Phosphodiesterase inhibitors:
Gespeichert in:
| Format: | Buch |
|---|---|
| Sprache: | English |
| Veröffentlicht: |
San Diego [u.a.]
Acad. Press
1996
|
| Schriftenreihe: | The handbook of immunopharmacology
|
| Schlagworte: | |
| Online-Zugang: | Inhaltsverzeichnis |
| Beschreibung: | XVI, 228 S. graph. Darst. |
| ISBN: | 0122107209 |
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Datensatz im Suchindex
| _version_ | 1804125603345989632 |
|---|---|
| adam_text | PHOSPHODIESTERASE INHIBITORS EDITED BY CHRISTIAN SCHUDT DEPARTMENT OF
BIOCHEMISTRY BYK GULDEN PHARMACEUTICALS KONSTANZ, GERMANY GORDON DENT
AND KLAUS F. RABE KRANKENHAUS GROFIHANSDORF ZENTRUM FUR PNEUMOLOGIE UND
THORAXCHIRURGIE GROFIHANSDORF, GERMANY ACADEMIC PRESS HARCOURT BRACE AND
COMPANY, PUBLISHERS SAN DIEGO LONDON NEW YORK BOSTON SYDNEY TOKYO
TORONTO CONTENTS CONTRIBUTORS IX SERIES PREFACE XIII PREFACE XV 1.
IDENTIFICATION AND QUANTIFICATION OF PDE ISOENZYMES AND SUBTYPES BY
MOLECULAR BIOLOGICAL METHODS 1 KATE LOUGHNEY AND KEN FERGUSON 1.
INTRODUCTION 1 2. THE PDE GENE FAMILY 1 3. MOLECULAR CLONING AND
LOCALIZATION OF THE MAMMALIAN PDES 3 3.1 PDE1 3 3.8 ADDITIONAL PDES 14
3.2 PDE2 5 3.3 PDE3 6 4. 5. 3.4 3.5 3.6 3.7 3.8 PDE4 PDE5 PDE6 PDE7 7 12
12 13 ADDITIONAL PDES SUMMARY ] REFERENCES L4 14 2. ANALYSIS OF PDE
ISOENZYME PROFILES IN CEUS AND TISSUES BY PHARMACOLOGICAL METHODS
HERMANN TENOR AND CHRISTIAN SCHUDT 21 1. INTRODUCTION 21 2. ANALYSIS OF
PDE ISOENZYME ACTIVITIES IN CELLS AND TISSUES 22 2.1 PROCEDURE FOR
ESTABLISHMENT OF PDE ISOENZYME ACTIVITY PROFILES 22 2.2 PDE ISOENZYME
ACTIVITY PROFILES 23 3. REGULATION OF PDE ISOENZYME ACTIVITIES 30 3.1
REGULATION OF PDE ACTIVITY BY CYCLIC NUCLEOTIDE CONCENTRATIONS AND CA 2+
/CALMODULIN 30 3.2 4. 5. SHORT-TERM REGULATION OF PDE ACTIVITY BY
PHOSPHORYLATION 32 LONG-TERM PDE4 INDUCTION BY CAMP-ELEVATING AGENTS 32
ELEVATED PDE ACTIVITY IN ATOPIC MONONUCLEAR CELLS 33 CONCLUSIONS 34
REFERENCES 34 3.3 3.4 3. EFFECTS OFTHEOPHYLLINE AND NON-SELECTIVE
XANTHINE DEMATIPES ON PDE ISOENZYMES AND CELLULAR FUNCTION 41 GORDON
DENT AND KLAUS F. RABE 1. INTRODUCTION 41 2. INHIBITION OF PDE 42 2.1
INHIBITION OF TISSUE PDE ACTIVITY 42 2.2 INHIBITION OF ISOENZYMES 42 3.
EFFECTS ON CELL FUNCTION 44 3.1 IMMUNE CELLS 45 3.2 OTHER CELLS 54 4.
