Receptors and Cellular Pharmacology (eBook)

Front Cover 1
Receptors And Cellular pharmacology 4
Copyright Page 5
Table of Contents 6
List of Authors 8
Preface 10
Part 1: Invited lectures 12
Chapter 1. HISTAMINE RECEPTORS 14
Pharmacological taxonomy 14
Classification of histamine receptors 16
Histamine receptors in gastric mucosa 21
Histamine receptors on leucocytes 22
Histamine receptors in blood vessels 23
Histamine receptors in neurones 24
Histamine receptor blockade in medicine 25
References 25
Capter 2. PHARMACOLOGICAL INVESTIGATIONS ON CELLS IN CULTURE. 28
Advantages and disadvantages of cell culture research. 28
Background of pharmacological research on cell cultures 30
1. Effects of drugs on cellular morphology. 30
2. Effects of drugs on the general functions of cells. A. Effects upon cellular division. 31
3. A third group of results is, in our view, the most original, because it concerns the effects of drugs on specialised functions of the cell. 35
References 39
Chapter 3. HYDROPHOBIG PROPERTIES OF THE NEUROMUSCULAR BLOCKING AGENTS 44
D.A, Kharkevich 44
N-Adamantyl derivatives 45
Quaternary ammonium compounds with I-adamantyl radicals in different part of the molecule 50
On changing the mechanism of action of substances by gradual increase of hydrophobic properties 51
On the influence of hydrophobic radicals on the activity of substances 52
Conclusions 56
Acknowledgements 57
References 57
Part 2: Toxins as tools in receptor studies 60
Chapter 4. SNAKE TOXINS AS TOOLS TO STUDY CHOLINERGIC RECEPTORS: JUNCTIONAL AND EXTRAJUNCTIONAL ACETYLCHOLINE RECEPTORS IN SKELETAL MUSCLE 62
Site of action of extrinsic acetylcholine 62
Turnover of acetylcholine receptors 63
Regulation of acetylcholine receptors 64
References 66
Chapter 5. THE ACETYLCHOLINE RECEPTOR OF INTACT AND CULTURED CHICKEN RETINA CELLS 70
Zvi Voeel and Mathew P. Daniels 70
Experiments with Intact Retina 70
ACh receptors in the developing retina. 72
Distribution of a-BT binding sites in the retina 72
Experiments with Cultured Retina 73
Conclusions 75
Acknowledgements 76
References 77
Chapter 6. ACTIONS OF NEUROTOXINS ON THE ACETYLCHOLINE RECEPTOR-IONIC CONDUCTANCE MODULATOR UNIT AND ON SODIUM CHANNELS 78
Methods 78
Results 78
Acknowledgements 86
References 86
Chapter 7. SITUATION, PURIFICATION AND PROPERTIES OF ACETYLCHOLINE RECEPTORS OF MAMMALIAN STRIATED MUSCLE. 88
Characterization of receptors in the synaptic membranes 88
Purification of the ACh receptor 89
Properties of the purified ACh receptor 93
Conclusions 95
Acknowledgements 95
References 96
Chapter 8. STUDIES OF THE NICOTINIC ACETYLCHOLINE RECEPTOR FROM TORPEDO CALIFORNICA ELECTROPLAX 98
Introduction 98
Results and Discussion 98
References 106
Tetrodotoxin and Saxitoxin 108
Grayanotoxins 110
Conclusions 115
Acknowledgements 115
References 116
Part 3: Membrane receptors: Isolation and characterisation 120
Chapter 9. BIOCHEMICAL ASSAYS FOR NEUROTRANSMITTER RECEPTORS IN THE BRAIN: FOCUSON 7-AMINOBUTYRIC ACID 122
General principles 122
Saturability of receptors 123
Tissue Specificity 123
Biological and pharmacological specificity 124
Applications of receptor binding techniques 126
Regional distribution of receptors 126
Drug development and mechanism of action 126
Neurochemical analysis 127
Developmental neurobiology 128
Conclusions 128
Acknowledgements 128
References 128
Chapter 10. VASOPRESSIN-SENSITIVE ADENYLATE CYCLASE FROM THE MAMMALIAN KIDNEY. 132
General methodology 132
General properties of the vasopressin receptor 133
Anatomical distribution 134
Ontogenic development 134
Zoological specificity 135
Concluding remarks 140
References 141
Chapter 11. GLUCAGON, VIP AND SECRETIN RECEPTORS 142
Measurement of glucagon-receptor interactions 142
Structural requirements for hormonal recognition and action 144
Effects of nucleotides on binding and biological activation 145
Relationships between binding and biological activation 146
Subcellular localization of the receptors 147
Effects of physical, chemical and enzymatic modifications of the membranes 147
VIP and secretin receptors 148
Aknowledgments 149
References 149
Chapter 12. THE USE OF RADIOLABELED LIGANDS TO STUDY B-ADRENERGIC RECEPTORS 1 152
Conclusions 161
Acknowledgements 161
REFERENCES 161
Chapter 13. OPIATE RECEPTORS AND THEIR LIGANDS 164
Conclusions 171
Acknowledgements 172
References 172
Chapter 14. SOME FUNCTIONAL PROPERTIES OF THE CHOLINERGIC RECEPTOR PROTEIN FROM FISH ELECTRIC ORGAN IN ITS PURIFIED, MEMBRANE-BOUND AND REASSOCIATED STATES 176
CONCLUSIONS 185
REFERENCES 186
PART 4: Cyclic nucleotides as mediators of drug action 190
Chapter 15. CYCLIC NUCLEOTIDES AS MEDIATORS OF DRUG ACTION - OPENING REMARKS. 192
Chapter 16. CYCLIC NUCLEOTIDES AS MEDIATORS OF DRUG ACTION 196
References 200
Chapter 17. MECHANISM OF THE RELAXATION-PROMOTING EFFECTS OF EPINEPHRINE ON THE MAMMALIAN HEART 204
Introduction 204
Conclusions 211
Acknowledgments 211
References 211
Chapter 18. CYCLIC NUCLEOTIDES AND SMOOTH MUSCLE FUNCTION 214
Concluding remarks 219
Acknowledgements 220
References 220
Chapter 19. THE ROLE OF CYCLIC NUCLEOTIDES AND CALCIUM IN THE CONTROL OF SECRETION 224
Introduction 224
Calcium-dependent mechanisms 225
Calcium-dependent mechanisms modulated by cyclic AMP 226
Calcium- and cyclic AMP-dependent mechanisms 227
Conclusion 229
References 229
Chapter 20. GENETIC AND FUNCTIONAL STUDIES OF THE CYCLIC AMP RECEPTOR IN A CULTURED MAMMALIAN CELL 234
Genetic analysis of S49 cells 235
Mutations affecting the cAMP receptor 236
Structural alteration of the cAMP receptor 238
Mutation affecting adenylate cyclase 239
Receptors and cell regulation 240
Conclusions 241
Acknowledgements 242
References 242
Chapter 21. CONCLUDING REMARKS 244
References 247
Contents of Volumes 1—6 250
VOLUME 2. NEUROTRANSMISSION 251
VOLUME 3. CNS AND BEHAVIOURAL PHARMACOLOGY 252
VOLUME 4. DRUG THERAPY 254
VOLUME 5. CLINICAL PHARMACOLOGY 255
VOLUME 6. MECHANISMS OF TOXICITY AND METABOLISM 256
Subject Index 258