Excitatory amino acid receptor (EAAR) (EAAR)

Excitatory amino acid receptors are a diverse group of membrane proteins that mediate the signals of the primary excitatory neurotransmitters in the central nervous system, primarily L-glutamate and L-aspartate (StatPearls, NBK507814). These receptors are categorized into two main functional classes: ionotropic receptors (iGluRs), which are ligand-gated ion channels including NMDA, AMPA, and kainate receptors, and metabotropic receptors (mGluRs), which are G protein-coupled receptors (IUPHAR, Guide to Pharmacology). They are essential for fundamental brain functions such as fast synaptic transmission, synaptic plasticity, and the cellular mechanisms underlying learning and memory (Neuroscience, NBK10802). Dysregulation of the excitatory amino acid system is a key factor in various neurological and psychiatric conditions, including epilepsy, schizophrenia, and depression (Nature Reviews Drug Discovery, nrd.2017.228). Furthermore, excessive activation of these receptors can lead to excitotoxicity, a process of neuronal death that contributes significantly to the pathology of stroke and neurodegenerative diseases like Alzheimer's and Amyotrophic Lateral Sclerosis (PubMed, 28937951). Therapeutic interventions targeting these receptors include NMDA receptor antagonists like memantine for Alzheimer's disease and ketamine for treatment-resistant depression, although their clinical use is often constrained by side effects such as dissociation, cognitive impairment, and potential neurotoxicity.

Other names

Glutamate receptorGluREAA receptorExcitatory amino acidIonotropic glutamate receptorMetabotropic glutamate receptor

Antagonism of ionotropic glutamate receptors (NMDA, AMPA) or modulation of metabotropic glutamate receptors to regulate excitatory neurotransmission and prevent excitotoxicity.