Drug intelligence / Profile preview

alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid

Development stage
Unknown
Modality
Small Molecules
01

Overview

alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) is a synthetic, non-proteinogenic amino acid that acts as a potent and highly selective orthosteric agonist of the AMPA subtype of ionotropic glutamate receptors (AMPARs). AMPARs are ligand-gated cation channels composed of tetrameric assemblies of four subunits (GluA1–GluA4, encoded by GRIA1–GRIA4) that mediate the vast majority of fast excitatory synaptic transmission in the mammalian central nervous system. By binding to the orthosteric site of these receptors, AMPA induces a conformational change that opens the channel pore, allowing the influx of sodium (and in some cases calcium) ions, which depolarizes the postsynaptic membrane. AMPA is widely utilized as a standard pharmacological research tool and reference agonist in neurobiology to characterize non-NMDA receptor currents, study synaptic plasticity (such as long-term potentiation and long-term depression), and model excitotoxicity in vitro and in vivo.

Other names
(R,S)-AMPA(RS)-AMPAAMPAalpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionatealpha-amino3-hydroxy-5-methyl-4-isoxazolepropionatealpha-amino 3-hydroxy-5-methyl-4-isoxazolepropionatealpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acidalpha-amino3-hydroxy-5-methylisoxazole-4-propionic acidalpha-amino 3-hydroxy-5-methylisoxazole-4-propionic acid
02

Targets

GRIA1 (AMPA receptor subunit GluA1)GRIA2 (AMPA receptor subunit GluA2)GRM3 (mGluR3)GRM4 (mGluR4)

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