AMPA-type glutamate receptor (GluA2-lacking)

AMPA-type glutamate receptors are tetrameric ligand-gated ion channels predominantly mediating fast excitatory neurotransmission in the central nervous system. Each receptor is formed by different combinations of the GluA1–GluA4 (GluR1–GluR4) subunits. The presence or absence of the GluA2 subunit dictates functional properties, most critically the receptor’s permeability to calcium ions (Ca2+). GluA2-lacking AMPA receptors—composed of GluA1, GluA3, and/or GluA4 subunits—are permeable to Ca2+, exhibit inward rectification, and play crucial roles in synaptic plasticity, but are also associated with increased neuronal vulnerability to excitotoxicity. GluA2-lacking AMPA receptors are key functional subtypes implicated in neurological diseases and represent important therapeutic targets[1][3][5].

Other names

GluA2-lacking AMPA receptorGluR2-lacking AMPA receptorCalcium-permeable AMPA receptor (CP-AMPAR)GluA2(–) AMPA receptorGluR2(–) AMPA receptor

Competitive antagonism at the glutamate binding site - Non-competitive (allosteric) antagonism at sites distinct from the agonist - Block of calcium-permeable ion flux through AMPAR channel