GNE-9278 is a highly selective positive allosteric modulator ofNMDARthat acts at the GluN1 transmembrane domain (TMD). GNE-9278 acts on activatedNMDARsto increase peak current and agonist affinity^[1].

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 EC₅₀s of 0.74, 3.07, 0.47, and 0.32 μM, respectively^[1].

429.54

Solid

C₂₁H₂₇N₅O₃S

2315311-83-0

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