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Glutamate receptor 2 (GluA2) (GluA2)

Target
GluA2
Molecular classification
Ion channel, Receptor
01

Overview

The Glutamate receptor 2 (GluA2) is a primary subunit of the ionotropic AMPA-type glutamate receptor, which mediates the majority of fast excitatory synaptic transmission in the mammalian central nervous system (UniProt P42262). A defining feature of GluA2 is the post-transcriptional RNA editing of the Q/R site in its pore-forming loop, which renders the receptor impermeable to calcium ions and protects neurons from excitotoxic damage (PubMed: 25231077). In the context of disease, reduced GluA2 editing or expression is linked to motor neuron loss in amyotrophic lateral sclerosis (ALS) and neuronal death following ischemic stroke (PubMed: 22522442). GluA2 is a significant therapeutic target for epilepsy, where non-competitive antagonists like perampanel are used to dampen excessive glutamatergic signaling and prevent seizures (PubChem CID 10403507). Furthermore, the receptor is involved in synaptic plasticity mechanisms such as long-term potentiation and depression, making it a focus for research into cognitive enhancement and neurodegenerative disorders like Alzheimer's disease (PubMed: 21172320).

Other names
GRIA2GluR2Glutamate ionotropic receptor AMPA type subunit 2GluR-K2HBGR2GLURB
02

Mechanism of action

Non-competitive antagonism, competitive antagonism, and positive allosteric modulation of the AMPA receptor complex.

03

Biological functions

Signal transductionOther
04

Disease associations

Neurodegenerative diseaseOther
05

Safety considerations

DizzinessSomnolenceAtaxiaAggressionIrritabilityCognitive impairmentRisk of falls
06

Interacting drugs

Perampanel

5 more in the full profile.

07

Biomarkers

Anti-GluA2 antibodiesCSF GluA2 protein levels[11C]CPPC PET imaging

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