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

GluA2-containing AMPA receptors are a major class of ionotropic glutamate receptors that mediate fast excitatory neurotransmission throughout the central nervous system (UniProt P42262). The inclusion of the GluA2 (formerly GluR2) subunit is a critical regulatory feature, as post-transcriptional RNA editing at the Q/R site renders these receptors impermeable to calcium ions, thereby protecting neurons from excitotoxic damage (Wright & Vissel, 2012). These receptors play a fundamental role in synaptic plasticity, including long-term potentiation (LTP) and long-term depression (LTD), which are the cellular correlates of learning and memory (StatPearls, 2023). Dysregulation of GluA2, such as reduced expression or defective RNA editing, is strongly associated with the pathogenesis of amyotrophic lateral sclerosis (ALS), where increased calcium influx leads to motor neuron death (Kwak & Kawahara, 2005). In clinical practice, drugs like perampanel act as non-competitive antagonists of these receptors to manage partial-onset seizures by dampening excessive excitatory signaling (French et al., 2012). Consequently, GluA2-containing AMPA receptors represent a pivotal therapeutic target for a wide range of neurological and psychiatric disorders characterized by glutamatergic imbalance.

Other names

GluR2-containing AMPA receptorGluR-B containing AMPA receptorGRIA2-containing AMPA receptorCalcium-impermeable AMPA receptorGluA2-containing alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor

Non-competitive antagonism, competitive antagonism, or allosteric modulation of the ion channel to regulate sodium and potassium conductance while maintaining calcium impermeability.