A Brief History and the Significance of the GABAB Receptor.

γ-Aminobutyric acid (GABA) is the main inhibitory neurotransmitter in the brain. GABA type B (GABAB) receptors (GABABRs) are the only metabotropic G protein-coupled receptors for GABA and can be found distributed not only in the central nervous system, but also in the periphery. This chapter introduces important, fundamental knowledge related to GABABR function and the various potential therapeutic applications of the development of novel GABABR-active compounds, as documented through extensive studies presented in subsequent chapters of this Current Topic in Behavioral Neurosciences volume on the role of the neurobiology of GABABR function. The compounds that have received increased attention in the last few years compared to GABABR agonists and antagonists - the positive allosteric modulators - exhibit better pharmacological profiles and fewer side effects. As we continue to unveil the mystery of GABABRs at the molecular and cellular levels, we further understand the significance of these receptors. Future directions should aim for developing highly selective GABABR compounds for treating neuropsychiatric disorders and their symptomatology.