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-124569
    NAB-14
    		Antagonist 99.44%
    NAB-14 is a potent, selective, orally active and non-competitive GluN2C/2D antagonists with an IC50 of 580 nM for GluN1/GluN2D. NAB-14 shows >800-fold selective for recombinant GluN2C and GluN2D over GluN2A and GluN2B. NAB-14 can cross the blood-brain-barrier.
    NAB-14
  • HY-12882
    Ifenprodil
    		Antagonist 99.94%
    Ifenprodil (NP-120), a cerebral vasodilator, is a noncompetitive NMDA receptor antagonist. Ifenprodil exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM). Ifenprodil is an α1 adrenergic receptor antagonist. Ifenprodil inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil has reliable inhibitory effects against A/H1N1 strains (EC50 of 6.6 µM). Ifenprodil has neuroprotective, anticonvulsant and antinociceptive effects. Ifenprodil can be used for the study of cerebrovascular diseases and peripheral arterial obliterative disease.
    Ifenprodil
  • HY-108707
    LY3130481
    		Antagonist 99.73%
    LY3130481 is an orally available AMPA receptor antagonist, selectively inhibiting the IC50 value of AMPA/TARP γ-8 at 65 nM. LY3130481 has anticonvulsant, antiepileptic, and pain-relieving effects.
    LY3130481
  • HY-B0369A
    Orphenadrine citrate
    		Antagonist 98.05%
    Orphenadrine citrate is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine citrate relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine citrate is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases.
    Orphenadrine citrate
  • HY-112781
    Pesampator
    		Agonist 99.85%
    Pesampator (PF-04958242) is a potent and highly selective positive allosteric modulator of AMPA receptor (an AMPA potentiator) with an EC50 of 310 nM and a Ki of 170 nM.
    Pesampator
  • HY-18698
    L-701324
    		Antagonist 99.85%
    L-701324 is a potent, orally active NMDA receptor antagonist that antagonizes the activity of the NMDA receptor by blocking its glycine B binding site. L-701324 binds with high affinity to rat brain membranes (IC50=2 nM). L-701324 has antidepressant activity.
    L-701324
  • HY-B0340
    Nefiracetam
    		Activator 99.87%
    Nefiracetam is a cognition-enhancing agent. Nefiracetam is an activator of nAChR, N-methyl-D-aspartate receptor (NMDAR), mGluR5, PKC, gamma-aminobutyric acid (GABA), and N/L-type Ca2+ channels. Nefiracetam promotes neuroplasticity and enhances neuroprotection. Nefiracetam can be used in Alzheimer's disease, epilepsy, and cerebral ischemia research.
    Nefiracetam
  • HY-139897
    CX 717
    		Agonist 99.95%
    CX 717 is a positive allosteric modulator of AMPA receptor. Antidepressant-like effect. CX 717 can be used for the research of adult attention deficit hyperactivity disorder (ADHD).
    CX 717
  • HY-N0215S10
    L-Phenylalanine-13C9
    		Antagonist 98.09%
    L-Phenylalanine-13C9 is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals.
    L-Phenylalanine-<sup>13</sup>C<sub>9</sub>
  • HY-Y0966S2
    Glycine-2-13C
    		99.78%
    Glycine-2-13C is the 13C-labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
    Glycine-2-<sup>13</sup>C
  • HY-107601
    UBP316
    		Antagonist 99.95%
    UBP316 (ACET) is a highly potent and selective kainate receptor GluK1 (GluR5) antagonist, with a Kb value of 1.4 nM. UBP316 is effective at blocking the depression of both field excitatory postsynaptic potentials (fEPSPs) and monosynaptically-evoked GABAergic transmission induced by ATPA, a GluK1 selective agonist.
    UBP316
  • HY-B1487
    Procyclidine hydrochloride
    		Antagonist 99.55%
    Procyclidine (Tricyclamol, (±)-Procyclidine) hydrochloride , an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine hydrochloride can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy.
    Procyclidine hydrochloride
  • HY-76228
    1H-pyrazole
    		Modulator 99.78%
    1H-pyrazole (Pyrazole) is a five-membered heterocyclic compound, and its derivatives are orally effective antimalarial and antileishmanial agents with the potential to modulate targets such as alcohol dehydrogenase and NMDA receptors. 1H-pyrazole derivatives exhibit inhibitory effects on Plasmodium berghei in infected mice and on promastigotes of Leishmania aethiopica, respectively. 1H-pyrazole can be used in research related to malaria and leishmaniasis.
    1H-pyrazole
  • HY-138903
    L-Homocysteic acid
    		Agonist 98.0%
    L-Homocysteic acid (L-HCA) is an endogenous excitatory amino acid that acts as a NMDA receptor agonist (EC50: 14 μM). L-Homocysteic acid is neurotoxic, and can be used in the research of neurological disorders.
    L-Homocysteic acid
  • HY-P1594A
    Dynorphin A (1-10) TFA
    		Inhibitor 98.64%
    Dynorphin A (1-10) (TFA), an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) (TFA) also blocks NMDA-activated current with an IC50 of 42.0 μM.
    Dynorphin A (1-10) TFA
  • HY-Y0966S
    Glycine-15N
    		99.84%
    Glycine-15N is the 15N-labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
    Glycine-<sup>15</sup>N
  • HY-139580
    Plazinemdor
    		Agonist
    Plazinemdor (CAD-9303) is a positive allosteric modulator of N-methyl-D-aspartate (NMDA) receptors, which is used in the research of neurological diseases.
    Plazinemdor
  • HY-139142B
    Simufilam hydrochloride
    		Activator 99.85%
    Simufilam hydrochloride (PTI-125 hydrochloride) is an orally active FLNA modulator. Simufilam hydrochloride restores NMDAR signaling and Arc expression. Simufilam hydrochloride inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, improves insulin sensitivity, reduces Aβ42-induced neuroinflammation and tau protein hyperphosphorylation. Simufilam hydrochloride can be used for research of Alzheimer's disease.
    Simufilam hydrochloride
  • HY-90003
    Tianeptine
    		Agonist 99.84%
    Tianeptine is an atypical antidepressant. Tianeptine 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 is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. tianeptine increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects.
    Tianeptine
  • HY-107701
    CGP 78608 hydrochloride
    		Antagonist 99.56%
    CGP 78608 hydrochloride is a highly potent and selective antagonist at the glycine-binding site of the NMDA receptor, with an IC50 of 6 nM. CGP 78608 hydrochloride acts as a potentiator of GluN1/GluN3A-mediated glycine currents, with an estimated EC50 in the low nM range (26.3 nM). Anticonvulsant activity.
    CGP 78608 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
iGluR Isoform Comparison

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