Ionotropic Glutamate Receptor Modulators

Ionotropic glutamate receptors mediate the majority of excitatory neurotransmission in the brain. These receptors have also been implicated in medical conditions such as Alzheimer′s disease, Parkinson′s disease, chronic pain and stroke. There are three main subtypes of ionotropic glutamate receptors: AMPA, kainite, and NMDA. Pharmacological approaches to study these receptors generally involve the manipulation of glutaminergic synaptic transmission through the use of desensitizing modulators. Sigma offers several bioactive small molecules to modulate activation of this receptor class and better understand its functions.

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A3903 1-Aminocyclopropanecarboxylic acid ≥98% (TLC) 1-Aminocyclopropanecarboxylic acid (ACC) exhibits anticonvulsant, anxiolytic, anti-addictive, neuroprotective and antidepressant-like effects in rats and mice. ACC does not affect memory or learning processes.
NMDA agonist acting at the glycine site
A0430 1-Aminocyclopropanecarboxylic acid hydrochloride ≥98% NMDA glutamate receptor agonist acting at the glycine site
149101-M 1-Aminocyclopropane-1-carboxylic Acid - CAS 22059-21-8 - Calbiochem An agonist for the glycine modulatory site of the N-methyl-D-aspartate (NMDA) receptor complex. Primary Target
Glycine modulatory site of the N-methyl-D-aspartate (NMDA) receptor complex
Target IC50: 38 nM in blocking 3H-glycine binding to rat forebrain membrane; 131 µM in blocking NMDA-induced release of arachidonic acid; 131 µM in cerebellar granule cells
A1910 (±)-2-Amino-4-phosphonobutyric acid solid NMDA glutamate receptor antagonist.
165300 L-(+)-2-Amino-4-phosphonobutyric Acid - CAS 23052-81-5 - Calbiochem  
A5352 L-(+)-2-Amino-6-phosphonohexanoic acid ≥98% (HPLC), solid L-(+)-2-Amino-6-phosphonohexanoic acid (L-AP6) is an excitatory glutamate analogue that is able to depolarize L-quisqualic acid (QUIS)-sensitized CA1 rat hippocampal neurons.
A5282 DL-2-Amino-5-phosphonopentanoic acid solid Anticonvulsant; potent and selective NMDA receptor antagonist.
165304 D-(–)-2-Amino-5-phosphonopentanoic Acid - CAS 79055-68-8 - Calbiochem Active enantiomer of DL-2-amino-5-phosphonopentanoic acid (AP5) that is a commonly used as a competitive NMDA receptor antagonist. Cell permeable: no
Primary Target
NMDA receptor antagonist
Product does not compete with ATP.
Reversible: no
A0326 (S)-AMPA ≥98% Active enantiomer of (RS)-AMPA zwitterion. Potent agonist at the AMPA subclass of ionotropic glutamate receptors.
A6816 (±)-AMPA solid Potent excitatory amino acid that interacts selectively with central AMPA/kainate receptors.
A9111 (±)-AMPA hydrobromide ≥98% (HPLC) (±)-AMPA is a potent excitatory amino acid that interacts selectively with central AMPA/kainate receptors.
5.04913 Aniracetam - CAS 72432-10-1 - Calbiochem Primary Target
AMPA receptors
A0384 Arcaine sulfate salt Potent antagonist at the polyamine site of the NMDA glutamate receptor.
A263 ATPA solid Selective kainate receptor agonist.
A7845 ATPO solid Competitive antagonist at GluR1-4 (AMPA-preferring) receptors.
SML0635 AZD6765 dihydrochloride ≥97% (HPLC) AZD6765 is a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist and fast-acting antidepressant. In a recent study AZD6765 relieved depression within 80 minutes, unlike most antidepressants acting on serotonin or dopamine systems which can take several weeks to work. The effects lasted from about an hour up to 2 weeks. AZD6765 has an IC50 value of 1.3 μM. Unlike more potent drugs such as ketamine, which also has rapid antidepressant activity, AZD6765 has no dissociative side-effects such as hallucinations. Earlier studies inidcated the compound has neuroprotective and anticonvulsant effects.
