AMPA receptor potentiators: from drug design to cognitive enhancement

Curr Opin Pharmacol. 2015 Feb;20:46-53. doi: 10.1016/j.coph.2014.11.002. Epub 2014 Nov 27.

Abstract

Positive allosteric modulators of ionotropic glutamate receptors have emerged as a target for treating cognitive impairment and neurodegeneration, but also mental illnesses such as major depressive disorder. The possibility of creating a new class of pharmaceutical agent to treat refractive mental health issues has compelled researchers to redouble their efforts to develop a safe, effective treatment for memory and cognition impairments. Coupled with the more robust research methodologies that have emerged, including more sophisticated high-throughput-screens, higher resolution structural biology techniques, and more focused assessment on pharmacokinetics, the development of positive modulators of AMPA receptors holds great promise. We describe recent approaches that improve our understanding of the basic physiology underlying memory and cognition, and their application toward promoting human health.

Publication types

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

MeSH terms

  • Allosteric Regulation / drug effects
  • Animals
  • Cognition / drug effects
  • Cognition Disorders / drug therapy*
  • Cognition Disorders / physiopathology
  • Depressive Disorder, Major / drug therapy
  • Depressive Disorder, Major / physiopathology
  • Drug Design*
  • High-Throughput Screening Assays
  • Humans
  • Memory Disorders / drug therapy
  • Memory Disorders / physiopathology
  • Mental Disorders / drug therapy
  • Mental Disorders / physiopathology
  • Receptors, AMPA / drug effects*
  • Receptors, AMPA / metabolism

Substances

  • Receptors, AMPA