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-16728
    Rapastinel
    		Modulator 99.78%
    Rapastinel (GLYX-13) 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 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 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 is applicable to the research of major depressive disorder and hepatocellular carcinoma.
    Rapastinel
  • HY-101216
    Org-26576
    		Modulator 99.81%
    Org-26576 is a AMPA receptor positive allosteric modulator.
    Org-26576
  • HY-107498
    GNE-8324
    		Modulator 98.88%
    GNE-8324 is a selective GluN2A positive allosteric modulator. GNE-8324 selectively enhances NMDA receptor (NMDAR)-mediated synaptic responses in inhibitory but not excitatory neurons.
    GNE-8324
  • HY-177873
    AMPA receptor modulator-10
    		Modulator 98.78%
    AMPA receptor modulator-10 (Compound 9a) is an orally active AMPA receptor (AMPAR) positive allosteric modulator. AMPA receptor modulator-10 exhibits potent activity (pEC50 = 5.0) on the GluA2 subtype of AMPAR, significantly enhancing glutamate-induced calcium influx and current responses. AMPA receptor modulator-10 can reverse the memory impairment induced by Scopolamine (HY-N0296) and enhance cognitive function. AMPA receptor modulator-10 can be used for the research of neurological disease, such as schizophrenia.
    AMPA receptor modulator-10
  • HY-P991611
    ART5803
    		Modulator 98.64%
    ART5803 is a humanized IgG1 monoclonal antibody inhibitor targeting NMDAR. ART5803 binds to the N-terminal domain (NTD) of the NMDAR GluN1 subunit (GluN1-NTD) with a high affinity. ART5803 blocks NMDAR internalization induced by pathogenic autoantibodies and restores cell-surface NMDAR expression and functions. ART5803 reverses behavioral abnormalities and NMDAR expression in marmoset disease models. ABT-147 can be used to study anti-NMDAR encephalitis.
    ART5803
  • HY-155810
    DQP-26
    		Modulator 99.08%
    DQP-26 is a potent NMDAR negative allosteric modulator with IC50 values of 0.77 μM and 0.44 μM for GluN2C and GluN2D, respectively. DQP-26 has the potential for NMDAR-associated neurological disease research.
    DQP-26
  • HY-100822
    (R)-(+)-HA-966
    		Modulator 98.44%
    (R)-(+)-HA-966 ((+)-HA-966) is a partial agonist/antagonist of glycine site of the N-methyl-D-aspartate (NMDA) receptor complex. (R)-(+)-HA-966 selectively blocks the activation of the mesolimbic dopamine system by amphetamine. (R)-(+)-HA-966 can cross the blood-brain barrier and has the potential for neuropathic and acute pain.
    (R)-(+)-HA-966
  • HY-136275
    AMPA receptor modulator-2
    		Modulator 98.55%
    AMPA receptor modulator-2 (Example 134) is a AMPA receptor modulator, with a pIC50 of 10.1 for TARPγ8 dependent AMPA receptor. pIC50 = -lgIC50.
    AMPA receptor modulator-2
  • HY-122150
    AMPA receptor modulator-3
    		Modulator 99.57%
    AMPA receptor modulator-3 is an allosteric AMPA receptor modulator (EC50: 4.4 μM). AMPA receptor modulator-3 can be used in the research of mammalian nervous system, such as learning and memory.
    AMPA receptor modulator-3
  • HY-100667
    UBP608
    		Modulator 99.60%
    UBP608 is a potent N-Methyl-D-aspartate receptors (NMDARs) negative allosteric modulator. UBP608 has the potential for the research of neurological disorders.
    UBP608
  • HY-114753
    Neboglamine
    		Modulator
    Neboglamine (CR-2249; XY-2401) is a modulator for N-methyl-D-aspartate (NMDA) receptor. Neboglamine increases the levels of fos-like immunoreactivity (FLI)-positive cells in the prefrontal cortex, nucleus accumbens, and lateral septal nucleus in rat models, .restores NMDA (HY-17551) -mediated neurotransmitter release, and inhibits phencyclidine-induced hyperlocomotion.