SML0304 Caged MK801 ≥98% (HPLC) Caged MK801 is an inactive caged form of the potent selective non-competitive irreversible NMDA glutamate receptor open-channel blocker MK801. Caged MK801 is cleaved by exposure to UV light, liberating the active MK801. The caged compound is stable within cells. Intracellular compartment-specific photorelease allowed study the locus of induction and expression of timing-dependent long-term depression (t-LTD). Caged MK801 is thus a useful tool to uncover compartment-specific biological functions.
5.04467 L-CCG-I - CAS 117857-93-9 - Calbiochem Primary Target
mGlu₂ & mGlu₃
5.04844 7-Chlorokynurenic Acid Sodium Salt - CAS 1263094-00-3 - Calbiochem Primary Target
NMDA receptors
C127 CNQX ≥98% (HPLC), solid Potent, competitive AMPA/kainate glutamate receptor antagonist.
C239 CNQX disodium salt hydrate ≥98% (HPLC), solid CNQX(6-cyano-7-nitroquinoxaline-2,3-dioneis) is a potent, competitive AMPA/kainate receptor antagonist. It is a quinoxaline derivative and also an antagonist for non-N-methyl-d-aspartate (non-NMDA) glutamate receptor. CNQX mediates depolarization thalamic reticular nucleus via α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid receptors (AMPARs). It displays micromolar affinity towards AMPA/kainate receptor.
Potent, competitive AMPA/kainate receptor antagonist.
5.04914 CNQX - CAS 115066-14-3 - Calbiochem Secondary Target
Target Ki: 0.6 – 2.11 →M for GluA1 – 4 and Ki
C4238 CNS-1102 >98% (HPLC), solid Noncompetitive NMDA glutamate receptor antagonist.
C1733 [Glu3,4,7,10,14]-Conantokin G >90% (HPLC) Highly conserved polypeptide NMDA glutamate receptor antagonist; acts through a potent noncompetitive inhibition of polyamine responses; approximately 7-fold more potent than spermine
5.04713 CPCCOEt - CAS 179067-99-3 - Calbiochem Primary Target
mGlu₁ receptors
C104 (±)-CPP solid Potent and selective NMDA glutamate receptor antagonist; anticonvulsant.
5.04839 (R)-CPP - CAS 126453-07-4 - Calbiochem Primary Target
NMDA receptors
Target Ki: 0.041, 0.27, 0.63 and 1.99 →M for NMDA subtypes NR2A, NR2B, NR2C, and NR2D, respectively.
C2247 CPPHA ≥98% (HPLC) CPPHA is a selective positive allosteric modulator of mGluR5 receptor. It has no agonist activity alone, but reduces threshold response and shifts dose-response curves to glutamate, quisqualate, and DHPG by 4- to 7-fold to the left in recombinant CHO cells expressing human or rat mGluR5.
SML1191 CX516 ≥98% (HPLC) CX516 is a positive allosteric modulator at AMPA receptor that inhibits the deactivation of AMPA receptors. CX-516 is a nootropic and ampakine agent.
C271 CX546 ≥98% (HPLC), solid CX546 has antipsychotic functionality and has the potential to treat schizophrenia. It improves the defects associated with the prepulse inhibition (PPI) and latent inhibition (LI) in mice lacking metabotropic glutamate receptor type 5 (mGluR5). Additionally, CX546 potentiates synaptic plasticity, elicits neuroprotection and promotes the neurotrophin expression.
Positive AMPA glutamate receptor modulator.
5.05016 CX546 - CAS 215923-54-9 - Calbiochem Primary Target
C6880 D-Cycloserine D-cycloserine (DCS) was initially known as a tuberculostatic agent. It acts as a glutamatergic partial N-methyl-D-aspartate (NMDA) agonist. It binds at the glycine-binding site of the NMDA receptor and enable the opening of the NMDA channel. DCS has a an ability to improve various forms of learning and memory hence, this drug might be effective for improving social memory and cognition. DCS can be used as a potential therapeutic for psychiatric disorders such as phobias, social anxiety, obsessive-compulsive disorder, and posttraumatic stress disorder.
Mode of Action: Inhibits cell wall biosynthesis (D-Ala peptide bond formation). Also prevents conversion of D-Ala to L-Ala. Bacteriostatic.
Partial agonist at the glycine modulatory site of NMDA glutamatergic receptors; antibiotic against Gram-negative bacteria.
Mode of Resistance: D-Ala transport interference.