SUMMARY AND DIRECTIONS FOR FUTURE RESEARCH 55 5. REFERENCES 56 VI
CONTENTS 4. CA 2+ 1 CALMODULIN-DEPENDENT CYCLIC NUCLEOTIDE
PHOSPHODIESTERASE (PDE1) 65 RAJENDRA K. SHARMA AND ROBERT A. HICKIE 1.
INTRODUCTION 65 2. PURIFICATION AND CHARACTERIZATION 66 3. ISOENZYMES OF
CAM-PDE 66 3.1 DEMONSTRATION OF ISOENZYMES 66 3.2 KINETIC PROPERTIES 68
3.3 DIFFERENTIAL ACTIVATION BY CALMODULIN AND CA 2+ 68 3.4 REGULATION BY
PHOSPHORYLATION 69 3.5 INHIBITORS 73 4. ACTIVITY IN CANCER CELLS 74 5.
CONCLUSIONS 74 6. ACKNOWLEDGEMENTS 74 7. REFERENCES 75 3.4 3.5 3.6 5.
EHNA AS AN INHIBITOR OFPDE2: A PHARMACOLOGICAL AND BIOCHEMICAL STUDY IN
CARDIAC MYOCYTES 81 PIERRE-FRANCPIS MERY, CATHERINE PAVOINE, FRANCHISE
PECKER AND RODOLPHE FISCHMEISTER INTRODUCTION 81 1.1 CARDIAC CA 2+
CURRENT IS INHIBITED BY CGMP VIA ACTIVATION OF PDE2 81 1.2 USE OF THE
CARDIAC I & IN DETERMINING THE EFFECTS OF EHNA ON PDE2 82 1.3 USE OF
PURIFIED CARDIAC PDE ISOFORMS TO DETERMINE THE SELECTIVITY OF ACTION 82
4. METHODS 82 2.1 ELECTROPHYSIOLOGY 82 2.2 PDE ASSAYS FOR CAMP 83
RESULTS 83 3.1 EHNA HAS NO EFFECT ON 1^ IN THE ABSENCE OF 5. CGMP 83 6.
3.2 EHNA ANTAGONIZES THE INHIBITORY EFFECT OF CGMP ON I & 84 3.3 EHNA
ANTAGONIZES THE INHIBITORY EFFECT OF NITRIC OXIDE DONORS ON I & 84 EHNA
INHIBITS A CGMP-STIMULATED PDE IN THE CRUDE PANICULATE FRACTION 85 EHNA
SELECTIVELY INHIBITS THE PURIFIED SOLUBLE PDE2 86 PARTICIPATION OF
ADENOSINE DEAMINASE IN THE EFFECTS OF EHNA? 86 DISCUSSION 86 4.1 EHNA
ACTS AS A SELECTIVE INHIBITOR OF PDE2 IN CARDIAC MYOCYTES 86 4.2 EHNA
SHOULD BE USEFUL IN EVALUATING THE ROLE OF PDE2 IN VARIOUS TISSUES 87
ACKNOWLEDGEMENTS 87 REFERENCES 87 6. CGMP-INHIBITEDPHOSPHODIESTERASES
(PDE3) 89 NARCISSE KOMAS, MATTHEW MOVSESIAN, SASKO KEDEV, EVA DEGERMAN,
PER BELFRAGE AND VINCENT C. MANGANIELLO 1. INTRODUCTION 89 2.
