Glutamate receptor ionotropic, NMDA 2A (GluN2A) (GluN2A)

The NMDA receptor GluN2A subunit, encoded by the GRIN2A gene, is a key component of the N-methyl-D-aspartate (NMDA) receptor, a ligand-gated ion channel essential for excitatory neurotransmission in the brain (UniProt P35436). These receptors are heterotetramers typically composed of two GluN1 and two GluN2 subunits, where the GluN2A subunit confers specific kinetic properties such as rapid deactivation (PubMed: 24074970). GluN2A is vital for synaptic plasticity, particularly long-term potentiation (LTP), which is the cellular basis for learning and memory (StatPearls: NMDA Receptor). Mutations in the GRIN2A gene are associated with a range of disorders, including epilepsy-aphasia spectrum and intellectual disability (NCBI Gene: 2903). While non-selective antagonists like memantine are used clinically, subunit-selective positive allosteric modulators (PAMs) like GNE-0723 are being researched for cognitive enhancement in schizophrenia (PubMed: 27170061). Therapeutic targeting requires precise modulation to avoid the risks of excitotoxicity or psychotomimetic side effects associated with NMDA receptor imbalance.

Other names

GRIN2ANR2ANMDAR2AGlutamate [NMDA] receptor subunit epsilon-1L-glutamate-binding receptor subunit

Non-competitive antagonism via channel pore blockade and subunit-selective positive or negative allosteric modulation.