C3909 D-Cycloserine synthetic Mode of Action: Inhibits cell wall biosynthesis (D-Ala peptide bond formation). Also prevents conversion of D-Ala to L-Ala. Bacteriostatic.
Partial agonist at the glycine modulatory site of NMDA glutamatergic receptors; antibiotic against Gram-negative bacteria.
Mode of Resistance: D-Ala transport interference.
C9847 Cyclothiazide Blocks the rapid desensitization of the AMPA glutamate receptors and markedly prolongs the decay time of the evoked excitatory post-synaptic current.
5.05415 Cyclothiazide - CAS 2259-96-3 - Calbiochem Primary Target
AMPA receptor
C1276 L-Cysteine hydrochloride anhydrous, ≥98% (TLC) Cysteine (Cys) is a functional sulfur-containing aminoacid that regulates metabolism for growth, reproduction and immunity. It provides the disulfide linkage in proteins and is involved in the transport of sulfur. Cysteine is involved in the formation of hydrogen sulfide that functions as a signaling molecule. Cys residues are present at the catalytic sites of various enzymes.
NMDA glutamatergic receptor agonist that is also an agonist at AMPA glutamatergic receptors at high concentrations.
C7880 L-Cysteine hydrochloride monohydrate reagent grade, ≥98% (TLC) NMDA glutamatergic receptor antagonist.
D1068 DCB ≥98% (HPLC), solid 3,3′-dichlorobenzaldazine (DCB) serves as an allosteric ligand with neutral cooperativity. It helps to block the positive allosteric regulation of mGluRs (metabotropic glutamate receptor subtype 5 (mGluR5) with the help of 3,3′-difluorobenzaldazine (DFB) and the negative modulatory effect of 3,3′-dimethoxybenzaldazine (DMeOB).
Neutral allosteric modulator of the metabotropic glutamate receptor mGluR5.
D9684 Dextromethorphan hydrobromide meets USP testing specifications  
D2531 Dextromethorphan hydrobromide monohydrate ≥99% (TLC) Dextromethorphan hydrobromide is an allosteric antagonist at N-methyl D- aspartate (NMDA)-controlled ion channels and antagonist at voltage-dependent channels. Dextromethorphan hydrobromide is useful in treating dry cough.
D127 Dextrorphan tartrate powder Noncompetitive NMDA glutamate receptor antagonist that attenuates glutamate neurotoxicity in cortical cell cultures.
5.09706 DFB - CAS 15332-10-2 - Calbiochem Primary Target
5.04841 5,7-Dichlorokynurenic Acid, Sodium Salt - CAS 1184986-70-6 - Calbiochem Primary Target
NMDA receptors
D8941 2,6-Difluoro-4-[2-(phenylsul­fonyl­amino)­ethyl­thio]­phenoxy­acet­amide ≥98% (HPLC), solid 2,6-Difluoro-4-[2-(phenylsul­fonyl­amino)­ethyl­thio]­phenoxy­acet­amide is a structurally novel, selective, high affinity AMPA ionotropic glutamate receptor agonist that reduces ischemia-induced performance deficits in rats.
D1064 Dihydrokainic acid ≥98% (HPLC), powder Dihydrokainic acid is a selective inhibitor of the GLT-1 glutamate transporter. At higher concentrations, dihydrokainate is a weak inhibitor of AMPA/kainate glutamic acid receptors.
Dihydrokainic favors neuronal cell death. It modulates anxiety and depression behaviors.
D8816 N-(3,3-Diphenylpropyl)glycinamide >98% (HPLC), solid NMDA glutamate receptor open channel blocker.
D6317 DMeOB ≥98% (HPLC), solid Negative allosteric modulator at the metabotropic glutamate receptor mGluR5.
D0540 DNQX ≥98% (TLC) A competitive kainate, quisqualate (non-NMDA) glutamate receptor antagonist.
DNQX is a quinoxaline derivative.
D6152 Domoic acid ≥90% (HPLC) Domoic acid is a potent agonist at receptors for excitatory amino acids glutamate and kainate. It has highest affinity for AMPA/kainate receptor of any kainate agonist. It can causes excessive excitation of neurons leading to depletion of energy stores.
Domoic acid serves as an antihelminthic. It is capable of binding and stimulating the kainic acid glutamate receptor in the central nervous system.
