Elsevier S & T

Phosphodiesterase Inhibitors

Page, Clive

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Table of contents
  • Contentsv
  • Contributorsix
  • Series Prefacexiii
  • Prefacexv
  • Chapter 1. Identification and Quantification of PDE Isoenzymes and Subtypes by Molecular BiologicaI1
  • 1. Introduction1
  • 2. The PDE Gene Family1
  • 3. Molecular Cloning and Localization of the Mammalian PDEs3
  • 4. Summary14
  • 5. References14
  • Chapter 2. Analysis of PDE Isoenzyme Profiles in Cells and Tissues by Pharmacological Methods21
  • 1. Introduction21
  • 2. Analysis of PDE Isoenzyme Activities in Cells and Tissues22
  • 3. Regulation of PDE Isoenzyme Activities30
  • 4. Conclusions34
  • 5. References34
  • Chapter 3. Effects of Theophylline and Non-selective Xanthine Derivatives on PDE Isoenzymes and Cell41
  • 1. Introduction41
  • 2. Inhibition of PDE42
  • 3. Effects on Cell Function44
  • 4. Summary and Directions for Future Research55
  • 5. References56
  • Chapter 4. Ca 2+/Calmodulin-dependent Cyclic Nucleotide Phosphodiesterase (PDE1)65
  • 1. Introduction65
  • 2. Purification and Characterization66
  • 3. Isoenzymes of CaM-PDE66
  • 4. Activity in Cancer Cells74
  • 5. Conclusions74
  • 6. Acknowledgements74
  • 7. References75
  • Chapter 5. EHNA as an Inhibitor of PDE2: a Pharmacological and Biochemical Study in Cardiac Myocytes81
  • 1. Introduction81
  • 2. Methods82
  • 3. Results83
  • 4. Discussion86
  • 5. Acknowledgements87
  • 6. References87
  • Chapter 6. cGMP-Inhibited Phosphodiesterases (PDE3)89
  • 1. Introduction89
  • 2. Purification and Characterization89
  • 3. Molecular Cloning and Domain Organization92
  • 4. Structure/Function Relationships93
  • 5. Pharmacology and Potential Therapeutic Usage of PDE3 Inhibitors96
  • 6. Therapeutic Usage of PDE3 Inhibitors101
  • 7. Acknowledgements101
  • 8. References101
  • Chapter 7. Interaction of PDE4 Inhibitors with Enzymes and Cell Functions111
  • 1. The PDE4 Isoenzyme Family111
  • 2. Pharmacology of PDE4 Inhibitors115
  • 3. Adverse Effects of PDE4 Inhibitors119
  • 4. PDE4 Alterations in Allergic Diseases119
  • 5. Summary and Future Directions120
  • 6. References121
  • Chapter 8. Inhibition of Phosphodiesterase Isoenzymes and Cell Function by Selective PDE5 Inhibitors127
  • 1. Introduction127
  • 2. Scientific Rationale for PDE5 Inhibitors127
  • 3. PDE5 Inhibition and Vasorelaxation128
  • 4. Potential Therapeutic Applications of PDE5 Inhibitors130
  • 5. Additional Indications for PDE5 Inhibitors131
  • 6. Newer PDE5 Inhibitors131
  • 7. Combination Inhibitors132
  • 8. Summary132
  • 9. Acknowledgement132
  • 10. References132
  • Chapter 9. Design and Synthesis of Xanthines and Cyclic GMP Analogues as Potent Inhibitors of PDE5135
  • 1. Introduction135
  • 2. Strategy for the Design of PDE5 Inhibitors136
  • 3. Synthesis of IBMX and cGMP Analogues as PDE Inhibitors136
  • 4. Selectivity of the IBMX Analogues as PDE Inhibitors138
  • 5. cGMP Analogues as PDE Inhibitors142
  • 6. Smooth Muscle Relaxation by IBMX and cGMP Analogues143
  • 7. Conclusions144
  • 8. Acknowledgements145
  • 9. References145
  • Chapter 10. Enzymatic and Functional Aspects of Dual-selective PDE3/4 Inhibitors147
  • 1. Introduction147
  • 2. Dual Inhibitors of PDE3/4 for Asthma Therapy148
  • 3. Preclinical Pharmacology of PDE3/4 Inhibitors149
  • 4. Clinical Experience with PDE3/4 Inhibitors152
  • 5. Conclusions157
  • 6. References158
  • Chapter 11. An Isoform-selective Inhibitor of Cyclic AMP-specific Phosphodiesterase (PDE4) with Anti161
  • 1. Introduction161
  • 2. Materials and Methods162
  • 3. Results165
  • 4. Discussion169
  • 5. Acknowledgements170
  • 6. References170
  • Chapter 12. Characterization of Different States of PDE4 by Rolipram and RP 73401173
  • 1. Introduction173
  • 2. Pharmacology of RP 73401173
  • 3. Interactions of RP 73401 and Rolipram with Eosinophil PDE4175
  • 4. Inhibition of PDE4 from Other Cells and Tissues178
  • 5. Possible Therapeutic Implications181
  • 6. Conclusions182
  • 7. References182
  • Chapter 13. MolecularAspects of Inhibitor Interaction with PDE4185
  • 1. Introduction185
  • 2. Molecular Biology of PDE4190
  • 3. Rolipram-Binding Site193
  • 4. Mechanistic Enzymology195
  • 5. Structure-Activity Relationships199
  • 6. Summary and Conclusions202
  • 7. References203
  • Glossary209
  • Key to Illustrations219
  • Index225
  • Color Plate SectionColor Plate-1
Book details
  • Vendor Elsevier S & T
  • SKU 9780122107207
  • ISBN-13 9780080538815
  • Author Page, Clive
  • Category Medical
  • Subject Immunology

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Description eBook delivery & access Reviews
Non-selective inhibitors of cyclic nucleotide phosphodiesterase (PDE), such as theophylline, have been used extensively since 1958. In the decade of the '70s, various PDE isoenzymes were defined which led to the development of the second generation of PDE inhibitors. Currently a variety of these new inhibitors are under test as potential anti-inflammatory drugs. During the past five years, molecular biology has revealed a superfamily of these phosphodiesterase isoenzymes. This book summarizes the present state of knowledge, as well as giving a comprehensive description of the compounds available. It will be invaluable for everyone who wants to choose the most suitable PDE inhibitor for their research or who is dealing with such drugs in a clinical setting.

Key Features
* Utilizes actual testing and research of new PDE inhibitors
* Valuable for researchers and students alike