Ions-Cyclic Nucleotides-Cholinergy (eBook)

Front Cover 1
Ions - Cyclic Nucleotides - Cholinergy 4
Copyright Page 5
Table of Contents 6
Introduction 10
Part I: Ions 12
Chapter 1. The Control of Calcium Metabolism in Health and Disease 14
SUMMARY 14
INTRODUCTION 14
DISTRIBUTION OF CALCIUM AND PHOSPHATE 14
HORMONES ACTING ON CALCIUM METABOLISM 16
THE MAJOR CONTROLLING HORMONES 17
THE ROLE OF THE SKELETON 19
INTEGRATION OF INDIVIDUAL ORGAN RESPONSES 20
CONTROL OF PLASMA CALCIUM 20
THE INFLUENCING HORMONES 21
COUPLING OF BONE FORMATION AND RESORPTION 22
DISORDERS OF CALCIUM HOMEOSTASIS 23
DRUGS ACTING ON CALCIUM METABOLISM 24
REFERENCES 25
Chapter 2. Vitamin D and its Metabolites: Physiology, Biochemistry and Pharmacology 
26 
I. Introduction 26
II. Functions of Vitamin D 26
III. Metabolism of Vitamin D in Preparation for Function 27
IV. Other Metabolism of Vitamin D 28
V. Regulation of Vitamin D Metabolism 29
VIII. Subcellular Location and Mechanism of Action of l,25-(OH)2D3 30
Summary 31
REFERENCES 32
ACKNOWLEDGMENTS 35
Chapter 3. Clinical Pharmacology and Application of the Active Forms of Vitamin D 36
PHYSIOLOGIC AND PHARMACOLOGIC ACTIONS OF 1,25-DIHYDROXY-VITAMIN D IN NORMAL MAN 36
CLINICAL CONDITIONS WITH REDUCED ACTION OF VITAMIN D 39
OTHER ANALOGUES OF VITAMIN D 44
24,25-DIHYDROXY-VITAMIN D3 44
SUMMARY 45
ACKNOLWEDGEMENTS 46
REFERENCES 46
Chapter 4. Biosynthesis, Metabolism, and Mode of Action of Parathyroid Hormone 48
INTRODUCTION 48
BIOSYNTHESIS 49
METABOLISM 51
MODE OF ACTION 53
REFERENCES 55
Chapter 5. Calcitonin: From Physiology toTherapeutic Uses 56
CONCLUDING REMARKS 63
BIBLIOGRAPHY 70
Chapter 6. Diphosphonates 72
INTRODUCTION 72
EXPERIMENTAL INVESTIGATIONS 72
CLINICAL APPLICATION OF DIPHOSPHONATES 76
PROSPECTS 79
ACKNOWLEDGEMENTS 79
REFERENCES 79
Chapter 7. Summary 84
Part II: Invited Lectures 90
Chapter 8. Ca Ion and Muscle Contraction 92
INTRODUCTION 92
REGULATORY SYSTEM IN VERTEBRATE SMOOTH MUSCLE 93
BRIEF NOTES ON TROPONIN 99
SOME PROBLEMS IN EXCITATION-CONTRACTION COUPLING 101
ADDITIONAL REMARKS 103
ACKNOWLEDGEMENT 104
REFERENCES 104
Chapter 9. The Sodium Channels in Excitable Membranes 110
REFERENCES 114
Part III: Cyclic Nucleotides 116
Chapter 10. Cyclic Nucleotides and Muscle Function: Introduction 
118 
REFERENCES 120
Chapter 11. The Possible Role of Cyclic GMP in the Actions of Hormones and Drugs on Smooth Muscle Tone: Effects of Exogenous Cyclic GMP Derivatives 
124 
CYCLIC AMP AND SMOOTH MUSCLE FUNCTION 124
CYCLIC GMP AND SMOOTH MUSCLE FUNCTION 124
EFFECTS OF EXOGENOUS CYCLIC GMP DERIVATIVES ON TISSUE TONE 125
CONCLUDING REMARKS 130
ACKNOWLEDGEMENTS 131
REFERENCES 131
Chapter 12. Effect of Nitro-Compound Smooth Muscle Relaxants and Other Materials on Cyclic GMP Metabolism 
134 
INTRODUCTION 134
REFERENCES 141
Chapter 13. Adenylate Cyclase in Heart and Skeletal Muscle 
144 
ABSTRACT 144
INTRODUCTION 144
METHODS 145
RESULTS 146
DISCUSSION 150
REFERENCES 151
Chapter 14. Cyclic Nucleotide Accumulation and Hormonal Modulation of Cardiac Metabolism and Contraction 
154 
INTRODUCTION 154
METHODS 155
POTASSIUM DEPOLARIZATION AND CYCLIC AMP ACCUMULATION IN MOUSE ATRIA 156
HORMONE-SPECIFIC EXPRESSION OF CARDIAC PROTEIN KINASE ACTIVITY 157
CHARACTERIZATION OF GUINEA PIG HEART PHOSPHORYLASE b KINASE 160
ACKNOWLEDGMENTS 162
REFERENCES 162
Chapter 15. Possible Regulation of the Calcium Permeability of Cardiac Cell Membranes by Cyclic Nucleotides 164
ABSTRACT 164
BETA-ADRENERGIC REGULATION OF CALCIUM PERMEABILITY 164
MUSCARINIC CHOLINERGIC REGULATION OF CALCIUM PERMEABILITY 167
