Brain Receptor Methodologies. Part B: Amino Acids. Peptides. Psychoactive Drugs

331 Pages·1984·9.33 MB·English

by  Paul J. Marangos

NEUROBIOLOGICAL RESEARCH
EDITORS
PAUL J. MARANGOS IAIN C. CAMPBELL
UNIT ON NEUROCHEMISTRY DEPARTMENT OF BIOCHEMISTRY
BIOLOGICAL PSYCHIATRY BRANCH INSTITUTE OF PSYCHIATRY
NATIONAL INSTITUTE OF MENTAL HEALTH LONDON,ENGLAND
BETHESDA, MARYLAND
ROBERT M. COHEN
CLINICAL NEUROPHARMACOLOGY BRANCH
NATIONAL INSTITUTE OF MENTAL HEALTH
BETHESDA, MARYLAND
PAUL J. MARANGOS, IAIN C. CAMPBELL, AND ROBERT M. COHEN
Brain Receptor Methodologies, Parts A and B, 1984.
BRAIN RECEPTOR
METHODOLOGIES
Part B Amino Acids. Peptides.
Psychoactive Drugs
Edited by
Paul J. Marangos
UNIT ON NEUROCHEMISTRY
BIOLOGICAL PSYCHIATRY BRANCH
NATIONAL INSTITUTE OF MENTAL HEALTH
BETHESDA, MARYLAND
Iain C. Campbell
DEPARTMENT OF BIOCHEMISTRY
INSTITUTE OF PSYCHIATRY
LONDON, ENGLAND
Robert M. Cohen
CLINICAL NEUROPHARMACOLOGY BRANCH
NATIONAL INSTITUTE OF MENTAL HEALTH
BETHESDA, MARYLAND
ACADEMIC PRESS, INC.
(Harcourt Brace Jovanovich, Publishers)
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COPYRIGHT © 1984, BY ACADEMIC PRESS, INC.
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Library of Congress Cataloging in Publication Data
Main entry under title:
Brain receptor methodologies.
(Neurobiological research)
Includes index.
Contents: pt. A. General methods and concepts. Amines
and acetylcholine -- pt. B. Amino acids. Peptides.
Psychoactive drugs.
1. Neurotransmitter receptors—Collected works.
2. Neural receptors—Collected works. 3. Brain chemistry
—Collected works. I. Marangos, Paul J. II. Cohen,
Robert M. III. Campbell, Iain (Iain C.) III. Series.
[DNLM: 1. Neuroregulators—Physiology. 2. Brain-
Physiology. 3. Receptors, Endogenous substances-
Physiology. WL 300 B81365]
QP364.7.B73 1984 599'.0188 83-22479
ISBN 0-12-470352-6 (pt. B : alk. paper)
PRINTED IN THE UNITED STATES OF AMERICA
84 85 86 87 9 8 7 6 5 4 3 2 1
Contributors
Numbers in parentheses indicate the pages on which the authors' contributions begin.
JEAN-PHILIPPE BOULENGER (297), French National Institute for Health and
Medical Research (INSERM), 75013 Caen, France, and Biological Psychiatry
Branch, National Institute of Mental Health, Bethesda, Maryland 20205
DAVID R. BURT (129), Department of Pharmacology and Experimental Ther­
apeutics, University of Maryland School of Medicine, Baltimore, Maryland
21201
IAN CREESE (249), Department of Neurosciences, University of California at
San Diego School of Medicine, La Jolla, California 92093
F. V. DEFEUDIS1 (3), Institut Henri Beaufour, 92350 Le Plessis Robinson,
France
MICHAEL R. HANLEY (151), Department of Biochemistry, Imperial College
of Science and Technology, London SW7 2AZ, England
JAMES D. HIRSCH2 (59), Department of Biological Research, G. D. Searle
and Co., Skokie, Illinois 60077
ROBERT B. INNIS (111), Department of Psychiatry, Yale University School of
Medicine, New Haven, Connecticut 06508
MICHAEL J. KUHAR (111), Department of Neuroscience, Johns Hopkins Uni­
versity School of Medicine, Baltimore, Maryland 21205
L. M. FREDRIK LEEB-LUNDBERG3 (189), Department of Biochemistry,
University of California at Riverside, Riverside, California 92521
STUART E. LEFF (249), Department of Neurosciences, University of Califor­
nia at San Diego School of Medicine, La Jolla, California 92093
PAUL J. MARANGOS (177, 297), Unit on Neurochemistry, Biological
Psychiatry Branch, National Institute of Mental Health, Bethesda, Maryland
20205
FRANK L. MARGOLIS (59), Department of Physiological Chemistry and Phar­
macology, Roche Institute of Molecular Biology, Nutley, New Jersey 07110
TERRY W. MOODY (101), Department of Biochemistry, The George Washing­
ton University School of Medicine and Health Sciences, Washington, D.C.
