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-125931
    Unifiram
    		Activator 99.68%
    Unifiram (DM232) is a AMPA receptor activator and cognitive enhancer. Unifiram activates the AMPA-mediated neurotransmission system. Unifiram reverses NBQX-induced amnesia in the passive avoidance test in mice. Unifiram reverses the antagonistic effect of kynurenic acid on NMDA-mediated [3H]NA release in rat hippocampal slices. Unifiram enhances excitatory synaptic transmission in the rat hippocampus in vitro. Unifiram can be used in studies related to amnesia and cognitive dysfunction, including age-related memory decline, neurodegenerative diseases such as Alzheimer's disease or Parkinson's disease, multiple sclerosis, schizophrenia, and attention deficit hyperactivity disorder.
    Unifiram
  • HY-B1283
    Mephenesin
    		Antagonist 99.69%
    Mephenesin is an NMDA receptor antagonist. Mephenesin is also a central muscle relaxant with antianxiety, muscle-paralyzing and anticonvulsant effects. Mephenesin acts directly on the skeletal muscle fibres to produce skeletal muscle relaxation. Mephenesin is promising for research of spasticity or painful muscle spasm.
    Mephenesin
  • HY-113416R
    Dehydroepiandrosterone sulfate (Standard)
    		Activator
    Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) (Standard) is the analytical standard of Dehydroepiandrosterone sulfate (HY-113416). 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 (Standard)
  • HY-172419
    Blixeprodil
    		Antagonist
    Blixeprodil (GM-1020) is an orally active, blood-brain barrier-penetrant NMDA receptor inhibitor with a Ki of 3.25 µM in rat cortical tissues. Blixeprodil binds to the MK-801 ion channel site and blocks NMDA receptor-mediated currents in hyperpolarized states in a voltage-dependent manner. Blixeprodil modulates the power of cortical EEG frequency bands, alters spontaneous motor activity, and induces ataxia at high doses. Blixeprodil can be used in the research of depression.
    Blixeprodil
  • HY-100714C
    DL-AP5 sodium
    		Antagonist 99.20%
    DL-AP5 (2-APV) sodium is a competitive NMDA (N-methyl-D-aspartate) receptor antagonist. DL-AP5 sodium shows significantly antinociceptive activity. DL-AP5 sodium specifically blocks on channels in the rabbit retina.
    DL-AP5 sodium
  • HY-160604
    Remacemide
    		Antagonist
    Remacemide (FPL 12924) is an orally active, non-competitive, low-affinity NMDA receptor antagonist. Remacemide shows neuroprotection activity in animal models of hypoxia and ischemic stroke. Remacemide is also an anticonvulsant, and can be used in Parkinson's disease and Huntington's disease research.
    Remacemide
  • 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-15071
    YM90K
    		Antagonist 98.32%
    YM90K is a potent and selective AMPA receptor antagonist with a Ki of 84 nM. YM90K is less potent in inhibiting kainate (Ki of 2.2 μM) and NMDA (Ki of 37 μM) receptors. YM90K has neuroprotective actions.
    YM90K
  • HY-100547
    IEM-1754
    		Inhibitor 98.44%
    IEM-1754, a dicationic adamantane derivative, is a potent blocker of open channels of native ionotropic glutamate receptors including quisqualate-sensitive receptors in insect muscles, NMDAR in cultured rat cortical neurons, and AMPAR in freshly isolated hippocampal cells. IEM-1754 shows anticonvulsant potency in vivo.
    IEM-1754
  • HY-14608S4
    L-Glutamic acid-13C5,15N,d5
    		Agonist 99.9%
    L-Glutamic acid-13C5,15N,d5 is the deuterium, 13C-, and 15-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-<sup>13</sup>C<sub>5</sub>,<sup>15</sup>N,d<sub>5</sub>
  • HY-170410
    EMD-95885
    		Antagonist 98.74%
    EMD-95885 is a selective NR2B-containing NMDA receptors antagonist with an IC50 of 3.9 nM. EMD-95885 does not interact with other sites on the NMDA receptor.
    EMD-95885
  • HY-100797
    (RS)-CPP
    		Antagonist 99.0%
    (RS)-CPP ((±)-CPP) is a potent and selective NMDA antagonist. (RS)-CPP inhibits central neuron responses, and has anticonvulsant activity.
    (RS)-CPP
  • HY-14608S
    L-Glutamic acid-13C
    		Agonist 99.9%
    L-Glutamic acid-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-<sup>13</sup>C
  • HY-139192A
    Brophenexin free base
    		Inhibitor 99.24%
    Brophenexin free base (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. Brophenexin free base shows neuroprotective activity. Brophenexin free base prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. Brophenexin free base protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss.
    Brophenexin free base
  • HY-101216
    Org-26576
    		Modulator 99.81%
    Org-26576 is a AMPA receptor positive allosteric modulator.
    Org-26576
  • HY-150138
    Gavestinel
    		Antagonist 98.74%
    Gavestinel (GV 150526) is a selective and potent the glycine site of the NMDA receptor antagonist. Gavestinel has neuroprotectant effects.
    Gavestinel
  • 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-101620
    MRZ 2-514
    		Antagonist
    MRZ 2-514 is an antagonist of the strychnine-insensitive modulatory site of the NMDA receptor (glycineB), with Ki of 33 μM.
    MRZ 2-514
  • HY-15072
    Zonampanel
    		Antagonist 99.02%
    Zonampanel (YM 872) is a selective antagonist of the glutamate receptor subtype, α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor.
    Zonampanel
  • HY-15086
    Selfotel
    		Antagonist 99.67%
    Selfotel (CGS 19755) is a selective and competitive antagonist at N-methyl-D-aspartate (NMDA)-preferring receptor. CGS 19755 inhibits the binding of [3H]-3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid to NMDA-type receptors with an IC50 of 50 nM.
    Selfotel
Cat. No. Product Name / Synonyms Application Reactivity
iGluR Isoform Comparison

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