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Glutamate [NMDA] receptor subunit epsilon-1 (GluN2A)
- Target
- GluN2A
- Molecular classification
- Ion channel, Ligand-gated ion channel, Ionotropic glutamate receptor, Receptor
01
Overview
Glutamate [NMDA] receptor subunit epsilon-1 (GluN2A) is part of the heterotetrameric N-methyl-D-aspartate (NMDA) receptor complex, which is a ligand-gated ion channel with high calcium permeability and voltage-dependent magnesium block. NMDA receptors are critical for excitatory synaptic transmission and play key roles in cognitive functions such as memory and learning. The receptor is composed of essential GluN1 subunits along with GluN2A or other GluN2 subunits, conferring specific functional and pharmacological properties. Mutations or dysregulation of GluN2A are linked to a range of neurological and psychiatric disorders, making it a prominent target in neuropharmacology and disease research
- Other names
- NMDA receptor subunit GluN2AGRIN2ANMDA2Aepsilon-1
02
Mechanism of action
Antagonists (block channel activation by glutamate/glycine, e.g., memantine, ketamine)\nModulation of receptor activity (allosteric modulators, e.g., ifenprodil)\nInhibitors of channel conductance
03
Biological functions
Signal transductionSynaptic transmissionCalcium transportLearning and memory (especially through long-term potentiation)
04
Disease associations
Epilepsy (including refractory epilepsy)Intellectual disabilityAutism spectrum disordersDevelopmental delaySchizophreniaNeurodegenerative diseases (protective effect in Parkinson's disease observed)
05
Safety considerations
CNS toxicity (resulting in cognitive impairment, sedation, psychotomimetic effects)Excitotoxicity (overactivation of receptor associated with neuronal death)Seizure risk (particularly with antagonists or genetic disruption)Psychiatric disturbances (hallucinations, dissociation with antagonist use)
06
Interacting drugs
Memantine
6 more in the full profile.
07
Biomarkers
Mutations in GRIN2A can be screened for epilepsy and neurodevelopmental disorders
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