Glutamate-based therapeutic approaches: ampakines

Curr Opin Pharmacol. 2006 Feb;6(1):82-8. doi: 10.1016/j.coph.2005.09.005. Epub 2005 Dec 19.

Abstract

Ampakines are a structurally diverse family of small molecules that positively modulate alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)-type glutamate receptors, and thereby enhance fast, excitatory transmission throughout the brain. Surprisingly, ampakines have discrete effects on brain activity and behavior. Because their excitatory synaptic targets mediate communication between cortical regions, serve as sites of memory encoding, and regulate the production of growth factors, ampakines have a broad range of potential therapeutic applications. Several of these possibilities have been tested with positive results in preclinical models; preliminary clinical work has also been encouraging.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Animals
  • Brain / drug effects
  • Brain / metabolism
  • Cognition Disorders / drug therapy
  • Cognition Disorders / metabolism
  • Dioxoles / pharmacology
  • Dioxoles / therapeutic use
  • Drug Evaluation, Preclinical
  • Excitatory Amino Acid Agonists / pharmacology*
  • Excitatory Amino Acid Agonists / therapeutic use
  • Humans
  • Memory / drug effects
  • Mental Disorders / drug therapy
  • Mental Disorders / metabolism
  • Nerve Growth Factors / metabolism
  • Oxazines / pharmacology
  • Oxazines / therapeutic use
  • Piperidines / pharmacology
  • Piperidines / therapeutic use
  • Protein Conformation
  • Receptors, AMPA / antagonists & inhibitors*
  • Receptors, AMPA / metabolism

Substances

  • 1-(1,4-benzodioxan-6-ylcarbonyl)piperidine
  • 1-(quinoxalin-6-ylcarbonyl)piperidine
  • Dioxoles
  • Excitatory Amino Acid Agonists
  • Nerve Growth Factors
  • Oxazines
  • Piperidines
  • Receptors, AMPA
  • 2H,3H,6aH-pyrrolidino(2'',1''-3',2')1,3-oxazino(6',5'-5,4)benzo(e)1, 4-dioxan-10-one