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-16728A
    Rapastinel acetate
    		Modulator
    Rapastinel (GLYX-13) acetate is a potent NMDAR modulator capable of crossing the blood-brain barrier, and it exhibits extremely high affinity for human NMDAR (EC50=0.0017-9.9 nM). Rapastinel acetate enhances ERK signaling and activates the mTOR pathway, thereby upregulating the expression of BDNF and VGF, and inducing significant neuroplastic changes such as enhanced LTP and increased mature dendritic spine density in the hippocampus. Rapastinel acetate moderately elevates the efflux of dopamine, norepinephrine and 5-HT in the prefrontal cortex, and uniquely avoids side effects of traditional antidepressants such as dissociation, addiction or sedation. Rapastinel acetate is applicable to the research of major depressive disorder and hepatocellular carcinoma.
    Rapastinel acetate
  • HY-107606
    UBP301
    		Antagonist
    UBP301 is a potent and selective antagonist of kainate receptor with IC50 and KD of 164 μM and 5.94 μM, respectively. UBP301 has ∼30-fold selectivity of kainate receptor over AMPA receptor. UBP301 is the derivative of willardiine.
    UBP301
  • HY-W415121
    Bupivacaine hydrochloride monohydrate
    		Inhibitor
    Bupivacaine hydrochloride monohydrate is a NMDA receptor inhibitor. Bupivacaine hydrochloride monohydrate can block sodium, L-calcium, and potassium channels. Bupivacaine hydrochloride monohydrate potently blocks SCN5A channels with the IC50 of 69.5 μM. Bupivacaine hydrochloride monohydrate can be used for the research of chronic pain.
    Bupivacaine hydrochloride monohydrate
  • HY-134525
    Ro 8-4304
    		Antagonist
    Ro 8-4304 is a non-competitive, voltage-independent and state-dependent antagonist for NMDA receptor. Ro 8-4304 inhibits 10 μM NMDA-induced currents and 100 μM NMDA-induced currents with IC50s of 2.3 μM and 0.36 μM.
    Ro 8-4304
  • HY-138973A
    Neramexane mesylate
    		Antagonist
    Neramexane mesylate is an α9α10 cholinergic nicotinic receptors and N-methyl-D-aspartate receptors(NMDA) antagonist. Neramexane mesylate can improve moderate to severe tinnitus, and also shows neuroprotective effects.
    Neramexane mesylate
  • HY-155049
    NMDA receptor antagonist 6
    		Antagonist
    NMDA receptor antagonist 6 (compound 13b) is an antagonist of NMDA receptor, targeting to the glycine binding site. NMDA receptor antagonist 6 shows cytoneuroprotective potency, and protects PC12 cells against NMDA-induced injury and cell apoptosis.
    NMDA receptor antagonist 6
  • HY-19434A
    cis-ACPD
    		Agonist
    cis-ACPD is a potent agonist of NMDA receptor, with an IC50 of 3.3 μM. cis-ACPD is also a selective agonist of group II mGluR, with EC50s of 13 μM and 50 μM for mGluR2 and mGluR4, respectively.
    cis-ACPD
  • HY-181828
    SePP
    		Antagonist
    SePP is a blood-brain barrier-permeable NMDAR antagonist and dopamine/norepinephrine reuptake inhibitor, with a Ki of 28.7 nM for rat NMDAR. SePP exerts anticonvulsant effects. SePP can be used in research related to fragile X syndrome.
    SePP
  • HY-146101
    NMDA receptor antagonist 5
    		Antagonist
    NMDA receptor antagonist 5 (Compound 10e) is a potent, brain permeable and non-toxic NMDA receptor antagonist. NMDA receptor antagonist 5 can be used for neurological disorder research.
    NMDA receptor antagonist 5
  • HY-P1594
    Dynorphin A (1-10)
    		Inhibitor
    Dynorphin A (1-10) an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) also blocks NMDA-activated current with an IC50 of 42.0 μM.
