Pyrazolopyridinones as functionally selective GABAA ligands

Bioorg Med Chem Lett. 2005 Nov 15;15(22):4998-5002. doi: 10.1016/j.bmcl.2005.08.006.

Abstract

2,5-Dihydro-3H-pyrazolo[4,3-c]pyridin-3-ones are GABAA receptor benzodiazepine binding site ligands, which can exhibit functional selectivity for the alpha3 subtype over the alpha1 subtype. SAR studies to optimize this functional selectivity are described.

MeSH terms

  • Azo Compounds / chemical synthesis*
  • Azo Compounds / chemistry
  • Azo Compounds / metabolism*
  • Ligands
  • Molecular Structure
  • Pyridines / chemical synthesis
  • Pyridines / chemistry*
  • Pyridines / metabolism*
  • Receptors, GABA-A / metabolism*
  • Sensitivity and Specificity
  • Structure-Activity Relationship
  • Substrate Specificity

Substances

  • Azo Compounds
  • Ligands
  • Pyridines
  • Receptors, GABA-A
  • pyridine