glun2a

GNE-0723 is a selective positive allosteric modulator of the NMDA receptor, with an EC50 of 21 nM for GluN2A. It can cross the blood-brain barrier (BBB) and improve outcomes in Dravet syndrome (DS) and Alzheimer's disease (AD).

GNE-5729 is a positive allosteric modulator of NMDAR with the advantage of crossing the blood-brain barrier and being orally available, with EC50 values of 37 nM, 4.7 μM and 9.5 μM for GluN2A, GluN2C and GluN2D, respectively, and can be used for the study of neurological and psychiatric disorders.

(RS)-(Tetrazol-5-yl)glycine is a potent and selective N-methyl-D-aspartate (NMDA) receptor agonist that can induce seizure models and Fos expression in mice. Its EC50 values for GluN1/GluN2D and GluN1/GluN2A are 99 nM and 1.7 μM, respectively.

TCN 201 is a selective antagonist of NMDA receptors containing the NR2A subunit.

GluN2A Allosteric modulator 1 (Compound 11) is an orally bioavailable compound that effectively crosses the blood-brain barrier and functions as a highly selective negative allosteric modulator of GluN2A. It exhibits an IC50 of 0.042 μM for GluN2A and 13 μM for GluN2B. This compound is useful for research in neurological disorders.

TP-050 is a chemical probe, which has oral activity and selectively acts on NMDAR. The EC₅₀ of GluN2A and GluN2D are 0.51 μM and 9.6 μM respectively, and it can penetrate the blood-brain barrier. TP-050 can induce long-term potentiation effect (LTP) in hippocampus, thus promoting neuronal signal transmission.

TCN 213 is an antagonist of NMDA receptor that has a selective for NR1/NR2A over NR1/NR2B

JNJ-78911118 is a potent, blood-brain barrier-penetrating selective GluN2A antagonist (IC50= 44 nM). It demonstrates over 200-fold selectivity for GluN1/2B, 2C, and 2D receptors. As a negative allosteric modulator (NAM), JNJ-78911118 significantly reduces the potency of glutamate at GluN1/2A receptors and decreases the efficacy of glycine. It exhibits notable pharmacodynamic effects in vivo and is applicable in depression-related research.

GNE-6901 is a selective GluN2A PAM.

GNE-8324 is a GluN2A selective positive allosteric modulator that selectively enhances NMDAR-mediated synaptic responses in inhibitory, but not excitatory, neurons.GNE-8324 is used in the study of neurological disorders.

UBP608 is an allosteric modulator of NMDA receptor family. It selectively inhibits GluN1/GluN2A receptors with a 23-fold selectivity compared to GluN1/GluN2D receptors.

(3S,6R)-NML is an NMDA receptor antagonist with pIC50 values of 4.8 [GluN1-GluN2A], 4.6 [GluN1-GluN2B], 5.0 [GluN1-GluN2C], and 5.0 [GluN1-GluN2D]. It is applicable in the study of depression.

NMDA receptor modulator9 is an orally active positive allosteric modulator (PAM) of the NMDA receptor. It enhances the activity of the GluN2A receptors. In a chronic restraint stress (CRS) induced depression mouse model, NMDA receptor modulator9 exhibits significant antidepressant-like effects. It is used for research on depression.

UCM-A86 is a selective positive allosteric modulator of GluN1/GluN3 NMDA receptors, exhibiting EC50 values of 21 µM and 19 µM for GluN1/GluN3A and GluN1/GluN3B receptors, respectively. It specifically enhances the activity of GluN1/GluN3A/B receptors without significantly affecting GluN1/GluN2A-D receptors. UCM-A86 is useful for research on central nervous system diseases.

DQP 1105 is a NMDA receptor antagonist.

MPX-007, a potent NMDA inhibitor, inhibits GluN2A-containing NMDA receptors expressed in HEK cells with IC50s of 27 nM.

GNE-3476 is an NMDA receptor PAM. Ge-3476 has different degrees of activity on different receptors.GNE-3476 has relatively low efficacy on GluN2A, some activity as an AMPAR PAM, and weak activity at GluN2B-containing receptors.

NAB-14 is a powerful and selective chemical compound that acts as a non-competitive antagonist for GluN2C and GluN2D receptors. With an IC50 value of 580 nM for GluN1/GluN2D, NAB-14 demonstrates high potency. This compound exhibits a remarkable selectivity of more than 800-fold towards recombinant GluN2C and GluN2D when compared to GluN2A and GluN2B. Furthermore, NAB-14 possesses the ability to penetrate the blood-brain-barrier effectively [1].

PEAQX, also known as NVP-AAM077; is a competitive antagonist at the NMDA receptor. Although originally described as 100-fold selective for GluN1/GluN2A receptors vs. GluN1/GluN2B receptors, more detailed studies of the Ki of PEAQX revealed it only shows a 5 fold difference in affinity for GluN1/GluN2A vs. GluN1/GluN2B receptors. It is also a potent anticonvulsant in animal tests.

NYX-2925, an orally active NMDAR (N-methyl-D-aspartate receptor) modulator, enhances activated Src levels and Src phosphorylation at GluN2A and GluN2B sites in the mPFC (medial prefrontal cortex), without affecting CAMKII (Ca2+/calmodulin-dependent protein kinase II) or exhibiting addictive or sedative/ataxic side effects. It is utilized in the study of various CNS (central nervous system) disorders mediated by NMDA receptors.

GluN2B (formally NR2B) selective, competitive antagonist of the NMDA receptor. Blocks NMDA-evoked current in mouse cortical neurons (IC50 = 480 nM); also inhibits NMDA-evoked responses in oocytes expressing GluN2B (formally NR2B), but not GluN2A (formally