The Serotonin Receptors: From Molecular Pharmacology to Human Therapeutics (The Receptors)

Leading Experts Comprehensively Examine The Current Understanding Of The Molecular And Structural Biology Of 5-ht Receptors And Their Pharmacological Use. The Authors Describe The Anatomical, Cellular, And Subcellular Distribution Of 5-ht Recptors And Demonstrate A Powerful Approach To Elulcidating Their Physiological Role Using Knockout Mice In Which The 5-ht Receptors Were Deleted. They Also Review Current Understanding Of The Physiological Role(s) Of 5-ht Receptors Based Mainly On Studies Performed In Genetically Engineered Mice. 1. Molecular Biology And Genomic Organization Of G Protein-coupled Serotonin Receptors / Wesley K. Kroeze And Bryan L. Roth -- 2. Structure And Function Reveal Insights In The Pharmacology Of 5-ht Receptor Subtypes / Richard B. Westkaemper And Bryan L. Roth -- 3. Polymorphic And Posttranscriptional Modifications Of 5-ht Receptor Structure : Functional And Pathological Implications / Marilyn A. Davies, Chiao-ying Chang And Bryan L. Roth -- 4. Strategies For The Development Of Selective Serotonergic Agents / Richard A. Glennon -- 5. 5-ht Receptor Signal Transduction Pathways / John R. Raymond, Justin H. Turner, Andrew K. Gelasco, Henry B. Ayiku, Sonya D. Coaxum, John M. Arthur And Maria N. Garnovskaya -- 6. Agonist-directed Trafficking Of 5-ht Receptor-mediated Signal Transduction / Kelly A. Berg And William P. Clarke --^ 7. Identification Of 5-ht[subscript 2] And 5- Ht[subscript 4] Receptor-interacting Proteins : A Proteomic Approach / Joel Bockaert, Carine Becamel, Lara Joubert, Sophie Gavarini, Aline Dumuis And Philippe Marin -- 8. 5-ht Receptor-associated Proteins (fraps) : Relevance For Targeting, Trafficking, And Signal Transduction / Zongqi Xia, Douglas J. Sheffler And Bryan L. Roth -- 9. Cellular And Subcellular Localization Of Serotonin Receptors In The Central Nervous System / Laurent Descarries, Virginia Cornea-hebert And Mustapha Riad -- 10. Chemical Neuroanatomy Of 5-ht Receptor Subtypes In The Mammalian Brain / Guadalupe Mengod, M. Teresa Vilaro, Roser Cortes, Juan F. Lopez-gimenez, Andreu Raurich And Jose M. Palacios -- 11. Modulation Of The Neuronal Activity And Neurotransmitter Release By 5- Ht[subscript 1a] And 5-ht[subscript 1b/1d] Receptors / Pau Celada, Albert Adell And Francesc Artigas --^ 12. Electrophysiology Of 5-ht[subscript 2a] Receptors And Relevance For Hallucinogen And Atypical Antipsychotic Drug Actions / Evelyn K. Lambe And George K. Aghajanian -- 13. The Emergence Of 5-ht[subscript 2b] Receptors As Targets To Avoid In Designing And Refining Pharmaceuticals / Vincent Setola And Bryan L. Roth -- 14. The 5-ht[subscript 3] Receptor / Andrew J. Thompson, Li Zhang And Sarah C.r. Lummis -- 15. 5-ht[subscript 3] And 5-ht[subscript 4] Receptors As Targets For Drug Discovery For Dementia / Frank Lezoualc'h And Magali Berthouze -- 16. Electrophysiological Properties Of G[alpha][subscript S]- Coupled 5-ht Receptors (5-ht[subscript 4], 5-ht[subscript 6], 5-ht[subscript 7]) / Rodrigo Andrade -- 17. 5- Ht[subscript 6] Receptors As Targets For The Treatment Of Cognitive Deficits In Schizophrenia / Rudy Schreiber, Andrew Sleight And Marie Woolley --^ 18. 5-ht[subscript 7] Receptors As Favorable Pharmacological Targets For Drug Discovery / Peter B. Hedlung And J. Gregor Sutcliffe -- 19. Serotonin System Gene Knockouts : A Story Of Mice With Implications For Man / Miles Berger And Laurence H. Tecott -- 20. Effects Of Serotonin-related Gene Deletion On Measures Of Anxiety, Depression, And Neurotransmission / Anita J. Bechtholt And Irwin Lucki. Edited By Bryan L. Roth. Includes Bibliographical References And Index. Mode Of Access: World Wide Web. Front Matter....Pages i-xvii Molecular Biology and Genomic Organization of G Protein-Coupled Serotonin Receptors....Pages 1-38 Structure and Function Reveal