Partial agonists and subunit selectivity at NMDA receptors

Chemistry. 2010 Dec 17;16(47):13910-8. doi: 10.1002/chem.201001366.

Abstract

Subunit-selective ligands for glutamate receptors remains an area of interest as glutamate is the major excitatory neurotransmitter in the brain and involved in a number of diseased states in the central nervous system (CNS). Few subtype-selective ligands are known, especially among the N-methyl-D-aspartic acid (NMDA) receptor class. Development of these ligands seems to be a difficult task because of the conserved region in the binding site of the NMDA receptor subunits. A few scaffolds have been developed showing potential to differentiate between the NMDA receptors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Binding Sites
  • Crystallography, X-Ray
  • Excitatory Amino Acid Agonists / chemistry*
  • Glutamates / chemistry*
  • Glutamates / metabolism
  • Ligands
  • Models, Molecular
  • Molecular Sequence Data
  • Receptors, Glutamate / chemistry*
  • Receptors, Glutamate / metabolism
  • Receptors, Metabotropic Glutamate / chemistry*
  • Receptors, Metabotropic Glutamate / metabolism*
  • Receptors, N-Methyl-D-Aspartate / chemistry*
  • Receptors, N-Methyl-D-Aspartate / metabolism
  • alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid / chemistry*

Substances

  • Excitatory Amino Acid Agonists
  • Glutamates
  • Ligands
  • Receptors, Glutamate
  • Receptors, Metabotropic Glutamate
  • Receptors, N-Methyl-D-Aspartate
  • alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid