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-183200
    NMDA receptor antagonist 10
    		Antagonist
    NMDA receptor antagonist 10 is a NMDA receptor antagonist with an IC50 of 28 μM. NMDA receptor antagonist 10 inhibits glycine action at the NMDA receptor glycine site. NMDA receptor antagonist 10 can be used for research on neurological diseases.
    NMDA receptor antagonist 10
  • HY-133732
    Alaproclate hydrochloride
    		Antagonist
    Alaproclate (GEA 654) hydrochloride is a selective and orally active serotonin re-uptake inhibitor (SSRI). Alaproclate hydrochloride also acts as a potent, reversible and noncompetitive antagonist of the NMDA receptor coupled ion flow.
    Alaproclate hydrochloride
  • HY-W882667
    Pregn-5-en-3β-ol
    Pregn-5-en-3β-ol, a steroid compound, when formulated as the biscarboxylic acid hemiesters along with androst-5-en-3β-ol, serves as a potent positive allosteric modulator of NMDA (N-methyl-D-aspartate) receptors, making it applicable for research into psychiatric disorders.
    Pregn-5-en-3β-ol
  • HY-161665
    BDZ-P7
    		Inhibitor
    BDZ-P7 inhibits AMPA receptor GluA2, GluA1/2, GluA2/3, and GluA1 subunit with IC50s of 3.03 μM, 3.14 μM, 3.19 μM, 3.2 μM. BDZ-P7 has neuroprotective effect and reinstates locomotor abilities in a mouse model of Parkinson’s disease.
    BDZ-P7
  • HY-144224S
    Tianeptine-d6 (hydrochloride)
    		Agonist
    Tianeptine-d6 hydrochloride is the deuterium labeled Tianeptine hydrochloride. Tianeptine hydrochloride is an atypical antidepressant. Tianeptine hydrochloride 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 hydrochloride is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. Tianeptine hydrochloride increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine hydrochloride exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine hydrochloride inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine hydrochloride can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects.
    Tianeptine-d<sub>6</sub> (hydrochloride)
  • HY-19225
    Ensaculin
    		Antagonist
    Ensaculin is an NMDA receptor channel blocker. Ensaculin has neuroprotective effects in NMDA toxicity models and promotes neuronal growth in primary cultures of rat brain cells. Ensaculin has the potential to be developed as an anti-dementia drug that acts on various neurotransmitter systems.
    Ensaculin
  • HY-108011R
    Naftazone (Standard)
    		Inhibitor
    Naftazone (Standard) is the analytical standard of Naftazone. This product is intended for research and analytical applications. Naftazone is a naphthoquinone derivative, it can be used for the research of venous insufciency. Naftazone protects blood vessels, increases venous tonicity and capillary resistance, and improves lymphatic and venous circulation.
    Naftazone (Standard)
  • HY-138110R
    Toladryl (Standard)
    Toladryl (Standard) is the analytical standard of Toladryl. This product is intended for research and analytical applications. Toladryl is a derivative of Diphenhydramine (HY-B0303), capable of penetrating the blood-brain barrier and possessing oral activity, as well as antihistamine and anticholinergic activities. The anticholinergic activity of Toladryl is approximately one-tenth that of Diphenhydramine (HY-B0303), and its protective effect against lethal doses of histamine in guinea pigs is 2 to 4 times that of Diphenhydramine (HY-B0303). The side effects of Toladryl are fewer and milder than those of Diphenhydramine (HY-B0303), but at higher doses, it may cause central nervous system symptoms such as insomnia, agitation, and disorientation. Toladryl can be used for research in allergic diseases.
    Toladryl (Standard)
  • HY-120020
    LY-395153
    LY-395153 is an AMPA receptor enhancer with the activity of binding to AMPA receptors. LY-395153 can bind to natural and recombinant AMPA receptors, and its binding is affected by AMPA receptor agonists and can be competitively or non-competitively inhibited by some compounds. It is a useful probe for marking unique regulatory sites of AMPA receptors.
