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

iGluR Antagonist

iGluR Antagonists (341):

Cat. No. Product Name Effect Purity
  • HY-100714A
    D-AP5
    Antagonist 99.94%
    D-AP5 (D-APV) is a selective and competitive NMDA receptor antagonist with a Kd of 1.4 μM. D-AP5 (D-APV) inhibits the glutamate binding site of NMDA receptors.
  • HY-15084
    Dizocilpine maleate
    Antagonist 99.99%
    Dizocilpine maleate (MK-801 maleate) is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.
  • HY-N0215
    L-Phenylalanine
    Antagonist 99.98%
    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.
  • HY-15084B
    Dizocilpine
    Antagonist 99.95%
    Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca2+ flux.
  • HY-100806
    Kynurenic acid
    Antagonist 99.93%
    Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.
  • HY-15066
    CNQX
    Antagonist 99.65%
    CNQX (FG9065) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX is a competitive non-NMDA receptor antagonist. CNQX blocks the expression of fear-potentiated startle in rats.
  • HY-15068
    NBQX
    Antagonist 99.82%
    NBQX (FG9202) is a highly selective and competitive AMPA receptor antagonist. NBQX has neuroprotective and anticonvulsant activity.
  • HY-30008
    Cycloleucine
    Antagonist 98.0%
    Cycloleucine is a specific inhibitor of S-adenosyl-methionine mediated methylation. Cycloleucine is antagonist of NMDA receptor associated glycine receptor, with a Ki of 600 μM. Cycloleucine is also a competitive inhibitor of ATP: L-methionine-S-adenosyl transferase in vitro. Cycloleucine has anxiolytic and cytostatic effects.
  • HY-N5134
    5'-Guanylic acid
    Antagonist 99.96%
    5'-Guanylic acid is a purine nucleotide that participates in physiological processes such as energy metabolism, signal transduction, and gene expression regulation. 5'-Guanylic acid regulates the expression of genes related to fatty acid metabolism. 5'-Guanylic acid is the weak agonist for ionotropic glutamate receptors (iGluR), reduces the activity of the glutamatergic system and exhibits neuroprotective effect. 5'-Guanylic acid also causes neuronal cell death at high concentrations.
  • HY-100714
    DL-AP5
    Antagonist 99.70%
    DL-AP5 (2-APV) is a competitive NMDA (N-methyl-D-aspartate) receptor antagonist. DL-AP5 shows significantly antinociceptive activity. DL-AP5 specifically blocks on channels in the rabbit retina.
  • HY-B0591
    Memantine
    Antagonist 99.89%
    Memantine is an orally active, noncompetitive N-methyl-D-aspartate receptor (NMDAR) antagonist. Memantine can be used for the research of moderate-to-severe Alzheimer's disease (AD).
  • HY-N0215S12
    L-Phenylalanine-d5
    Antagonist 99.90%
    L-Phenylalanine-d5 is the deuterium 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.
  • HY-B0122
    Topiramate
    Antagonist 99.76%
    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.
  • HY-B0303
    Diphenhydramine
    Antagonist 99.85%
    Diphenhydramine is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) .
  • HY-15067
    DNQX
    Antagonist 99.67%
    DNQX (FG 9041), a quinoxaline derivative, is a selective, potent competitive non-NMDA glutamate receptor antagonist (IC50s = 0.5, 2 and 40 μM for AMPA, kainate and NMDA receptors, respectively).
  • HY-15068A
    NBQX disodium
    Antagonist 98.96%
    NBQX disodium (FG9202 disodium) is a highly selective and competitive AMPA receptor antagonist. NBQX disodium has neuroprotective and anticonvulsant activity.
  • HY-I0096
    Indole-2-carboxylic acid
    Antagonist 99.86%
    Indole-2-carboxylic acid (I2CA) is a competitive antagonist of the glycine site of the NMDA receptor (Ki=15 μM, 5-fluoro-I2CA) and an inhibitor of HIV-1 integrase. Indole-2-carboxylic acid is selective for the glycine site of the NMDA receptor and blocks the enhancement of NMDA receptor by competitively inhibiting the binding of glycine to the NMDA receptor. Indole-2-carboxylic acid can also inhibit the strand transfer activity of HIV-1 integrase by chelating Mg2+ at the active site of integrase and interacting with the hydrophobic cavity. Indole-2-carboxylic acid can be used in the study of neurological diseases (such as stroke, epilepsy) and HIV-1 infection.
  • HY-17001
    Flupirtine Maleate
    Antagonist 99.97%
    Flupirtine (D 9998) Maleate is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine Maleate is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine Maleate stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine Maleate exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine Maleate functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine Maleate can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis.
  • HY-12882A
    Ifenprodil tartrate
    Antagonist 99.94%
    Ifenprodil (NP-120) tartrate, a cerebral vasodilator, is a noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM). Ifenprodil tartrate is an α1 adrenergic receptor antagonist. Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has reliable inhibitory effects against A/H1N1 strains (EC50 of 6.6 µM). Ifenprodil tartrate has neuroprotective, anticonvulsant and antinociceptive effects. Ifenprodil tartrate can be used for the study of cerebrovascular diseases and peripheral arterial obliterative disease.
  • HY-100834
    5,7-Dichlorokynurenic acid
    Antagonist 99.98%
    5,7-Dichlorokynurenic acid (5,7-DCKA) is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid reduces NMDA-induced neuron injury. 5,7-Dichlorokynurenic acid increases social interaction time, increases open arm exploration time, disinhibits suppressed conflict responding in rodent models. 5,7-Dichlorokynurenic acid exhibits anxiolytic-like activity in rodent models and supports exploration of glycine’s role in NMDA receptor-mediated synaptic transmission.