E2031 Eliprodil ≥98% (HPLC), powder NR2B selective NMDA glutamate receptor antagonist which appears to target the "polyamine site" on the NMDA receptor, setting it apart from other NR2B receptor antagonists. Possesses neuroprotective effects in models of ischemia, but prolongs the QT interval in patients; currently under investigation for acute and chronic pain.
5.38096 GluN2B NMDA Receptor Antagonist, 93-31 - Calbiochem Primary Target
GluN2B NMDA Receptor
Reversible: yes
SML0109 GLYX-13 trifluoroacetate ≥98% (HPLC) GLYX-13 is a glycine-site functional partial agonist (GFPA) selective modulator of the NMDA receptor (NMDAR). It is a brain penetrable tetrapeptide which acts as a positive allosteric modulator of the NMDA receptor, acting via the glycine site. GLYX-13 has been found to be a cognitive enhancer in learning models and is currently in clinical trials as an antidepressant.
G119 GYKI 52466 hydrochloride solid GYKI 52466 serves as an antagonist of several processes, mediated by glutamate.
Selective allosteric AMPA receptor antagonist; anti­convulsant; skeletal muscle relaxant.
H130 R(+)-HA-966 solid Antagonist of the strychnine-insensitive glycine modulatory site associated with the NMDA receptor. More active enantiomer of (±)-HA-966.
H9633 L-Homocysteic acid L-Homocysteic acid (L-HCA) is an endogenous neurotransmitter ligand of NMDA (N-methyl-D-aspartate) receptors. It is an analog of glutamate and competitively suppresses glutamate-cystine (xc-) antiporter function in neurons, causing decrease in cysteine uptake.
SML1873 (2R,6R)-Hydroxynorketamine hydrochloride ≥98% (HPLC) (2R,6R)-Hydroxynorketamine is a ketamine metabolite that has rapid antidepressant activity without ketamine-related side effects. The NMDAR antagonist (R,S)-ketamine must be metabolized to (2S,6S;2R,6R)-hydroxynorketamine (HNK) to have antidepressant effects. The (2R,6R)-HNK enantiomer appears to be the enantiomer most responsible for antidepressant effects in a mouse study and unlike (2S,6S)-HNK, (2R,6R)-HNK caused no significant changes in locomotion or coordination. (2R,6R)-HNK does not seem to have the same addiction potential as ketamine, since mice did not self-administer pharmacologically relevant doses of (2R,6R)-HNK under the same conditions where ketamine was readily self-administered. The (2R,6R)-HNK antidepressant appears to involve activation of AMPA glutamate receptors rather than inhibition of NMDA glutamate receptors.
SML1875 (2S,6S)-Hydroxynorketamine hydrochloride ≥98% (HPLC) (2S,6S)-Hydroxynorketamin
I2765 Ibotenic acid ~95%, solid Ibotenic acid is an analog of glutamate. It is involved in the excitation of cell bodies and destroys the thalamic reticular nucleus (NRT). It induces high calcium influx leading to neuronal injury. Ibotenic acid is used to induce neurodegeneration due to its excitotoxic functionality.
Non-selective agonist with preference for NMDA glutamate receptors; neurotoxin; neuroexcitatory amino acid originally isolated from Amanita species.
5.05024 Ibotenic Acid - CAS 2552-55-8 - Calbiochem  
I5773 IDRA 21 ≥98% Blocks the rapid desensitization of the AMPA receptors and markedly prolongs the decay time of the evoked excitatory post-synaptic current.
I2892 Ifenprodil (+)-tartrate salt NMDA antagonist acting at the polyamine site; neuroprotective agent; α-adrenergic central and peripheral vasodilator; α2 adrenergic receptor ligand.
SML1747 JNJ-55511118 ≥98% (HPLC) JNJ-55511118 is also known as 5-[2-chloro-6-(trifluoromethoxy)phenyl]-1,3-dihydrobenzimidazol-2-one. It acts as an anticonvulsant or neuroprotectant. It is considered as a reversible α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor inhibitor, mainly in the hippocampus region.
JNJ-55511118 is an orally available, brain penetrant, potent and selective negative modulator of AMPA receptors that requires the presence of the accessory protein CACNG8 (TARP-γ8). JNJ-55511118 exhibit potent inhibition of neurotransmission within hippocampus, and a strong anti-convulsant effect.
