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-110175
    CX614
    		Modulator 99.94%
    CX614 is a positive variant modulator of AMPA receptors that enhances excitatory postsynaptic potentials (amplitude and duration) by blocking and slowing the inactivation of responses to glutamate and automatically evokes excitatory postsynaptic currents in neuronal cultures. CX614 can be used in the study of psychiatric disorders such as depression.
    CX614
  • HY-18699
    CIQ
    		Activator 99.75%
    CIQ is a subunit-selective potentiator of NMDA receptors containing the NR2C or NR2D subunit.
    CIQ
  • HY-100785
    gamma-DGG
    		Inhibitor 99.16%
    gamma-DGG is a competitive AMPA receptor blocker.
    gamma-DGG
  • HY-12509
    PEPA
    		Activator 99.53%
    PEPA is an AMPA receptor allosteric potentiator. PEPA shows preferential action of PEPA on the flop form of AMPA receptors. PEPA is a more potent suppressor of desensitization of receptors containing GluR3 and GluR4 as opposed to those containing GluR1. PEPA has antianxiety effects.
    PEPA
  • HY-121964
    cis-Piperidine-2,3-dicarboxylic acid
    		Agonist
    Cis-piperidine-2,3-dicarboxylic acid is a non-specific antagonist of NMDA, AMPA and kainate ionotropic receptors and a partial agonist for NMDA receptors. Cis-piperidine-2,3-dicarboxylic acid can be used in blocking general excitatory synaptic transmissions.
    cis-Piperidine-2,3-dicarboxylic acid
  • HY-B0504S1
    Creatinine-13C
    		Modulator 99.93%
    Creatinine-13C is the 13C-labeled Creatinine. 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>13</sup>C
  • HY-104020A
    Philanthotoxin 74 dihydrochloride
    		Antagonist 99.72%
    Philanthotoxin 74 dihydrochloride (PhTx 74) is an AMPAR antagonist; inhibits GluR3 and GluR1 with IC50s of 263 and 296 nM, respectively.
    Philanthotoxin 74 dihydrochloride
  • HY-101261
    ATPA
    		Agonist 98.90%
    ATPA is a selective glutamate receptor GluR5 activator with EC50s of 0.66, 9.5, 1.4, 23, 32, 18, and 14 μM for GluR5wt, GluR5(S741M), GluR5(S721T), GluR5(S721T, S741M), GluR5(S741A), GluR5(S741L), and GluR5(S741V), respectively.
    ATPA
  • HY-109164
    Zelquistinel
    		Agonist 99.92%
    Zelquistinel (AGN-241751) is the orally active N-methyl-D-aspartate (NMDA) receptor partial agonist used for the research of depression, anxiety and other related psychiatric disorders.
    Zelquistinel
  • HY-117483
    Gly-Pro-Glu
    		Inhibitor 99.77%
    Gly-Pro-Glu is a neuroactive peptide with a potent action on acetylcholine release. Gly-Pro-Glu is the N-terminal tripeptide of insulin-like growth factor-I. Gly-Pro-Glu inhibits glutamate binds to N-methyl-D-aspartate (NMDA) receptor with an IC50 value of 14.7 μM. Gly-Pro-Glu can be used for the research of neuroprotection .
    Gly-Pro-Glu
  • HY-101310
    SYM 2081
    		Agonist 98.0%
    SYM 2081 is a kainate receptor agonist. SYM 2081 is a substrate of EAAT1 (Km of 54 μM). SYM 2081 inhibits EAAT2-mediated glutamate transport (Kb is 3.4 μM in Xenopus oocytes), modulates Apoptotic signaling pathways (increases Bcl-2 and decreases Bax/caspase-3 expression). SYM 2081 exhibits neuroprotective activity. SYM 2081 can be used in the study of hypoxic-ischemic brain damage and inflammatory or neuropathic pain.
    SYM 2081
  • HY-W747599
    Ganglioside GQ1b (bovine) sodium
    		Activator ≥98.0%
    Ganglioside GQ1b (​Tetrasialoganglioside GQ1b) (bovine) sodium is a central and peripheral nervous system ganglioside and an immunostimulator. Ganglioside GQ1b (bovine) sodium modulates NMDA receptor signaling via ERK1/2, PKA, CREB, NR2A, NR2B, and GSK3β, and increases BDNF expression. Ganglioside GQ1b (bovine) sodium reduces Aβ pathology, tau phosphorylation, and APP levels. Ganglioside GQ1b (bovine) sodium can be used for the research of Alzheimer’s disease.
    Ganglioside GQ1b (bovine) sodium
  • HY-141921S
    Dehydroepiandrosterone sulfate sodium-d6
    		Activator 99.61%
    Dehydroepiandrosterone sulfate sodium salt-d6 (DHEA sulfate sodium salt-d6; Prasterone sulfate sodium salt-d6) is the deuterium labeled Dehydroepiandrosterone sulfate sodium salt (HY-B0765). Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium salt has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate sodium salt 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 sodium salt 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 sodium salt may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality.
    Dehydroepiandrosterone sulfate sodium-d<sub>6</sub>
  • HY-100808S
    D-Serine-d3
    		Agonist 99%
    D-Serine-d3 ((R)-Serine-d3) is a deuterium labeled D-Serine (HY-100808). 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.
    D-Serine-d<sub>3</sub>
  • HY-103230
    IEM-1460
    		Inhibitor 98.0%
    IEM-1460 blocks both AMPA and NMDA glutamate receptor with anticonvulsant effect in vivo.
    IEM-1460
  • HY-139048
    Fluoroethylnormemantine
    		Antagonist 98.0%
    Fluoroethylnormemantine, a derivative of Memantine, is an antagonist of the N-methyl-D-aspartate (NMDA) receptor. [18F]-Fluoroethylnormemantine can be used as a positron emission tomography (PET) tracer. Fluoroethylnormemantine exhibits anti-amnesic, neuroprotective, antidepressant-like and fear-attenuating effects.
    Fluoroethylnormemantine
  • HY-W015309S3
    Decanoic acid-d5
    		Inhibitor
    Decanoic acid-d5 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects.
    Decanoic acid-d<sub>5</sub>
  • HY-90003A
    Tianeptine sodium salt
    		Agonist 99.90%
    Tianeptine sodium salt is an atypical antidepressant. Tianeptine sodium salt is a moderate-intensity agonist of the μ-opioid receptor (MOR), and to a lesser extent, is an agonist of the δ-opioid receptor (DOR). Tianeptine sodium salt is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. Tianeptine sodium salt increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine sodium salt exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine sodium salt inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine sodium salt can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects.
    Tianeptine sodium salt
  • HY-14608S1
    L-Glutamic acid-1-13C
    		Agonist 99.85%
    L-Glutamic acid-1-13C 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-1-<sup>13</sup>C
  • HY-16728B
    Rapastinel Trifluoroacetate
    		Modulator 98.0%
    Rapastinel (GLYX-13) Trifluoroacetate 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 Trifluoroacetate 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 Trifluoroacetate 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 Trifluoroacetate is applicable to the research of major depressive disorder and hepatocellular carcinoma.
    Rapastinel Trifluoroacetate
Cat. No. Product Name / Synonyms Application Reactivity
iGluR Isoform Comparison

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