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

Blanca Angelica Vega AlanisMaria Teresa IorioLuca L Silva Konstantina Bampali Margot Ernst Michael Schnürch Marko D Mihovilovic

Published in: Molecules (Basel, Switzerland) (2020)

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.

Keyphrases

small molecule
clinical trial
binding protein
signaling pathway
risk assessment
open label
amino acid