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Inhibition of GluN2B-containing N-methyl-d-aspartate receptors by radiprodil.


ABSTRACT: N-methyl-D-aspartate receptors mediate a slow, Ca2+ permeable component of excitatory synaptic transmission in the brain and participate in neuronal development and synaptic plasticity. Most NMDA receptors are tetrameric assemblies of two GluN1 and two GluN2 subunits encoded by five genes (GRIN1, GRIN2A-D), which produce GluN1 and GluN2A-D subunits. NMDA receptors that contain the GluN2B subunit have unique pharmacological properties, being inhibited by multiple structurally distinct series of biaryl compounds with high potency and selectivity. These agents are of considerable therapeutic interest, given the numerous roles that GluN2B-containing NMDA receptors play in normal brain function and pathological situations. Among GluN2B-selective negative allosteric modulators, radiprodil inhibi

SUBMITTER: Banke TG 

PROVIDER: S-EPMC12677382 | biostudies-literature | 2025 Sep

REPOSITORIES: biostudies-literature