NMDA Antagonists

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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.
C104 (±)-CPP solid Potent and selective NMDA glutamate receptor antagonist; anticonvulsant.
K2753 (±)-Ketamine hydrochloride solid Selective NMDA glutamate receptor antagonist; veterinary anesthetic.
A1910 (±)-2-Amino-4-phosphonobutyric acid solid NMDA glutamate 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.
A8054 D(−)-2-Amino-5-phosphonopentanoic acid NMDA receptor antagonist Anticonvulsant; potent and selective N-methyl-D-aspartate (NMDA) receptor antagonist; active enantiomer of 2-amino-5-phosphonopentanoic acid.
NMDA antagonists have muscle relaxation property and are known to offer neuron protection against brain damage induced by ischemia. 2-Amino-5-phosphonopentanoic acid has been proved to block the iontophoresis induced depolarization of NMDA.
A5282 DL-2-Amino-5-phosphonopentanoic acid solid Anticonvulsant; potent and selective NMDA receptor antagonist.
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.
A0384 Arcaine sulfate salt Potent antagonist at the polyamine site of the NMDA glutamate receptor.
SML0050 CGP 37849 ≥98% (HPLC) CGP 37849 induces phencyclidine-like behavioral syndrome in amygdala-kindled rats that includes ataxia, locomotion and stereotypies.
CGP 37849 is a potent orally active competitive NMDA antagonist and anticonvulsant.
SML0058 CGP 39551 ≥98% (HPLC) CGP 39551 is an orally active competitive NMDA antagonist and anticonvulsant.
CGP 39551 produces excitatory effects and causes psychotomimetic effects in humans.
C4238 CNS-1102 >98% (HPLC), solid Noncompetitive NMDA glutamate receptor antagonist.
SML0053 CP-101,606 ≥98% (HPLC) CP-101,606 (Traxoprodil) plays a role in inhibiting glutamate-induced death in rats. It may exhibit therapeutic effects against human ischemia and neurodegenerative disorders. Traxoprodil is metabolized by cytochrome P450 (CYP) 2D6.
Traxoprodil (CP-101,606) is a potent noncompetitive antagonist of N-methyl-D-aspartate (NMDA) receptors, selective for the NR2B subunit. It has been shown to be neuroprotective in animal models of brain injury and stroke.
PZ0255 CP-101606 mesylate ≥98% (HPLC) CP-101,606 is an NR2B (N-methyl D-aspartate receptor subtype 2B) subunit antagonist, that can increase dyskinesia. It reduces Ca2+/calmodulin-dependent protein kinase II level, at threonine-286 hyperphosphorylation (pCaMKII-Thr286). It has no effect on the α1-adrenergic receptors. CP-101,606 has the ability to inhibits the habits, stimulated by cocaine. It also possesses hallucinogenic properties.
CP-101606 mesylate (Traxoprodil mesylate) is a potent noncompetitive antagonist of N-methyl-D-aspartate (NMDA) receptors, selective for the NR2B subunit. CP-101606 mesylate has been shown to be neuroprotective in animal models of brain injury and stroke.
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.
D6317 DMeOB ≥98% (HPLC), solid Negative allosteric modulator at the metabotropic glutamate receptor mGluR5.
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.
D9684 Dextromethorphan hydrobromide meets USP testing specifications  
D127 Dextrorphan tartrate powder Noncompetitive NMDA glutamate receptor antagonist that attenuates glutamate neurotoxicity in cortical cell cultures.
SML0206 EAA-090 ≥98% (HPLC) EAA-090 inhibits the binding of ligands to glutamate receptors and blocks NMDA-induced currents. It is neuroprotective against glutamate and ischemia-induced toxicity.
EAA-090 is a potent NMDA receptor antagonist with neuroprotective properties. In isoflurane-anesthetized dogs, EAA-090 reduces the minimum alveolar concentration (MAC) of isoflurane and increases systolic, mean, and diastolic arterial blood pressure.
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.
I2892 Ifenprodil (+)-tartrate salt NMDA antagonist acting at the polyamine site; neuroprotective agent; α-adrenergic central and peripheral vasodilator; α2 adrenergic receptor ligand.
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.
SML0824   Lubeluzole dihydrochloride ≥98% (HPLC) Lubeluzole is an NMDA antagonist. Lubeluzole blocks glutamate release, as well as sodium and calcium gated ion channels. Lubeluzole displays neuroprotective properties in ischemia models.
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.
D8816 N-(3,3-Diphenylpropyl)glycinamide >98% (HPLC), solid NMDA glutamate receptor open channel blocker.
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.
H130 R(+)-HA-966 solid Antagonist of the strychnine-insensitive glycine modulatory site associated with the NMDA receptor. More active enantiomer of (±)-HA-966.
SML0335 Remacemide hydrochloride ≥98% (HPLC) Remacemide HCl is a low affinity NMDA antagonist with anticonvulsant properties. Remacemide also been shown to block voltage-dependent sodium channels.
Remacemide possesses neuroprotective and anti-epileptic actions. It supports reducing the frequency of seizures. Remacemide is also known to be a potential therapeutic for Huntington′s disease.
R7150 Ro 25-6981 hydrochloride hydrate ≥98% (HPLC), powder Potent and selective antagonist of NMDA glutamate receptors containing the NR2B subunit.
SML0495 Ro 25-6981 maleate salt ≥98% (HPLC) Ro 25-6981 maleate salt is a potent and selective antagonist of NMDA glutamate receptors containing the NR2B subunit with IC50 values of .009 μM for NR2B vs. 52 μM for NR2A subunits. Ro 25-6981 has been shown to have neuroprotectant effects and to reduce inflammatory and neuropathic pain in rodent models.
R8900 Ro 8-4304 solid NR2B-selective, noncompetitive NMDA glutamate receptor antagonist
K1884 S-(+)-Ketamine hydrochloride Selective 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.
SML0416 TCN-201 ≥98% (HPLC) TCN-201 is a sulphonamide derivative, that negatively modulates glycine binding to the GluN1 (glutamate receptor subunit) subunit of the receptor.
TCN-201 is the first NMDA receptor antagonist that is specific for NR2A-subunit containing receptors. The pIC50 for NR2A NMDA receptors is 6.8. TCN-201has no effect on NR2B-containing receptors at concentrations up to 50 mM.
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.
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