GNE-8324 

GNE-8324 is a selective GluN2A positive allosteric modulator. GNE-8324 selectively enhances NMDA receptor (NMDAR)-mediated synaptic responses in inhibitory but not excitatory neurons^[1].

A reciprocal allosteric interaction between the GNE-8324 and glutamate binding sites at GluN2A NMDARs such that binding of glutamate enhances binding of GNE-8324 and vice versa. GNE-8324 selectively potentiates GluN2A subunit-containing NMDARs. As a consequence, GNE-8324 potentiation is highly dependent on glutamate site occupancy with enhanced GNE-8324 binding to glutamate-bound NMDARs compared to glutamate-free NMDARs^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

343.42

C₁₈H₁₈FN₃OS

1698901-76-6

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• [1]. Lulu Yao, et al. Higher ambient synaptic glutamate at inhibitory versus excitatory neurons differentially impacts NMDA receptor activity. Nat Commun. 2018 Oct 1;9(1):4000.  [Content Brief]