Biogenic Amine Receptors

314 Pages·1975·7.89 MB·English

by  Floyd E. Bloom (auth.)

if
Handbook
Psychopharmacology
Volume 6
Biogenic Amine Receptors
Handbook oj
Psychopharmacology
SECTION I: BASIC NEUROPHARMACOLOGY
Volume 1 Biochemical Principles and Techniques in Neuropharmacology
Volume 2 Principles of Receptor Research
Volume 3 Biochemistry of Biogenic Amines
Volume 4 Amino Acid Neurotransmitters
Volume 5 Synaptic Modulators
Volume 6 Biogenic Amine Receptors
in preparation
SECTION II: BEHAVIORAL PHARMACOLOGY IN ANIMALS
SECTION III: HUMAN PSYCHOPHARMACOLOGY
Volume 6
Biogenic Amine Receptors
Edited by
Leslie L. Iversen
Department of Pharmacology
University of Cambridge
Susan D. Iversen
Department of Psychology
University of Cambridge
and
Solomon H. Snyder
Departments of Pharmacology and Psychiatry
The Johns Hopkins University
School of Medicine
PLENUM PRESS • NEW YORK AND LONDON
Library of Congress Cataloging in Publication Data
Main entry under title:
Handbook of psy~ophannacology.
Includes bibliographies and indexes.
CONTENTS: v. 1. Biochemical principles and techniques in neuropharma·
cology. - v. 2. Principles of receptor research. - v. S. Biochemistry of biogenic
amines. - v. 4. Amino acid' neurotransmitters. - v. 5. Synaptic modulators.
- v. 6. Biogenic amine receptors.
1. Psychopharmacology. I. Iversen, Leslie Lars. n. Iversen, Susan D., 1940·
m. Snyder, Solomon R., 19S8· [DNLM: 1. Psychopharmacology.
QV77 R2S6]
RC48S.HS6 615'.78 75-6851
ISBN·13: 978·1-4684·8516·5 e·ISBN·13: 978·1·4684·8514·1
DOl: 10.10071978·1-4684·8514·1
© 1975 Plenum Press, New York
Softcover reprint of the hardcover 1st edition 1975
A Division of Plenum Publishing Corporation
227 West 17th Street, New York, N.Y. 10011
United Kingdom edition published by Plenum Press, London
A Division of Plenum Publishing Company, Ltd.
Davis House (4th Floor), 8 Scrubs Lane, Harlesden, London, NWIO 6SE, England
All rights reserved
No part of this book may be reproduced, stored in a retrieval system, or transmitted,
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recording or otherwise, without written permission from the Publisher
CONTRIB UTORS
TO VOLUME 6
GEORGE K. AGHAjANIAN, Department of Psychiatry, Yale University School of
Medicine, New Haven, Connecticut
JAMES L. BENNETT, Department of Psychiatry, Yale University School of
Medicine, New Haven, Connecticut
FLOYD E. BLOOM, Laboratory of Neuropharmacology, Division of Special Mental
Research, St. Elizabeths Hospital, Washington, D.C.
JEAN-PIERRE CHANGEUX, Neurobiologie Moleculaire Institut Pasteur, and
College de France, Paris, France.
HENRY j. HAIGLER, Department of Psychiatry, Yale University School of
Medicine, New Haven, Connecticut
K. KRNjEVIC, Department of Research in Anaesthesia, McGill University,
Montreal, Quebec, Canada
GORAN SEDVALL, Department of Pharmacology, Karolinska Institutet, Stockholm,
Sweden
LENNART STjARNE, Department of Physiology, Karolinska Institutet, Stockholm,
Sweden
DONALD H. YORK, Department of Physiology, University of Missouri, Columbia,
Missouri
CONTENTS
CHAPTER 1
Amine Receptors in CNS. I. Norepinephrine
FLOYD E. BLOOM
1. Introduction . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 1
2. Localizing Norepinephrine-Containing Synapses . . . . . . . . . 3
3. Effects of Norepinephrine on Central Neurons. . . . . . . . . . . . 4
3.1. Overview of Microiontophoretic Studies ............. 4
3.2. Identification of Test Neurons ...................... 4
4. Action of Norepinephrine on Defined Postsynaptic
Neurons............................................. 8
4.1. The Noradrenergic Projection to Rat Cerebellar
Purkinje Cells .................................... 8
4.2. Characterization of the Purkinje Cell Adrenergic
Receptor......................................... 9
4.3. Activation of the Adrenergic Pathway. . . . . . . . . . . . . . . . 10
5. The Noradrenergic Projection to Rat Hippocampal
Pyramidal Cells and Other Brain Stem Areas. . . . . . . .. . . . . . 11
6. Cyclic 3',5'-Adenosine Monophosphate as a Mediator of
Norepinephrine Action in the Central Nervous System. .. . . 11
6.1. Interpreting the "Failures to Confirm" Neuronal
Depression by Cyclic AMP ......................... 12
6.2. Actions of Calcium .. ...... .......... . . .. .......... 16
7. Conclusions.......................................... 17
8. References................................ .. . . . . . . . . . 18
vii
viii CONTENTS
CHAPTER 2
Amine Receptors in CNS. II. Dopamine
DONALD H. YORK
1. Introduction . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 23
2. Localization and Function of Dopamine. . . . . . . . . . . . . . . . . 24
2.1. Cerebral Cortex. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . " 24
2.2. Retina ......................................... 24
