GABAB receptors: targets for drug development

Abstract

GABA is a major inhibitory neurotransmitter in the CNS where it regulates neuronal excitability. These actions of GABA are mediated through GABA receptor sub-types, one of which is the GABAB receptor (GBR). The development of specific agonists and antagonists for GBRs has led to a better understanding of their functional roles, which mainly focus on the long-term modulation of neural activity. In this review, the authors emphasize the current knowledge of the structure-action profile of compounds active at GBRs, characterizing their physiology and pharmacology and highlighting their potential as targets for drug development.