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Glutamate receptor ionotropic AMPA type subunit 1 (GluA1) and subunit 2 (GluA2) are principal subunits of the AMPA-type ionotropic glutamate receptor, which is a ligand-gated cation channel responsible for fast excitatory synaptic transmission in the mammalian central nervous system. These receptors are tetrameric complexes typically consisting of combinations of GluA1–4 subunits. GluA1 and GluA2 are the most prevalent and functionally significant in synaptic plasticity, memory, learning, and several neuropathologies. Upon glutamate binding, AMPA receptors open to allow sodium and, depending on subunit composition, calcium influx, resulting in neuronal depolarization. Abnormal function or expression is implicated in a variety of neurological and neuropsychiatric disorders.
Antagonism of glutamate binding (competitive/non-competitive antagonists) - Inhibition of cation conductance through receptor-associated ion channel - Reduction of excitatory neurotransmission - Allosteric modulation
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