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-182548
    BTS 72664
    		Inhibitor
    BTS 72664 is a broad-spectrum, non-sedating, orally effective anticonvulsant. Its anticonvulsant effect mainly arises from enhancing GABAA receptor (GABAA receptor)-mediated chloride channel currents, while it exerts weak blocking effects on Na+ channels (Ki = 350 μM) and NMDA receptors (NMDA receptor) (IC50 = 43 μM). BTS 72664 prevents the elevation of extracellular glutamate, glycine and serine concentrations in neurons, reduces cerebral infarct size, promotes functional recovery, prevents multiple types of epileptic seizures, and has low sedative potential. BTS 72664 can be used for the research of epilepsy, stroke and migraine.
    BTS 72664
  • HY-P5487
    GluR23Y
    GluR23Y is a biological active peptide. (This GluR23Y peptide was used in ELISA cell-surface assay for the insulin-stimulated endocytosis of native AMPA receptors in cultured hippocampal neurons. GluR23Y prevented any insulin-induced reduction. The blockade of insulin action was observed when the GluR23Y peptide was delivered into neurons by fusing it to the membrane transduction domain of HIV-1.)
    GluR23Y
  • HY-100808R
    D-Serine (Standard)
    		Agonist
    D-Serine (Standard) is the analytical standard of D-Serine. This product is intended for research and analytical applications. D-Serine ((R)-Serine), an endogenous amino acid involved in glia-synapse interactions that has unique neurotransmitter characteristics, is a potent co-agonist at the NMDA glutamate receptor. D-Serinee has a cardinal modulatory role in major NMDAR-dependent processes including NMDAR-mediated neurotransmission, neurotoxicity, synaptic plasticity, and cell migration[1][2].
    D-Serine (Standard)
  • HY-100782
    DL-AP7
    		Antagonist
    DL-AP7 is a competitive NMDA antagonist and an anticonvulsant. DL-AP7 blocks the NMDA-induced convulsions and impairs learning performance in a passive avoidance task in mice.
    DL-AP7
  • HY-155185
    NMDA receptor antagonist 7
    		Antagonist
    NMDA receptor antagonist 7 (Compound (S)-10a) is GluN2B subunit-selective NMDA Receptor antagonist, with an Ki of 93 nM and an IC50 of 72 nM. NMDA receptor antagonist 7 can be used for research of neurodegenerative diseases.
    NMDA receptor antagonist 7
  • HY-P2307A
    Tat-NR2Baa TFA
    Tat-NR2BAA TFA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA TFA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95.
    Tat-NR2Baa TFA
  • HY-131691
    NMDAR blocker 1
    NMDAR blocker 1 is an NMDA receptor channel blocker with an IC50 of 5.0 μM. NMDAR blocker 1 exhibits fast on-off blockade kinetics and strong voltage dependence, and does not compete with glutamate or glycine. NMDAR blocker 1 prevents glutamate/NMDA-induced intracellular Ca2+ overload, modulates the glutamate-nitric oxide-cGMP pathway. NMDAR blocker 1 prevents in vitro excitotoxic neurodegeneration of cultured cerebellar and hippocampal neurons. NMDAR blocker 1 attenuates excitotoxic insult in an mouse model of hyperammonemia-induced excitotoxicity. NMDAR blocker 1 can be used for the research of neurodegenerative diseases.
    NMDAR blocker 1
  • HY-103231
    (S)-CPW 399
    		Agonist
    (S)-CPW 399 is a subtype-selective full agonist of AMPA receptors, with a 20-fold higher selectivity for GluA1 and GluA2 subunits over GluA3 and GluA4 subunits. (S)-CPW 399 can significantly increase the spontaneous firing rate (FR) of LC noradrenergic neurons by activating AMPA receptors containing GluA1 subunits. (S)-CPW 399 can be used for the study of neurological diseases.
    (S)-CPW 399
  • HY-B1585B
    Caramiphen (edisylate)
    		Antagonist
    Caramiphen edisylate (Parpanil edisylate) is an anticholinergic agent with NMDA receptor antagonist activity. Caramiphen edisylate can be used to inhibit diseases related to cholinergic neurotransmission. Caramiphen edisylate exerts its pharmacological effects by blocking cholinergic effects.
    Caramiphen (edisylate)
  • HY-139350
    AMPA receptor antagonist-1
    		Antagonist
    AMPA receptor antagonist-1 (Example 143) is an AMPA receptor antagonist. AMPA receptor antagonist-1 can be used in the research of neurological disorders.
    AMPA receptor antagonist-1
  • HY-145370
    GluN2B receptor modulator-1
    		Modulator
    GluN2B receptor modulator-1 is a selective GluN2B negative allosteric modulator with an IC50 value of 31 nM.
    GluN2B receptor modulator-1
  • HY-B1487A
    Procyclidine
    		Antagonist
    Procyclidine (Tricyclamol; (±)-Procyclidine), an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy.
    Procyclidine
  • HY-182631
    CX1763
    		Modulator
    CX1763 is an AMPAR allosteric modulator. CX1763 allosterically potentiates glutamate-evoked currents, accelerates channel opening, and increases the surface levels of AMPAR containing Glur2 (R). CX1763 enhances synaptic transmission in the rat hippocampus. CX1763 improves attention in rats and attenuates amphetamine-induced hyperactivity in mice. CX1763 can be used in studies related to attention deficit hyperactivity disorder and opioid-induced respiratory depression.
    CX1763
  • HY-19243
    GV-196771A
    		Antagonist
    GV-196771A is the sodium salt form of GV196771, is an NMDA receptor antagonist.
    GV-196771A
  • HY-B0765R
    Dehydroepiandrosterone sulfate sodium (Standard)
    		Activator
    Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt (Standard) is the analytical standard of Dehydroepiandrosterone sulfate sodium salt (HY-B0765). This product is intended for research and analytical applications. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality.
    Dehydroepiandrosterone sulfate sodium (Standard)
  • HY-186183
    Normethyl-ZCAN262
    		Modulator
    Normethyl-ZCAN262 (Normethyl-262) is a blood-brain barrier-permeable selective GluR2/AMPAR receptor modulator. Normethyl-ZCAN262 inhibits AMPA-mediated neurotoxicity, the formation of the GAPDH-GluR2 complex, and GluR2/AMPAR neurotoxicity. Normethyl-ZCAN262 enables in vivo imaging of brain AMPA receptors and is used in research related to multiple sclerosis, amyotrophic lateral sclerosis, neuroinflammation, stroke, epilepsy, Parkinson's disease, Alzheimer's disease, dementia, and Huntington's disease.
    Normethyl-ZCAN262
  • HY-107716
    Ro 8-4304 hydrochloride
    		Antagonist
    Ro 8-4304 hydrochloride is a potent NMDA receptor antagonist. Ro 8-4304 hydrochloride is a NR2B selective, non-competitive, voltage-independent antagonist.
    Ro 8-4304 hydrochloride
  • HY-172884
    MDAR-IN-1
    		Antagonist
    MDAR IN-1 (Compound 5m) is a brain-penetrant inhibitor of acetylcholinesterase (AChE) and antagonist of the GluN1/GluN2B subtype of NMDAR receptor. MDAR IN-1 effectively inhibits AChE activity, enhances cholinergic neurotransmission, and blocks NMDAR, reducing excitatory neurotoxicity. MDAR IN-1 is promising for research of Alzheimer's disease.
    MDAR-IN-1
  • HY-174899
    AMPA-IN-2
    		Inhibitor
    AMPA-IN-2 is an orally active AMPA inhibitor that can cross the blood-brain barrier. AMPA-IN-2 improves epileptic seizures by inhibiting the intrinsic excitability of neurons and inhibiting the excitability of glutamatergic transmission. AMPA-IN-2 exerts anti-epileptic effects in the pentylenetetrazol (PTZ) model and can be used as a promising candidates with high broad-spectrum anti-epileptic potential.
    AMPA-IN-2
  • HY-P3354
    p3Ysh-3
    p3Ysh-3 is a peptide inhibitor of STEP Phosphatase-GluA2 AMPA receptor interaction with a Ki of 1.09 μM. p3Ysh-3 restores the memory deficits and displays anxiolytic and antidepressant effects in a scopolamine-treated rat model. p3Ysh-3 is a promising lead compound for novel cognitive enhancers and/or behavioral modulators.
    p3Ysh-3
Cat. No. Product Name / Synonyms Application Reactivity
iGluR Isoform Comparison

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