Target intelligence / Profile preview

Alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid receptor (AMPA Receptor)

Target
AMPA Receptor
Molecular classification
Ionotropic glutamate receptor, Receptor, Ligand-gated ion channel
01

Overview

The AMPA receptor is a subtype of ionotropic glutamate receptors that mediates fast excitatory synaptic transmission in the central nervous system. It is a tetrameric ion channel composed of GluA1-4 subunits and is crucial for rapid neuronal communication, learning, memory, and synaptic plasticity. Upon glutamate binding, the channel opens, allowing Na+ influx and neuronal depolarization. Auxiliary proteins modulate its trafficking, gating, and pharmacology. The defining agonist is AMPA itself.

Other names
AMPARGluA1GluA2GluA3GluA4GRIA1GRIA2GRIA3GRIA4
02

Mechanism of action

Agonists bind to the ligand-binding domain of the AMPA receptor, causing a conformational change that opens the ion channel pore, allowing influx of Na+ (and Ca2+ in some cases) and subsequent neuronal depolarization.

03

Biological functions

Fast excitatory postsynaptic potentials (EPSPs)Synaptic strength modulationLearning and memory formationSynaptic plasticityNeurotransmission
04

Disease associations

Neurodegenerative diseasesEpilepsyStrokeSchizophreniaDepressionAnxietyAutism Spectrum Disorder
05

Safety considerations

ExcitotoxicitySeizuresNeurodegeneration
06

Interacting drugs

AMPA

6 more in the full profile.

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