20037
'Present address: Université Louis Pasteur, 67085 Strasbourg Cedex, France.
2Present address: Central Nervous System Research, Lederle Laboratories, American Cyanamid
Company, Pearl River, New York 10965.
3Present address: Department of Medicine, Duke University Medical Center, Durham, North
Carolina 27710.
xi
Xll CONTRIBUTORS
RICHARD W. OLSEN4 (189, 211), Department of Biomedicai Sciences, and
Department of Biochemistry, University of California at Riverside, Riverside,
California 92521
JITENDRA PATEL (177, 297), Unit on Neurochemistry, Biological Psychiatry
Branch, National Institute of Mental Health, Bethesda, Maryland 20205
STEVEN M. PAUL (279), Clinical Neuroscience Branch, National Institute of
Mental Health, Bethesda, Maryland 20205
MOSHE REHAVI (279), Department of Physiology and Pharmacology, Sackler
School of Medicine, Tel Aviv University, 69978 Tel Aviv, Israel
PHIL SKOLNICK (279), Laboratory of Bioorganic Chemistry, National Institute
of Arthritis, Metabolism, and Digestive Diseases, National Institutes of
Health, Bethesda, Maryland 20205
SOLOMON H. SNYDER (111), Department of Neuroscience, Johns Hopkins
University School of Medicine, Baltimore, Maryland 21205
MAH AR A J K. TICKU (211), Division of Molecular Pharmacology, Depart­
ments of Pharmacology and Psychiatry, The University of Texas Health Sci­
ence Center, San Antonio, Texas 78284
H. P. TOO (151), Department of Biochemistry, Imperial College of Science and
Technology, London SW7 2AZ, England
ANNE B. YOUNG (37), Department of Neurology, University of Michigan,
Ann Arbor, Michigan 48109
MARCO A. ZARBIN (111), Departments of Neuroscience, Pharmacology, and
Experimental Therapeutics, Psychiatry, and Behavioral Sciences, Johns Hop­
kins University School of Medicine, Baltimore, Maryland 21205
R. SUZANNE ZUKIN (77), Departments of Biochemistry and Neuroscience,
Albert Einstein College of Medicine, Bronx, New York 10461
STEPHEN R. ZUKIN (231), Departments of Psychiatry and Neurçscience,
Albert Einstein College of Medicine, Bronx, New York 10461 ?
4Present address: Department of Pharmacology, University of California at Los Angeles School of
Medicine, Los Angeles, California 90024.
General Preface
Neurobiology or neuroscience is a multidisciplinary subject that has grown out
of a common interest in nervous tissue by biochemists, physiologists, and phar­
macologists. Researchers in this field therefore require an expertise within their
own specialty as well as knowledge of other related areas. The degree of cross-
fertilization between the various subdisciplines within neurobiology is extensive,
and in most cases is required for the conduct of relevant research in the field.
