Jacob Receptors

Proceedings of the 7th International Congress of Pharmacology, Paris, 1978
1. Auflage 2016
ISBN: 978-1-4831-5796-2
Verlag: Elsevier Science & Techn.
Format: PDF
Kopierschutz: 1 - PDF Watermark

E-Book, Englisch, 304 Seiten, Web PDF

Advances in Pharmacology and Therapeutics, Volume l: Receptors contains the proceedings of the 7th International Congress of Pharmacology held in Paris, France, in 1978. The papers explore advances in the understanding of receptors, their pharmacology, and their therapeutic applications. Topics covered range from opiate receptors and their endogenous ligands to membrane receptors in eukaryotic cells. Applications of binding to pharmacological research are also discussed. This volume is comprised of 29 chapters and opens with an overview of the chemistry and biochemistry of pituitary endorphins, paying particular attention to the correlation between the analgesic potency, receptor binding properties, preferred solution conformation, and metabolic stability of natural and synthetic opioid peptides. The reader is then introduced to the biosynthesis and release of the enkephalins; opiate receptors and their endogenous ligands; denervation supersensitivity in skeletal muscle; and biochemistry and physiology of dopaminergic and beta-adrenergic receptors in mammalian central nervous system. The following chapters explore the role of guanylnucleotides in the regulation of hormonally stimulated adenylate cyclase; interactions of cholera toxin with cell membranes; problems in studying hormone receptor binding; and the mechanism of action of anti-hormones. This book will be of interest to practitioners in biosciences, pharmacology, physiology, and medicine.

Autoren/Hrsg.

Jacob, J.

