glun1/glun2a

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

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.

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.

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.

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.

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