Target intelligence / Profile preview

NMDA Receptor (NR1-NR2A Subunit) (None)

Target
None
Molecular classification
Ion channel, Ligand-gated ion channel, Glutamate receptor
01

Overview

The NMDA receptor is an ionotropic glutamate receptor that plays a crucial role in excitatory neurotransmission, synaptic plasticity, learning, and memory. It is a heterotetramer composed of two NR1 (GluN1) subunits and two NR2A (GluN2A) subunits. Activation requires simultaneous binding of glycine/D-serine to NR1 and glutamate to NR2A, leading to the influx of Ca²⁺ and Na⁺ ions and efflux of K⁺ ions. The NR1-NR2A receptor exhibits high calcium permeability, voltage-dependent Mg²⁺ block, and sensitivity to allosteric modulators like Zn²⁺. It is widely expressed in the brain and its function is implicated in various neurological disorders.

Other names
GluN1/GluN2A ReceptorNR1-NR2A Glutamate Receptor
02

Mechanism of action

Ion channel agonist/antagonist; Allosteric modulation of channel activity

03

Biological functions

Excitatory neurotransmissionSynaptic plasticityLearningMemoryNeuronal development
04

Disease associations

Neurodegenerative diseaseStrokeEpilepsySchizophreniaAlzheimer's diseaseChronic pain
05

Safety considerations

ExcitotoxicityPsychotomimetic effects (ketamine)Neurotoxicity
06

Interacting drugs

Glycine

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