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.
Inhaltsverzeichnis
Molecular Biology and Genomic Organization of G Protein-Coupled Serotonin Receptors. - Structure and Function Reveal Insights in the Pharmacology of 5-HT Receptor Subtypes. - Polymorphic and Posttranscriptional Modifications of 5-HT Receptor Structure. - Strategies for the Development of Selective Serotonergic Agents. - 5-HT Receptor Signal Transduction Pathways. - Agonist-Directed Trafficking of 5-HT Receptor-Mediated Signal Transduction. - Identification of 5-HT2 and 5-HT4 Receptor-Interacting Proteins. - 5-HT Receptor-Associated Proteins (FRAPs). - Cellular and Subcellular Localization of Serotonin Receptors in the Central Nervous System. - Chemical Neuroanatomy of 5-HT Receptor Subtypes in the Mammalian Brain. - Modulation of the Neuronal Activity and Neurotransmitter Release by 5-HT1A and 5-HT1B/1D Receptors. - Electrophysiology of 5-HT2A Receptors and Relevance for Hallucinogen and Atypical Antipsychotic Drug Actions. - The Emergence of 5-HT2B Receptors as Targets to Avoid in Designing and Refining Pharmaceuticals. - The 5-HT3 Receptor. - 5-HT3 and 5-HT4 Receptors as Targets for Drug Discovery for Dementia. - Electrophysiological Properties of G? s-Coupled 5-HT Receptors (5-HT4, 5-HT6, 5-HT7). - 5-HT6 Receptors as Targets for the Treatment of Cognitive Deficits in Schizophrenia. - 5-HT7 Receptors as Favorable Pharmacological Targets for Drug Discovery. - Serotonin System Gene Knockouts. - Effects of Serotonin-Related Gene Deletion on Measures of Anxiety, Depression, and Neurotransmission.
