Target intelligence / Profile preview

Glutamate receptor ionotropic, NMDA 2A subunit (GluN2A (also known as NR2A))

Target
GluN2A (also known as NR2A)
Molecular classification
Receptor, Ion channel, Ligand-gated ion channel
01

Overview

Glutamate receptor ionotropic, NMDA 2A subunit (GluN2A/NR2A) is a critical component of the NMDA subtype of ionotropic glutamate receptors, which function as ligand-gated ion channels permeable to calcium, sodium, and potassium ions[5][2][3]. The receptor is a heterotetramer, typically composed of two GluN1 and two GluN2A subunits; the GluN2A subunit binds glutamate and determines key channel properties such as conductance, gating kinetics, and pharmacological profile. GluN2A is primarily expressed in the forebrain and cerebral cortex and is essential for normal synaptic plasticity, learning, and memory[1][3]. The NMDA receptor, and specifically its GluN2A subunit, is implicated in a variety of neurological disorders, including epilepsy, schizophrenia, and cognitive deficits. Drugs targeting this subunit modulate synaptic transmission by influencing channel opening and calcium permeability, but carry significant safety concerns related to excitotoxicity, neurotoxicity, and neuropsychiatric effects[7][5][3].

Other names
NR2AGluN2AGRIN2AGlutamate receptor NMDA type subunit 2AN-methyl-D-aspartate receptor subunit 2A
02

Mechanism of action

Noncompetitive antagonism (e.g., memantine, ketamine block the ion channel pore); Competitive antagonism (at the glutamate or glycine binding site); Allosteric modulation (by zinc and other modulators binding the ATD)

03

Biological functions

Signal transductionSynaptic transmissionSynaptic plasticityLearning and memoryCalcium ion influx regulation
04

Disease associations

Neurodegenerative diseaseEpilepsySchizophreniaIntellectual disabilityNeurodevelopmental disorders
05

Safety considerations

Excitotoxicity due to overactivation (can lead to neuronal death)Cognitive impairment (with excessive inhibition)Psychotomimetic effects (ketamine, PCP)Seizures (potential with both antagonists and gain-of-function mutations)
06

Interacting drugs

Memantine

6 more in the full profile.

07

Biomarkers

GRIN2A gene mutations (in genetic epilepsies, neurodevelopmental disorders)Expression level in the cortex (as a biomarker for excitatory neurotransmission)

Beyond the preview

Go deeper on Glutamate receptor ionotropic, NMDA 2A subunit (GluN2A (also known as NR2A)).

Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.

Drug pipeline

Full profile access

Explore the programs pursuing this target and their development progress.

  • Drug candidates
  • Developers
  • Development stage

Clinical trials

Full profile access

Follow the clinical studies evaluating therapies directed at this target.

  • Trial design
  • Status
  • Readouts

Competitive landscape

Full profile access

Compare approaches across drug candidates, modalities, and indications.

  • Programs
  • Modalities
  • Indications

Literature & evidence

Full profile access

Investigate the research and source evidence behind target biology and development.

  • Publications
  • Sources
  • Analysis

Patents

Full profile access

Explore patent activity around therapies and technologies addressing this target.

  • Patents
  • Assignees
  • Technologies

Research & analysis

Full profile access

Connect target biology, drug development, and emerging evidence in your research.

  • Biology
  • Development news
  • Analysis

Bring the full picture into focus.

See how Gosset can support your research on Glutamate receptor ionotropic, NMDA 2A subunit (GluN2A (also known as NR2A)).

Explore the full profile

Gosset Free

Get started with Gosset.

Enter your work email and we’ll be in touch with next steps.

Work email preferred.

Book a call