ADCI, a noncompetitive NMDA antagonist, is a broad-spectrum anticonvulsant agent[1].
GYKI53655 hydrochloride is an α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) antagonist.
NBQX is a highly selective and competitive AMPA receptor antagonist.
L-Phenylalanine-13C6 ((S)-2-Amino-3-phenylpropionic acid-13C6) is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
7-Chlorokynurenic acid is a selective antagonist at the glycine modulatory site of the N-methyl-D-aspartate receptor complex and also a potent inhibitor of the reuptake of glutamate into synaptic vesicles with a Ki of 0.59 μM.
Ibotenic acid has agonist activity at both the N-methyl-D-aspartate (NMDA) and trans-ACPD or metabolotropic quisqualate (Qm) receptor sites.
Glycine-d2 is the deuterium labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
UBP296 is a potent and selective antagonist of GLUK5-containing kainate receptor in the spinal cord. UBP296 reversibly blocks ATPA-induced depressions of synaptic transmission, and affects AMPA receptor-mediated synaptic transmission directly in rat hippocampal slices[1].
Felbamate (FBM) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA) .Target: NMDA ReceptorFelbamate (marketed under the brand name Felbatol by MedPointe) is an anti-epileptic drug used in the treatment of epilepsy. It is used to treat partial seizures (with and without generalization) in adults and partial and generalized seizures associated with Lennox-Gastaut syndrome in children. However, an increased risk of potentially fatal aplastic anemia and/or liver failure limit the drugs usage to severe refractory epilepsy.Felbamate has been proposed to a unique dual mechanism of action as a positive modulator of GABAA receptors and as a blocker of NMDA receptors, particularly isoforms containing the NR2B subunit. Although it is clear that felbamate does cause pharmacological inhibition of NMDA receptor of relevance of NMDA receptor blockade as a strategy for the treatment of human epilepsy has been questioned. Therefore, the importance of the effects of felbamate on NMDA receptors to its therapeutic action in epilepsy is uncertain.
Procyclidine (Tricyclamol; (±)-Procyclidine), an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy[1][2].
Rapastinel Trifluoroacetate is an NMDA receptor modulator with glycine-site partial agonist properties and currently in a phase II clinical development program as an adjunctive therapy for major depressive disorder.
(R,S)-3,4-Dicarboxyphenylglycine ((RS)-3,4-DCPG) is an AMPA receptor antagonist. (R,S)-3,4-Dicarboxyphenylglycine antagonizes AMPA-mediated depolarization of motor neurons in neonatal rats. (R,S)-3,4-Dicarboxyphenylglycine can be used in the study of neurological diseases[1].
L-Phenylalanine-d1 ((S)-2-Amino-3-phenylpropionic acid-d1) is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
GNE 5729 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 37 nM for GluN2A, 4.7 and 9.5 μM for GluN2C and GluN2D, respectively.
(R)-Lanicemine ((R)-AZD6765) is the less active R-enantiomer of Lanicemine. Lanicemine (AZD6765) is a low-trapping NMDA channel blocker (Ki of 0.56-2.1 μM for NMDA receptor; IC50s of 4-7 μM and 6.4 μM in CHO and Xenopus oocyte cells, respectively). Antidepressant effects[1].
L-Phenylalanine-13C9,15N ((S)-2-Amino-3-phenylpropionic acid-13C9,15N) is the 13C- and 15N-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
Co 101244 (PD 174494) hydrochloride is a NR2B-containing NMDA receptor antagonist[1].
D-AP5 is a NMDA receptor antagonist.
(Rac)-Lanicemine ((Rac)-AZD6765) is the racemate of Lanicemine. Lanicemine (AZD6765) is a low-trapping NMDA channel blocker (Ki of 0.56-2.1 μM for NMDA receptor; IC50s of 4-7 μM and 6.4 μM in CHO and Xenopus oocyte cells, respectively). Antidepressant effects[1].
YM90K is a potent and selective AMPA receptor antagonist with a Ki of 84 nM. YM90K is less potent in inhibiting kainate (Ki of 2.2 μM) and NMDA (Ki of 37 μM) receptors. YM90K has neuroprotective actions[1].
1-BCP is a centrally active drug that modulates AMPA receptor gated currents. 1-BCP is a memory-enhancing agent[1][2].
Cyclothiazide, a positive allosteric modulator of AMPA receptors, is used frequently to block the desensitization of both native and heterologously expressed AMPA receptors. Cyclothiazide is known to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current[1].
L-Cysteine S-sulfate is a potent N-methyl-d-aspartate (NMDA) glutamatergic receptors agonist. L-Cysteine S-sulfate is the substrate for cystine lyase[1].
GYKI 52466 is a potent antagonist of kainate- and AMPA-activated currents (IC50 values, 7.5 and 11 μM, respectively), GYKI 52466 can be used for the research of neurological disorders, such as Parkinson's disease[1].
4-PPBP maleate is a potent σ 1 receptor ligand and agonist. 4-PPBP maleate is a non-competitive, selective NR1a/2B NMDA receptors (expressed in Xenopus oocytes) antagonist. 4-PPBP maleate provides neuroprotection[1][2][3].
PMPA (NMDA antagonist) is an NMDA receptor antagonist with Ki values of 0.84, 2.74, 3.53 and 4.16 μM for NR2A, NR2B, NR2C and NR2D, respectively[1].
BDZ-g is a potent, selective antagonist of AMPA receptor. BDZ-g has the potential for the research of various neurological disorders involving excessive activity of AMPA receptors[1].
DL-AP7 is a competitive NMDA antagonist and an anticonvulsant. DL-AP7 blocks the NMDA-induced convulsions and impairs learning performance in a passive avoidance task in mice[1].
DL-AP5 is a NMDA (N-methyl-D-aspartate) receptor antagonist. DL-AP5 shows significantly antinociceptive activity. DL-AP5 specifically blocks on channels in the rabbit retina[1][2].
PF-4778574 is a positive allosteric modulation of AMPA receptor with EC50 of 45 to 919 nM in differenct cells.