YY-23 is a selective inhibitor of NMDAR (containing GluN2C or GluN2D). YY-23 inhibits GABAergic neurotransmission and enhances excitatory transmission by inhibiting NMDARs containing GluN2D on GABAergic interneurons in the prefrontal cortex. YY-23 has antidepressant activity and can be used for the research of neurological diseases.

Methalthiazide enhances the activity of natural stimulators of AMPA receptors and can be used in the study of schizophrenia.

Metaphit methylsulfate is a specific PCP antagonist and site-directed acylating agent of the [3H]phencyclidine binding site in rat brain homogenates. Metaphit methylsulfate prevents PCP-induced locomotor behavior through presynaptic mechanisms.

Lu AF90103 (Compound 42e) is a methyl ester prodrug of compound 42d capable of penetrating the blood-brain barrier. Compound 42d acts as a partial agonist of the GluN1/GluN2B complex, exhibiting 24% efficacy, and has an EC50 value of 78 nM. Lu AF90103 plays an important role in neuropsychiatric diseases research.

gamma-DGG TFA is the antagonist for excitatory amino acid, that blocks NMDA-, Kainate- and Quisqualate- induced depolarization, and antagonises the excitatory postsynaptic potential (e.p.s.p.) in rat hippocampal slices.

FLY26 is a selective partial GluN2B antagonist with an IC50 value of 0.64 μM. FLY26 partially inhibits the GluN2B subunit of NMDA receptors, reduces calcium ion influx and reactive oxygen species (ROS) production and activates the BDNF/TrkB/CREB neuroprotective signaling pathway to alleviate neuronal excitotoxicity and mitochondrial dysfunction. FLY26 is promising for research of neurological deficits caused by cerebral ischemia-reperfusion injury.

EU 1622-240 is a biased positive allosteric modulator of GluN2B, GluN2C, and GluN2D, with EC50s of 0.57, 0.82, 1.1 μM respectively. EU 1622-240 has good physicochemical properties, in vitro stability, and permeability.

EMD-95885 is a selective NR2B-containing NMDA receptors antagonist with an IC50 of 3.9 nM. EMD-95885 does not interact with other sites on the NMDA receptor.

Blixeprodil (GM-1020) is the orally active antagonist for NMDA receptor with an affinity of Ki=3.25 µM in rat cortical tissue. Blixeprodil inhibits NR1/2A-NMDAR-mediated currents in HEK293 cell with IC50 of 1.192 µM. Blixeprodil exhibits antidepressant in rats models. Blixeprodil can cross blood-brain barrier.

Argiotoxin 636 is a toxin and the non-specific, non-competitive, and potent ionotropic glutamate receptor (iGluR) antagonist. Argiotoxin 636 blocks excitatory synaptic transmission in neurons and has paralysis and muscle relaxation effects. Argiotoxin 636 can be used in the study of nervous system diseases.

3-Methoxy PCE (3-MEO PCE) hydrochloride is structurally classified as an arylcyclohexylamine and is an /b>NMDA receptor antagonist with a pKi value of 7.22.

(3S,6R)-NML is a NMDA receptor antagonist, with pIC50s of 4.8 (GluN1-GluN2A), 4.6 (GluN1-GluN2B), 5.0 (GluN1-GluN2C), 5.0 (GluN1-GluN2D) respectively. (3S,6R)-NML can be used for depression research.

FP802 is a novel small molecule with significant neuroprotective properties, specifically designed to target and disrupt the TwinF interface within the NMDAR/TRPM4 death signaling complex. This unique mechanism allows FP802 to selectively eliminate extrasynaptic NMDAR (eNMDAR)-mediated toxicity, which is implicated in various neurodegenerative diseases, while preserving the essential physiological functions of synaptic NMDARs. This selectivity makes FP802 a promising therapeutic candidate for conditions involving excitotoxicity and neuronal cell death.

BZAD-01 is a potent, selective and orally active inhibitor of NMDA NR2B subunit, with a Ki of 72 nM. BZAD-01 can improve postural asymmetry as well as Apomorphine-induced rotation.

GYKI 52466 dihydrochloride is a selective non-competitive AMPA receptor antagonist (IC50 values are 10-20, ~ 450 and >> 50 μM for AMPA- , kainate- and NMDA-induced responses respectively). Skeletal muscle relaxant and orally-active anticonvulsant.

ZCAN262 is a small molecule that prevents AMPA-mediated excitotoxicity (IC50=8.5 nM) by targeting an allosteric binding site of AMPA glutamate receptor 2 (GluA2).

ZCAN155 is a small molecule that prevents AMPA-mediated excitotoxicity (IC50=35 nM) by targeting an allosteric binding site of AMPA glutamate receptor 2 (GluA2), restores neurological function and myelination.

UBP792 is a novel negative allosteric modulator (antagonist) of NMDA receptors, displays partial subtype-selectivity by having a varied maximal inhibition of GluN2A-, GluN2B-, GluN2C-, and GluN2D-containing receptors (52%, 70%, 87%, 89%, respectively) wit

UBP791 is a subtype-selective competitive antagonist of GluN2C/2D-containing NMDA receptors with Ki of 80-90 nM, 50-fold selectivity over GluN2A and GluN2B.

UBP1700 is a subtype-selective competitive antagonist of GluN2C/2D-containing NMDA receptors with Ki of 7-9 nM, 50-fold selectivity over GluN2A and GluN2B.

PTC-174 is a selective, positive allosteric modulator of NMDA receptors containing GluN2C or GluN2D subunits with EC50 of 4.1 uM (GluN1/2C) and 5.7 uM (GluN1/2D).

Org 26576 (MK 8777.

GluN2A PAM (R)-9 is a potent, brain penetrant, GluN2A-selective positive allosteric modulator with EC50 of 0.51 uM, Emax 350%.

DQP-997-74 is a potent, selective GluN2C- and GluN2D-containing NMDARs negative allosteric modulator with IC50 of 0.35 and 0.13 uM, respectively, exhibits >100-fold over GluN2A- and GluN2B-containing receptors.

(S)-(-)-DQP-997-74 is a potent, selective GluN2C- and GluN2D-containing NMDARs negative allosteric modulator with IC50 of 69 and 35 nM, respectively, exhibits >100- and >300-fold over GluN2A- and GluN2B-containing receptors.

(R)-OF-NB1 is a small molecule splice variant GluN2B-selective NMDAR antagonist with IC50 of 675 nM and 97 nM for F-NB1 for splice variant containing exon 5 and GluN1-1a in X. laevis oocytes.

Topiramate D12 (McN 4853 D12) is a deuterium labeled Topiramate. Topiramate is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase.

Ro 25-6981 is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit.

NVP-AAM077 is a potent antagonist for NMDA receptors.

UoS12258 (UoS-12258) is a selective, positive allosteric modulator of the AMPA receptor with pEC50 of 5.6.