Glutamate ionotropic receptor AMPA type subunit 2-containing receptor (GluA2-containing AMPAR) (GluA2-containing AMPAR)

The Glutamate ionotropic receptor AMPA type subunit 2-containing receptor (GluA2-containing AMPAR) is a primary mediator of fast excitatory synaptic transmission in the central nervous system (Traynelis et al., 2010, Pharmacological Reviews). These receptors are typically heterotetrameric complexes, where the inclusion of the GluA2 subunit critically dictates the channel's biophysical properties, most notably its permeability to calcium ions (Isaac et al., 2007, Neuron). In a healthy adult brain, nearly all GluA2 subunits undergo post-transcriptional RNA editing at the Q/R site, which renders the receptor calcium-impermeable and protects neurons from calcium-induced excitotoxicity (Kwak and Weiss, 2006, Neurobiology of Disease). Dysregulation of GluA2 expression or a failure in the Q/R editing process is strongly implicated in the pathogenesis of neurodegenerative diseases like Amyotrophic Lateral Sclerosis (ALS) and conditions such as epilepsy and ischemic stroke (Wright and Vissel, 2012, Frontiers in Molecular Neuroscience). Pharmacologically, these receptors are targeted by non-competitive antagonists like perampanel, which bind to an allosteric site on the receptor to reduce over-excitation and manage seizures (Hanada et al., 2011, Epilepsia). Understanding the specific composition and editing status of GluA2-containing receptors remains a vital area of research for developing neuroprotective strategies and precision therapies for neurological disorders (UniProt, P42262).

Other names

GRIA2-containing AMPA receptorGluR2-containing AMPA receptorGluR-B containing AMPA receptorAMPA receptor subunit 2

Non-competitive antagonism of the AMPA receptor ion channel to inhibit glutamate-induced depolarization.