Insights in the Pharmacology of 5-HT Receptor Subtypes....Pages 39-58 Polymorphic and Posttranscriptional Modifications of 5-HT Receptor Structure....Pages 59-90 Strategies for the Development of Selective Serotonergic Agents....Pages 91-142 5-HT Receptor Signal Transduction Pathways....Pages 143-206 Agonist-Directed Trafficking of 5-HT Receptor-Mediated Signal Transduction....Pages 207-235 Identification of 5-HT 2 and 5-HT 4 Receptor-Interacting Proteins....Pages 237-255 5-HT Receptor-Associated Proteins (FRAPs)....Pages 257-276 Cellular and Subcellular Localization of Serotonin Receptors in the Central Nervous System....Pages 277-317 Chemical Neuroanatomy of 5-HT Receptor Subtypes in the Mammalian Brain....Pages 319-364 Modulation of the Neuronal Activity and Neurotransmitter Release by 5-HT 1A and 5-HT 1B/1D Receptors....Pages 365-401 Electrophysiology of 5-HT 2A Receptors and Relevance for Hallucinogen and Atypical Antipsychotic Drug Actions....Pages 403-417 The Emergence of 5-HT 2B Receptors as Targets to Avoid in Designing and Refining Pharmaceuticals....Pages 419-438 The 5-HT 3 Receptor....Pages 439-457 5-HT 3 and 5-HT 4 Receptors as Targets for Drug Discovery for Dementia....Pages 459-479 Electrophysiological Properties of Gα s -Coupled 5-HT Receptors (5-HT 4 , 5-HT 6 , 5-HT 7 )....Pages 481-494 5-HT 6 Receptors as Targets for the Treatment of Cognitive Deficits in Schizophrenia....Pages 495-515 5-HT 7 Receptors as Favorable Pharmacological Targets for Drug Discovery....Pages 517-535 Serotonin System Gene Knockouts....Pages 537-575 Effects of Serotonin-Related Gene Deletion on Measures of Anxiety, Depression, and Neurotransmission....Pages 577-606 Back Matter....Pages 607-618 The recent cloning and identification of a large number of serotonin (5-HT) receptors-a major family of therapeutic targets-holds out the possibility of developing novel, subtype-selective 5-HT receptor agonists and antagonists for use as psychiatric, cardiovascular, and neurological medications. In The Serotonin Receptors: From Molecular Pharmacology to Human Therapeutics, leading experts comprehensively examine our current understanding of the molecular and structural biology of 5-HT receptors and their pharmacological use. The authors describe the anatomical, cellular, and subcellular distribution of 5-HT receptors and demonstrate a powerful approach to elucidating their physiological role using knockout mice in which the 5-HT receptors were deleted. They also review our understanding of the physiological role(s) of 5-HT receptors based mainly on studies performed in genetically engineered mice. Highlights include discussions of the behavioral phenotypes of 5-HT receptor knockout animals, the molecular biology and pharmacology of 5-HT receptors, and insights into the complexity of 5-HT receptor signal transduction. Comprehensive and state of the art, The Serotonin Receptors: From Molecular Pharmacology to Human Therapeutics provides an illuminating "snapshot" of the 5-HT receptor field today and prospects for the future, taking it from the genomic to a systems level of understanding. A comprehensive, state-of-the-art review of our current understanding of the molecular and structural biology of 5-HT receptors and their potential use for drug discovery. The authors describe the anatomical, cellular, and subcellular distribution of 5-HT receptors and demonstrate a powerful approach to elucidating their physiological role using knockout mice in which the 5-HT receptors were deleted. They also review our understanding of the physiological role(s) of 5-HT receptors based mainly on studies performed in genetically engineered mice. Highlights include discussions of the behavioral phenotypes of 5-HT receptor knockout animals, the molecular biology and pharmacology of 5-HT receptors, and insights into the complexity of 5-HT receptor signal transduction.