Neuropeptide Y and Drug Development
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Table of contents
- Contentsv
- Contributorsviii
- Prefacex
- Chapter 1. Multiple receptors and multiple actions1
- 1.1 Multiple receptor types1
- 1.2 Yl receptors2
- 1.3 Y2 receptors3
- 1.4 Y3 receptors5
- 1.5 PPl/Y receptors5
- 1.6 Y5 receptors10
- 1.7 Other receptors and targets11
- Acknowledgements11
- References11
- Chapter 2. Central effects of neuropeptide Y with emphasis on its role in obesity and diabetes15
- 2.1 Introduction15
- 2.2 Pathways mediating the central effects of neuropeptide Y18
- 2.3 Neuropeptide Y and the regulation of feeding19
- 2.4 NPY and fat deposition21
- 2.5 NPY and pituitary function23
- 2.6 Other central effects of NPY26
- 2.7 NPY and obesity26
- 2.8 NPY, bulimia and anorexia nervosa28
- 2.9 NPY and diabetes29
- 2.10 Conclusion30
- References30
- Chapter 3. Neuropeptide Y in sympathetic nerves: evidence for Yl receptor mediated vascular control41
- 3.1 Introduction41
- 3.2 Prejunctional regulation of sympathetic transmitter release42
- 3.3 NPY in plasma and its clearance42
- 3.4 NPY in sympathetic neurotransmission43
- 3.5 NPY and cardiovascular disorders48
- References49
- Chapter 4. Neuropeptide Y receptor types in mammalian brain: species differences and status in the h57
- 4.1 Introduction57
- 4.2 Comparative distribution of NPY receptor types59
- 4.3 Functional significance of various NPY receptor types70
- 4.4 Conclusion78
- Acknowledgements79
- References79
- Chapter 5. Extraordinary structural diversity of NPY-family receptors87
- 5.1 Introduction87
- 5.2 Yl receptors89
- 5.3 Y2 receptors92
- 5.4 Pancreatic polypeptide receptors96
- 5.5 Discussion100
- Acknowledgements103
- References103
- Chapter 6. The importance of various parts of the NPY molecule for receptor recognition107
- 6.1 Neuropeptide Y: sequence and secondary structure107
- 6.2 Analoguesfor the characterization of the receptor types108
- 6.3 Structure-activity relationships110
- 6.4 A model of active conformations118
- References122
- Chapter 7. Peptide antagonists of neuropeptide Y: design, structure and pharmacological characteriza127
- 7.1 Background127
- 7.2 Design of small peptide antagonists of neuropeptide Y128
- 7.3 High-affinity peptide ligands135
- 7.4 Peptide dimers as potent NPY antagonists142
- 7.5 Pentapeptide dimers and multimers149
- Conclusion151
- Acknowledgements151
- References151
- Chapter 8. SR 120819A or the first generation of orally active Yl receptor antagonists157
- 8.1 Introduction157
- 8.2 Discovery of SR 120819A158
- 8.3 Biochemical profile of SR 120819A159
- 8.4 In vitro functional studies with SR 120819A164
- 8.5 Pharmacological profile of SR 120819A in vivo164
- 8.6 Conclusion168
- Acknowledgements170
- References170
- Chapter 9. BIBP 3226, a potent and selective neuropeptide Y Yl receptor antagonist. Structure-activi175
- 9.1 Introduction175
- 9.2 The design of the Yl-receptor antagonist BIBP 3226176
- 9.3 The first structure-activity relationships178
- 9.4 The receptor binding model of BIBP 3226178
- 9.5 The pharmacological profile of BIBP 3226185
- 9.6 Conclusions188
- References189
- Chapter 10. Discovery of neuropeptide Y receptor antagonists191
- 10.1 Introduction191
- 10.2 Design and synthesis of peptide or peptide-like NPY receptor antagonists based on the analysis192
- 10.3 Design and synthesis of non-peptide NPY receptor antagonists based on pharmacophore information195
- 10.4 Identification of non-peptide NPY receptor antagonists through the screening of combinational l200
- References201
- Index203
- List of abbreviations (for plate section)211
- Color Plate Section212
Neuropeptide Y (NPY) is a ubiquitous and important messenger in the nervous system, with a wide range of physiological roles. It is involved in the body energy balance and is one of the most potent stimuli of food intake known. NPY also acts to regulate central and peripheral autonomic functions.
This book, written by academic and industrial experts in the field, links the most recent basic experimental knowledge about NPY and its receptors with areas of clinical importance.
This book will be of interest to those working in all areas of research affected by NPY, such as food intake and energy homeostasis, cardiovascular regulation and G-protein-coupled receptors, as well as those interested in the development of drugs as NPY targets.
Key Features
* The hypothalamic role of NPY and its relationship with eating disorders and diabetes
* The sympathetic nervous system role of NPY and its involvement in cardiovascular disorders
* Characterization of NPY receptor types and their brain distribution, molecular biology and pharmacology
* Development of peptide and non-peptide receptor antagonists
This book, written by academic and industrial experts in the field, links the most recent basic experimental knowledge about NPY and its receptors with areas of clinical importance.
This book will be of interest to those working in all areas of research affected by NPY, such as food intake and energy homeostasis, cardiovascular regulation and G-protein-coupled receptors, as well as those interested in the development of drugs as NPY targets.
Key Features
* The hypothalamic role of NPY and its relationship with eating disorders and diabetes
* The sympathetic nervous system role of NPY and its involvement in cardiovascular disorders
* Characterization of NPY receptor types and their brain distribution, molecular biology and pharmacology
* Development of peptide and non-peptide receptor antagonists