GABA(B) RECEPTORS - TARGETS FOR DRUG DEVELOPMENT

GABA is a major inhibitory neurotransmitter in the CNS where it regula tes neuronal excitability. These actions of GABA are mediated through GABA receptor subtypes, one of which is the GABA(B) receptor (GBR). Th e 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 au thors emphasize the current knowledge of the structure-action profile of compounds active at GBRs, characterizing their physiology and pharm acology and highlighting their potential as targets for drug developme nt.