Inhaltsverzeichnis

1;Front Cover;1
2;Receptors;4
3;Copyright Page;5
4;Table of Contents;6
5;Introduction;9
6;Part 1: Opiate Receptors and Their Endogenous Ligands;11
6.1;Chapter 1. Chemistry and Biochemistry of Pituitary Endorphins;13
6.1.1;ABSTRACT;13
6.1.2;INTRODUCTION;13
6.1.3;STRUCTURAL REQUIREMENTS FOR ANALGESIC EFFECT;13
6.1.4;PROTEINASES INVOLVED IN THE GENERATION OF PITUITARY ENDORPHINS;17
6.1.5;REFERENCES;21
6.2;Chapter 2. Multiple Opiate Receptors;25
6.2.1;INTRODUCTION;25
6.2.2;INTERACTIONS OF OPIATES AND ENDOGENOUS OPIOID PEPTIDES WITH OPIATE RECEPTORS;25
6.2.3;PHARMACOLOGICAL PATTERN OF ENKEPHALIN ANALOGUES;27
6.2.4;POSSIBLE PHYSIOLOGICAL SIGNIFICANCE;28
6.2.5;SUMMARY;31
6.2.6;ACKNOWLEDGEMENTS;31
6.2.7;REFERENCES;31
6.3;Chapter 3. Pituitary Endorphins: Recent Progress;35
6.3.1;Abstract.;35
6.3.2;Slow-Reversing Endorphin; A Different Pituitary Opioid Peptide;35
6.3.3;Role of the Pituitary in the Hyperalgesic Effect of Naloxone.;37
6.3.4;Acknowledgements.;38
6.3.5;References.;38
6.4;Chapter 4. The Biosynthesis and Releaseof the Enkephalins;41
6.4.1;INTRODUCTION;41
6.4.2;RELEASE OF ENKEPHALINS;42
6.4.3;BIOGENESIS OF ENKEPHALINS;44
6.4.4;CONCLUDING REMARKS;45
6.4.5;Acknowledgements;46
6.4.6;REFERENCES;46
6.5;Chapter 5. Opiate Receptors: A) Functional Heterogeneity Demonstrated with an Apparently Irreversible Naloxone Derivative: B) Regulation by Guanine Nucleotides;49
6.5.1;ABSTRACT;49
6.5.2;KEYWORDS;49
6.5.3;Naloxazine Influences Upon Opiate Receptor Binding and Analgesia:;50
6.5.4;REFERENCES;55
6.6;Chapter 6. Opiate Receptors, Their Endogenous Ligands and the Development of Tolerance/Dependence;57
6.6.1;ABSTRACT;57
6.6.2;INTRODUCTION;57
6.6.3;I. Changes at the Receptor Level;58
6.6.4;II. Chronic Opiate Actions and Endogenous Ligands;59
6.6.5;III. Manifestation of Opiate Tolerance/Dependence at the Single Neurone Level;62
6.6.6;IV. Concluding Remarks - Neuronal Sensitivity and Chronic Opiate Action;64
6.6.7;REFERENCES;64
6.7;Chapter 7. Physiological and Patho Physiological Relevance of the Endogenous Ligands of the Opiate Receptors;67
6.7.1;ABSTRACT;67
6.7.2;INTRODUCTION;67
6.7.3;INTEGRATED FUNCTION;68
6.7.4;INTERACTION BETWEEN ENDOGENOUS LIGANDS OF OPIATE RECEPTORS AND OTHER HORMONES, MEDIATORS OR MODULATORS;73
6.7.5;PATHOLOGICAL STATES;74
6.7.6;CONCLUSIONS;75
6.7.7;AKNOWLEDGMENTS;75
6.7.8;REFERENCES;75
7;Part 2: Membrane Receptors in Eucaryotic Cells;81
7.1;Chapter 8. Multiple Classes of Muscarinic Receptor Binding Sites in the Brain;83
7.1.1;REFERENCES;55
7.2;Chapter 9. Opiate Receptors, Their Endogenous Ligands and the Development of Tolerance/Dependence;57
7.2.1;ABSTRACT;57
7.2.2;INTRODUCTION;57
7.2.3;I. Changes at the Receptor Level;58
7.2.4;II. Chronic Opiate Actions and Endogenous Ligands;59
7.2.5;III. Manifestation of Opiate Tolerance/Dependence at the Single Neurone Level;62
7.2.6;IV. Concluding Remarks - Neuronal Sensitivity and Chronic Opiate Action;64
7.2.7;REFERENCES;64
7.3;Chapter 10. Physiological and Pathophysiological Relevance of the Endogenous Ligands of the Opiate Receptors;67
7.3.1;ABSTRACT;67
7.3.2;INTRODUCTION;67
7.3.3;INTEGRATED FUNCTION;68
7.3.4;INTERACTION BETWEEN ENDOGENOUS LIGANDS OF OPIATE RECEPTORS AND OTHER HORMONES, MEDIATORS OR MODULATORS;73
7.3.5;PATHOLOGICAL STATES;74
7.3.6;CONCLUSIONS;75
7.3.7;AKNOWLEDGMENTS;75
7.3.8;REFERENCES;75
