1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
    Neuronal Signaling
  3. iGluR

iGluR

Ionotropic glutamate receptors

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N2311R
    Ibotenic acid (Standard)
    Agonist
    Sulfiram (Standard) is the analytical standard of Sulfiram. This product is intended for research and analytical applications. Sulfiram, an ectoparasiticide, is a agent applied topically to treat scabies.
    Ibotenic acid (Standard)
  • HY-B0303R
    Diphenhydramine (Standard)
    Antagonist
    Diphenhydramine (Standard) is the analytical standard of Diphenhydramine. This product is intended for research and analytical applications. Diphenhydramine is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) .
    Diphenhydramine (Standard)
  • HY-100814
    (R)-CPP
    Antagonist 98.99%
    (R)-CPP is a highly potent NMDA receptor antagonist.
    (R)-CPP
  • HY-B0122R
    Topiramate (Standard)
    Antagonist
    Topiramate (Standard) is the analytical standard of Topiramate. This product is intended for research and analytical applications. Topiramate (McN 4853) is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase.
    Topiramate (Standard)
  • 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-108337
    GNE-0723
    Agonist 99.91%
    GNE-0723 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 21 nM for GluN2A, 7.4 and 6.2 μM for GluN2C and GluN2D, respectively.
    GNE-0723
  • HY-111500A
    NMDAR antagonist 1
    Antagonist 99.02%
    NMDAR antagonist 1 is a potent and orally bioavailable NR2B-selective NMDAR antagonist.
    NMDAR antagonist 1
  • HY-B0030R
    D-Cycloserine (Standard)
    Agonist
    D-Cycloserine (Standard) is the analytical standard of D-Cycloserine. This product is intended for research and analytical applications. D-Cycloserine is an antibiotic which targets sequential bacterial cell wall peptidoglycan biosynthesis enzymes. D-Cycloserine is a partial NMDA agonist that can improve cognitive functions. D-Cycloserine can be used for multidrug-resistant tuberculosis research.
    D-Cycloserine (Standard)
  • 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-108235B
    (Rac)-Lanicemine
    Antagonist 99.63%
    (Rac)-Lanicemine ((Rac)-AZD6765) is the racemate of Lanicemine. Lanicemine (AZD6765) is a low-trapping NMDA channel blocker (Ki of 0.56-2.1 μM for NMDA receptor; IC50s of 4-7 μM and 6.4 μM in CHO and Xenopus oocyte cells, respectively). Antidepressant effects.
    (Rac)-Lanicemine
  • HY-113416AS
    Dehydroepiandrosterone sulfate-d6 sodium dihydrate
    Activator 99.9%
    Dehydroepiandrosterone sulfate sodium dihydrate-d6 sodium dihydrate is the deuterium labeled Dehydroepiandrosterone sulfate sodium dihydrate. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium dihydrate is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium dihydrate has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate sodium dihydrate 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 dihydrate 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 dihydrate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality.
    Dehydroepiandrosterone sulfate-d<sub>6</sub> sodium dihydrate
  • HY-N6065
    Praeruptorin A
    Inhibitor 99.57%
    Praeruptorin A ((+)-Praeruptorin A) is an orally active isomer of (±)-Praeruptorin A (HY-N0081). Praeruptorin A also acts as a Calcium channel blocker. Praeruptorin A can be isolated from Peucedanum. Praeruptorin A serves as a substrate for CYP3A4. Praeruptorin A downregulates NMDA receptors containing GluN2B and inhibits neuronal Apoptosis. Praeruptorin A mediates vasodilation, inhibits vascular hypertrophy and reduces blood pressure. Praeruptorin A can be used in research related to neurological diseases, myocardial ischemia, heart failure, exertional angina, renovascular hypertension and spontaneous hypertension.
    Praeruptorin A
  • HY-B1752
    Quinpirole
    Activator 98.95%
    Quinpirole (LY 171555; (-)-LY 141865) is a D2/D3 dopamine receptor agonist and a CaV1.3 calcium channel modulator. Quinpirole normalizes dendritic spine density in dopamine-depleted striatum, upregulates the protein expression of BCL2 and GluR2, downregulates the protein expression of BAX, and delays the onset of seizures. Quinpirole enhances learning and memory, inhibits neuronal apoptosis (apoptosis), and induces anxiety-like, stereotyped, and compulsive behaviors. Quinpirole disrupts prepulse inhibition in rhesus monkeys, enhances the activity of paraventricular thalamic neurons to promote recovery from Isoflurane anesthesia, and alters the composition of the gut microbiota in rats. Quinpirole can be used in research related to dyskinesia, pain, epilepsy, and neurological disorders including anxiety disorder, obsessive-compulsive disorder, and schizophrenia.
    Quinpirole
  • 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-19168
    Perzinfotel
    Inhibitor 99.43%
    Perzinfotel (EAA-090) is a potent, selective, and competitive NMDA receptor antagonist with neuroprotective effects. Perzinfotel (EAA-090) shows high affinity (IC50=30 nM) for the glutamate site.
    Perzinfotel
  • HY-110097
    Aptiganel hydrochloride
    Antagonist 99.89%
    Aptiganel hydrochloride (Cerestat) is a non-competitive NMDA receptor antagonist with neuroprotective effect.
    Aptiganel hydrochloride
  • HY-164795
    SBI-810
    Inhibitor 98.25%
    SBI-810 is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 is applicable to research related to multiple pain disorders.
    SBI-810
  • HY-106408
    Nelonemdaz
    Antagonist 99.84%
    Nelonemdaz (Salfaprodil free base) is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA). Nelonemdaz is also a free radical scavenger. Nelonemdaz has excellent neuroprotection against NMDA- and free radical-induced cell death.
    Nelonemdaz
  • HY-172997
    GluN1/3A-IN-1
    Inhibitor 98.99%
    GluN1/3A-IN-1 (Compound GM-10) is a GluN1/GluN3A NMDA receptor inhibitor. GluN1/3A-IN-1 exhibits potent inhibitory activity against GluN1/GluN3A (IC50: 0.98 µM). GluN1/3A-IN-1 exerts its inhibitory effect by targeting the pre-M1 region and forming hydrogen bond interactions with key residues. GluN1/3A-IN-1 can be used to study GluN1/GluN3A-related neurological diseases.
    GluN1/3A-IN-1
Cat. No. Product Name / Synonyms Application Reactivity

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