Kainate receptor agonists, antagonists and allosteric modulators

Curr Pharm Des. 2002;8(10):873-85. doi: 10.2174/1381612024607108.

Abstract

Interest in kainate receptors has increased over the past few years. Our understanding of their physiology and pharmacology has improved markedly since their original cloning and expression in the early 1990s. For example, agonist profiles at recombinant kainate receptors have been used to identify and distinguish kainate receptors in neurons. Furthermore, the development of selective antagonists for kainate receptor subtypes has increased our understanding of the functional roles of kainate receptors in neurons and synaptic transmission. In this review we described the activity of agonists and antagonists at kainate receptors and their selectivity profiles at NMDA and non-NMDA receptors.

Publication types

  • Review

MeSH terms

  • Allosteric Regulation
  • Animals
  • Excitatory Amino Acid Agonists / chemistry*
  • Excitatory Amino Acid Agonists / pharmacology*
  • Excitatory Amino Acid Antagonists / chemistry*
  • Excitatory Amino Acid Antagonists / pharmacology*
  • Molecular Structure
  • Neurons / drug effects
  • Neurons / metabolism
  • Receptors, Kainic Acid / agonists*
  • Receptors, Kainic Acid / antagonists & inhibitors*
  • Receptors, Kainic Acid / genetics
  • Receptors, Kainic Acid / metabolism
  • Receptors, N-Methyl-D-Aspartate / agonists
  • Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors
  • Structure-Activity Relationship
  • Substrate Specificity

Substances

  • Excitatory Amino Acid Agonists
  • Excitatory Amino Acid Antagonists
  • Receptors, Kainic Acid
  • Receptors, N-Methyl-D-Aspartate