Glutamate ionotropic receptor NMDA type subunit 2B (GRIN2B)

The Glutamate ionotropic receptor NMDA type subunit 2B (GRIN2B), also known as GluN2B or NR2B, is a critical component of the N-methyl-D-aspartate (NMDA) receptor complex, which functions as a ligand-gated, calcium-permeable ion channel in the central nervous system [1, 2]. It plays a fundamental role in excitatory neurotransmission, synaptic plasticity, and the molecular mechanisms underlying learning and memory [1, 3]. Dysregulation or mutations in the GRIN2B gene are linked to various neurological and psychiatric conditions, including treatment-resistant depression, Alzheimer's disease, and neurodevelopmental disorders like autism [2, 3]. Unlike non-selective NMDA receptor antagonists, selective GluN2B negative allosteric modulators are being developed to provide therapeutic benefits with a reduced risk of psychotomimetic side effects [4]. These drugs typically bind to the amino-terminal domain of the subunit to inhibit channel activity in a use-dependent manner [3, 4]. Consequently, GRIN2B remains a high-priority target for drug discovery in neuropsychiatry and neurology [4]. Sources: [1] UniProt (Q13224); [2] NCBI Gene (2904); [3] PubMed (PMID: 24631114); [4] ClinicalTrials.gov (NCT02459236).

Other names

GluN2BNR2BN-methyl D-aspartate receptor subtype 2BGlutamate receptor subunit epsilon-2hNR2B

Negative allosteric modulation and non-competitive antagonism of the NMDA receptor complex, specifically targeting the GluN2B subunit to modulate calcium influx and downstream signaling.