2. Signalwege
  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
Art. -Nr. Produktname Wirkung Reinheit Chemical Structure
  • HY-111751
    JNJ-61432059
    		Modulator 99.18%
    JNJ-61432059 is a blood-brain barrier-permeable, orally active TARP γ-8-associated AMPAR modulator with anticonvulsant activity. JNJ-61432059 negatively regulates GluA1 and positively modulates GluA2-containing AMPARs. JNJ-61432059 exerts potent protective effects in rodent epilepsy models. JNJ-61432059 is applicable for epilepsy-related research.
    JNJ-61432059
  • HY-139142
    Simufilam
    		Activator 99.78%
    Simufilam (PTI-125) is an orally active FLNA modulator. Simufilam restores NMDAR signaling and Arc expression. Simufilam inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, improves insulin sensitivity, reduces Aβ42-induced neuroinflammation and tau protein hyperphosphorylation. Simufilam can be used for research of Alzheimer's disease.
    Simufilam
  • HY-16713A
    (S)-(-)-5-Fluorowillardiine (hydrochloride)
    		Agonist 99.03%
    (S)-(-)-5-Fluorowillardiine ((5S)-Fluorowillardiine; (S)-5-Fluorowillardiine) hydrochloride is a potent, highly selective non-NMDA ionotropic glutamate receptor (iGluR, AMPA/Kainate receptor) agonist. (S)-(-)-5-Fluorowillardiine hydrochloride activates high-affinity AMPA-preferring receptors (EC50 = 0.70 μM) and low-affinity kainate-preferring receptors (EC50 = 170 μM), thereby inducing biphasic dose-dependent neurotoxicity/excitotoxicity. (S)-(-)-5-Fluorowillardiine hydrochloride is applicable to research related to schizophrenia, temporal lobe epilepsy, and bipolar disorder.
    (S)-(-)-5-Fluorowillardiine (hydrochloride)
  • HY-B0405S
    Bupivacaine-d9
    		99.04%
    Bupivacaine-d99 is a deuterium labeled Bupivacaine. Bupivacaine is a NMDA receptor inhibitor.Bupivacaine can block sodium, L-calcium, and potassium channels.Bupivacaine potently blocks SCN5A channels with the IC50 of 69.5 μM. Bupivacaine can be used for the research of chronic pain.
    Bupivacaine-d<sub>9</sub>
  • HY-15703
    QNZ46
    		Antagonist 99.46%
    QNZ46 is a highly selective noncompetitive NMDA receptor antagonist targeting GluN2C/D (IC50=3.9 μM), GluN1/GluN2C (IC50=7.1 μM), and GluN1/GluN2D (IC50=182 μM) subunits. QNZ46 inhibits glutamate-mediated calcium influx, thereby blocking excitotoxicity. QNZ46 is membrane permeable and can cross the blood-brain barrier, where it inhibits myelin damage and axonal degeneration.
    QNZ46
  • HY-16502
    Crocetin disodium
    		Antagonist 99.30%
    Crocetin (Transcrocetin) disodium, extracted from saffron (Crocus sativus L.), acts as an NMDA receptor antagonist with high affinity.
    Crocetin disodium
  • HY-17388
    (±)-Huperzine A
    		Antagonist 98.73%
    (±)-Huperzine A is the racemate of (-)-Huperzine A (HY-17387). (-)-Huperzine A is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease.
    (±)-Huperzine A
  • HY-175443
    AMPA-IN-3
    		Modulator 99.94%
    AMPA-IN-3 is an AMPA receptor inhibitor. AMPA-IN-3 inhibits TARP J2-dependent AMPA receptor activity with a pIC50 value of 10.7. A AMPA-IN-3 can be used for the research of neurological disease.
    AMPA-IN-3
  • HY-107706
    Co 101244 hydrochloride
    		Antagonist 99.87%
    Co 101244 (PD 174494) hydrochloride is a NR2B-containing NMDA receptor antagonist.
    Co 101244 hydrochloride
  • HY-P1195
    PDZ1 Domain inhibitor peptide
    		99.21%
    PDZ1 Domain inhibitor peptide, a cyclic peptide, incorporates a β-Ala lactam side chain linker and targets the PDZ1 domains of the postsynaptic density protein 95 (PSD-95). PDZ1 Domain inhibitor peptide disrupts the GluR6/PSD-95 interaction and is very efficient in competing against the C terminus of GluR6 for the PDZ1 domain.
