Target intelligence / Profile preview

Glutamate receptor ionotropic, NMDA type subunit (NR (e.g., NR1, NR2A, NR2B, NR2C, NR2D, NR3A, NR3B) or GluN (GluN1, GluN2A, etc.))

Target
NR (e.g., NR1, NR2A, NR2B, NR2C, NR2D, NR3A, NR3B) or GluN (GluN1, GluN2A, etc.)
Molecular classification
Ion channel, Receptor, Ligand-gated ion channel, Glutamate receptor (Ionotropic glutamate receptor)
01

Overview

The **NMDA receptor ionotropic, NMDA type subunits** are integral membrane proteins (GluN1, GluN2A-D, GluN3A-B) that assemble as heterotetramers to form the NMDA receptor, a ligand-gated ion channel permeable to Ca²⁺, Na⁺, and K⁺ ions. Activation requires glutamate and either glycine or D-serine as co-agonists, and opening the receptor channel leads to calcium influx and cellular signaling pathways governing plasticity, development, and repair. NMDA receptor subunits are highly regulated by alternative splicing, post-translational modifications, and interactions with intracellular proteins, determining their localization and function. Dysfunction or excessive activity contributes to neurological and psychiatric diseases, making them key drug targets[1][2][3][4][5][7].

Other names
NMDA receptor subunitNR1NR2ANR2BNR2CNR2DNR3ANR3BGluN1GluN2AGluN2BGluN2CGluN2DGluN3AGluN3B
02

Mechanism of action

Antagonists block the ion channel (noncompetitive or competitive inhibition), reducing calcium influx Partial agonists modulate receptor activity Allosteric modulators alter channel opening or ligand binding

03

Biological functions

Signal transductionNeurotransmissionSynaptic plasticity (including learning and memory)Calcium signalingExcitatory postsynaptic potential mediationNeuronal development
04

Disease associations

Neurodegenerative disease (e.g., Alzheimer's, Parkinson's)EpilepsyIschemic strokePsychiatric disorders (e.g., schizophrenia, depression)PainCognitive dysfunction
05

Safety considerations

Excitotoxicity risk (excessive stimulation leads to neuronal cell death)Cognitive impairment or dissociation (especially with antagonists like ketamine)Potential psychotomimetic effectsNegative impact on normal synaptic plasticity
06

Interacting drugs

Memantine

7 more in the full profile.

07

Biomarkers

NR2 subunit expression or phosphorylation state (as a biomarker of disease state or therapeutic response)CSF or plasma glutamate levels (in some cases)Imaging of receptor occupancy (experimental)

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