The Neurobiological Research series provides a comprehensive and current
view of various subdisciplines within neurobiology. Each volume will cover a
specific area and will present in great detail the methods involved, so that the
reader can grasp the general scope of the subdiscipline as well as have sufficient
information to actually perform a given methodology. Each subdiscipline will be
covered in an extensive manner in order to maximize the probability of finding a
given methodology within each volume. This series, therefore, will differ from
most existing works in this area, which generally present a few long reviews of
selected areas within the realm of neurobiology and do not provide comprehen­
sive coverage of any subdiscipline or the details of methodology.
An additional major emphasis throughout the series will concern how each
methodology can be used to address various basic and clinical problems. Critical
evaluations of each technique and the meanings of the data obtained from it are
intended from each contributor. It is a major goal of the series to facilitate the
flow of basic research strategies toward clinical application, and authors have
been encouraged to review and to evaluate both past and potential future clinical
studies. In this regard the editors are keenly aware of the need for a more rational
and critical approach toward clinical neuroscience research.
The Neurobiological Research series should be a unique and valuable addition
to the libraries of all neuroscientists. It is hoped that the series will be of equal
value for both basic as well as clinical scientists. The first volume (Parts A and
B) of the series deal with the area of neurotransmitter and neuromodulator
receptors in brain, and future volumes will cover the subdisciplines of neuroanat-
omy, neurophysiology, brain-specific macromolecules, neurochemistry, and be­
havioral neurobiology.
Xlll
Preface to Part B
Part B continues from Part A with the rest of Section II, specific receptor
binding methodologies. Subsection II,B deals with receptors for amino acids and
neuropeptides and covers areas including GAB A (Chapter 1 by DeFeudis), gly­
cine (Chapter 2 by Young), carnosine (Chapter 3 by Hirsch and Margolis),
opiates (Chapter 4 by R. S. Zukin), bombesin (Chapter 5 by Moody), CCK
(Chapter 6 by Innis et al.), TRH (Chapter 7 by Burt), and substance P (Chapter 8
by Too and Hanley). The major omissions are glutamate and aspartate receptors.
Amino acids probably represent the majority of brain neurotransmitter sub­
stances, at least relative to the amines and acetylcholine, although with the
exception of GABA, the amino acids remain relatively uncharacterized in brain.
Their further study should receive high priority.
The neuropeptides also represent an area of rapidly expanding knowledge.
Whether these agents represent neurotransmitters or neuromodulators is currently
debated, and the chapters in this section should be reviewed with regard to
Chapter 4 by Polak and Bloom in Part A. It is likely that much of the current
explosion in neuropeptide research will soon settle, and that clearer concepts of
their role in neurotransmission will emerge.
Subsection II,C deals with receptors and binding sites for psychoactive drugs.
This represents an intriguing area of receptor research in that systems have been
defined for which the endogenous ligands have not been identified, and includes
reviews on the benzodiazepines (Chapters 9 and 10 by Marangos and Patel and
by Leeb-Lundberg and Olsen, respectively), picrotoxin (Chapter 11 by Ticku and
Olsen), PCP (Chapter 12 by S. R. Zukin), neuroleptics (Chapter 13 by Leff and
Creese), tricyclic antidepressants (Chapter 14 by Rehavi et al.), and adenosine
(Chapter 15 by Patel et al.). The characterization of these sites has added enor­
mously to our understanding of the mechanism of action of these drugs and holds
the potential of defining new neurotransmitter and neuromodulator systems if
and when endogenous ligands for some of the sites are identified. The potential
for such studies is best illustrated by the developments that have occurred con­
cerning the opiate peptides during the past 10 years. The adenosine receptor has
been included in this subsection because it was not appropriate in any other
section, although it is obviously not considered a psychoactive drug receptor at
this time.
Brain Receptor Methodologies, Parts A and B, provide a treatment of brain
receptors that is of broader scope than has previously been attempted. The
information contained here can well constitute the cornerstone of one's library
relating to receptor psychopharmacology.