    PDZ1 Domain inhibitor peptide
  • HY-14608S6
    L-Glutamic acid-5-13C
    		Agonist 99.6%
    L-Glutamic acid-5-13C is the 13C-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-5-<sup>13</sup>C
  • HY-12508
    CMPDA
    		Agonist 99.31%
    CMPDA is a positive allosteric modulator of AMPA receptors with EC50s of 45.
    CMPDA
  • HY-10936
    S 18986
    		Agonist 99.90%
    S 18986 is a selective, orally active, brain penetrant positive allosteric modulator of AMPA-type receptors. S 18986 shows cognitive enhancing properties in rodents. S 18986 activates the release of noradrenaline and acetylcholine in rat hippocampus and enhances rat memory in object-recognition tests.
    S 18986
  • HY-171844
    CX1739
    		Activator 99.9%
    CX1739 is an orally active, blood-brain barrier permeable, low-efficacy AMPA-glutamate receptor (AMPAR) potentiator. CX1739 enhances excitatory neurotransmission by potentiating glutamate-induced excitatory currents and promoting in vivo long-term potentiation. CX1739 eliminates amphetamine-induced locomotor activity, reverses opioid-, pentobarbital- and ethanol-induced respiratory depression, and exerts pro-cognitive effects in animals. CX1739 impairs motor function recovery and increases the risk of post-injury complications. CX1739 can be used in research related to attention-deficit/hyperactivity disorder, dementia, respiratory depression and spinal cord injury.
    CX1739
  • HY-129692
    Withanone
    		Inhibitor
    Withanone is an active ingredient from the roots of Withania somnifera and a GRP75 inhibitor. Withanone has multifunctional neuroprotective effects in alleviating cognitive dysfunction. In neuron-like cells, Withanone can inhibit NMDA-induced excitotoxicity. Withanone can inhibit white adipose tissue browning by blocking the formation of the GRP75-ANT2-UCP1 complex, thereby alleviating cancer-related cachexia. Withanone can be used in the research of tumors and nervous system diseases.
    Withanone
  • HY-P1523
    Leptin (22-56), human
    		99.90%
    Leptin (22-56), human is the fragment of leptin, mediated via several isoforms of receptors (Ob-Rs).
    Leptin (22-56), human
  • HY-148939
    MPX-004
    		Antagonist 99.58%
    MPX-004 is a potent GluN2A antagonist. MPX-004 inhibits GluN2A-containing NMDA receptors expressed in HEK cells with an IC50 of 79 nM. MPX-004 has no inhibitory effect on GluN2B or GluN2D receptor-mediated responses. MPX-004 has the potential for neuropsychiatric and developmental disorders research.
    MPX-004
  • HY-135741
    NYX-2925
    		Modulator 98.98%
    NYX-2925 is an orally active NMDAR modulator. NYX-2925 restores levels of activated Src and Src phosphorylation sites on GluN2A and GluN2B in the mPFC. NYX-2925 shows no effect on CAMKII, and any addictive or sedative/ataxic side effects. NYX-2925 can be used for research of a variety of NMDA receptor-mediated central nervous system disorders.
    NYX-2925
  • HY-18663
    CP-465022
    		Antagonist 98.24%
    CP-465022 is a potent, and selective noncompetitive AMPA receptor antagonist with anticonvulsant activity. CP-465022 is against Kainate-induced response with an IC50 of 25 nM in rat cortical neurons. CP-465022 provides a new tool to investigate the role of AMPA receptors in physiological and pathophysiological processes.
    CP-465022
  • HY-155811
    DQP-997-74
    		Inhibitor 99.85%
    DQP-997-74 (compound 2i) is a selective negative allosteric modulator of N-methyl-d-aspartate receptor (NMDAR), specifically targeting GluN2C/D (IC50: 0.069 μM and 0.035 μM), with blood-brain barrier penetrability. Where DQP refers to dihydroquinoline-pyrazoline. DQP-997-74 acts synergistically with the agonist glutamate to exhibit time-dependent enhanced potency in inhibiting hypersynchronous activity driven by high-frequency excitatory synaptic transmission. DQP-997-74 reduces the number of epileptogenesis in a murine model of tuberous sclerosis complex (TSC)-induced epilepsy. DQP-997-74 can be used for research on NMDAR-related neurological diseases.
    DQP-997-74
Art. -Nr. Produktname / Synonyms Application Reactivity
iGluR Isoform Comparison

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