Home Neuronal Signaling iGluR

iGluR Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S4721 L-Glutamic acid monosodium salt L-Glutamic acid monosodium salt is the sodium salt of glutamic acid, found naturally in tomatoes, cheese and other foods. This compound acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). It shows a direct activating effect on the release of DA from dopaminergic terminals.
Heliyon, 2024, 10(1):e23945
Acta Biomater, 2022, 152:255-272
S2251 (-)-Huperzine A (HupA) (-)-Huperzine A is a potent, highly specific and reversible inhibitor of acetylcholinesterase (AChE) with Ki of 7 nM, exhibiting 200-fold more selectivity for G4 AChE over G1 AChE. Also acts as an NMDA receptor antagonist. Phase 4.
Acta Pharmacol Sin, 2019, 10.1038/s41401-018-0206-4
S6906 Capric acid Capric acid (DA, Decanoic acid, Decylic acid), a component of medium-chain triclycerides occurring naturally in coconut oil and palm kernel oil, contributes to seizure control through direct AMPA receptor inhibition. This compound is also a modulating ligand for PPARs. Due to its specific melting range the product may be solid, liquid, a solidified melt or a supercooled melt.
Pharmaceuticals (Basel), 2023, 16(5)692
S5032 Mephenesin Mephenesin (Decontractyl, Cresoxydiol, Memphenesin, Mephedan) is centrally acting muscle relaxant, a topical analgesic and may be an NMDA receptor antagonist.
Cell Rep Methods, 2023, 3(10):100599
S1998 D-Cycloserine D-cycloserine (RO-1-9213) is an analog of the amino acid D-alanine, used as an antibiotic in the treatment of tuberculosis.
S1281 Aniracetam Aniracetam (RO 13-5057) is a nootropics and neuroprotective drug.
S3624 Quinolinic acid Quinolinic Acid (pyridine-2,3-dicarboxylic acid, QUIN), a neuroactive metabolite of the kynurenine pathway, is an agonist of N-methyl-D-aspartate (NMDA) receptor.
S0509 NMDAR antagonist 1 NMDAR antagonist 1 is a potent and orally bioavailable NR2B-selective antagonist of NMDAR. It has neuroprotective activity.
S5129 D-Aspartic acid D-Aspartic acid (D-Asp, Aminosuccinic acid, asparagic acid, asparaginic acid) is an endogenous amino acid occurring in several tissues and cells of both invertebrates and vertebrates. It can regulate testosterone synthesis and may act on a stimulatory receptor (NMDA).
E1259 DNQX DNQX is an AMPA receptor antagonist that prevents excess calcium influx via voltage-gated calcium channels.
E1246 D-AP5 D-AP5 (D-APV; D-2-Amino-5-phosphonovaleric acid) is a selective and competitive NMDA receptor antagonist that inhibits the glutamate binding site of NMDA receptors.
E0484 CNQX CNQX (6-cyano-7-nitroquinoxaline-2,3-dione) is an AMPA and kainate receptor antagonist with IC50 values are 0.3 μM and 1.5 μM for AMPA and kainate receptors, respectively. This compound is also an antagonist at the glycine modulatory site on the NMDA receptor complex (IC50 = 25 μM). It shows neuroprotective effects in models of ischemia and inhibits seizure-like activity in hippocampal neurons.
S4957 Linalool Linalool (Phantol), a monoterpene compound commonly found as major component of essential oils of several aromatic species, is a competitive antagonist of NMDA receptors.
S3070 Piracetam Piracetam (UCB 6215) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.
S6804 CX546 CX546, a prototypical ampakine agent, is a selective positive AMPA receptor modulator.
S4745 L-Phenylalanine L-Phenylalanine is an essential amino acid and a competitive antagonist against NMDAR glycine- and glutamate-binding sites with a Kb of 573 μM. It is widely used in food flavor and pharmaceutical production.
S6907 Rapastinel (GLYX-13) Rapastinel (GLYX-13, BV-102, TPPT-amide) is a partial agonist of N-methyl-D-aspartate receptor (NMDAR) that targets a glycine site, and it has long-lasting antidepressant effects.
S6224 (R)-Serine (R)-Serine is the R-enantiomer of serine, which is used in the biosynthesis of proteins. This compound acts as obligatory coagonist at the glycine site associated with the N-methyl-D-aspartate subtype of glutamate receptors (NMDAR) and has a cardinal modulatory role in major NMDAR-dependent processes including NMDAR-mediated neurotransmission, neurotoxicity, synaptic plasticity, and cell migration.
E1050 PEAQX PEAQX (NVP-AAM077) is an effective and orally available human NMDA antagonist, which shows preference in excess of 100-fold for hNMDA 1A/2A (IC50=of 270 nM) over hNMDA 1A/2B receptors (IC50=29,600 nM).
S5669 Isoxsuprine hydrochloride Isoxsuprine hydrochloride is a beta-adrenergic agonist with vasodilator activity.
S5664 Orphenadrine Hydrochloride Orphenadrine Hydrochloride is an uncompetitive NMDAR antagonist, H1 receptor antagonist and nonselective mAChR antagonist with muscle relaxant activity.
S9686 NBQX (FG9202) NBQX (FG9202, NNC 079202) is a highly selective and competitive antagonist of AMPA receptor (AMPAR) with anti-epileptic effect.
S6803 1-BCP 1-BCP (Piperonylic acid piperidide) is a memory-enhancing agent that enhances AMPA-induced currents.
S4280 Meclofenoxate (Centrophenoxine) HCl Meclofenoxate (Centrophenoxine) HCl is an anti-aging drug used to treat the symptoms of senile dementia and Alzheimer's disease, and also inhibits the activity of cholinephosphotransferase.
E5887New Osavampator Osavampator (TAK-653, NBI-1065845) is a positive allosteric modulator (PAM) of AMPA receptors. It enhances glutamate-induced calcium influx in CHO cells expressing human AMPA receptors with an EC50 of 3.3 µM and potentiates AMPA receptor-mediated currents in rat primary hippocampal neurons with an EC50 of 4.4 µM.