Target intelligence / Profile preview

Glutamate receptor 4 (AMPA subtype) (GRIA4)

Target
GRIA4
Molecular classification
Ion channel, Ligand-gated ion channel, Receptor, AMPA receptor
01

Overview

Glutamate receptor 4 (GRIA4), also known as GluA4, is a subunit of the AMPA-type ionotropic glutamate receptors. These receptors are ligand-gated ion channels that mediate fast excitatory neurotransmission in the central nervous system by responding to the neurotransmitter L-glutamate. AMPA receptors are tetrameric complexes typically formed as heterotetramers from combinations of any of the four subunits (GluA1–GluA4). Each subunit has a large extracellular amino-terminal domain (ATD), a ligand-binding domain (LBD), a transmembrane domain (TMD), and an intracellular C-terminal domain (CTD). GRIA4-containing AMPARs function as ligand-gated cation channels, allowing Na+ influx and K+ efflux upon binding L-glutamate, leading to rapid depolarization in neurons. GRIA4 is highly expressed throughout various regions of the brain including the hippocampal formation, amygdala, basal ganglia, and midbrain. Some haplotypes of GRIA4 have shown positive associations with schizophrenia.

Other names
GluA4GLUR4GLURDGluR-Dglutamate ionotropic receptor AMPA type subunit 4
02

Mechanism of action

Ligand-gated ion channel activation

03

Biological functions

Ligand-gated cation channel activityFast excitatory neurotransmissionSynaptic plasticityRegulation of membrane potential
04

Disease associations

SchizophreniaNeurodevelopmental disorders
05

Safety considerations

Potential for excitotoxicityOff-target effects on other glutamate receptors

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