8;Part 3: Membrane Receptors in Eucaryotic Cells;81
8.1;Chapter 11. Multiple Classes of Muscarinic Receptor Binding Sites in the Brain;83
8.1.1;ABSTRACT;83
8.1.2;REFERENCES;89
8.2;Chapter 12. Biophysical Aspects of Agonist Action at Frog Endplate;91
8.2.1;INTRODUCTION;91
8.2.2;FLUCTUATION AND RELAXATION TECHNIQUES;91
8.2.3;SIMPLE MOLECULAR MODELS;93
8.2.4;CONCENTRATION DEPENDENCE OF CHANNEL KINETICS;94
8.2.5;DECAMETHONIUM BOTH OPENS AND BLOCKS CHANNELS;97
8.2.6;REFERENCES;99
8.3;Chapter 13. Some Observations on Denervation Supersensitivity in Skeletal Muscle;101
8.3.1;INTRODUCTION;101
8.3.2;RESULTS AND DISCUSSION;101
8.3.3;REFERENCES;106
8.4;Chapter 14. Structural and Functional Properties of the Acetylcholine-Regulator;109
8.4.1;I - STRUCTURE OF THE ACh-REGULATQR IN ACh-RECEPTQR RICH MEMBRANE FRAGMENTS;109
8.4.2;II - ALLOSTERIC INTERACTION BETWEEN AChR AND I0N0PH0RE IN AChR-RICH MEMBRANE FRAGMENTS;111
8.4.3;Ill - ISOLATION OF A PROTEIN CARRYING THE LOCAL ANESTHETIC BINDING SITE AND RECONSTITUTION OF A FUNCTIONAL ACh-REGULATOR;113
8.4.4;IV - CONCLUSIONS;114
8.4.5;REFERENCES;114
8.5;Chapter 15. Glutamate Receptors in Eucaryotes;117
8.5.1;Evolutionary Comments;117
8.5.2;Structure/Activity Phenomena;118
8.5.3;Glutamate Receptor Populations on Locust Muscle;119
8.5.4;Glutamate Receptors on Denervated Locust Muscle;120
8.5.5;Desensitisation of Glutamate Receptors on Locust Muscle;123
8.5.6;Concanavalin A and Glutamate Receptors on Locust Muscle;123
8.5.7;Glutamate Antagonist;123
8.5.8;Conclusion;124
8.5.9;References;124
8.6;Chapter 16. Biochemistry and Physiology of Dopaminergic and Beta-Adrenergic Receptors in Mammalian Central Nervous System;127
8.6.1;DOPAMINE RECEPTORS;127
8.6.2;Multiple Classes of Dopamine Receptors;127
8.6.3;Dopaminergic Ergots Distinguish Between Receptors.;128
8.6.4;Linkage of Dopamine Receptors to Adenylyl Cyclase;130
8.6.5;BETA-ADRENERGIC RECEPTOR IN THE BRAIN;131
8.6.6;Beta-Adrenergic Regulation of Brain Adenylyl Cyciase;133
8.6.7;Binding of 3H-Dihydroalprenolol to Cerebellar Homogenate;133
8.6.8;REFERENCES;135
8.7;Chapter 17. Beta-Adrenergic Receptors in C6 Glioma Cells and Central Nervous System;137
8.7.1;INTRODUCTION;137
8.7.2;RESULTS;137
8.7.3;CONCLUSION;144
8.7.4;REFERENCES;144
8.8;Chapter 18. Recent Studies on Opiate Receptors;147
8.8.1;DISCOVERY OF OPIATE RECEPTORS AND THEIR PROPERTIES;147
8.8.2;C0NF0RMATI0NAL STATES OF THE OPIATE RECEPTOR;147
8.8.3;THE ROLE OF PHOSPHOLIPIDS IN OPIATE RECEPTOR BINDING;149
8.8.4;A TISSUE CULTURE MODEL FOR THE STUDY OF OPIATE RECEPTORS;151
8.8.5;PROGRESS IN SOLUBILIZATION AND PURIFICATION OF OPIATE RECEPTORS;152
8.8.6;DISCOVERY OF ENDOGENOUS OPIOID PEPTIDES;153
8.8.7;CONCLUDING COMMENTS;154
8.8.8;REFERENCES;154
8.9;Chapter 19. The Role of Guanylnucleotides in the Regulation of Hormonally Stimulated Adenylate Cyclase;159
8.9.1;A GTP-BINDING PROTEIN IS PART OF THE ADENYLATE CYCLASE COMPLEX;159
8.9.2;ACKNOWLEDGEMENT;166
8.9.3;REFERENCES;166
8.10;Capter 20. Catecholamine-Sensitive Adenylate Cyclase: Identification and Partial Characterization of Some of its Components;169
8.10.1;INTRODUCTION;169
8.10.2;METHODS;170
8.10.3;RESULTS;170
8.10.4;CONCLUSIONS;179
8.10.5;REFERENCES;179
8.11;Chapter 21. Interactions of Cholera Toxin with Cell Membranes;181
8.11.1;BINDING OF CHOLERA TOXIN TO CELLS;182
8.11.2;PASSAGE OF SUBUNIT A THROUGH THE CELL MEMBRANE;183