    Neboglamine
  • HY-101363
    1-BCP
    		Modulator 99.90%
    1-BCP (Piperonylic acid piperidide) is a centrally active agent that modulates AMPA receptor gated currents. 1-BCP is a memory-enhancing agent.
    1-BCP
  • HY-21297
    3,5-Dihydroxy-2-naphthoic acid
    		Modulator
    3,5-Dihydroxy-2-naphthoic acid is a Naphthoic acid derivative. Naphthoic acid is a NMDA receptor allosteric modulator.
    3,5-Dihydroxy-2-naphthoic acid
  • HY-117734
    PYD-106
    		Modulator 98.13%
    PYD-106 is a stereoselective pyrrolidinone (PYD) positive allosteric modulator for GluN2C-containing NMDA receptors. PYD-106 increases opening frequency and open time of single channel currents activated by maximally effective concentrations of agonist but only has modest effects on glutamate and glycine EC50. PYD-106 selectively enhances the responses of diheteromeric GluN1/GluN2C receptors but not triheteromeric GluN1/GluN2A/GluN2C receptors.
    PYD-106
  • HY-107774
    BMS-986163
    		Modulator
    BMS-986163 is a negative allosteric modulator of GluN2B. The proagent BMS-986163 rapidly converts to its active parent molecule BMS-986169 (Ki=4 nM, IC50=24 nM).
    BMS-986163
  • HY-B0504S5
    Creatinine-15N
    		Modulator
    Creatinine-15N (NSC13123-15N) is the 15N-labeled Creatinine (HY-B0504). Creatinine (NSC13123) is an orally active, blood-brain barrier-permeable modulator of GABAA and NMDA receptors, with activities of antioxidation and metabolic regulation. Creatinine is generated via non-enzymatic conversion of creatine and phosphocreatine in muscle. Creatinine serum levels correlate with muscle mass, glomerular filtration rate, and extrarenal clearance, serving as an evaluation biomarker for renal function, muscle mass, and clinical outcomes, and used for perioperative renal risk assessment. In addition, Creatinine can induce specific Cryptococcus species to produce creatinine deiminase and act as their nitrogen source, while it can be secreted via renal tubules. Creatinine is widely used in research related to various diseases such as neurodegenerative diseases, psychiatric disorders, acute kidney injury, chronic kidney disease, and renal failure.
    Creatinine-<sup>15</sup>N
  • HY-103491
    PF-06462894
    		Modulator
    PF-06462894 is an alkyne-lacking metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator profiled in both rat and nonhuman primates.
    PF-06462894
  • HY-17670
    AMPA receptor modulator-11
    		Modulator
    AMPA receptor modulator-11 (example 210) is a positive allosteric AMPA receptor modulator. AMPA receptor modulator-11 can be used for research on depression, schizophrenia, Alzheimer's disease or attention deficit hyperactivity disorder (ADHD).
    AMPA receptor modulator-11
  • HY-124160
    JNJ-56022486
    		Modulator
    JNJ-56022486 is an orally active and potent negative AMPA receptor modulator (Ki=19 nM) selective for?TARP-γ8. JNJ-56022486 is also a TARP-γ8 receptor antagonist, with blood?brain?barrier (BBB) permeability. JNJ-56022486 can be used for research of Epilepsy.
    JNJ-56022486
  • HY-143390
    NMDA receptor modulator 2
    		Modulator
    NMDA receptor modulator 2 (Compound 1) is a potent NMDA receptor modulator. NMDA receptor modulator 2 can be used for neurological disorder research.
    NMDA receptor modulator 2
Cat. No. Product Name / Synonyms Application Reactivity
iGluR Isoform Comparison

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