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Ionotropic Glutamate Receptor Modulators
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Description
Biochem/physiol Actions
Product #
1-Aminocyclopropanecarboxylic acid hydrochloride 97%
NMDA glutamate receptor agonist acting at the glycine site
A0430
1-Aminocyclopropanecarboxylic acid ≥98% (TLC)
NMDA agonist acting at the glycine site
A3903
(±)-2-Amino-4-
phosphonobutyric acid solid
NMDA glutamate receptor antagonist.
A1910
D
(−)-2-Amino-
7-phosphonoheptanoic acid solid
Selective NMDA glutamate receptor antagonist; anticonvulsant; active enantiomer of 2-amino-7-phosphonoheptanoic acid.
A167
DL
-2-Amino-7-
phosphonoheptanoic acid ~95%
Selective NMDA glutamate receptor antagonist; anticonvulsant.
A5157
L
-(+)-2-Amino-6-
phosphonohexanoic acid ≥98% (HPLC), solid
Selective agonist of the quisqualate site on the ionotropic Q type excitatory amino acid receptors.
A5352
DL
-2-Amino-5-
phosphonopentanoic acid solid
Anticonvulsant; potent and selective NMDA receptor antagonist.
A5282
(
S
)-AMPA ≥98%
Active enantiomer of (RS)-AMPA zwitterion. Potent agonist at the AMPA subclass of ionotropic glutamate receptors.
A0326
(±)-AMPA hydrobromide solid
Potent excitatory amino acid that interacts selectively with central AMPA/kainate receptors.
G017
(±)-AMPA solid
Potent excitatory amino acid that interacts selectively with central AMPA/kainate receptors.
A6816
Arcaine sulfate salt
Potent antagonist at the polyamine site of the NMDA glutamate receptor.
A0384
ATPA solid
Selective kainate receptor agonist.
A263
ATPO solid
Competitive antagonist at GluR1-4 (AMPA-preferring) receptors.
A7845
CNQX disodium salt solid
Potent, competitive AMPA/kainate receptor antagonist.
C239
CNQX ≥98% (HPLC), solid
Potent, competitive AMPA/kainate glutamate receptor antagonist.
C127
CNS-1102 >98% (HPLC), solid
Noncompetitive NMDA glutamate receptor antagonist.
C4238
[Glu
3,4,7,10,14
]-
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
C1733
(±)-CPP solid
Potent and selective NMDA glutamate receptor antagonist; anticonvulsant.
C104
CX546 ≥98% (HPLC), solid
Positive AMPA glutamate receptor modulator.
C271
D
-Cycloserine microbial, powder
Mode of Action: Inhibits cell wall biosynthesis (
D
-Ala peptide bond formation). Also prevents conversion of
D
-Ala to
L
-Ala. Bacteriostatic.
Mode of Resistance:
D
-Ala transport interference.
Partial agonist at the glycine modulatory site of NMDA glutamatergic receptors; antibiotic against Gram-negative bacteria.
C6880
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.
Mode of Resistance:
D
-Ala transport interference.
Partial agonist at the glycine modulatory site of NMDA glutamatergic receptors; antibiotic against Gram-negative bacteria.
C3909
Cyclothiazide
Blocks the rapid desensitization of the AMPA glutamate receptors and markedly prolongs the decay time of the evoked excitatory post-synaptic current.
C9847
L
-Cysteine hydrochloride anhydrous, ≥98% (TLC)
NMDA glutamatergic receptor agonist that is also an agonist at AMPA glutamatergic receptors at high concentrations.
C1276
L
-Cysteine hydrochloride monohydrate reagent grade, ≥98% (TLC)
NMDA glutamatergic receptor antagonist.
C7880
DCB ≥98% (HPLC), solid
Neutral allosteric modulator of the metabotropic glutamate receptor mGluR
5
D1068
Dextromethorphan hydrobromide meets USP testing specifications
D9684
Dextromethorphan hydrobromide monohydrate Sigma Reference Standard
D1053
Dextrorphan tartrate solid
Noncompetitive NMDA glutamate receptor antagonist that attenuates glutamate neurotoxicity in cortical cell cultures.
D127
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.
D138
6,7-Dichloroquinoxaline-2,3-
dione
Antagonist at the NMDA glutamate receptor glycine site.
D133
2,6-Difluoro-4-[2-
(phenylsulfonylamino)
ethylthio]phenoxyacetamide >98% (HPLC), solid
A structurally novel, selective, high affinity AMPA ionotropic glutamate receptor agonist that reduces ischemia-induced performance deficits in rats.
D8941
Dihydrokainic acid ≥97% (NMR), solid
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.
D1064
N
-(3,3-
Diphenylpropyl)glycinamide >98% (HPLC), solid
NMDA glutamate receptor open channel blocker.
D8816
DMeOB ≥98% (HPLC), solid
Negative allosteric modulator at the metabotropic glutamate receptor mGluR
5
.
D6317
DNQX ~98%
A competitive kainate, quisqualate (non-NMDA) glutamate receptor antagonist.