K0250 Kainic acid monohydrate ≥99% (TLC) Kainic acid monohydrate is an agonist at the kainate class of ionotropic glutamate receptors, which induces seizures and neurodegeneration in vivo and is used to induce experimental epilepsy in rodents and study the mechanisms of excitation-induced neuronal apoptosis.
K2389 Kainic acid monohydrate ≥98% (HPLC), from Digenea simplex Ionotropic glutamate receptors form ion channels, and conduct Na+ and K+ fluxes. The receptors possess an agonist binding site and it encounters a conformational change upon agonist binding to it. Kainate gated channels participate in glutamate-induced excitatory postsynaptic neuronal potential.
Kainic acid monohydrate is an agonist at the kainate class of ionotropic glutamate receptors, which induces seizures and neurodegeneration in vivo and is used to induce experimental epilepsy in rodents and study the mechanisms of excitation-induced neuronal apoptosis.
420318 Kainic Acid - CAS 487-79-6 - Calbiochem An excitatory amino acid receptor agonist selective for the kainate receptor subtype (Ki = 21 nM for ³H-kainate binding in rat striatum). Cell permeable: no
Primary Target
Kainate receptor subtype
Product does not compete with ATP.
Reversible: no
Target Ki: 21 nM for 3H-kainate binding in rat striatum
K2753 (±)-Ketamine hydrochloride solid Selective NMDA glutamate receptor antagonist; veterinary anesthetic.
K1884 S-(+)-Ketamine hydrochloride Selective NMDA glutamate receptor antagonist.
K3375 Kynurenic acid ≥98% Kynurenic acid (KynA) is a non-selective antagonist of N-methyl-d-aspartate (NMDA), α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) and kainate receptors. It blocks kainic acid neurotoxicity. Kynurenic acid also blocks nicotinic acetylcholine receptors. It is a by-product of tryptophan catabolic pathway. Kynurenic acid is a neuromodulator and controls the levels of glutamate, dopamine, acetylcholine and α-aminobutyric acid (GABA). KynA controls neuroendocrine functions and altered levels of KynA is a potential marker in depression, schizophrenia Alzheimer′s and Huntington′s diseases. Normal levels of KynA in the brain is crucial for the cognitive function.
L0258 L-701,324 ≥98% (HPLC), solid L-701,324 is a high affinity, selective antagonist at the glycine site of the NMDA glutamate receptor. L-701,324 is a potent, active anticonvulsant with a reduced propensity to activate mesolimbic dopaminergic systems in rodents.
5.04685 LY 354740 - CAS 176199-48-7 - Calbiochem Primary Target
mGlu2/3 receptors
L1170 LY-487379 hydrochloride ≥98% (HPLC) LY-487379 is a positive allosteric modulator of the metabotropic glutamate receptor mGluR2. EC50 = 1.7 μM. LY-487379 shows no intrinsic agonist or antagonist activity at hmGluR2 and has no activity at human mGluR3. LY-487379 markedly potentiates glutamate-stimulated [35S]GTPγS binding in a concentration-dependent manner at hmGluR2, shifting the glutamate dose-response curve leftward by 3-fold and increasing the maximum levels of [35S]GTPγS stimulation. LY-487379 has anxiolytic effects in fear-potentiated startle. This activity profile is useful in all symptom domains of schizophrenia.
M216 MDL 105,519 ≥98% (HPLC), solid MDL 105,519 is a high affinity N-methyl-D-aspartate (NMDA) glutamate receptor antagonist at the glycine site. It inhibits NMDA-dependent responses.
M9292 Memantine hydrochloride ≥98% (GC) Low-affinity NMDA glutamate receptor antagonist; stimulates dopamine release.
Memantine is effective against Alzheimer′s disease and Parkinson′s disease. It is also useful in treating epilepsy, motor neurone disease and trauma.
454575 N-Methyl-D-aspartic Acid, Hydrate - CAS 6384-92-5 - Calbiochem Excitatory amino acid neurotransmitter. Cell permeable: no
Primary Target
Glutamate receptor that regulates Ca2+ channels
Product does not compete with ATP.
