5-HT2C Receptors in the Pathophysiology of CNS Disease

Part of Springer’s “The Receptors,” series, this text is the first ever overview on the research of 5-HT2c receptors. 5-HT2c receptor research has been productive for twenty-five years, but recent years have seen an extraordinary increase in both amount produced and insight gained. 5-HT2c is a prominent central serotonin receptor subtype widely expressed within the central and the peripheral nervous system and is thought to play a key role in the regulation of numerous behaviors. This text covers the molecular, cellular, anatomical, biochemical and behavioral aspects of this receptor, highlighting its distinctive regulatory properties and the emerging functional significance of constitutive activity and RNA-editing in vivo. It also investigates the receptors’ therapeutic potential in many diseases, treated individually in separate chapters, including depression, drug abuse, schizophrenia, eating disorders, Parkinson’s disease, Prader-Willi Syndrome, Alzheimer’s disease and epilepsy.

Research of 5-HT2c receptors stretches back twenty-five years, and while much of it has been productive, the past decade of research has been extraordinary in terms of both amount produced and insights gained. It is hardly surprising that 5-HT2c receptor research has grown so fruitful, given that it is a prominent central serotonin receptor subtype widely expressed within the central and the peripheral nervous system and is thought to play a major role in the regulation of numerous behaviors. It has further been shown by experimental and clinical observation that it may represent a possible therapeutic target for the development of drugs for a range of central nervous system disorders. The time, therefore, is more than appropriate to offer the first ever overview of the research of 5-HT2c receptors.

Part of the popular and important series, “The Receptors,” The 5-HT2c Receptor provides a thorough update of the functional status of the 5-HT2c receptor. It covers the molecular, cellular, anatomical, biochemical and behavioral aspects of this receptor so as to highlight its distinctive regulatory properties and the emerging functional significance of constitutive activity and RNA-editing in vivo. In addition, the book investigates the receptors’ therapeutic potential in a range of different diseases, treated individually in separate chapters, including depression, drug abuse, schizophrenia, eating disorders, Parkinson’s disease, Prader-Willi Syndrome, Alzheimer’s disease and epilepsy.

While not exhaustive, this text is a vital tool in understanding the past and inspiring the future of interdisciplinary research on the 5-HT2c receptor.

Chapter 1 The making of the 5-HT2C receptor
Jose M. Palacios, Angel Pazos and Daniel Hoyer

Chapter 2 Serotonin 5-HT2C receptors: chemical neuronatomy in the mammalian brain
Guadalupe Mengod

Chapter 3 The medicinal chemistry of 5-HT2C receptor ligands
Marcello Leopoldo, Enza Lacivita, Paola De Giorgio, Francesco Berardi, Roberto Perrone

Chapter 4 Insights into 5-HT2C receptor function gained from transgenic mouse models
Stephen J. Bonasera

Chapter 5 Serotonin 5-HT2C receptor signal transduction
Maria N. Garnovskaya and John R. Raymond

Chapter 6 Homology modeling of 5-HT2C receptors
Nicolas Renault, Amaury Farce, Philippe Chavatte

Chapter 7 5-HT2C receptor dimerization
Katharine Herrick-Davis and Dinah T. Farrington

Chapter 8 RNA editing of 5-HT2C receptor and neuropsychiatric diseases
Kazuya Iwamoto, Miki Bundo and Tadafumi Kato

Chapter 9 Serotonergic control of adult neurogenesis: focus on 5-HT2C receptors
Annie Daszuta

Chapter 10 The constitutive activity of 5-HT2C receptors as an additional modality of interaction of the serotonergic system
Sylvia Navailles, Philippe De Deurwaerdère

Chapter 11 The 5-HT2C receptor subtype controls central dopaminergic systems: evidence from electrophysiological and neurochemical studies
Giuseppe Di Giovanni, Ennio Esposito and Vincenzo Di Matteo

Chapter 12 The role of serotonin-2C receptors in the pathophysiology of depression
Eliyahu Dremencov, Joost HA Folgering, Sandra Hogg, Laurence Tecott and Thomas I.F.H. Cremers

Chapter 13 5-HT2C receptors and suicidal behaviour
Fabio Panariello, Naima Javaid and Vincenzo De Luca

Chapter 14 The 5-HT2C receptor as a target for schizophrenia
Herbert Y Meltzer, Liwen Sun and Hitoshi Hashimoto

Chapter 15 Serotonin and reward-related behaviour: focus on 5-HT2C receptors
Paul J. Fletcher and Guy A. Higgins

Chapter 16 Tat-3L4F: a novel peptide for treating drug addiction by disrupting interaction between PTEN and 5-HT2C receptor
Amy Hu, Lintao Jia, Jean-Christian Maillet, Xia Zhang

Chapter 17 The role of serotonin in eating behaviour: focus on 5-HT2C receptors
Jason C.G. Halford

Chapter 18 Physiological and pathophysiological aspects of 5-HT2C receptors in basal ganglia
Philippe De Deurwaerdère, Laurence Mignon and Marie-Françoise Chesselet

Chapter 19 Modeling tardive dyskinesia: predictive 5-HT2C receptor antagonist treatment
Richard M. Kostrzewa

Chapter 20 The role of 5-HT2A/2C receptors in sleep and waking
Jaime M. Monti and Héctor Jantos

Chapter 21 Role of alternative splicing of the 5-HT2C in the Prader-Willi syndrome
Shivendra Kishore and Stefan Stamm

Chapter 22 The role of 5-HT2C receptor in epilepsy
Rita Jakus and Gyorgy Bagdy

Chapter 23 The role of serotonin on attentional processes and executive functioning: focus on 5-HT2C receptors
Eleftheria Tsaltas and Vasileios Boulougouris

Chapter 24 5-HT2C receptors in learning
López-Vázquez Miguel Ángel, Gutiérrez-Guzmán Blanca Érika, Cervantes Miguel and Olvera-Cortés María Esther

Chapter 25 The role of 5-HT2C polymorphisms in behavioural and psychological symptoms of alzheimer's disease
Antonia Pritchard

Chapter 26 Ocular hypotension: involvement of serotonergic 5-HT2C receptors
Najam A. Sharif