XV
Contents of Part A
1. Receptors: A Historical Perspective
Iain C. Campbell
2. Preparation of Labeled Receptor Ligands
Yieh-Ping Wan and Stephen Ζλ Hurt
3. Heterogeneous Receptors and Binding Curve Analysis in Neurobiology
Peter J. Munson
4. The Distribution of Peripheral Regulatory Peptides: A Dual
Immunochemical (Immunocytochemistry and Radioimmunossay)
Approach
Julia M. Polak and Stephen R. Bloom
5. The Solubilization of Membrane Proteins
Andrew C. Newby
6. Solubilization and Characterization of Brain Benzodiazepine Binding
Sites
John W. Thomas and John F. Tollman
7. Solubilization of the Dopamine Receptor
Pierre M. Laduron
8. Autoradiographic Demonstration of Receptor Distributions
Miles Herkenham
9. Afffinity and Photoaffinity Labeling of Receptors
Mordechai Sokolovsky
10. Cyclic Nucleotide and Adenylate Cyclase in Brain:
Electrophysiological Studies
Trevor W. Stone
11. Calmodulin in the Nervous System
Robert J. DeLorenzo and James R. Goldenring
12. Preparation of the Catalytic Subunit of cAMP-Dependent Protein Kinase
David A. Flockhart and Jackie D. Corbin
13. Phospholipid Methylation in Brain and Other Tissues
Fulton T Crews
xvii
XV111 CONTENTS OF PART A
14. ß-Adrenergic Receptors
Ernst Bürgisser and Robert J. Lefkowitz
15. a-Adrenergic Receptors in Neural Tissues: Methods and Applications
of Radioligand Binding Assays
Bruce D. Perry and David C. U'Prichard
16. Dopamine Receptors in Brain
Philip Seeman
17. Radioactive Ligand Binding Studies: Identification of Central
Serotonin Receptors
M. Ramon
18. Muscarinic Receptor [3H]Ligand Binding Methods
Frederick J. Ehlert, William R. Roeske, and Henry I. Yamamura
Index
Chapter 1
GABA RECEPTORS IN THE
VERTEBRATE CNS
F. V. DeFEUDlS'
Institut Henri Beaufour Laboratories
Le Plessis-Robinson, France
I. Introduction 4
II. Methods for Studying GABA Binding 4
A. Preparation of Tissue Particles 4
B. GABA Binding Assay in the Presence of Na+ and Other
Inorganic Ions 6
C. GABA Binding Assay Using a Crude Membrane Fraction
in the Absence of Added Na + 6
D. GABA-Binding Assay in Tissue Culture Particles in the Absence
of Added Na+ 7
III. Kinetic Analysis of the Data 8
A. Lineweaver-Burk Analysis 8
B. Scatchard Analysis 8
C. Eadie-Hofstee Analysis 9
D. Pellet-Supernatant Distribution Ratios; Correction of Data
Using Sucrose Spaces 9
E. Hill Plots 9
F. Determination of IC Values 10
50
IV. Representative Experimental Results 10
A. [3H]GABA Binding to a P Fraction in a Bicarbonate-Buffered
2
Physiological Medium 10
B. [3H]Muscimol and [3H]GABA Binding to Cerebral Subcellular
Particles in the Absence of Added Na + 11
V. CNS Regional Distribution of GABA Binding 13
VI. Subcellular Distribution of GABA Binding 14
VII. Effects of Various Factors on GABA Binding 15
A. Kinetic Constants for GABA Binding to Various Subcellular
Preparations in the Presence or Absence of Added Na + 15
B. Analog Specificity of GABA Binding in the Presence or Absence
of Added Na+ 17
C. Effects of Some Psychoactive Agents on GABA Binding 17
D. Effects of Inorganic Ions on GABA Binding 21
E. Comments on the Use of Tris Buffers 22
1 Present address: Université Louis Pasteur, 67085 Strasbourg Cedex, France.
Brain Receptor Methodologies J Copyright © 1984 by Academic Press, Inc.
Part B All rights of reproduction in any form reserved.
ISBN 0-12-470352-6