glun2c

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.

R-(+)-EU-1180-453 is a novel GluN2C D selective NMDAR-positive modulator for the study of neurological disorders.

(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.

DQP 1105 is a NMDA receptor antagonist.

NSC339614 potassium is a selective GluN1/GluN2C and GluN1/GluN2D receptors potentiator.

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].

DQP-26, a potent negative allosteric modulator of NMDA receptors (NMDARs), exhibits IC50 values of 0.77 μM for GluN2C and 0.44 μM for GluN2D subunits, indicating potential application in research on NMDAR-associated neurological diseases [1].

Dihydroquinoline-pyrazoline DQP-997-74 (compound 2i) is a selective N-methyl-d-aspartate receptor (NMDAR) inhibitor that preferentially targets GluN2C D subunits, with IC50 values of 0.069 μM and 0.035 μM, respectively, and possesses blood-brain barrier permeability. It enhances its inhibitory potency in a time-dependent manner when combined with the agonist glutamate, reducing epileptogenic events in a murine model of tuberous sclerosis complex (TSC)-induced epilepsy. DQP-997-74 is potentially applicable for the study of NMDAR-related neurological diseases [1].