iGluR Inhibitor

Evans Blue (Direct Blue 53) is a potent inhibitor of L-glutamate uptake via the membrane bound excitatory amino acid transporter (EAAT). Evans Blue is a L-glutamate and kainate receptor-mediated currents inhibitor. Evans Blue has a strong affinity towards serum albumin, making it a high molecular weight protein tracer. Evans Blue is also used to study BBB (blood-brain barrier) permeability.

Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy.

GluN1 (356-385) is a polypeptide targeting NMDAR GluN1. GluN1 (356-385) induces the production of autoantibodies, which reduce the density of cell surface NMDAR clusters, impair long-term potentiation, and decrease NMDAR-mediated Ca²⁺ influx. As an immunogen, GluN1 (356-385) induces symptoms similar to anti-NMDAR encephalitis, including memory loss, in mice. GluN1 (356-385) can be used to establish a mouse model that mimics the pathogenesis of anti-NMDAR encephalitis. GluN1 (356-385) is applicable to research related to anti-NMDAR encephalitis.

Bupivacaine is a NMDA receptor inhibitor. Bupivacaine can block sodium, L-calcium, and potassium channels.Bupivacaine potently blocks SCN5A channels with the IC₅₀ of 69.5 μM. Bupivacaine can be used for the research of chronic pain.

Linalool is a natural monoterpene which is a competitive NMDA receptor antagonist. Linalool is orally active and crosses the blood-brain barrier. Linalool has anticancer, antibacterial, anti-inflammatory, neuroprotective, anxiolytic, antidepressant, anti-stress, cardioprotective, hepatoprotective, nephroprotective and pulmonary protective activities.

Bupivacaine hydrochloride is a NMDA receptor inhibitor.Bupivacaine can block sodium, L-calcium, and potassium channels.Bupivacaine potently blocks SCN5A channels with the IC₅₀ of 69.5 μM. Bupivacaine hydrochloride can be used for the research of chronic pain.

Naspm (1-Naphthyl acetyl spermine), a synthetic analogue of Joro spider toxin, is a calcium permeable AMPA (CP-AMPA) receptors antagonist.

Tacrine hydrochloride is a potent brain-penetrant inhibitor of both AChE and BChE, with IC₅₀s of 31 nM and 25.6 nM, respectively. Tacrine hydrochloride is also a NMDAR inhibitor, with an IC₅₀ of 26 μM. Tacrine hydrochloride can be used for the research of Alzheimer’s disease.

Naspm trihydrochloride (1-Naphthylacetyl spermine trihydrochloride), a synthetic analogue of Joro spider toxin, is a calcium permeable AMPA (CP-AMPA) receptors antagonist.

Tat-NR2B9c (Tat-NR2Bct; NA-1) is a postsynaptic density-95 (PSD-95) inhibitor, with EC₅₀ values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC₅₀ values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy.

GluN1 (359-378) is an anti-N-methyl-D-aspartate receptor (NMDAR) peptide. GluN1 (359-378) can cross the blood-brain barrier. GluN1 (359-378) can be used to study anti-NMDAR encephalitis therapy targeting the immune system.

Coniferyl ferulate is an orally active phenolic acid compound. Coniferyl ferulate is a potent inhibitor of glutathione S-transferase (GST) (IC₅₀ = 0.3 μM), which downregulates P-gp expression, induces apoptosis in B-MD-C1 (ADR+/+) cells, and reverses multidrug resistance. Coniferyl ferulate blocks the NMDAR/NR2B-CaMKII-MAPKs signaling pathway, inhibits ROS production and mitochondrial apoptosis, while reshapes the intestinal microbiota and microbial metabolism, ameliorates colonic inflammation and alleviates depressive symptoms in mice. Coniferyl ferulate can alleviate the toxicity of xylene to hematopoietic stem and progenitor cells by targeting Mgst2. Coniferyl ferulate exhibits antibacterial activity against the Gram-positive Bacillus subtilis and Staphylococcus aureus.

Phenylpiracetam (Carphedon) is a positive allosteric modulator of nicotinic acetylcholine receptors (nAChR) with an IC₅₀ of 5.86 μM. Phenylpiracetam is applicable to studies on scopolamine (Scopolamine) (HY-N0296)-induced amnesia, depression and immune stress.

MDL 105519 is a potent and selective antagonist of glycine binding to the NMDA receptor.

Felbamate (W-554) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA).

Ganglioside GM1 is a type of glycosphingolipid, mainly found on the cell membranes of the central nervous system of vertebrates. Ganglioside GM1 exerts neuroprotective effects by reducing excessive activation of NMDAR, activating TrkA and ERK1/2, and inhibiting oxidative stress and cell apoptosis and autophagy. Ganglioside GM1 can be used in the research of diseases such as traumatic brain injury, Parkinson's disease, Alzheimer's disease, and Huntington's disease.

Decanoic acid-d₁₉9 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects.

SBI-810 hydrochloride is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 hydrochloride promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 hydrochloride 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 hydrochloride effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 hydrochloride is applicable to research related to multiple pain disorders.

ZL006 is a potent inhibitor of nNOS/PSD-95 interaction, and inhibits NMDA receptor-mediated NO synthesis.

JNJ-55511118 is a selective TARP γ-8 binding AMPA receptor modulator with oral bioavailability and blood-brain barrier permeability, with a K_i of 26 nM. JNJ-55511118 reduces voluntary intake of sweetened alcohol in male mice. In rodent models, JNJ-55511118 inhibits hippocampal neurotransmission, reduces specific electroencephalogram frequency bands, induces transient hyperlocomotion, impairs learning and memory abilities, and exerts anticonvulsant effects. JNJ-55511118 is applicable to research related to alcohol use disorder and seizures.