Molecular Biology and Genomic Organization of G Protein-Coupled Serotonin Receptorsn Wesley K. Kroeze and Bryan L. Rothn n Structure and Function Reveal Insights in the Pharmacology of 5-HT Receptor Subtypesn Richard B. Westkaemper and Bryan L. Rothn n Polymorphic and Posttranscriptional Modifications of 5-HT Receptor Structure: Functional and Pathological Implications,n Marilyn A. Davies, Chiao-ying Chang, and Bryan L. Rothn n Strategies for the Development of Selective Serotonergic Agentsn Richard A. Glennonn n 5-HT Receptor Signal Transduction Pathwaysn John R. Raymond, Justin H. Turner, Andrew K. Gelasco, Henry B. Ayiku, Sonya D. Coaxum, John M. Arthur, and Maria N. Garnovskayan n Agonist-Directed Trafficking of 5-HT Receptor-Mediated Signal Transductionn Kelly A. Berg and William P. Clarken n Identification of 5-HT2 and 5-HT4 Receptor-Interacting Proteins: A Proteomic Approachn Joël Bockaert, Carine Bécamel, Lara Joubert, Sophie Gavarini, Aline Dumuis, and Philippe Marinn n 5-HT Receptor-Associated Proteins (FRAPs): Relevance for Targeting, Trafficking, and Signal Transductionn Zongqi Xia, Douglas J. Sheffler, and Bryan L. Rothn n Cellular and Subcellular Localization of Serotonin Receptors in the Central Nervous Systemn Laurent Descarries, Virginia Cornea-Hébert, and Mustapha Riadn n Chemical Neuroanatomy of 5-HT Receptor Subtypes in the Mammalian Brainn Guadalupe Mengod, M. Teresa Vilaró, Roser Cortés, Juan F. López-Giménez, Andreu Raurich, and José M. Palaciosn n Modulation of the Neuronal Activity and Neurotransmitter Release by 5-HT1A and 5-HT1B/1D Receptorsn Pau Celada, Albert Adell, and Francesc Artigasn n Electrophysiology of 5-HT2A Receptors and Relevance for Hallucinogen and Atypical Antipsychotic Drug Actionsn Evelyn K. Lambe and George K. Aghajaniann n The Emergence of 5-HT2B Receptors as Targets toAvoid in Designing and Refining Pharmaceuticalsn Vincent Setola and Bryan L. Rothn n The 5-HT3 Receptorn Andrew J. Thompson, Li Zhang, and Sarah C. R. Lummisn n 5-HT3 and 5-HT4 Receptors as Targets for Drug Discovery for Dementian Frank Lezoualc'h and Magali Berthouzen n Electrophysiological Properties of Gas-Coupled 5-HT Receptors (5-HT4, 5-HT6, 5-HT7)n Rodrigo Andraden n 5-HT6 Receptors as Targets for the Treatment of Cognitive Deficits in Schizophrenian Rudy Schreiber, Andrew Sleight, and Marie Woolleyn n 5-HT7 Receptors as Favorable Pharmacological Targets for Drug Discoveryn Peter B. Hedlund and J. Gregor Sutcliffen n Serotonin System Gene Knockouts: A Story of Mice With Implications for Mann Miles Berger and Laurence H. Tecottn n Effects of Serotonin-Related Gene Deletion on Measures of Anxiety, Depression, and Neurotransmissionn Anita J. Bechtholt and Irwin Luckin n Index
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.