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The AMPA receptor (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor, also known as AMPAR or quisqualate receptor) is a type of ionotropic glutamate receptor that mediates fast excitatory neurotransmission in the central nervous system (CNS). It functions primarily as a ligand-gated cation channel, allowing the flow of sodium (Na⁺) and, depending on subunit composition, calcium (Ca²⁺) ions into postsynaptic neurons upon activation by glutamate. The AMPA receptor is a tetramer composed of four subunits: GluA1–GluA4, encoded by genes GRIA1–GRIA4. Subunit composition determines functional properties such as ion permeability and gating kinetics. AMPA receptors play essential roles in synaptic plasticity mechanisms such as long-term potentiation/depression, learning/memory formation, and general cognitive processing.
Agonists bind to the ligand-binding domain, opening the cation channel and allowing influx of Na+ and Ca2+ ions, leading to neuronal depolarization and excitation. Antagonists block this channel, preventing ion flow and inhibiting neuronal excitation.
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