Allosteric GABAA Receptor Modulators-A Review on the Most Recent Heterocyclic Chemotypes and Their Synthetic Accessibility

Molecules. 2020 Feb 24;25(4):999. doi: 10.3390/molecules25040999.

Abstract

GABAA receptor modulators are structurally almost as diverse as their target protein. A plethora of heterocyclic scaffolds has been described as modulating this extremely important receptor family. Some made it into clinical trials and, even on the market, some were dismissed. This review focuses on the synthetic accessibility and potential for library synthesis of GABAA receptor modulators containing at least one heterocyclic scaffold, which were disclosed within the last 10 years.

Keywords: GABAA modulators; allosteric modulators; heterocyclic modulators; heterocyclic synthesis; nitrogen heterocycles.

Publication types

  • Review

MeSH terms

  • Allosteric Regulation
  • Animals
  • Clinical Trials as Topic
  • GABA-A Receptor Agonists / chemical synthesis*
  • GABA-A Receptor Agonists / pharmacology
  • GABA-A Receptor Antagonists / chemical synthesis*
  • GABA-A Receptor Antagonists / pharmacology
  • Heterocyclic Compounds / chemical synthesis*
  • Heterocyclic Compounds / pharmacology
  • Humans
  • Molecular Structure
  • Receptors, GABA-A / chemistry*
  • Small Molecule Libraries / chemical synthesis*
  • Small Molecule Libraries / pharmacology
  • Structure-Activity Relationship

Substances

  • GABA-A Receptor Agonists
  • GABA-A Receptor Antagonists
  • Heterocyclic Compounds
  • Receptors, GABA-A
  • Small Molecule Libraries