iGluR

TAK-137 is an AMPA receptor enhancer with antidepressant effects. TAK-137 has the ability to improve cognition and could be used to study schizophrenia.

Dalzanemdor (SAGE-718) is an NMDA receptor-positive modulator of metabolism that can be used to study Huntington's chorea, Alzheimer's disease, and cognitive dysfunction.

D-AP5 (D-APV) is an NMDA receptor antagonist.

MK-801 (Dizocilpine (MK-801)) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM.

Transcrocetinate disodium (Disodium trans-crocetinate), extracted from saffron (Crocus sativus L.), is a high-affinity antagonist of NMDA receptor.

Dizocilpine Maleate (MK 801) is a potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) with Kd of 37.2 nM in rat brain membranes. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role.

Dasolampanel (NGX-426) is an orally available ionotropic glutamate receptor AMPA and Kainate receptor antagonist for the study of chronic pain disorders, including neuropathic pain and migraine.

L-Glutamic acid (Glutaminol) acts as an excitatory transmitter, shows a direct activating effect on the release of DA from dopaminergic terminals.

UK-240455 is a potent and selective N-methyl-D-aspartic acid (NMDA) glycine receptor antagonist with neuroprotective effects and improvements in motor function in Parkinson's disease models, making it a potential candidate for Parkinson's disease treatment.

N-Methyl-D-aspartic acid is an amino acid that, as the D-isomer, is the defining agonist for the NMDA (N-Methyl-D-aspartic acid) receptor subtype of glutamate receptors.

CGP 78608 hydrochloride is a specific antagonist at the glycine binding site of the NMDA receptor (IC50 = 6 nM). CGP 78608 hydrochloride exhibits anticonvulsant activity. CGP 78608 hydrochloride potentiates GluN1 GluN3A-mediated glycine currents (estimated EC50 = 26.3 nM).

CFM-2, a potent and selective non-competitive antagonist of AMPAR (AMPAR), exhibits anticonvulsant activity across various seizure models.

glycine (2-Aminoacetic acid) is a non-essential amino acid. It is found primarily in gelatin and silk fibroin and used therapeutically as a nutrient. It is also a fast inhibitory neurotransmitter.

TAK-653, a selective positive allosteric modulator (PAM) of AMPA receptors exhibiting minimal agonistic activity, elicits an antidepressant-like response while maintaining a favorable safety profile in rat models.

L-Phenylalanine (3-Phenyl-L-alanine) is an essential amino acid and the precursor of the amino acid tyrosine, acts as an antagonist at α2δ calcium channels.

Corticosterone-d8 is a 2H-labeled corticosteroid, an orally active adrenal corticosteroid with mineralocorticoid and glucocorticoid activity, involved in hormonal regulation in animals.

AMPA receptor modulator-1 can be activated by glutamate, thereby modulating ion channels.

CNQX (FG9065) is a competitive, non-NMDA glutamate receptor antagonist (IC50s = 0.3 and 1.5 μM for AMPA and kainate receptors, respectively)

YM90K (6-(1H-imidazol-1-yl)-7-nitro-2,3(1H,4H)-) hydrochloride is an antagonist of AMPA receptor.

Quinolinic acid (QUIN) is an endogenous N-methyl-D-aspartate (NMDA) receptor agonist synthesized from L-tryptophan via the kynurenine pathway.

D-Cycloserine (RO-1-9213) is a broad spectrum antibiotic used as a second line agent for treatment of drug resistant tuberculosis, always in combination with other antituberculosis agents.

Tat-NR2B9c (NA-1) is a postsynaptic density-95 (PSD-95) inhibitor with neuroprotective and antiepileptic effects.Tat-NR2B9c inhibits PSD-95d2, PSD-95d1, and PSD-95, which prevents the activation of NMDA-induced NADPH oxidase in neurons, thereby blocking the production of superoxide, which reduces ischemic injury in the acute phase after stroke.

PEAQX tetrasodium hydrate (PEAQX tetrasodium hydrate (459836-30-7 free base)) is an orally available NMDA antagonist that is potent and selective. The IC50 value of PEAQX tetrasodium hydrate (459836-30-7 free base) against hNMDAR 1A 2A was 270 nM and 29600 nM against hNMDAR 1A 2B, respectively.

Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with partial agonist properties at the glycine site.

Memantine hydrochloride (Memantine HCl) is an AMANTADINE derivative that has some dopaminergic effects. Memantine hydrochloride has been proposed as an antiparkinson agent.

JNJ-61432059 is an orally active and selective negative modulator of TARP γ-8 selective AMPAR (pIC50: 9.7).

Rapastinel (TPPT-amide) (GLYX-13) is an N-methyl-D-aspartate receptor (NMDAR) modulator.

MDL-29951 is a novel glycine antagonist for NMDA receptor activation.

NMDAR TRPM4-IN-2 is a potent interfacial inhibitor of NMDAR TRPM4 interaction.NMDAR TRPM4-IN-2 protects against MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss in mice.NMDAR TRPM4-IN-2 has neuroprotective activity against NMDA-induced hippocampal neuronal cell death and mitochondrial dysfunction. NMDAR TRPM4-IN-2 showed neuroprotective activity against NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons with an IC50 value of 2.1 μM.

CX546 is an AMPA receptor modulator. CX546 enhances cognitive function in rats. It has also been proposed as a treatment for schizophrenia.

NBQX (FG9202) is a potent, selective and competitive AMPA receptor antagonist. Neuroprotective and anticonvulsant; active in vivo.

(S)-Willardiine (L-willardiine) is present in the seeds of Acacia and Mimosa. (S)-Willardiine is an AMPA kainate receptor agonist (EC50 = 44.8 μM).

1. Linalool (Linalol), a natural compound of the essential oils, has been shown to have antinociceptive, antimicrobial, and anti-inflammatory properties. 2. Linalool was protected against LPS GalN-induced liver injury through induction of antioxidant defense via Nrf2 activating and reduction inflammatory response via NF-κB inhibition. 3. Linalool biosynthesis and accumulation might be involved in plant defense against bacterial and fungal pathogens and be associated with field resistance to citrus canker. 4. Linalool significantly increased the expression of antioxidant enzymes regulated by Nrf-2 and diminished lung tissue levels of several pro-inflammatory cytokines, including tumor necrosis factor α (TNF-α) and interleukin (IL)-6.

NMDAR antagonist 1 is an orally active, NR2B-selective NMDAR antagonist.

Decanoic Acid (Caprynic acid) acts as a non-competitive AMPA receptor antagonist.

L-Glutamic acid monosodium salt (MSG) (Monosodium glutamate) is an activator of mGlu1 receptor.

Sepimostat exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat dimethanesulfonate inhibits the Ifenprodil binding with a Ki value of 27.7 μM.

Topiramate (RWJ 17021) is a unique antiseizure medication that is used in the treatment of partial and generalized seizures. Topiramate has been rarely associated with hepatic injury and largely when used in combination with other anticonvulsant medications.

Rislenemdaz (CERC-301) (CERC-301) is an antagonist of the N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B).

Flupirtine maleate (Katadolon maleate), a centrally acting non-opioid analgesia, is the salt form of Flupirtine. It is an NMDA receptor antagonist , and also a specific neuronal potassium channel opener.

LY392098 (AMPA receptor modulator-3) is an allosteric modulator of AMPA receptor with EC50 of 4.4 μM and can be used in studies about mammalian nervous system.

Transcrocetin (8,8'-Diapocarotenedioic Acid) is a singlet oxygen quencher.

(-)-Huperzine A (HupA) , an active Lycopodium alkaloid extracted from the traditional Chinese herb, is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor and has been widely used in China for the treatment of Alzheimer's disease (AD).

D-Serine ((R)-Serine), an endogenous amino acid, is a potent co-agonist at the NMDA glutamate receptor.

DNQX (FG 9041) is a competitive, non-NMDA glutamate receptor antagonist (IC50s = 0.5 and 0.1 μM for AMPA and kainate receptors, respectively)

Aniracetam (Ro 13-5057)(Ro 13-5057), a nootropic and neuroprotective drug, selectively modulates the AMPA receptor and nAChR.

TCN 201 is a selective antagonist of NMDA receptors containing the NR2A subunit.

(-)-Aspartic acid (L-Homoproline) is an endogenous amino acid existing in invertebrates and vertebrates. It can regulate testosterone synthesis and is an agonist of NMDA receptor.