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