PURIFICATION AND CHARACTERIZATION 89 3. MOLECULAR CLONING AND DOMAIN
ORGANIZATION 92 4. STRUCTURE/FUNCTION RELATIONSHIPS 93 4.1 CATALYTIC
DOMAIN 93 4.2 MEMBRANE-ASSOCIATION DOMAIN 95 4.3 REGULATORY DOMAIN
PHOSPHORYLATION/ACTIVATION 95 5. PHARMACOLOGY AND POTENTIAL THERAPEUTIC
USAGE OF PDE3 INHIBITORS 96 6. 7. 8. 5.1 5.2 5.3 5.4 5.5 97 INOTROPIC
AGENTS VASODILATORS 98 RELAXATION OF AIRWAY SMOOTH MUSCLE ANTITHROMBOTIC
AGENTS 100 ANTI-INFLAMMATORY AGENTS 100 THERAPEUTIC USAGE OF PDE3
INHIBITORS 101 ACKNOWLEDGEMENTS 101 REFERENCES 101 99 7. INTERACTION
OFPDE4 INHIBITORS WITH ENZYMES AND CELL FUNCTIONS GORDON DENT AND MARK
A. GIEMBYCZ 111 1 . THE PDE4 ISOENZYME FAMILY 111 1.1 ENZYME
CHARACTERISTICS 111 1.2 ENZYME DISTRIBUTION 112 1.3 SELECTIVE INHIBITORS
112 CONTENTS VII 2. PHARMACOLOGY OF PDE4 INHIBITORS 115 2.1 IN VIM 115
2.2 INVTVO 117 3. ADVERSE EFFECTS OF PDE4 INHIBITORS 119 4. PDE4
ALTERATIONS IN ALLERGIC DISEASES 119 5. SUMMARY AND FUTURE DIRECTIONS
120 6. REFERENCES 121 8. INBMTMOFPFOSPHODWSTEMELSOMZYMESANDCEUFUNC^ 127
PAUL J. SILVER 1. INTRODUCTION 127 2. SCIENTIFIC RATIONALE FOR PDE5
INHIBITORS 127 3. PDE5 INHIBITION AND VASORELAXATION 128 4. POTENTIAL
THERAPEUTIC APPLICATIONS OF PDE5 INHIBITORS 130 5. ADDITIONAL
INDICATIONS FOR PDE5 INHIBITORS 131 6. NEWER PDE5 INHIBITORS 131 7.
COMBINATION INHIBITORS 132 8. SUMMARY 132 9. ACKNOWLEDGEMENT 132 10.
REFERENCES 132 9. DESIGN AND SYNTHESIS OFXANTHINES AND CYCLIC GMP
ANALOGUES AS POTENT INHIBITORS OFPDE5 KONJETI R. SEKHAR, PASCAL GRONDIN,
SHARRON H. FRANCIS AND JACKIE D. CORBIN 135 1. INTRODUCTION 135 2.
STRATEGY FOR DIE DESIGN OF PDE5 INHIBITORS 136 3. SYNTHESIS OFLBMX AND
CGMP ANALOGUES AS PDE 5. INHIBITORS 136 6. 4. SELECTIVITY OF DIE IBMX
ANALOGUES AS PDE INHIBITORS 138 7. 4.1 IBMX ANALOGUES AS PDE5 INHIBITORS
138 8. 4.2 EFFECTS OF HYDROPHOBIC SUBSTITUTIONS ON 9. IBMX 141 4.3 IBMX
ANALOGUES AS INHIBITORS OF OTHER PDES 141 CGMP ANALOGUES AS PDE
INHIBITORS 142 SMOOTH MUSCLE RELAXATION BY IBMX AND CGMP ANALOGUES 143
CONCLUSIONS 144 ACKNOWLEDGEMENTS 145 REFERENCES 145 10. ENZYMATIC AND
FUNCTIONAL ASPECTS OF DUAL-SELECTIVE PDE3/4 INHIBITORS 147 ARMIN
HATZELMANN, RENATE ENGELSTATTER, JOHN MORLEY AND LAZZARR O MAZZONI 1.
INTRODUCTION 147 2. DUAL INHIBITORS OF PDE3/4 FOR ASTHMA THERAPY 148 2.1
AIRWAY SMOOTH MUSCLE RELAXATION 2.2 MODULATION OF INFLAMMATORY CELL
FUNCTIONS 148 2.3 SIDE-EFFECTS 148 3. PREDINICAL PHARMACOLOGY OF PDE3/4
INHIBITORS 149 3.1 AH 21-132 (BENAFENTRINE) 149 3.2 ZARDAVERINE 151 3.3
OTHERS (TOLAFENTRINE, ORG 20241, ORG 30029, EMD 54622) 151 4. CLINICAL
EXPERIENCE WITH PDE3/4 INHIBITORS 152 148 4.1 AH 21-132 152 4.2
ZARDAVERINE 153 4.3 OTHER SELECTIVE PDE INHIBITORS (TIBENELAST,
ENOXIMONE/ISOMAZOLE/SDZ-MKS 492, ZAPRINAST) 157 5. CONCLUSIONS 157 6.
