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-170325
    17alpha-Hydroxywithanolide D
    Modulator
    17alpha-Hydroxywithanolide D is the allosteric modulator for NMDA receptor with an IC50 of 44.24 nM. 17alpha-Hydroxywithanolide D exhibits neuroprotective activity and can be used in research of Alzheimer's disease disease.
    17alpha-Hydroxywithanolide D
  • HY-108920
    4-Chlorokynurenine
    99.94%
    4-Chlorokynurenine (4-Cl-KYN) is a prodrug of 7-Chlorokynurenic acid (NMDA receptor antagonist) (HY-100811). 4-Chlorokynurenine has orally activity and blood-brain permeability. 4-Chlorokynurenine can reduce depressive symptoms and neurotoxicity. 4-Chlorokynurenine can be used for the research of neurological disease, such as depression and seizure.
    4-Chlorokynurenine
  • HY-155355
    LY836
    Inhibitor
    LY836 is an orally active neuroprotective agent. LY836 significantly blocks PSD95-nNOS association in cortical neurons. LY836 can be used in study ischemic stroke.
    LY836
  • HY-100785A
    gamma-DGG acetate
    Antagonist
    gamma-DGG acetate (γDGG acetate) is a competitive AMPA receptor blocker. gamma-DGG acetate is also a reversible Excitatory post-synaptic potentials (e.p.s.p.s) antagonist.
    gamma-DGG acetate
  • HY-107603
    NS3763
    Antagonist
    NS3763 is a selective and noncompetitive GLUK5 receptor antagonist with an IC50 of 1.6 µM. NS3763 does not show significant antagonistic properties on GLUK6, AMPA or NMDA receptors.
    NS3763
  • HY-W001158S1
    N,N-Dimethylglycine-d3 hydrochloride
    Agonist
    N,N-Dimethylglycine-d3 (Dimethylglycine-d3) 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>3</sub> hydrochloride
  • HY-P1285
    Conantokin R
    Antagonist
    Conantokin R (Con-R) is an NMDA receptor peptide antagonist with an IC50 of 93 nM. Conantokin R binds Zn2+ and Mg2+ with Kds of 0.15 μM and 6.5 μM, respectively. Conantokin R shows anticonvulsant activity.
    Conantokin R
  • HY-19225A
    Ensaculin free base
    Antagonist
    Ensaculin free base (KA-672) is a NMDA antagonist and have high affinities to serotonergic 5-HT1A and 5-HT7 receptors, adrenergic α1, and dopaminergic D2 and D3 receptors. Ensaculin free base is a memory-enhancing agent. Ensaculin free base has the potential as an antidementia agent acting on various transmitter systems.
    Ensaculin free base
  • HY-12962A
    NMDA-IN-1 dihydrochloride
    Antagonist
    NMDA-IN-1 dihydrochloride is a selective NMDA NR2B antagonist with a Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM. NMDA-IN-1 dihydrochloride inhibits Glu/Gly stimulated Ca2+ flux in Ltk- cells expressing the hNR1a/NR2B with a IC50 of 9.7 nM. NMDA-IN-1 dihydrochloride has no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor. NMDA-IN-1 dihydrochloride shows excellent activity in the mechanical hyperalgesia assay in rats. NMDA-IN-1 dihydrochloride can be used for the studies of stroke, parkinson, and neuropathic pain.
    NMDA-IN-1 dihydrochloride
  • HY-B0585R
    Piracetam (Standard)
    Modulator
    Piracetam (Standard) is the analytical standard of Piracetam. This product is intended for research and analytical applications. 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 (Standard)
  • HY-136299A
    Sepimostat dimethanesulfonate
    Antagonist
    Sepimostat dimethanesulfonate (FUT-187) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat dimethanesulfonate inhibits the Ifenprodil binding with a Ki value of 27.7 µM.
    Sepimostat dimethanesulfonate
  • HY-156626
    Nevadistinel
    Modulator
    Nevadistinel (NYX-458; NYX-3054) is a positive allosteric modulator of N-methyl-D-aspartate (NMDA) receptor. Nevadistinel can be used to inhibit cognitive impairment associated with neurodegenerative diseases, such as mild cognitive impairment, mild Alzheimer's disease, Parkinson's disease, Lewy body disease.
    Nevadistinel
  • HY-N0215S9
    L-Phenylalanine-13C9,15N,d8
    Antagonist
    L-Phenylalanine-13C9,15N,d8 is the deuterium, 13C-, and 15-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,d<sub>8</sub>
  • HY-P1056
    pep2-SVKI
    Inhibitor
    pep2-SVKI is a selective peptide inhibitor. pep2-SVKI inhibits the binding of AMPA-type glutamate receptor (GluA2) (C-terminal PDZ site) to glutamate receptor interacting protein (GRIP), AMPA receptor binding protein (ABP), and C-kinase interacting protein (PICK1). pep2-SVKI increases the amplitude of AMPA receptor-mediated currents and blocks long-term depression (LTD). pep2-SVKI can be used to study neurological diseases.
    pep2-SVKI
  • HY-135131
    Synthalin hydrochloride
    Synthalin hydrochloride is a K+ channel blocker with neuronal excitability modulating activity. Synthalin hydrochloride has an effect on NMDA-mediated depolarization, possibly through receptor-mediated modulation of L-glutamate and serotonin (5-HT). The use of Synthalin hydrochloride can enhance the understanding of changes in membrane potential of different neurons and help study the role of polyamines in neuronal excitability.
    Synthalin hydrochloride
  • HY-147352
    NMDA receptor potentiator-1
    Modulator
    NMDA receptor potentiator-1 (Compound 1368) is a subunit selective NMDA receptor potentiator with IC50s of 4 μM and 5 μM against NR2C and NR2D expression, respectively.
    NMDA receptor potentiator-1
  • HY-108200
    UK-315716
    Antagonist
    UK-315716 is an NMDA receptor antagonist. UK-315716 has a synergistic neuroprotective effect. UK-315716 can be used for research on neurological diseases such as stroke and headache.
    UK-315716
  • HY-B1488R
    Tacrine hydrochloride (Standard)
    Inhibitor
    Tacrine (hydrochloride) (Standard) is the analytical standard of Tacrine (hydrochloride). This product is intended for research and analytical applications. 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 (Standard)
  • HY-109097A
    Otaplimastat hydrochloride
    Antagonist
    Otaplimastat (SP-8203) hydrobromide, a matrix metalloproteinase (MMP) inhibitor, blocks N-methyl-D-aspartate (NMDA) receptor-mediated excitotoxicity in a competitive manner. Otaplimastat hydrobromide also exhibits anti-oxidant activity. Otaplimastat hydrobromide can be used for the research of brain ischemic injury.
    Otaplimastat hydrochloride
  • HY-100922
    N-Acetylglycyl-D-glutamic acid
    Agonist
    N-Acetylglycyl-D-glutamic acid is a peptide with excitatory effect. N-Acetylglycyl-D-glutamic acid induces seizures in mice.
    N-Acetylglycyl-D-glutamic acid
Cat. No. Product Name / Synonyms Application Reactivity

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