title: The AMPA receptor as a therapeutic target: current perspectives and emerging possibilities.
abstract: 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.
authors.affiliation: University of Nottingham, University Park, Nottingham, NG7 2RD, UK. ian.mellor@nottingham.ac.uk
authors.forename: Ian R
authors.initials: IR
authors.lastname: Mellor
mesh_terms: D000818:Animals; D055808:Drug Discovery; D018690:Excitatory Amino Acid Agonists / Q000737:chemistry* / Q000494:pharmacology*; D018691:Excitatory Amino Acid Antagonists / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D009422:Nervous System Diseases / Q000188:drug therapy / Q000378:metabolism; D018091:Receptors, AMPA / Q000819:agonists / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000378:metabolism; D017470:Receptors, Glutamate / Q000737:chemistry / Q000378:metabolism*
chemical_list: D018690:Excitatory Amino Acid Agonists; D018691:Excitatory Amino Acid Antagonists; D018091:Receptors, AMPA; D017470:Receptors, Glutamate; C492973:alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid subtype glutamate receptor, human