D0540
Domoic acid ~90%, solid
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.
D6152
Eliprodil ≥98% (HPLC), solid
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.
E2031
γ-
D
-
Glutamylaminomethylsulfonic acid solid
Selective antagonist at AMPA/kainate glutamatergic receptors; anticonvulsant.
G111
GYKI 52466 hydrochloride solid
Selective allosteric AMPA receptor antagonist; anticonvulsant; skeletal muscle relaxant.
G119
R(+)-HA-966 solid
Antagonist of the strychnine-insensitive glycine modulatory site associated with the NMDA receptor. More active enantiomer of (±)-HA-966.
H130
L
-Homocysteic acid
Neurotransmitter candidate at NMDA receptors.
H9633
D
-
Homocysteinesulfinic acid ≥98% (TLC)
Potent, fast-acting NMDA glutamate receptor agonist.
H3899
Ibotenic acid ~95%, solid
Non-selective agonist with preference for NMDA glutamate receptors; neurotoxin; neuroexcitatory amino acid originally isolated from
Amanita
species.
I2765
IDRA 21 ≥98%
Blocks the rapid desensitization of the AMPA receptors and markedly prolongs the decay time of the evoked excitatory post-synaptic current.
I5773
IEM-1460 solid
Selective inhibitor of a subtype of AMPA receptors (Ca
2+
permeable, lacking GluR2 subunits); tool for functionally discriminating between AMPA receptors of different subunit composition
I0154
Ifenprodil (+)-tartrate salt
NMDA antagonist acting at the polyamine site; neuroprotective agent; α-adrenergic central and peripheral vasodilator; α
2
adrenergic receptor ligand.
I2892
Kainic acid monohydrate ≥99%
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.
K0250
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.
K2389
(±)-Ketamine hydrochloride solid
Selective NMDA glutamate receptor antagonist; veterinary anesthetic.
K2753
S-(+)-Ketamine hydrochloride
Selective NMDA glutamate receptor antagonist.
K1884
Kynurenic acid ≥98%
Kynurenic acid is a non-selective antagonist at NMDA and AMPA/kainate receptors; blocks kainic acid neurotoxicity. Kainic acid also blocks nicotinic acetycholine receptors (J. Neuroscience, 2001)
K3375
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.
L0258
MDL 105,519 solid
High affinity NMDA glutamate receptor antagonist at the glycine site.
M216
Memantine hydrochloride ≥98% (GC)
Low-affinity NMDA glutamate receptor antagonist; stimulates dopamine release.
M9292
d
-3-Methoxy-N-
methylmorphinan hydrobromide ≥99 (TLC)
Allosteric antagonist at NMDA-controlled ion channels; antagonist at voltage-dependent channels
D2531
(2S,4R)-4-Methylglutamic acid solid
Selective and high affinity kainate receptor antagonist.
G137
(+)-MK-801 hydrogen maleate solid
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.
M107
(−)-MK-801 hydrogen maleate solid
Less active enantiomer of (+)-MK-801 hydrogen maleate
M108
1-Naphthylacetyl spermine trihydrochloride >97%, solid, ≥98% (HPLC)
Blocks Ca
2+
permeable AMPA receptor channels.
N193
NBQX hydrate solid, ≥98% (HPLC)
Neuroprotective AMPA/kainate glutamate receptor antagonist.
N171
NBQX disodium salt hydrate ≥98% (HPLC), solid
NBQX disodium salt hydrate is a neuroprotective AMPA/kainate glutamate receptor antagonist.
N183
NS 102 solid
Competitive glutamate receptor antagonist with high selectivity for the low-affinity [
3
H] kainate binding site.
N179
NS3763 ≥98% (HPLC), solid
First non-competitive antagonist of GluK5 receptor.
N1162
PEAQX tetrasodium hydrate ≥98% (HPLC), solid
NMDA receptor antagonist.
P1999
Pentamidine isethionate salt powder
Neuroprotective; inhibits constitutive nitric oxide synthase in the brain; NMDA glutamate receptor antagonist.
P0547
cis
-2,3-
Piperidinedicarboxylic acid solid, ≥97% (NMR)
NMDA receptor agonist at the glutamate recognition site.
P8782
Quisqualic acid powder
Active enantiomer of quisqualic acid; excitatory amino acid at glutamate receptors.
Q2128
Ro 25-6981 hydrochloride ≥98% (HPLC), solid
Potent and selective antagonist of NMDA glutamate receptors containing the NR2B subunit.
R7150
Ro 8-4304 solid
NR2B-selective, noncompetitive NMDA glutamate receptor antagonist
R8900
Supercinnamaldehyde ≥98% (HPLC), solid
Supercinnamaldehyde is a transient receptor potential ankyrin 1 (TRPA1) activator; EC
50
= 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.
S3322
Topiramate ≥98% (HPLC), solid
Kainate GluR5 receptor antagonist; anticonvulsant.
T0575
S(−)-Willardiine solid
AMPA/kainate glutamate receptor agonist.
W105
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