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-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-113084
    L-Cysteine S-sulfate
    Agonist
    L-Cysteine S-sulfate is a potent N-methyl-d-aspartate (NMDA) glutamatergic receptor agonist. L-Cysteine S-sulfate is the substrate for cystine lyase, and can be used in mass spectrometry operations.
    L-Cysteine S-sulfate
  • 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-120970
    Bis(7)-tacrine dihydrochloride
    Inhibitor
    Bis(7)-tacrine dihydrochloride is a dimeric AChE inhibitor derived from tacrine. Bis(7)-tacrine dihydrochloride prevents glutamate-induced neuronal apoptosis by blocking NMDA receptors. Bis(7)-tacrine dihydrochloride is a potent GABAAreceptor antagonist. Bis(7)-tacrine dihydrochloride has the potential for the research of Alzheimer's disease .
    Bis(7)-tacrine dihydrochloride
  • 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-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
  • HY-143393
    NMDA receptor modulator 4
    Modulator
    NMDA receptor modulator 4 (Compound 169) is a potent NMDA receptor modulator. NMDA receptor modulator 4 can be used for neurological disorder research.
    NMDA receptor modulator 4
  • HY-I0096S
    Indole-2-carboxylic acid-13C
    Inhibitor
    Indole-2-carboxylic acid-13C is the 13C-labeled Indole-2-carboxylic acid. Indole-2-carboxylic acid is a strong inhibitor of lipid peroxidation. Indole-2-carboxylic acid (I2CA) specifically and competitively inhibits the potentiation by glycine of NMDA-gated current.
    Indole-2-carboxylic acid-<sup>13</sup>C
  • HY-B1126R
    Orphenadrine hydrochloride (Standard)
    Antagonist
    Orphenadrine (hydrochloride) (Standard) is the analytical standard of Orphenadrine (hydrochloride). This product is intended for research and analytical applications. Orphenadrine hydrochloride is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine hydrochloride relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine hydrochloride is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases.
    Orphenadrine hydrochloride (Standard)
Cat. No. Product Name / Synonyms Application Reactivity

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