2.3. Hypothalamus ................................. ". 25
2.4. Basal Ganglia . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 27
3. Synthesis and Degradation of Striatal Dopamine . . . . . . . . . 28
4. Stimulus-Evoked Release of Dopamine in Striatum . . . . . . . 29
5. Dopamine Receptor Activation: Effects of Dopamine on
Striatal Neurons . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 29
6. Pharmacological Characterization of Presumed
Dopaminergic Neurons. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 35
7. Presynapticvs. Postsynaptic Dopamine Receptors... . . . . . 37
B. Behavioral Studies . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 39
B.l. Turning Behavior . . .. . . . . . . . . . . . . .. . . . . . . . . . . . . . 39
8.2. Stereotyped Behavior. . . . . . . . . . . . . . . . . . . . . . . . . . . . 42
B.3. Compulsive Gnawing Syndrome. . . . . . . . . . . . . . . . . . . 4~
9. Structural Conformations. . . . . . . . . . . . . . . . . . . . . . . . . . . . . 44
9.1. Dopamine. .. .. ................................. 44
9.2. Dopamine Agonists . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 45
9.3. Dopamine Antagonists. . . . . . . . . . . . . . . . . . . . . . . . . . . 47
10. Dopamine Receptor: Adenylate Cyclase. . . . . . . . . . . . . . . . . 47
11. Conclusion............. .. . . . . . . . . . . . . . . . . . . . . . . . . . . . 49
12. References.......................................... 50
CHAPTER 3
Amine Receptors in CNS. III. 5-Hydroxytryptamine in Brain
GEORGE K. AGHAJANIAN, HENRY J. HAIGLER, and JAMES L. BENNETT
1. Introduction....... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 63
2. Experimental Studies on 5-HT Receptors . . . . . . . . . . . . . . . . 66
2.1. Physiological Effects of 5-HT on Brain Neurons. . . . . . . 66
2.2. Studies on Putative 5-HT Agonists and Antagonists
in Brain......... ................................ 77
2.3. Studies on in Vitro Binding of 5-HT and LSD: Possible
Relationship to 5-HT Receptors .................... 85
3. Conclusions ........ "... .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 89
4. References........................................... 90
CONTENTS IX
CHAPTER 4
Acetylcholine Receptors in Vertebrate CNS
K. KRNJEVIC
1. Introduction .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 97
2. In Vivo Effects of ACh and Agonists on CNS. . . . . . . . . . . . . . . 9S
2.1. Gross Applications and Recording. . . . . . . . . . . . . . . . . . 98
2.2. Effects of Microapplications. . . . . . . . . . . . . . . . . . . . . . . . 99
2.3. Distribution of Different Kinds of ACh Receptors. . . . . 110
2.4. ACh Receptors on Other Tissue Components. . . . . . . . 113
3. In Vitro Effects of ACh and Agonists on CNS . . . . . . . . . . . . . . 114
3.1. ACh Responses of Neuroblastoma Cells. . . . . . . . . . . . . 114
3.2. Isolation of Central ACh Receptors. . . . . . . . . . . . . . . . . 114
3.3. Role of Guanosine Derivatives in ACh Response. . . . . . 116
4. Significance of ACh Receptors. . . . . . . . . . . . . . . . . . . . . . . . . . 117
5. Evidence for Central Cholinergic Neurotransmission and Its
Functional Significance . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 118
5.1. Fast Excitation ................................... 118
5.2. Slow Excitation. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . lIS
5.3. Inhibition ....................................... 120
6. References........................................... 120
CHAPTERS
Receptor Feedback and Dopamine Turnover in CNS
GORAN SEDVALL
1. Introduction ......................................... 127
1.1. Brain Dopamine. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 127
1.2. Dopamine Receptors. . . . . ...... . . ... ... ...... . . .. . 12S
2. Dopamine as a Transmitter Substance in CNS. . . . . . . . . . . . . 130
2.1. Chemical Identification. . . . . . . . . . . . . . . . . . . . . . . . . . . . 130
2.2. Distribution of Dopamine Neurons ................. 131
3. 1 ransmitter Metabolism in Brain Dopamine Neurons. . . . . . 135
3.1. Synthesis............................ ............ 135
3.2. Dopamine Metabolism. . . . . . . . . . . . . . . . . . . . . . . . . . . . 137
3.3. Dopamine Turnover. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 138
4. Effect of Dopamine Receptor Blocking Drugs on
Transmitter Turnover. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 140
4.1. Neuroleptics..................................... 140
4.2. Chlorpromazine Metabolites. . ... .. ... ... . . . . ... . .. 159
x CONTENTS
5. Effect of Dopamine Receptor Stimulating Drugs on
Transmitter Turnover. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 160
5.1. Apomorphine and Related Compounds . . . . . . . . . . . . . 160
5.2. Piribedil......................................... 162
