GNE-9278

GNE-9278 is a highly selective positive allosteric modulator of NMDAR that acts at the GluN1 transmembrane domain (TMD). GNE-9278 acts on activated NMDARs to increase peak current and agonist affinity[1].

Signaling Pathways >> Neuronal Signaling >> iGluR

Research Areas >> Neurological Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR

NMDAR[1]

GNE-9278 (50 μM) slows deactivation with multiple agonists (D-Glu, L-Glu and L-CCG-IV) and enhances the potency of both Glu and Gly[1]. GNE-9278 robustly potentiates GluN2A, 2B, 2C and 2D-containing NMDARs as measured by calcium influx assays from HEK cell lines with the EC50s of 0.74, 3.07, 0.47, and 0.32 μM, respectively[1].

[1]. Wang TM, et, al. A novel NMDA receptor positive allosteric modulator that acts via the transmembrane domain. Neuropharmacology. . 2017 Jul 15; 121: 204-218.