Target intelligence / Profile preview

N-methyl-D-aspartate Receptor Subunit 1 (GluN1)

Target
GluN1
Molecular classification
Ion channel, Receptor, Glutamate receptor, NMDA receptor subunit
01

Overview

The NR1 subunit, also known as GluN1, is an essential component of the N-methyl-D-aspartate (NMDA) receptor, a type of ionotropic glutamate receptor. NMDA receptors are critical for synaptic transmission and plasticity in the central nervous system and play key roles in learning, memory, and excitotoxicity. The functional NMDA receptor is a heterotetrameric complex typically composed of two obligatory NR1 subunits and two regulatory subunits from either the NR2 or NR3 families. Activation requires simultaneous binding of glutamate (to GluN2) and glycine or D-serine (to GluN1), along with membrane depolarization to relieve Mg²⁺ block. Once activated, it functions as a non-selective cation channel allowing Ca²⁺ influx—critical for downstream signaling—and Na⁺ influx/K⁺ efflux across neuronal membranes.

Other names
NR1GRIN1
02

Mechanism of action

NMDA receptor channel blocker, Glycine/D-serine binding

03

Biological functions

Synaptic transmissionSynaptic plasticityLong-term potentiationLong-term depressionLearningMemoryNeuronal excitability
04

Disease associations

Neurodegenerative diseaseExcitotoxicityStrokeEpilepsySchizophreniaAlzheimer's diseaseParkinson's disease
05

Safety considerations

ExcitotoxicityPsychotomimetic effectsCognitive impairment
06

Interacting drugs

Memantine

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