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.