Bioactivity | 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]. |
Invitro | 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]. |
Name | GNE-8324 |
CAS | 1698901-76-6 |
Formula | C18H18FN3OS |
Molar Mass | 343.42 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |