An up-to-date comprehensive overview of the GABA B receptor system with a particular focus on the most recent therapeutic applications and potential. This receptor system has recently been implicated in several diseases and disorders including gastroesophageal reflux disease, epilepsy, mood disorders, depression, and alcohol and substance use disorder. The authors, leading researchers in the field, explore a number of approaches, including medicinal chemistry, molecular biology, physiology, and preclinical and clinical pharmacology. This overview provides a translational perspective on the potential of the GABA B receptor pharmacology.

1. Historical Perspectives on the GABAB Receptor.- Section 1. Chemistry.- 2. Chemistry of GABAB Receptor Ligands: Focus on Agonists and Antagonists.- 3. Chemistry of GABAB Receptor Ligands: Focus on Positive Allosteric Modulators.- Section 2. Molecular Biology, Biochemistry, & Physiology.- 4. Molecular Structure and Trafficking of the GABAB Receptor.- 5. Distribution and Localization of the GABAB Receptor.- 6. Activation Mechanism and Allosteric Properties of the GABAB Receptor.- 7. Modulation of Neurotransmission by the GABAB Receptor.- 8. GABAB Receptor Functions In The Mesolimbic Dopamine System.- Section 3. Pharmacology.- 9. Drug Discrimination Studies for Investigations on the Mechanisms of Action of GABAB Receptor Ligands.- 10. Targeting the GABAB Receptor for the Treatment of Epilepsy.- 11. Targeting the GABAB Receptor for the Treatment of Pain.- 12. Targeting the GABAB Receptor for the Treatment of Psychiatric Disorders.- 13. Targeting the GABAB Receptor for the Treatment of Fragile X Syndrome and Autism Spectrum Disorders.- 14. Targeting the GABAB Receptor for the Treatment of Substance Use Disorder.- 15. Targeting the GABAB Receptor for the Treatment of Alcohol Use Disorder.- 16. Targeting GABAB Receptors for the Treatment of Gastroesophageal Reflux Disease and Chronic Cough.- 17. Baclofen: Therapeutic Use and Potential of the Prototypic GABAB Receptor Agonist.- 18. Allosteric Modulators: The New Generation of GABAB Receptor Ligands.- 19. GABAB Receptor Antagonists as Cognition Enhancers.