Reversible: no
5.31145 mGlu7 Antagonist, XAP044 - Calbiochem Cell permeable: yes
Primary Target
Reversible: yes
Target IC50: 3.5 and 2.8 &micro
445874 mGluR5 Antagonist, MTEP - CAS 329205-68-7 - Calbiochem The mGluR5 Antagonist, MTEP, also referenced under CAS 329205-68-7, controls the biological activity of mGluR5. This small molecule/inhibitor is primarily used for Neuroscience applications. Cell permeable: yes
Primary Target
Product does not compete with ATP.
Reversible: no
Target IC50: 5 nM in Ca2+-flux assay
Target Ki: 16 nM for mGluR5 (metabotropic glutamate receptor subtype-5)
445865 mGluR5 Ligand, CDPPB - CAS 781652-57-1 - Calbiochem A pyrazole amide compound that crosses the blood-brain barrier and acts as a potent, selective, reversible, positive allosteric modulator for metabotropic glutamate receptor subtype 5 (mGluR5). Cell permeable: no
EC50 = 10 nM in potentiating the response to glutamate (~300 nM) in CHO-mGluR5 cells for human, 4-fold potentiation; 20 nM for rat, 4.3-fold potentiation
Primary Target
Metabotropic glutamate receptor subtype 5 (mGluR5)
Product does not compete with ATP.
Reversible: yes
M108 (−)-MK-801 hydrogen maleate ≥98% (HPLC) Less active enantiomer of (+)-MK-801 hydrogen maleate
MK-801 functions as a selective non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist.
M107 (+)-MK-801 hydrogen maleate powder Highly potent and selective non-competitive NMDA glutamate receptor antagonist that acts at the NMDA receptor-operated ion channel as an open channel blocker. Inhibits behavioral sensitization to psychostimulants and ethanol.
MK-801 [(+)-5-methyl-10, 11-dihydroxy-5H-dibenzo (a, d) cyclohepten-5, 10-imine] functions as a selective non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist and stimulates locomotion in monoamine-depleted mice. Experimental study shows that MK-801, influence circling behavior in a direction-specific manner, modify swimming activity and place preference in zebrafish. Acute injection of MK-801, dose dependently, enhances extracellular acetylcholine (ACh) release in the rat parietal cortex. For intracerebral hematomas, MK-801 might act as a potent supplement to reduce delayed edema after recombinant tissue plasminogen activator (rtPA) clot lysis. MK-801 functions as an antidepressant in the social defeat stress model, but it doesn’t have long-lasting effect.
475878 (+)-MK 801 Maleate - CAS 77086-22-7 - Calbiochem A highly potent, selective, and non-competitive NMDA receptor antagonist that acts by binding to a site located within the NMDA-associated ion channel, thus preventing Ca2+ flux. Cell permeable: no
Primary Target
NMDA receptor
Reversible: no
N193 1-Naphthylacetyl spermine trihydrochloride Blocks Ca2+ permeable AMPA receptor channels.
N183 NBQX disodium salt hydrate ≥98% (HPLC) NBQX disodium salt hydrate is a neuroprotective AMPA/kainate glutamate receptor antagonist.
N171 NBQX hydrate powder, ≥98% (HPLC) NBQX [2,3-dihydroxy-6-nitro-7-sulphamoyl-benzo(F)quinoxaline], an anticonvulsant provides protection against white matter damage in spinal cord crush injury and also protects oligodendrocyte in experimental autoimmune encephalomyelitis (EAE). However, its role in preventing inflammation in EAE is not yet clear.
Neuroprotective AMPA/kainate glutamate receptor antagonist.
5.05764 NMDA Antagonist XI, N1-dansyl-spermine - Calbiochem Primary Target
454586 NMDAR2C/2D Inhibitor, DQP-1105 - Calbiochem The NMDAR2C/2D Inhibitor, DQP-1105 controls the biological activity of NMDAR2C/2D. This small molecule/inhibitor is primarily used for Neuroscience applications.  
N1162 NS3763 ≥98% (HPLC), solid First non-competitive antagonist of GluK5 receptor.
5.04528 NVP-AAM077 Tetrasodium Hydrate - CAS 459836-30-7 - Calbiochem Primary Target
NMDA receptors
Target IC50: 0.015 and 0.078 µM for NR2A and NR2B, respectively.
P1999 PEAQX tetrasodium hydrate ≥98% (HPLC) NMDA receptor antagonist.
PEAQX is more specific for N-methyl-D-aspartate (NMDA) receptor 2A (NR2A) than N-methyl-D-aspartate (NMDA) receptor 2B (NR2B) and induces striatal apoptosis. It is less potent in activating caspase-3 than its stereomer NVP-AAM007.
