Therapeutic potential of GABAB receptor ligands in drug addiction, anxiety, depression and other CNS disorders

Glutamate and γ-aminobutyric acid (GABA) are the major excitatory and inhibitory neurotransmitter systems, respectively in the central nervous system (CNS). Dysregulation, in any of these or both, has been implicated in various CNS disorders. GABA acts via ionotropic (GABAA and GABAC receptor) and metabotropic (GABAB) receptor. Dysregulation of GABAergic signaling and alteration in GABAB receptor expression has been implicated in various CNS disorders. Clinically, baclofen-a GABAB receptor agonist is available for the treatment of spasticity, dystonia etc., associated with various neurological disorders. Moreover, GABAB receptor ligands has also been suggested to be beneficial in various neuropsychiatric and neurodegenerative disorders. The present review is aimed to discuss the role of GABAB receptors and the possible outcomes of GABAB receptor modulation in CNS disorders.