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| Contributors | |
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| Preface | |
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| 5-HT<sub>6</sub> Medicinal Chemistry | |
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| Introduction | |
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| 5-HT<sub>6</sub> Antagonists | |
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| 5-HT<sub>6</sub> Agonists | |
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| Summary | |
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| References | |
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| Patents | |
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| Introduction | |
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| Patent Applications Filed: Evolution over Time | |
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| Results Described and Claimed in Patent Related to 5-HT6 Receptors: Main Focus, Therapeutical Areas, and Chemical Diversity | |
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| Preclinical and Clinical Candidates: Status of the Studies Reported | |
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| Conclusion | |
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| References | |
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| 5-HT6 Receptor Characterization | |
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| Evidence of Existence of 5-HT6 Receptor before Receptor Cloning | |
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| Cloning of 5-HT6 Receptor: Receptor Binding and Functional Characterization | |
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| Pharmacological Characterization of 5-HT6 Receptor: Affinity and Functional Profile of Serotoninergic, Antipsychotic, and Antidepressant Agents, and Tool Molecules | |
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| Binding and Functional Methods for Receptor Characterization and Screening of Putative Ligands | |
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| Conclusions | |
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| References | |
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| 5-HT<sub>6</sub> Receptor Signal Transduction: Second Messenger Systems | |
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| Introduction | |
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| The cAMP Signal Transduction Pathway | |
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| Functional 5-HT<sub>6</sub> Receptor/G�15 Interaction: Calcium-Based Signaling | |
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| Functional 5-HT<sub>6</sub> Receptor/Fyn Tyrosine Kinase Interaction | |
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| Discussion | |
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| Conclusion | |
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| Acknowledgment | |
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| References | |
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| Electrophysiology of 5-HT6 Receptors | |
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| Introduction | |
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| Electrophysiological Effects of Serotonin | |
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| Anatomy and Physiology of 5-HT6 Receptors | |
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| Preclinical Pharmacology of 5-HT6 Receptor Modulators | |
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| Conclusions | |
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| References | |
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| Genetic Variations and Association | |
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| 5-HT6 Receptor Human Gene | |
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| Cloning and Mapping of the Human 5-HT6 Receptor Gene | |
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| Comparison of Human and Rat 5-HT6 Receptor Gene Sequences | |
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| Gene Expression Profile of 5-HT6 Receptors | |
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| 5-HT6 mRNA Levels in Peripheral Tissues | |
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| Orthologs of HTR6 Gene | |
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| Regulation of 5HTR6 Gene and Pathway Interaction | |
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| Genetic Variation within HTR6 Gene | |
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| C257T and Alzheimer's Disease | |
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| C257T and Schizophrenia | |
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| C267T Pharmacogenetic Studies of Antipsychotics | |
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| C267T and Mood Disorders | |
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| C267T and Pharmacogenetic Studies of Antidepressants | |
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| Conclusion | |
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| Acknowledgments | |
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| References | |
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| Pharmacokinetics of 5-HT<sub>6</sub> Receptor Ligands | |
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| Introduction | |
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| Preclinical Pharmacokinetic Results | |
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| Clinical Pharmacokinetic Results | |
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| Concluding Remarks | |
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| Acknowledgments | |
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| References | |
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| Index | |
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| Contents of Recent Volumes | |