6. Relation Between Drug Effects on Dopamine Turnover
Regulation in Vivo and Dopamine-Stimulated Adenylate
Cyclase Activity in Vitro . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 163
7. Evidence for Receptor-Mediated Control of Brain
Dopamine Turnover in Man. . . . . . . . . . . . . . . . . . . . . . . . . . . . 164
8. References........................................... 167
CHAPTER 6
Basic Mechanisms and Local Feedback Control of Secretion of
Adrenergic and Cholinergic Neurotransmitters
LENNART STJARNE
1. Introduction . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 179
2. Secretion of Adrenergic and Cholinergic
Neurotransmitters. . . .. . .... . . . . . . . . . . . . . . . . . . . . . . . . . . 180
2.1. Basic Mechanisms ................................ 180
2.2. Conflicting Current Concepts of Basic Mechanisms in
Neurotransmitter Secretion . . . . . . . . . . . . . . . . . . . . . . . . 181
2.3. Circumstantial Evidence Against a Quantum Size of
15,000 or More Transmitter Molecules ...... .. . . . . . . 182
2.4. Validity of the Electrophysiological Method for
Measuring Neurotransmitter Secretion. . . . . .. . . . . . . . 192
2.5. Fractional Secretion from Vesicles? ................. 200
2.6. Conclusions. .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 202
3. Local Feedback Control of Secretion of Adrenergic and
Cholinergic Neurotransmitters. . . . . . . . . . . . . . . . . . . . . . . . . 203
3.1. Definition ....................................... 203
3.2. Immediate Historical Background. . . . . . . . . . . . . . . . . . 204
3.3. Facilitation of Neurotransmitter Secretion on
Repetitive Stimulation. . . . . . . . . . . . . . . . . . . . . . . . . . . . . 207
3.4. Depression of Neurotransmitter Secretion on
Repetitive Stimulation. . . . . . . . . . . . . . . . . . . . . . . . . . . . . 209
3.5. Dual Negative-Feedback Control of Probability for
Quantal Secretion of NE from Sympathetic Nerves . . .. 215
3.6. Levels and Mechanisms Involved in Feedback
Control. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 218
3.7. Conclusions...................................... 222
4. References. .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 223
CONTENTS xi
CHAPTER 7
The Cholinergic Receptor Protein from Fish Electric Organ
JEAN-PIERRE CHANGEUX
1. Introduction........................................ 235
2. A Model for the Electrogenic Action of Acetylcholine . . . . . 237
3. Anatomy of the Electric Organs and of the
Electroplaques ...................................... 24 I
4. The Electric Discharge and the Electrophysiology of the
Electroplaques ...................................... 244
5. Pharmacology of the Isolated Electroplaque from
Electrophorus. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 246
5. I. Response of the Isolated Electroplaque to
Bath-Applied Agonists . . . . . . . . . . . . . . . . . . . . . . . . . . . 247
5.2. Concentration-Effect Curves: Effects of Agonists,
Antagonists, and Local Anesthetics. . . . . . . . . . . . . . . . . 249
5.3. Effects of -SH and S-S Reagents on Response to
Agonists. . . . . . . . . . . . .. . .. . . . . . . .. . . . . . . . . . . . . . . . 253
5.4. Affinity Labelingofthe Receptor Site. . . . . . . . . . . . . . . 254
5.5. Distinction Between the Catalytic Site of
Acetylcholinesterase and the Cholinergic Receptor
Site.. . . .. . . . . . .. . . . . . . .. . . . ... .. . . . . .. . . . . . . . . . 255
5.6. Snake Venom a-Toxins as Specific Reagents of the
Nicotinic Receptor Site. . . . . . . . . . . . .. . . . . . . . . . . . . . 256
6. Localization of the Cholinergic Receptor Site in
Electrophorus Electroplaque . . . . . . . . . . . . . . . . . . . . . . . . . . . 258
7. Subcellular Fractionation of the Electric Organ .......... 261
8. Permeability Response of Isolated Microsacs to Cholinergic
Agonists . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .. . . . . 263
9. Characterization of the Cholinergic Receptor Site on
Excitable Microsacs .................................. 266
10. Solubilization and Purification of the Cholinergic Receptor
Protein. . . . . .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 271
11. Chemical Properties of the Purified Receptor Protein. . . . . 276
12. Physical Properties ofthe Cholinergic Receptor Protein. . . 278
13. Binding Properties of the Purified Protein. . . . . . . . . . . . . . . 280
13.1. Electrophorus................................... 280
13.2. Torpedo ....................................... 283
14. Immunological Characterization of the Cholinergic
Receptor Protein from Electrophorus . . . . . . . . . . . . . . . . . . . . 284
15. Conformational Transitions of the Receptor Protein
Associated with Its Physiological Function. . . . . . . . . . . . . . . 286
16. Turnover Number ofthe Cholinergiclonophore ........ 287