4.7 Article

Developing a complete pharmacology for AMPA receptors: A perspective on subtype-selective ligands

Journal

BIOORGANIC & MEDICINAL CHEMISTRY
Volume 18, Issue 4, Pages 1381-1387

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.12.072

Keywords

AMPA receptor; Subtype-selective ligand; Agonist; Antagonist; Polyamine toxin; Pore blocker; Allosteric modulator

Funding

  1. Sandler Foundation
  2. Wheeler Center
  3. National Institutes of Health
  4. McKnight Foundation

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AMPA receptors are a family of ligand-gated ion channels that play central roles in rapid neural signaling and in regulation of synaptic strength. Additionally, these receptors are implicated in a number of major psychiatric and neurological diseases. A comprehensive understanding of the roles that AMPA receptors play in the mammalian nervous system has been hampered by the dearth of ligands available to select between individual AMPA receptors subtypes. Here we provide a perspective on opportunities for developing a complete pharmacology for AMPA receptors. (C) 2010 Elsevier Ltd. All rights reserved.

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