    LY-395153
  • HY-182068
    NFI23
    		Inhibitor
    NFI23 is a GluN2B-NMDAR inhibitor with an IC50 of 1.31 μM and a Ki of 5.98 nM against GluN2B-NMDAR. NFI23 can cross the blood-brain barrier. NFI23 binds to the ifenprodil binding site of GluN2B-NMDAR, reduces NMDA-induced Ca2+ influx and reactive oxygen species (ROS) production, maintains mitochondrial membrane potential, inhibits neuronal apoptosis, and restores the expression of p-ERK1/2. NFI23 exerts neuroprotective effects against NMDA-induced cytotoxicity and in the rat middle cerebral artery occlusion (MCAO) model. NFI23 can be used for the research of ischemic stroke.
    NFI23
  • HY-W415121R
    Bupivacaine hydrochloride monohydrate (Standard)
    		Inhibitor
    Bupivacaine (hydrochloride monohydrate) (Standard) is the analytical standard of Bupivacaine (hydrochloride monohydrate). This product is intended for research and analytical applications. Bupivacaine hydrochloride monohydrate is a NMDA receptor inhibitor. Bupivacaine hydrochloride monohydrate can block sodium, L-calcium, and potassium channels. Bupivacaine hydrochloride monohydrate potently blocks SCN5A channels with the IC50 of 69.5 μM. Bupivacaine hydrochloride monohydrate can be used for the research of chronic pain.
    Bupivacaine hydrochloride monohydrate (Standard)
  • HY-117467
    BMT-108908
    BMT-108908 is a negative allosteric modulator with selective activity on the NR2B subtype of the NMDA receptor. BMT-108908 has been shown to damage cognition in research, affecting cognitive functions in multiple areas. BMT-108908 failed to show a significant impact on the γ wave power of the EEG in the experiment, but it had a significant inhibitory and enhancement effect on the β wave and δ wave power.
    BMT-108908
  • HY-154798
    AMPA receptor modulator-5
    		Modulator
    AMPA receptor modulator-5 (Example 217) is an AMPA receptor modulator. AMPA receptor modulator-5 can be used for research of neurological disease.
    AMPA receptor modulator-5
  • HY-126123
    NR2B-selective NMDA receptor antagonist 1
    		Inhibitor
    NR2B-selective NMDA receptor antagonist 1 (compound 29) is a potent antagonist of NR1/NR2B receptors, with IC50s of 0.05 μM, 0.73 μM, 2.4 μM to NR1/NR2B NMDA receptor, hERG, α1-AdR, respectivity. NR2B-selective NMDA receptor antagonist 1 exhibites efficient permeability across the blood–brain barrier.
    NR2B-selective NMDA receptor antagonist 1
  • HY-105403
    Besonprodil
    		Antagonist
    Besonprodil (CI-1041) is a potent NMDA antagonist.
    Besonprodil
  • HY-148828C
    LSP-GR3 sodium scrambled negative control
    		Inhibitor
    LSP-GR3 sodium scrambled negative control is the sequence scrambled negative control of LSP-GR3 sodium.
    LSP-GR3 sodium scrambled negative control
  • HY-126939
    MN-05
    		Inhibitor
    MN-05 is a dual neuroprotective and vasodilatory NMDA receptor inhibitor.MN-05 blocks calcium influx, reduces free radical production, and maintains mitochondrial membrane potential in cortical neurons exposed to glutamate.MN-05 dilates aortic rings against phenylephrine-induced contraction.MN-05 protects neurons against glutamate-induced injury in vitro.MN-05 can be used for the research of neurodegenerative diseases.
    MN-05
  • HY-100781
    D-AP4
    		Antagonist
    D-AP4 (D-APB; D-2-Amino-4-phosphonobutyric acid), a phosphono analogue of glutamate, is an NMDA broad spectrum excitatory amino acid receptor antagonist. D-AP4 also is an agonist for a quisqualate-sensitized AP6 site in hippocampus. D-AP4 inhibits AMPA receptor-stimulated 57Co2+ influx in cultured cerebellar granule cells (IC50 ≥ 100 μM).
    D-AP4
  • HY-Y0966S11
    Glycine-13C2,15N,d2
    Glycine-13C2,15N,d2 is the deuterium, 13C and 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>13</sup>C<sub>2</sub>,<sup>15</sup>N,d<sub>2</sub>
  • HY-178251S
    L-Phenylalanine-d1
    L-Phenylalanine-d is the deuterium labeled L-Phenylalanine (HY-N0215). 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 Ca2+ 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-d<sub>1</sub>
Cat. No. Product Name / Synonyms Application Reactivity
iGluR Isoform Comparison

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