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Glutamate ionotropic receptor AMPA type subunit alpha

Molecular classification
Ion channel, Receptor, Ligand-gated ion channel, Ionotropic glutamate receptor
01

Overview

The "Glutamate ionotropic receptor AMPA type subunit alpha" refers to the **AMPA receptor subunits** (GluA1, GluA2, GluA3, GluA4), which are integral membrane proteins forming a class of ligand-gated ion channels in the central nervous system[1][4][5]. These subunits coassemble as tetramers to form the **AMPA receptor**, the primary mediator of **fast excitatory neurotransmission** in the mammalian brain[1][2][4]. Upon binding glutamate, the receptor undergoes conformational change that opens a central cation-conducting pore, principally allowing the passage of sodium (Na⁺) and, in some configurations, calcium (Ca²⁺)[1][3][6]. AMPA receptors are essential to synaptic plasticity mechanisms such as long-term potentiation and depression, and play a key role in learning and memory[5]. Dysfunction or altered regulation of AMPA receptors has been linked to numerous neurological and psychiatric diseases, including epilepsy, neurodegeneration, and cognitive disorders[5][6]. Several drugs (notably perampanel) target AMPA receptors for therapeutic purposes, usually as antagonists or negative modulators to reduce overexcitation seen in epilepsy and other CNS diseases[5]. Each subunit is encoded by a distinct gene (GRIA1–4); the alpha/α designation generically refers to any of the subunits, but is not standard nomenclature—each subunit should be specified as Glutamate ionotropic receptor AMPA type subunit 1 (GluA1), etc.[1][3]. **Note on correctness:** The term "Glutamate ionotropic receptor AMPA type subunit alpha" is not the canonical or specific standard molecular name, but appears to be a generic or composite. Each AMPA receptor subunit should be described as "Glutamate ionotropic receptor AMPA type subunit 1 (GluA1)" or similar for subunits 2–4[1][3]. Thus, "is_incorrect" is true in strict nomenclature.

Other names
GluA1GluA2GluA3GluA4GluR1GluR2GluR3GluR4GRIA1GRIA2GRIA3GRIA4AMPA receptor subunit alpha-1/2/3/4AMPAR subunitα-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor subunit
02

Mechanism of action

Noncompetitive antagonism (blockers of AMPA receptor action such as perampanel); Competitive antagonism (e.g., CNQX, NBQX); Negative allosteric modulation; Inhibition of ion channel conductance

03

Biological functions

Fast excitatory synaptic transmissionSignal transductionSynaptic plasticity (including learning and memory)Neuronal excitability
04

Disease associations

Neurodegenerative diseaseEpilepsyMood disordersDementiaIschemic brain injuryOther central nervous system disorders
05

Safety considerations

CNS adverse effects (e.g., confusion, psychosis, aggression with antagonists)Broad inhibition of excitatory neurotransmission may cause cognitive/psychiatric disturbancesPotential risk of seizures with certain modulators
06

Interacting drugs

Perampanel

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