Chemical Name: 4-Cyclohexyl-N-(7-hydroxy-5-methyl-2-propyl[1,2,4]triazolo[1,5-a]pyrimidin-6-yl)benzenesulfonamide
Biological ActivityPositive allosteric modulator of NMDA receptors. Potentiates NMDA receptors containing GluN2A, 2B, 2C and 2D subunits (EC50 values are 0.74, 3.07, 0.47 and 0.32 μM in a Ca2+ influx assay, respectively). Binds within the transmembrane domain and displays preference for agonist-bound NMDA receptors. Slows receptor deactivation and enhances the potency of glutamate and glycine.
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A novel NMDA receptor positive allosteric modulator that acts via the transmembrane domain.
Wang et al.
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