    Dynorphin A (1-10)
  • HY-106467
    Caroverine
    		Antagonist
    Caroverine is a potent, competitive and reversible antagonist of NMDA and AMPA glutamate receptor. Caroverine is also an antioxidant and calcium-blocking agent that exhibits vasorelaxant action. Caroverine can be used for the research of inner ear tinnitus.
    Caroverine
  • HY-B0184S1
    Felbamate-d5
    Felbamate-d5 is the deuterium labeled Felbamate. Felbamate (W-554) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA).
    Felbamate-d<sub>5</sub>
  • HY-148708A
    Oleoyl-D-lysine sodium
    		Inhibitor
    Oleoyl-D-lysine sodium is a selective Glycine Transporter-2 (GlyT2) inhibitor based on lipid. Oleoyl-D-lysine sodium reverses neuropathic pain in mice, shows antidrowsiness effect on chronic neuropathic pain. Oleoyl-D-lysine sodium is safe and effective without respiratory depression.
    Oleoyl-D-lysine sodium
  • HY-107694
    (Rac)-Dizocilpine
    		Control
    (Rac)-Dizocilpine ((Rac)-MK-801) is the racemate of Dizocilpine (HY-15084B). Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist.
    (Rac)-Dizocilpine
  • HY-157936
    GluN2B-NMDAR antagonist-2
    		Antagonist
    GluN2B-NMDAR antagonist-2 (compound S-58) is a potent, selective and cross the blood-brain barrier NMDAR-GluN2B antagonist with an IC50 value of 74.01, nM. GluN2B-NMDAR antagonist-2 shows mild cytotoxicity. GluN2B-NMDAR antagonist-2 decreases the cerebral infarction rates and neurologic deficit scores. GluN2B-NMDAR antagonist-2 has the potential for the research of stroke.
    GluN2B-NMDAR antagonist-2
  • HY-N5159
    Ampullosporin A
    Ampullosporin A is a peptaibol-type polypeptide that can be isolated from the fungus Sepedonium ampullosporum HKI-0053, exhibiting neuroleptic-like activity. Ampullosporin A can inhibit hyperactivity induced by NMDA receptor antagonist MK-801 (HY-15084B) and ameliorate social behavior abnormalities caused by subchronic drug treatment. Ampullosporin A alters the activity of glutamate receptors without affecting dopamine D1 and D2 receptors.
    Ampullosporin A
  • HY-101229
    (2R,3S)-Chlorpheg
    (2R,3R)-Chlorpheg is a week antagonist of L-homocysteic acid (L-HCA) induced depolarization.(2R,3R)-Chlorpheg also is a weak N-methyl-D-aspartate (NMDA) antagonist.
    (2R,3S)-Chlorpheg
  • HY-W709349S
    Flupirtine-d6 hydrochloride
    Flupirtine-d6 (D 9998-d6) hydrochloride is the deuterium labeled Flupirtine hydrochloride (HY-W709349). Flupirtine hydrochloride is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine hydrochloride is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine hydrochloride stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine hydrochloride exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine hydrochloride functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine hydrochloride can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis.
    Flupirtine-d<sub>6</sub> hydrochloride
  • HY-P1293
    Conantokin G
    		Antagonist
    Conantokin G, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G has neuroprotective properties.
    Conantokin G
  • HY-184078
    8-F-2-(Me-Pip-Me)-Tryptanthrin
    8-F-2-(Me-Pip-Me)-Tryptanthrin is a tryptanthrin derivative with blood-brain barrier penetration. 8-F-2-(Me-Pip-Me)-Tryptanthrin protects neurons from Aβ-induced apoptosis, inhibits Aβ-induced Tau protein hyperphosphorylation and neuronal synaptic damage, and improves learning and memory abilities in Alzheimer's disease mice. 8-F-2-(Me-Pip-Me)-Tryptanthrin can be used for the research of nervous system diseases, including diseases related to abnormal Tau protein phosphorylation and abnormal PSD-95 function.
    8-F-2-(Me-Pip-Me)-Tryptanthrin
Cat. No. Product Name / Synonyms Application Reactivity
iGluR Isoform Comparison

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