REFERENCES 158 11. AN ISOFAM-SELECTIPE INHIBITOR OF CYCLIC AMP-SPECIFIC
PHOSPHODIESTERASE (PDE4) WITH ANTI-INFLAMMATORY PROPERTIES 161 ROBERT
ALVAREZ, DONALD V. DANIELS, EARL R. SHELTON, PRESTON A. BAECKER, T.
ANNIE T. FONG, BRUCE DEVENS, ROBERT WILHELM, RICHARD M. EGLEN AND MARCO
CONTI 1. INTRODUCTION 161 2.3 PREPARATION OF RECOMBINANT HUMAN PDE4 2.
MATERIALS AND METHODS 162 ISOFORMS 163 2.1 CYCLIC NUCLEOTIDE PDE ASSAYS
162 2.4 PHOSPHORYLATION OF HUMAN PDE4D3 164 2.2 ACCUMULATION OF CYCLIC
AMP IN INTACT 43D 2.5 RECOMBINANT HUMAN PDE7 164 CELLS 163 2.6
INFLAMMATORY ASSAYS 164 VIII CONTENTS 2.7 BRONCHOCONSTRICTION AND CELL
INFILTRATION IN GUINEA PIGS 165 2.8 STATISTICAL ANALYSIS 165 2.9
CHEMICALS 165 RESULTS 165 3.1 BIOCHEMICAL STUDIES 165 3.2 RECOMBINANT
PDE4 ISOFORMS 166 3.3 BIOLOGICAL RESPONSES 168 4. DISCUSSION 169 5.
ACKNOWLEDGEMENTS 170 6. REFERENCES 170 12. CHARACTERIZATION OF DIFFERENT
STATES OFPDFA BY ROLIPRAM AND RP 73401 JOHN E. SOUNESS 173 1.
INTRODUCTION 173 2. PHARMACOLOGY OF RP 73401 173 3. INTERACTIONS OF RP
73401 AND ROLIPRAM WITH 4. EOSINOPHIL PDE4 175 3.1 POOR CORRELATION
BETWEEN PDE4 INHIBITION AND SUPPRESSION OF EOSINOPHIL FUNCTIONS 175 5.
3.2 EFFECTS OF SOLUBILIZATION AND 6. VANADATE/GLUTATHIONE COMPLEX 176 7.
3.3 POSSIBLE ROLE OF THE HIGH-AFFINITY ROLIPRAM-BINDING SITE 178
INHIBITION OF PDE4 FROM OTHER CELLS AND TISSUES 178 4.1 ENZYME DATA 178
4.2 WHOLE CELL DATA 180 POSSIBLE THERAPEUTIC IMPLICATIONS 181
CONCLUSIONS 182 REFERENCES 182 13. MOLECULAR ASPECTS OF INHIBITOR
INTERACTION WITH PDE4 185 SIEGFRIED B. CHRISTENSEN, WALTER E. DEWOLF,
JR, M.D. RYAN AND THEODORE J. TORPHY 1. INTRODUCTION 185 1.1 CHEMISTRY
AND CHARACTERISTICS OF THE PHOSPHODIESTERASES 185 1.2 HISTORICAL
PERSPECTIVE ON ISOENZYME-SELECTIVE PDE INHIBITORS 186 2. MOLECULAR
BIOLOGY OF PDE4 190 2.1 SUBTYPES AND MRNA SPLICE VARIANTS 190 2.2
FUNCTIONAL DOMAINS OF PDE4 191 2.3 ROLE OF CONSERVED HISTIDINES 192 3.
