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0.0
0 reviewsISBN 10: 0123786479
ISBN 13: 9780123786470
Author: Thomas Blackburn
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.
Articles written by leading investigators in the field
Informs and updates on all the latest developments
Introduction
GABAB Receptor Ligands
Receptor Distribution
Allosteric Modulation
Receptor Function
Potential Therapeutic Significance
Conclusion
Chemistry and Pharmacology of GABAB Receptor Ligands
GABAB Receptor Agonists
GABAB Receptor Partial Agonists
Positive Modulators of GABAB Receptors
GABAB Receptor Antagonists
Conclusion
Heterodimerization of the GABAB Receptor: Implications for GPCR Signaling and Drug Discovery
Identification of the GABAB Receptors
The Phylogeny of GABAB Receptors in Different Species
Structure of GABAB Receptors
Function of the GABAB Receptor Heterodimer
GABAB as a Model System for GPCR Dimerization
Conclusions
Mechanisms of GABAB Receptor Exocytosis, Endocytosis, and Degradation
Cell-Surface Trafficking of GABAB Receptors
Endocytosis of GABAB Receptors
Degradation of GABAB Receptors
Conclusions
Functional Modulation of GABAB Receptors by Protein Kinases and Receptor Trafficking
Phosphorylation of GABABR and Its Functional Modulation
Phosphorylation-Independent Desensitization of GABABRs by Protein Kinases
GABABR Endocytic Sorting and the Control of Receptor Cell Surface Stability
GABABR Phosphorylation and Diseases
Conclusion
GABAB Receptor Coupling to G-proteins and Ion Channels
GABAB Receptor Structure
GABAB Receptor Protein Expression
GABAB Receptor Effectors
Formation of a Macromolecular Signaling Heterocomplex
GABAB Receptor-Dependent Desensitization
Conclusion
GABAB Receptor-Mediated Modulation of Metabotropic Glutamate Signaling and Synaptic Plasticity in Central Neurons
Synaptic Organization Around Cerebellar Purkinje Cells
Possible Ligands for GABABR in Cerebellar Purkinje Cells
Functions of GABABR Near the Excitatory Synapses
Possible Physiological Significance of GABABR-Mediated Effects on mGluR1 Signaling
Conclusion
GABA Transporter GAT1: A Crucial Determinant of GABAB Receptor Activation in Cortical Circuits?
The Plasma Membrane GABA Transporter
Cellular and Subcellular Localization of GABABRs and GAT1
GABABR Activation by GABA Released from Endogenous Sources
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Tags: Thomas Blackburn, GABAReceptor, Pharmacology