1. Historical Perspective and Emergence of the GABAB Receptor Norman Bowery 2. Chemistry of GABAB Receptor Ligands Wolfgang Froestl 3. Heterodimerization of the GABAB Receptor - Implications for GPCR Signaling and Drug Discovery Fiona H. Marshall and Steven M. Foord 4. Mechanisms of GABAB Receptor Exocytosis, Endocytosis and Degradation Deitmar Benke 5. Functional Modulation of GABAB Receptors by Protein Kinases and Receptor Trafficking Miho Terunuma, Andres Couve, Menelas N. Pangalos, and Stephen J. Moss 6. GABAB Receptor Coupling to G Proteins and Ion Channels Claire Padgett and Paul A. Slesinger 7. GABAB Receptor-mediated Modulation of Metabotropic Glutamate Signaling and Synaptic Plasticity in Central Neurons M. Kano and Toshihide Tabata 8. GABA Transporter GAT1: A Crucial Determinant of GABAB Receptor Activation in Cortical Circuits? Guillermo Gonzalez-Burgos 9. The Role of GABAB Receptors in Cortical Network Activity Michael M. Kohl and Ole Paulsen 10. GABAB Receptors: Physiology Functions and Mechanisms of Diversity Andree Pinard, Riad Seddik, and Bernhard Bettler 11. Role of GABAB Receptors in Autonomic Control of Systemic Blood Pressure De-Pei Li and Hui-Lin Pan 12. GABAB Receptor Agonism as a Novel Therapeutic Modality in the Treatment of Gastroesophageal Reflux Disease Anders Lehmann, Jorgen Jensen, and Guy E. Boeckxstaens 13. GABAB Receptors in Reward Processes Styliani Vlachou and Athina Markou 14. GABAB Receptors in Addiction and Its Treatment David J. Nutt, Anne Lingford-Hughes, Laurence John Reed, and Robin J. Tyacke 15. GABAB - GIRK2 Mediated Signaling in Down Syndrome Nathan Cramer, Tyler Best, and Zygmunt Galdzicki 16. GABAB Receptors and Depression: Current Status John F. Cryan and David A. Slattery 17. GABAB Receptors in Drosophila Hari Manev and Svetlana Dzitoyeva
This monograph was assembled to honor Professor Norman Bowery and his work on the 30th anniversary of his discovery of the GABAB receptor. In the present volume, leading neuroscientists from academia and industry provide a perspective of current research, both basic and translational, in the discovery of drugs acting at the GABAB receptor. The topics covered provide a comprehensive review of the field and the current state of research in this area. Included are chapters on the chemistry of GABAB agonists and antagonists, on the genetics and molecular composition of the site, its regulation and trafficking, and its role in controlling cellular, autonomic, and behavioral function. There are also chapters describing the potential clinical utility of drugs regulating GABAB activity receptor in the areas of hypertension, gastroesophageal reflux disease, Down syndrome, depression, and substance abuse.
The information contained in this text will be of particular interest to neuroscientists in general and to neuropharmacologists in particular.