Glutamate receptor ionotropic AMPA subunit 2 (GluA2)

Glutamate receptor ionotropic AMPA subunit 2 (GluA2) is a core component of AMPA-type ionotropic glutamate receptors, which are ligand-gated ion channels mediating the majority of fast excitatory neurotransmission in the mammalian brain[5][7]. GluA2 assembles with other AMPA receptor subunits (GluA1, GluA3, GluA4) to form homo- or heterotetrameric channels, with GluA2-containing assemblies predominating in most forebrain regions[8][1]. The presence of GluA2 is critically important: due to RNA editing at the Q/R site, its incorporation renders the receptor Ca²⁺-impermeable, thus protecting neurons from excitotoxic calcium entry[3]. AMPA receptors are essential for synaptic plasticity, learning, memory, and proper neural network functioning. Dysfunction or dysregulation of GluA2-containing AMPA receptors has been implicated in a wide variety of neurological and psychiatric diseases, including epilepsy, neurodegeneration, and mood disorders[7]. Drugs targeting GluA2-containing AMPA receptors act as antagonists or allosteric modulators and are of therapeutic interest for conditions such as epilepsy, stroke, and certain neuropsychiatric disorders[4][5].

Other names

GluA2AMPA receptor subunit GluA2Glutamate receptor 2Glutamate receptor ionotropic, AMPA 2GRIA2 (gene name)GluR2

Non-competitive antagonism of the AMPA receptor (e.g., perampanel blocks channel opening) Allosteric modulation at the ligand-binding domain or dimer interface (e.g., cyclothiazide, (R,R)-2b) Inhibition of ion flow (mainly sodium, some calcium) by antagonists