeable AMPA (CP-AMPA) receptors antagonist.
    Naspm
  • HY-16940
    24(S)-Hydroxycholesterol
    Agonist 99.55%
    24(S)-Hydroxycholesterol (24S-OHC), the major brain cholesterol metabolite, plays an important role to maintain homeostasis of cholesterol in the brain. 24(S)-Hydroxycholesterol (24S-OHC) is one of the most efficient endogenous LXR agonist known and is present in the brain and in the circulation at relatively high levels. 24(S)-Hydroxycholesterol (24S-OHC) is a very potent, direct, and selective positive allosteric modulator of NMDARs with a mechanism that does not overlapthat of other allosteric modulators.
    24(S)-Hydroxycholesterol
  • HY-15085
    MDL 105519
    Inhibitor 99.67%
    MDL 105519 is a potent and selective antagonist of glycine binding to the NMDA receptor.
    MDL 105519
  • 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-107409
    GNE 5729
    Agonist 99.50%
    GNE 5729 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 37 nM for GluN2A, 4.7 and 9.5 μM for GluN2C and GluN2D, respectively.
    GNE 5729
  • HY-107512
    Kynurenic acid sodium
    Antagonist 99.79%
    Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8.
    Kynurenic acid sodium
  • HY-14608S7
    L-Glutamic acid-d5
    Agonist 99.8%
    L-Glutamic acid-d5 is the deuterium labeled L-Glutamic acid. L-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). L-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
    L-Glutamic acid-d<sub>5</sub>
  • HY-10932
    Aniracetam
    Modulator 99.89%
    Aniracetam (Ro 13-5057) is an orally active neuroprotective agent, possessing nootropics effects. Aniracetam potentiates the ionotropic quisqualate (iQA) responses in the CA1 region of rat hippocampal slices. Aniracetam also potentiates the excitatory post synaptic potentials (EPSPs) in Schaffer collateral-commissural synapses. Aniracetam can prevents the CO2-induced impairment of acquisition in hypercapnia model rats. Aniracetam can be used to research cerebral dysfunctional disorders.
    Aniracetam
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