Ligands targeting the excitatory amino acid transporters (EAATs).
This review provides an overview of ligands for the excitatory amino acid transporters (EAATs), a family of high-affinity glutamate transporters localized to the plasma membrane of neurons and astroglial cells. Ligand development from the perspective of identifying novel and more selective tools for elucidating transporter subtype function, and the potential of transporter ligands in a therapeutic setting are discussed. Acute pharmacological modulation of EAAT activity in the form of linear and conformationally restricted glutamate and aspartate analogs is presented, in addition to recent strategies aimed more toward modulating transporter expression levels, the latter of particular significance to the development of transporter based therapeutics.
Dunlop
John
J
Neuroscience Discovery Research, Wyeth Research, CN 8000, Princeton NJ 08543, USA. dunlopj@wyeth.com
Butera
John A
JA
D001224:Aspartic Acid / Q000031:analogs & derivatives; D018690:Excitatory Amino Acid Agonists / Q000737:chemistry* / Q000494:pharmacology*; D018691:Excitatory Amino Acid Antagonists / Q000737:chemistry* / Q000494:pharmacology*; D005786:Gene Expression Regulation; D018698:Glutamic Acid / Q000031:analogs & derivatives
D018690:Excitatory Amino Acid Agonists; D018691:Excitatory Amino Acid Antagonists; D001224:Aspartic Acid; D018698:Glutamic Acid