GABAb receptor pharmacology : a tribute to Norman Bowery / edited by Thomas P. Blackburn. Volume 58.
- Amsterdam ; Boston : Elsevier, 2010.
- 1st ed.
- Physical Description:
- 1 online resource (521 pages).
- Additional Creators:
- Blackburn, Thomas
- Advances in pharmacology, 1054-3589
- Language Note:
- Cover; GABAB Receptor Pharmacology: A Tribute to Norman Bowery; Copyright; Contents; Contributors; Preface; Historical Perspective and Emergence of the GABAB Receptor; Abstract; I. Introduction; II. GABAB Receptor Ligands; III. Receptor Distribution; IV. Allosteric Modulation; V. Receptor Function; VI. Potential Therapeutic Significance; VII. Conclusion; References; Chemistry and Pharmacology of GABAB Receptor Ligands; Abstract; I. Introduction; II. GABAB Receptor Agonists; III. GABAB Receptor Partial Agonists; IV. Positive Modulators of GABAB Receptors; V. GABAB Receptor Antagonists, VI. ConclusionAcknowledgments; List of Nonstandard Abbreviations; References; Heterodimerization of the GABAB Receptor-Implications for GPCR Signaling and Drug Discovery; Abstract; I. Introduction; II. Identification of the GABAB Receptors; III. The Phylogeny of GABAB Receptors GABAB Receptors in DifferentSpecies; IV. Structure of GABAB Receptors; V. Function of the GABAB Receptor Heterodimer; VI. GABAB as a Model System for GPCR Dimerization; VII. Conclusions; Abbreviations; References; Mechanisms of GABAB Receptor Exocytosis, Endocytosis, and Degradation; Abstract; I. Introduction, II. Cell-Surface Trafficking of GABAB ReceptorsIII. Endocytosis of GABAB Receptors; IV. Degradation of GABAB Receptors; V. Conclusions; Acknowledgments; Abbreviations; References; Functional Modulation of GABAB Receptors by ProteinKinases and Receptor Trafficking; Abstract; I. Introduction; II. Phosphorylation of GABABR and Its Functional Modulation; III. Phosphorylation-Independent Desensitization of GABABRs by ProteinKinases; IV. GABABR Endocytic Sorting and the Control of Receptor Cell SurfaceStability; V. GABABR Phosphorylation and Diseases; VI. Conclusion; Acknowledgments; Abbreviations, and III. Possible Ligands for GABABR in Cerebellar Purkinje CellsIV. Functions of GABABR Near the Excitatory Synapses; V. Possible Physiological Significance of GABABR-Mediated Effects onmGluR1 Signaling; VI. Conclusion; Acknowledgments; Non-standard abbreviations; References; GABA Transporter GAT1: A Crucial Determinant of GABAB Receptor Activation in Cortical Circuits?; Abstract; I. Introduction; II. The Plasma Membrane GABA Transporter; III. Cellular and Subcellular Localization of GABABRsand GAT1; IV. GABABR Activation by GABA Released from EndogenousSources
- 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 molecu.
- 1282770039, 9781282770034, 9786612770036, 6612770031, 0123786487, 9780123786487, and 9780123786470
- V. GAT1 Activity and GABABR Activation
- Bibliography Note:
- ReferencesGABAB Receptor Coupling to G-proteins and Ion Channels; Abstract; I. Introduction; II. GABAB Receptor Structure; III. GABAB Receptor Protein Expression; Iv. GABAB Receptor Effectors; V. Formation of a Macromolecular Signaling Heterocomplex; VI. GABAB Receptor-Dependent Desensitization; VII. Conclusion; Abbreviations; References; GABAB Receptor-Mediated Modulation of Metabotropic Glutamate Signaling and Synaptic Plasticity in Central Neurons; Abstract; I. Introduction; II. Synaptic Organization Around Cerebellar Purkinje Cells and Includes bibliographical references and index.
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