The AMPA receptor as a therapeutic target: current perspectives and emerging possibilities

Future Med Chem. 2010 May;2(5):877-91. doi: 10.4155/fmc.10.27.


The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) is a subtype of the ionotropic glutamate receptors that plays a prominent role in neurotransmission and is widespread throughout the CNS. Because of this, its malfunction can result in a multitude of nervous system diseases. This review looks at compounds that are able to modulate AMPAR function by binding to one of several sites on the receptor that either downregulate its function (competitive, noncompetitive and uncompetitive antagonists) or upregulate its function (positive modulators). It will also give an account of the various diseases that have implicated AMPAR dysfunction and how specific types of AMPAR modulator may be beneficial in their treatment. The AMPAR remains an unexploited but important therapeutic target.

Publication types

  • Review

MeSH terms

  • Animals
  • Drug Discovery
  • Excitatory Amino Acid Agonists / chemistry*
  • Excitatory Amino Acid Agonists / pharmacology*
  • Excitatory Amino Acid Antagonists / chemistry*
  • Excitatory Amino Acid Antagonists / pharmacology*
  • Humans
  • Nervous System Diseases / drug therapy
  • Nervous System Diseases / metabolism
  • Receptors, AMPA / agonists
  • Receptors, AMPA / antagonists & inhibitors
  • Receptors, AMPA / chemistry
  • Receptors, AMPA / metabolism
  • Receptors, Glutamate / chemistry
  • Receptors, Glutamate / metabolism*


  • Excitatory Amino Acid Agonists
  • Excitatory Amino Acid Antagonists
  • Receptors, AMPA
  • Receptors, Glutamate
  • alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid subtype glutamate receptor, human