8.11.3;ACTIVATION OF ADENYLATE CYCLASE BY FRAGMENT .1;185
8.11.4;REFERENCES;187
8.12;Chapter 22. Hybridization of Hormone Receptors with Adenylate Cyclase Systems of Different Cells;191
8.12.1;ABSTRACT;191
8.12.2;INTRODUCTION;192
8.12.3;EXPERIMENTAL AND DISCUSSION;192
8.12.4;CONCLUSIONS;196
8.12.5;Acknowledgements;196
8.12.6;REFERENCES;197
8.13;Chapter 23. Receptor Binding Studies of Beta-AdrenergicReceptors: New Insights into Activation and Desensitization of Adenylate Cyclase;199
8.13.1;REFERENCES;208
9;Part 4: Applications of Binding to Pharmacological Research;211
9.1;Chapter 24.Control of Hormone Receptor Levels and Function;213
9.1.1;INTRODUCTION;213
9.1.2;EFFECTS OF ESTROGENS ON TRH RECEPTOR LEVELS AND FUNCTION;213
9.1.3;AUTOREGULATION OF TRH RECEPTORS;215
9.1.4;INTERACTIONS OF SEX STEROIDS AND "INHIBIN" WITH LHRH RECEPTOR ACTION;215
9.1.5;AUTOREGULATION OF LHRH RECEPTORS;216
9.1.6;EFFECTS OF ESTROGENS ON PITUITARY DOPAMINE RECEPTORS AND FUNCTION;217
9.1.7;DOWN-REGULATION OF TESTICULAR AND OVARIAN RECEPTORS BY EN-DOGENOUS LH;219
9.1.8;REFERENCES;222
9.2;Cbhapter 25. Problems in Studying Hormone Receptor Binding;225
9.2.1;LABELED HORMONES;225
9.2.2;DISPLACEMENT CURVES;229
9.2.3;NON-SPECIFIC BINDING;229
9.2.4;REFERENCES;230
9.3;Chapter 26. Methodological Approach to Radioligand Binding Studies of Adrenergic Receptors;233
9.3.1;Radioligand;234
9.3.2;Tissue Preparations;235
9.3.3;Methods of Assaying Specific Radioligand Binding;236
9.3.4;Incubation Conditions;237
9.3.5;Specific and Non-Specific Binding;238
9.3.6;Potential Artifacts;239
9.3.7;REFERENCES;240
10;Part 5: Main Lectures;243
10.1;Chapter 27. Synaptic Receptor Proteolipids: Isolation and Molecular Biology;245
10.1.1;Proteolipids are involved in important membrane functions;246
10.1.2;Cholinergic proteolipids are separated by affinity chromatography in organics olvents.;248
10.1.3;The binding to the proteolipid is with the protein moiety and not with acidic lipids.;248
10.1.4;Receptor proteolipids for glutamate and GABA are present in artropod muscles.;249
10.1.5;Receptor proteolipids for amino acid neurotransmitters are present in the cerebral cortex of mammals.;251
10.1.6;The cholinergic proteolipid from the electroplax shows some similarities withthe proteodetergent.;253
10.1.7;The main protein band of the proteoiipid from Torpedo is about 39 Kdaltons;256
10.1.8;The ligand-proteolipid interaction can be studied by several physical methods;257
10.1.9;The ion-conducting mechanism is manifested by an in crease in membrane noise;258
10.1.10;The membrane "noise" may be observed in cholinergic proteolipid reconstituted in black lipid membranes.;259
10.1.11;A tentative model of the cholinergic receptor;263
10.1.12;REFERENCES;264
10.2;Chapter 28. The Mechanism of Action of Anti-Hormones;269
10.2.1;KINETICS OF THE INTERACTION WITH THE CYTOPLASMIC RECEPTOR;270
10.2.2;BIOLOGICAL ACTIVITY;274
10.2.3;ANTI-HORMONAL ACTIVITY;277
10.2.4;MULTIPLE EFFECTS OF ANTI-HORMONES;282
10.2.5;HYPOTHESES AND CONJECTURES;284
10.2.6;APPENDIX. Chemical names of the test-substances.;285
10.2.7;REFERENCES.;285
10.3;Chapter 29. Angiotensin Receptors;289
10.3.1;1. Angiotensin-receptor interaction.;289
10.3.2;2. Angiotensin III receptors in corticoadrenals.;295
10.3.3;3. Angiotensin receptor modulation.;296
10.3.4;References.;297
11;Index;301