CONCLUSION AND HYPOTHESIS 168
REFERENCES 169
Chapter 16. Some Characteristics of Low Molecular Weight Phosphoprotein Constituents of Cardiac Sarcoplasmic Reticulumand Sarcolemma 172
INTRODUCTION 172
ISOLATION OF SAROPLASMIC RETICULUM AND SARCOLEMMA FROM PIGEON HEART 174
THE 22,000 AND 15,000 Mr SARCOPLASMIC RETICULAR PROTEINS 174
THE 11,500 Mr SARCOLEMMAL PROTEIN 176
CONCLUSION 179
REFERENCES 180
Chapter 17. Phosphorylation and Regulation of Contractile Proteins 182
SUMMARY 182
CONTRACTILE PROTEINS 182
TROPONIN PHOSPHORYLATION 183
MYOSIN PHOSPHORYLATION 185
CONCLUSION 189
ACKNOWLEDGEMENTS 189
REFERENCES 189
Chapter 18. A Reassessment of the Criteria Used to Involve Cyclic Nucleotides in Hormone and Drug Mechanisms 192
INTRODUCTION 192
EFFECTS ON ENZYME ACTIVITIES 192
EFFECTS ON cAMP AND cGMP LEVELS 198
POTENTIATION OF HORMONE EFFECTS BY PHOSPHODIESTERASE INHIBITORS 199
EFFECTS OF EXOGENOUS CYCLIC NUCLEOTIDES 200
CONCLUSION 200
REFERENCES 201
Chapter 19. Radioimmunoassay of Cyclic AMP, Cyclic GMP, Cyclic CMP 204
INTRODUCTION 204
PREPARATION OF ANTIBODIES AND IODINATED DERIVATIVES 204
TREATMENT OF BIOLOGICAL SAMPLES AND INCUBATION 211
REFERENCES 215
Chapter 20. The Distribution of Cyclic Nucleotides and Their Protein Kinases in Tissues: An Immunocytochemical Approach 218
INTRODUCTION 218
TECHNIQUE OF CYCLIC NUCLEOTIDE IMMUNOCYTOCHEMISTRY 218
RECENT EXPERIENCE WITH CYCLIC NUCLEOTIDE IMMUNOCYTOCHEMISTRY 220
TECHNIQUE OF PROTEIN KINASE IMMUNOCYTOCHEMISTRY 221
PRELIMINARY EXPERIENCE WITH PROTEIN KINASE IMMUNOCYTOCHEMISTRY 225
CONCLUSION 228
ACKNOWLEDGEMENT 228
REFERENCES 228
Chapter 21. Contribution of Theoretical Simulation to the Study of the Cyclic AMP System 232
ABSTRACT 232
INTRODUCTION 232
HORMONAL DESENSITIZATION OF ADENYLATE CYCLASE SYSTEM 233
CONTROL OF PROTEIN KINASE ACTIVITY BY cAMP 235
CONCLUSION 238
ACKNOWLEDGEMENTS 238
REFERENCES 238
Part IV: Invited Lecture 240
Chapter 22. Cyclic Nucleotides, Phosphorylated Proteins and Drug Actions in the Central Nervous System 242
A. CYCLIC AMP, CYCLIC GMP AND NEURONAL FUNCTION 242
B. Cyclic AMP-Dependent Protein Phosphorylation 246
C. Regulation of Protein Phosphorylation by Calcium, Cyclic GMPand Steroid Hormones 249
REFERENCES 258
Part V: Cholinergy 262
Chapter 23. The Use of Affinity Constants for Studying Interactions Between Pharmacodynamic Groups and the Muscarinic Receptor 264
MEASUREMENT OF AFFINITY 264
CONTRIBUTIONS OF GROUPS TO AFFINITY 266
REFERENCES 269
Chapter 24. Structure and Activity of Some New Muscarine Derivatives and Acetylcholine Analogues 
272 
Results 272
Discussion 278
Conclusions 279
Acknowledgments 279
References 280
Chapter 25. The Conformation and Flexibility of Cholinergic Molecules 282
REFERENCES 290
Chapter 26. An NMR Study of the Conformations of Atropine and Scopolamine Cations in Aqueous Solution 292
ABSTRACT 292
INTRODUCTION 292
MATERIALS AND METHODS 293
RESULTS 294
DISCUSSION 301
REFERENCES 302
Chapter 27. The Conformation of Anticholinergic Substances 
304 
KEYWORDS 304
TECHNIQUE OF ANALYSIS 306
THE ANALYSIS 307
THE CONSISTENT CONFORMATION 308
References 313
Chapter 28. Biodegradable Neuromuscular Blocking Agents 314
INTRODUCTION 314
REFERENCES 322
Chapter 29. Effects of Anticholinergic Drugs on the Actions of Anticholinesterases on Cat Skeletal Muscle 324
REFERENCES 328
Chapter 30. Dual Mechanism of the Antidotal Action of Atropine-like Drugs in Poisoning by Organophosphorus Anticholinesterases 330
ABSTRACT 330
INTRODUCTION 330
METHODS AND RESULTS 331
DISCUSSION 333
REFERENCES 337
Index 338