Main description:

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.

Contents:

Molecular Biology and Genomic Organization of G Protein-Coupled Serotonin Receptors
Wesley K. Kroeze and Bryan L. Roth

Structure and Function Reveal Insights in the Pharmacology of 5-HT Receptor Subtypes
Richard B. Westkaemper and Bryan L. Roth

Polymorphic and Posttranscriptional Modifications of 5-HT Receptor Structure: Functional and Pathological Implications,
Marilyn A. Davies, Chiao-ying Chang, and Bryan L. Roth

Strategies for the Development of Selective Serotonergic Agents
Richard A. Glennon

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

Agonist-Directed Trafficking of 5-HT Receptor-Mediated Signal Transduction
Kelly A. Berg and William P. Clarke

Identification of 5-HT2 and 5-HT4 Receptor-Interacting Proteins: A Proteomic Approach
Joel Bockaert, Carine Becamel, Lara Joubert, Sophie Gavarini, Aline Dumuis, and Philippe Marin

5-HT Receptor-Associated Proteins (FRAPs): Relevance for Targeting, Trafficking, and Signal Transduction
Zongqi Xia, Douglas J. Sheffler, and Bryan L. Roth

Cellular and Subcellular Localization of Serotonin Receptors in the Central Nervous System
Laurent Descarries, Virginia Cornea-Hebert, and Mustapha Riad

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

Modulation of the Neuronal Activity and Neurotransmitter Release by 5-HT1A and 5-HT1B/1D Receptors
Pau Celada, Albert Adell, and Francesc Artigas

Electrophysiology of 5-HT2A Receptors and Relevance for Hallucinogen and Atypical Antipsychotic Drug Actions
Evelyn K. Lambe and George K. Aghajanian

The Emergence of 5-HT2B Receptors as Targets toAvoid in Designing and Refining Pharmaceuticals
Vincent Setola and Bryan L. Roth

The 5-HT3 Receptor
Andrew J. Thompson, Li Zhang, and Sarah C. R. Lummis

5-HT3 and 5-HT4 Receptors as Targets for Drug Discovery for Dementia
Frank Lezoualc'h and Magali Berthouze

Electrophysiological Properties of Gas-Coupled 5-HT Receptors (5-HT4, 5-HT6, 5-HT7)
Rodrigo Andrade

5-HT6 Receptors as Targets for the Treatment of Cognitive Deficits in Schizophrenia
Rudy Schreiber, Andrew Sleight, and Marie Woolley

5-HT7 Receptors as Favorable Pharmacological Targets for Drug Discovery
Peter B. Hedlund and J. Gregor Sutcliffe

Serotonin System Gene Knockouts: A Story of Mice With Implications for Man
Miles Berger and Laurence H. Tecott

Effects of Serotonin-Related Gene Deletion on Measures of Anxiety, Depression, and Neurotransmission
Anita J. Bechtholt and Irwin Lucki

Index