Glutamate receptor ionotropic, AMPA type (AMPAR)

The AMPA receptor (AMPAR) is a major subclass of ionotropic glutamate receptors that mediates the vast majority of fast excitatory neurotransmission in the mammalian central nervous system (StatPearls, NBK541031). Structurally, AMPARs are tetramers composed of combinations of four subunits (GluA1-4), which form a central pore permeable to cations such as sodium and, depending on subunit composition, calcium (UniProt, P42261; PubMed, 21852445). These receptors are central to synaptic plasticity, specifically long-term potentiation (LTP) and long-term depression (LTD), which are the cellular hallmarks of learning and memory. Dysregulation or overactivation of AMPARs (excitotoxicity) is linked to several neurological disorders, including epilepsy, where excessive excitatory signaling triggers seizures, and neurodegenerative diseases like ALS and Alzheimer's (NCBI, PMC6060416; PubMed, 24659437). Pharmacologically, AMPARs are targeted by non-competitive antagonists like perampanel to control seizures by reducing neuronal hyperexcitability, while positive allosteric modulators (Ampakines) are being investigated for cognitive enhancement in psychiatric conditions (PubMed, 29631610).

Other names

Alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptorAMPARQuisqualate receptorIonotropic glutamate receptor, AMPA-typeGluAGRIA

Non-competitive antagonism (e.g., Perampanel), Positive allosteric modulation (e.g., Ampakines), Competitive antagonism