P0547 Pentamidine isethionate salt powder Neuroprotective; inhibits constitutive nitric oxide synthase in the brain; NMDA glutamate receptor antagonist.
Pentamidine isethionate is used as a second line drug for leishmaniasis.
PZ0215 PF-04701475 ≥98% (HPLC) PF-04701475 is a potent and selective α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) positive allosteric potentiator.
PZ0216 PF-04725379 ≥98% (HPLC) PF-04725379 is a potent and selective α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) positive allosteric potentiator.
PZ0211 PF-4778574 ≥98% (HPLC) PF-4778574 is a potent AMPA receptor positive allosteric modulator (PAM) that has been shown to enhance cognition in animal models.
SML0393 QNZ46 ≥98% (HPLC) QNZ46 is a noncompetitive inhibitor of GluN2C/D containing NMDA receptors. KD and IC50 values for binding and inhibition of GluN1/Glun2D receptors by QNZ46 are 4.9 and 3.9 μM, respectively. QNZ46 does not compete for binding of glutamate or glycine, but QNZ46 receptor binding requires the binding of glutamate to the GluN2 subunit.
5.04535 QNZ46 - CAS 1237744-13-6 - Calbiochem Primary Target
NMDA receptors
Target IC50: 6, 3, 229, and >300 →M for NR2C, NR2D, NR2A, and NR2B, respectively.
Q2128 Quisqualic acid powder Active enantiomer of quisqualic acid; excitatory amino acid at glutamate receptors.
R7150 Ro 25-6981 hydrochloride hydrate ≥98% (HPLC), powder Potent and selective antagonist of NMDA glutamate receptors containing the NR2B subunit.
R8900 Ro 8-4304 solid NR2B-selective, noncompetitive NMDA glutamate receptor antagonist
SML0598 SDZ 220-581 hydrochloride ≥98% (HPLC) SDZ 220-581 is a competitive NMDA receptor antagonist that penetrates the blood brain barrier. ISDZ 220-581 selectively blocks the glutamate recognition-site of the NMDA receptor and reduces prepulse inhibition (PPI). SDZ 220-581 reduces prepulse inhibition (PPI) and has an ED50 of less than 3.2 mg/kg for protection against MES-induced seizures.
SML0811 SUN ≥95% (HPLC) SUN is am orally active and potent DAAO (DAO) inhibitor, which increases D-serine cerebellar and plasma concentrations. SUN was effective in rat models of neuropathic and inflammatory pain.
S3322 Supercinnamaldehyde ≥98% (HPLC) Supercinnamaldehyde is a transient receptor potential ankyrin 1 (TRPA1) activator; EC50 = 0.8 μM; derivative of cinnamaldehyde; covalently binds to and activates TRPA1 receptor (expressed in nociceptive neurons) by modifying its cysteine residues. Covalent modification of reactive cysteines within TRPA1 can cause channel activation, rapidly signaling potential tissue damage through the pain pathway.
T0575 Topiramate ≥98% (HPLC), solid Kainate GluR5 receptor antagonist; anticonvulsant.
Topiramate is a derivative of suphamate fructopyranose that inhibits the release of mesocorticolimbic dopamine. It facilitates GABA activity and inhibits glutamate function to alleviate the rewarding effects of alcohol. It modulates the trigeminovascular signaling that is effective in migraine prevention. Topiramate is structurally similar to fructose- 1,6-diphosphate and has the ability to inhibit the enzyme fructose 1,6-bisphosphatase, thereby preventing gluconeogenesis. It is found to inhibit the AMPA/kainate receptor-mediated signaling pathway in cultured neurons.
5.05017 UBP310 - CAS 902464-46-4 - Calbiochem Primary Target
Secondary Target
SML0606 UBP608 ≥98% (HPLC) UBP608 is NMDA receptor family allosteric modulator that selectively inhibits GluN1/GluN2A receptors with a 23-fold selectivity compared to GluN1/GluN2D receptors. It appears to distinguish between GluN2A and GluN2B, and between GluN2C and GluN2D. UBP608 does not act at either the glutamate or glycine binding sites, the ion channel, or the NTD. It appears that UBP608 is acting at the dimer interface between individual subunit ligand-binding domains.