GABAB Receptor, 1st ed. 2016 The Receptors Series, Vol. 29

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

Giancarlo Colombo is a researcher at the Neuroscience Institute, Section of Cagliari, National Research Council of Italy. He has previously worked at the Laboratory of Physiologic and Pharmacologic Studies, National Institute on Alcohol Abuse and Alcoholism, Rockville, MD, USA, and the Department of Physiology and Pharmacology, Bowman Gray School of Medicine, Wake Forest University, Winston-Salem, NC, USA.

His research interest is primarily on neurobiology and pharmacology of alcohol use disorder, with focus on the role of GABAB receptor in the control of multiple alcohol-related behaviors and the development of GABAB receptor ligands as possible pharmacotherapies for alcohol use disorder.

Focuses on recent therapeutic applications and future potential for drug discovery

Bench-to-bedside" translational approach

Explores different perspectives from various fields of study including medical medicinal chemistry, molecular biology, physiology, and preclinical and clinical pharmacology

Explores specific diseases and disorders in which GABAB receptors have been implicated recently