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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149101-M 1-Aminocyclopropane-1-carboxylic Acid - CAS 22059-21-8 - Calbiochem 1-Aminocyclopropane-1-carboxylic Acid - CAS 22059-21-8, is an agonist for the glycine modulatory site of the N-methyl-D-aspartate (NMDA) receptor complex., An agonist for the glycine modulatory site of the N-methyl-D-aspartate (NMDA) receptor complex.  
165300 L-(+)-2-Amino-4-phosphonobutyric Acid - CAS 23052-81-5 - Calbiochem  
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.  
324378 Domoic Acid, Mytilus edulis - CAS 14277-97-5 - Calbiochem A heat-stable neurotoxin.  
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).  
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).  
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.  
454575 N-Methyl-D-aspartic Acid, Hydrate - CAS 6384-92-5 - Calbiochem Excitatory amino acid neurotransmitter.  
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.  
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.  
5.04528 NVP-AAM077 Tetrasodium Hydrate - CAS 459836-30-7 - Calbiochem  
5.04535 QNZ46 - CAS 1237744-13-6 - Calbiochem  
5.04713 CPCCOEt - CAS 179067-99-3 - Calbiochem  
5.04820 Cinnabarinic acid - CAS 606-59-7 - Calbiochem  
5.04844 7-Chlorokynurenic Acid Sodium Salt - CAS 1263094-00-3 - Calbiochem  
5.05017 UBP310 - CAS 902464-46-4 - Calbiochem  
5.05024 Ibotenic Acid - CAS 2552-55-8 - Calbiochem  
5.38238 VU0409551 - Calbiochem An orally bioavailable, non-toxic, brain permeant mGlu₅ PAM that selectively potentiates mGlu₅-mediated signaling but not NMDAR function. Highly efficacious in rodent models and enhances recognition memory.  
A3903 1-Aminocyclopropanecarboxylic acid ≥98% (TLC) NMDA agonist acting at the glycine site
A0430 1-Aminocyclopropanecarboxylic acid hydrochloride ≥98% NMDA glutamate receptor agonist acting at the glycine site
A1910 (±)-2-Amino-4-phosphonobutyric acid solid NMDA glutamate receptor antagonist.
A5157 DL-2-Amino-7-phosphonoheptanoic acid ~95% Selective NMDA glutamate receptor antagonist; anticonvulsant.
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.
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.
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.
SML0274 CBIO ≥95% (HPLC) CBIO is a potent, cell-permeable, D-amino acid oxidase (DAO) reversible inhibitor. In rat model, CBIO prevents formalin-induced tonic pain but not acute nociception.
C127 CNQX ≥98% (HPLC), solid Potent, competitive AMPA/kainate glutamate receptor antagonist.
C239 CNQX disodium salt hydrate ≥98% (HPLC), solid Potent, competitive AMPA/kainate receptor antagonist.
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
C104 (±)-CPP solid Potent and selective NMDA glutamate receptor antagonist; anticonvulsant.
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 Positive AMPA glutamate receptor modulator.
C6880 D-Cycloserine powder 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.
C1276 L-Cysteine hydrochloride anhydrous, ≥98% (TLC) 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 Neutral allosteric modulator of the metabotropic glutamate receptor mGluR5.
D9684 Dextromethorphan hydrobromide meets USP testing specifications  
D2531 Dextromethorphan hydrobromide monohydrate ≥99% (TLC) Allosteric antagonist at NMDA-controlled ion channels; antagonist at voltage-dependent channels
D127 Dextrorphan tartrate powder Noncompetitive NMDA glutamate receptor antagonist that attenuates glutamate neurotoxicity in cortical cell cultures.
D138 5,7-Dichlorokynurenic acid monohydrate solid, ≥98% (HPLC) Potent excitatory amino acid receptor antagonist; active at the strychnine-insensitive glycine binding site of the NMDA glutamate receptor.
D133 6,7-Dichloroquinoxaline-2,3-dione Antagonist at the NMDA glutamate receptor glycine site.
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.
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.
D6152 Domoic acid ≥90% (HPLC) Potent agonist at receptors for excitatory amino acids glutamate and kainate; has highest affinity for AMPA/kainate receptor of any kainate agonist; causes excessive excitation of neurons leading to depletion of energy stores.
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.
G111 γ-D-Glutamylaminomethylsulfonic acid solid Gamma-D-Glutamylaminomethylsulfonic acid (GAMS) is used as a selective antagonist of AMPA/kainate glutamatergic receptors and as an anticonvulsant.
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 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.
H3899 D-Homocysteinesulfinic acid ≥98% (TLC) Potent, fast-acting NMDA glutamate receptor agonist.
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) New (2S,6S)-Hydroxynorketamin
I2765 Ibotenic acid ~95%, solid Non-selective agonist with preference for NMDA glutamate receptors; neurotoxin; neuroexcitatory amino acid originally isolated from Amanita species.
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 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 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.
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 is a non-selective antagonist at NMDA and AMPA/kainate receptors; blocks kainic acid neurotoxicity. Kynurenic acid also blocks nicotinic acetycholine receptors.
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.
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 NMDA glutamate receptor antagonist at the glycine site.
M9292 Memantine hydrochloride ≥98% (GC) Low-affinity NMDA glutamate receptor antagonist; stimulates dopamine release.
M108 (−)-MK-801 hydrogen maleate ≥98% (HPLC) 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.
N193 1-Naphthylacetyl spermine trihydrochloride Blocks Ca2+ permeable AMPA receptor channels.
N183 NBQX disodium salt hydrate ≥98% (HPLC), lyophilized solid NBQX disodium salt hydrate is a neuroprotective AMPA/kainate glutamate receptor antagonist.
N171 NBQX hydrate powder, ≥98% (HPLC) Neuroprotective AMPA/kainate glutamate receptor antagonist.
N179 NS 102 solid Competitive glutamate receptor antagonist with high selectivity for the low-affinity [3H] kainate binding site.
N1162 NS3763 ≥98% (HPLC), solid First non-competitive antagonist of GluK5 receptor.
P1999 PEAQX tetrasodium hydrate ≥98% (HPLC) NMDA receptor antagonist.
P0547 Pentamidine isethionate salt powder Neuroprotective; inhibits constitutive nitric oxide synthase in the brain; NMDA glutamate receptor antagonist.
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.
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.
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.