ROLIPRAM-BINDING SITE 193 3.1 HISTORICAL PERSPECTIVE 193 3.2 NATURE AND
FUNCTION OF DIE HIGH-AFFINITY ROLIPRAM-BINDING SITE 194 3.3 PROPOSALS ON
THE NATURE AND FUNCTION OF DIE HIGH-AFFINITY ROLIPRAM-BINDING SITE 194
3.4 BIOLOGICAL SIGNIFICANCE OF HIGH-AFFINITY ROLIPRAM BINDING 195 4.
MECHANISTIC ENZYMOLOGY 195 4.1 KINETIC BEHAVIOUR OF PDE4S 195 4.2
INHIBITION BY IT-ROLIPRAM 197 4.3 BINDING OF H-ROLIPRAM TO MET 265 886
199 5. STRUCTURE-ACTIVITY RELATIONSHIPS 199 5.1 INTRODUCTION 199 5.2
ROLIPRAM AND LEAD PDE4 INHIBITORS 200 5.3 ROLIPRAM AND DERIVATIVES 201
5.4 OVERLAY MODEL OF PDE4 INHIBITION 201 6. SUMMARY AND CONCLUSIONS 202
7. REFERENCES 203 A COLOUR PLATE SECTION APPEARS BETWEEN PP. 208-209
GLOSSARY 209 KEY TO ILLUSTRATIONS 219 INDEX 225
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| spelling | Phosphodiesterase inhibitors ed. by Christian Schudt ... San Diego [u.a.] Acad. Press 1996 XVI, 228 S. graph. Darst. txt rdacontent n rdamedia nc rdacarrier The handbook of immunopharmacology Phosphodiesterase Inhibitors pharmacology Phosphodiesterase Inhibitors therapeutic use Phosphodiesterases Inhibitors Phosphodiesterases Inhibitors Therapeutic use Phosphodiesterasen (DE-588)4174389-1 gnd rswk-swf Immunpharmakologie (DE-588)4026639-4 gnd rswk-swf Inhibitor (DE-588)4027007-5 gnd rswk-swf (DE-588)4143413-4 Aufsatzsammlung gnd-content Immunpharmakologie (DE-588)4026639-4 s Phosphodiesterasen (DE-588)4174389-1 s Inhibitor (DE-588)4027007-5 s DE-604 Schudt, Christian Sonstige oth GBV Datenaustausch application/pdf http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=007445241&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA Inhaltsverzeichnis |
| spellingShingle | Phosphodiesterase inhibitors Phosphodiesterase Inhibitors pharmacology Phosphodiesterase Inhibitors therapeutic use Phosphodiesterases Inhibitors Phosphodiesterases Inhibitors Therapeutic use Phosphodiesterasen (DE-588)4174389-1 gnd Immunpharmakologie (DE-588)4026639-4 gnd Inhibitor (DE-588)4027007-5 gnd |
| subject_GND | (DE-588)4174389-1 (DE-588)4026639-4 (DE-588)4027007-5 (DE-588)4143413-4 |
| title | Phosphodiesterase inhibitors |
| title_auth | Phosphodiesterase inhibitors |
| title_exact_search | Phosphodiesterase inhibitors |
| title_full | Phosphodiesterase inhibitors ed. by Christian Schudt ... |
| title_fullStr | Phosphodiesterase inhibitors ed. by Christian Schudt ... |
| title_full_unstemmed | Phosphodiesterase inhibitors ed. by Christian Schudt ... |
| title_short | Phosphodiesterase inhibitors |
| title_sort | phosphodiesterase inhibitors |
| topic | Phosphodiesterase Inhibitors pharmacology Phosphodiesterase Inhibitors therapeutic use Phosphodiesterases Inhibitors Phosphodiesterases Inhibitors Therapeutic use Phosphodiesterasen (DE-588)4174389-1 gnd Immunpharmakologie (DE-588)4026639-4 gnd Inhibitor (DE-588)4027007-5 gnd |
| topic_facet | Phosphodiesterase Inhibitors pharmacology Phosphodiesterase Inhibitors therapeutic use Phosphodiesterases Inhibitors Phosphodiesterases Inhibitors Therapeutic use Phosphodiesterasen Immunpharmakologie Inhibitor Aufsatzsammlung |
| url | http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=007445241&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA |
| work_keys_str_mv | AT schudtchristian phosphodiesteraseinhibitors |