Section 1: Molecular Biology, Biochemistry, and Functioning of the GABAB Receptor -- GABAB Receptor: Molecular Organization, Function, and Alternative Drug Development by Targeting Protein-Protein Interactions -- GABAB Receptor Functioning: Focus on Allosteric Modulation -- Section 2: Pharmacology of Baclofen -- Historical Overview on Baclofen, the Only GABAB Receptor Agonist Approved and Available for Clinical Use -- Baclofen for the Treatment of Spasticity and Dystonia in Cerebral Palsy -- Baclofen for the Treatment of Cough -- Baclofen for the Treatment of Alcohol Use Disorder -- Baclofen Safety, Toxicity, Withdrawal, and Overdose -- Section 3: Chemistry and Pharmacology of Positive Allosteric Modulators -- Recent Advances on Chemistry of GABAB Receptor Allosteric Modulators -- GABAB Receptor Positive Allosteric Modulators: Novel Approaches for Drug Design and Discovery -- Recent Advances on GABAB Receptor Positive Allosteric Modulators as Potential Pharmacotherapies for Neuropsychiatric Disorders -- Recent Advances on GABAB Receptor Positive Allosteric Modulators as Potential Pharmacotherapies for Substance Use Disorder and Food Addiction -- Recent Advances on GABAB Receptor Positive Allosteric Modulators as Potential Pharmacotherapies for Alcohol Use Disorder -- Section 4: Miscellanea -- γ-Hydroxybutiric Acid: A GABAB/GHB Receptor Agonist with a Unique Neuropharmacological and Therapeutic Profile -- Naturally Occurring GABAB Receptor Ligands -- Norman G. Bowery: A Founding Father of the GABAB Receptor Research Field – Reflections on His Contribution.

This new edition presents an up-to-date, comprehensive overview of the GABAB receptor system, including a particular focus on the most recent therapeutic applications and potential. This receptor system has 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. The new edition is completely reworked and updated, featuring the latest pharmacological advances on baclofen and positive allosteric modulators.