Histamine II and Anti-Histaminics: Chemistry, Metabolism and Physiological and Pharmacological Actions

714 Pages·1978·17.1 MB·English

by  B. Mauricio Altura

Handbuch der
experimentellen Pharmakologie
Handbook of
Experimental Pharmacology
HefTter-Heubner New Series
Herausgegeben von/Editorial Board
G. V. R. Born, Cambridge· O. Eichler, Heidelberg
A. Farah, Rensselaer, NY . H. Herken, Berlin· A. D. Welch, Memphis, TN
Beirat/ Advisory Board
E. J. Ariens . Z. M. Bacq . P. Calabresi . S. Ebashi . E. G. Erdos
v:
Erspamer . U. S. von Euler' W S. Feldberg· G. B. Koelle
O. Krayer . T. A. Loomis' H. Raskova . M. Rocha e Silva' F. Sakai
J. R. Vane' P. G. Waser . W Wilbrandt
Vol. XVIII/2
Springer-Verlag Berlin Heidelberg New York 1978
Histamine II
and Anti-Histaminics
Chemistry, Metabolism and Physiological
and Pharmacological Actions
Contributors
B. M. Altura' A. Antonio' C. G. Van Arman' M. A. Beaven
F. G. Van den Brink' A. F. Casy . N. Chakravarty . C. L. Faingold
C. R. Ganellin . A. Goth, F. Hahn' S. Halevy . Z. Horakova
L. R. Johnson· N. J. Lewis' E. J. Lien· W. T. Nauta
G. Pelletier' R. F. Rekker . M. Rocha e Silva' R. W. Schayer
B. Uvnas . H. Wetterqvist . D. T. Witiak
Editor
Mauricio Rocha e Silva
With the Collaboration of Hanna A. Rothschild
Springer-Verlag Berlin Heidelberg New York 1978
Professor Dr. M. Rocha e Silva, Department of Pharmacology, Faculty of Medicine
of Ribeirao Preto, University of Sao Paulo, 14.100 Ribeirao Preto, S.P.jBrazil
With 92 Figures
ISBN-13: 978-3-642-66447-2 e-lSBN-13: 978-3-642-66445-8
DOT: 10.1007/978-3-642-66445-8
Library of Congress Cataloging in Publication Data Revised. Main entry under title: Histamine and anti~histaminics. (Handbook' of
experimental pharmacology; new series; v. 18) English or German. Includes bibliographies and indexes. Contents; pt. l. Histamine.
its chemistry, metabolism and physiological and pharmacological actions. pt. 2. Histamine II and anti-histaminics. 1. Histamine.
2. Antihistamines. I. Alivisatos, S. G. A. II. Silva, Mauricio Rocha e, 1910 - III. Rothschild, Hanna A. IV. Series: Handbuch der
experinientellen Pharmakologlc: ~ew series; v. 18. QP905.H3 Bd. 18 615'.7 77-12444
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© by Springer-Verlag Berlin Heidelberg 1975.
Softcover reprint of the hardcover 1st edition 1978
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2122/3130-543210
Preface
In the preface to Part I of this volume, which appeared in 1966, we stated:
" ... we had to leave the Antihistaminics for another volume of unpredictable
dimensions. In 1924, eight pages inserted in a Chapter on Mutterkorn by Arthur
R.Cushing were considered enough, in Vol. II, Part II, pp. 1319-1326 of the Hand
buch. Now 922 pages did not suffice to cover all aspects of the subject ...
the subject has been expanded in so many directions, that the anti histaminic part
had to be excluded from the present volume. Possibly, another thousand pages will
be necessary to cover what remains of the subject."* This prediction was fulfilled,
and the subject of histamine has grown to such an extent that dealing with the
antihistaminics only in Part II would be quite inadequate. It is imperative to include
the large number of recent findings on the subject of histamine, namely the splitting
of its pharmacologic receptors, and the great variety of new contributions on ,its
participation in physiopathologic phenomena, metabolism and interaction with
newly found mediators.
The first three sections of this book are entirely devoted to a review of recent
developments of the histamine problem, and deal with cardiovascular effects (I-A),
release (I-B), metabolism and excretion of histamine (I-C). With such additions as
an introduction to the main subject of this volume, it becomes an up-to-date
source of information about autopharmacology, discussing basic and therapeutic
aspects of histamine and the many consequences of analyzing the two types of
receptors HI and H2 as defined by their antagonists. The two parts of Volume XVIII,
with 1700 pages, cover almost the entire literature on the subject since the
discovery of fJ-imidazolethylamine by Windaus and Vogt (1907) and the description
by Dale and Laidlaw (1910) of its physiopathologic importance.
For only certain substances such as histamine, that participate in the various
aspects of normal and pathologic physiology, we now have the complete array
of bibliographic data offered by this two-volume work (Vol. XVIII/1-2).
Both parts of Volume XVIII of this monumental Handbook, like any book on
experimental biology, contains good and bad food, stimulant and narcotic material,
excellent and common ideas, that constitute the real basis of experimental medicine.
However under the present circumstances of research on the subject no better group
of contributors could be selected to deal with the difficult problem of histamine
and antihistaminics.
The achievement was made possible through the exhaustive work of collaborators
to Parts 1 and 2 of this volume. Among them we should particularly stress the
contributions to Part II by: B. M.Altura, L.R.Johnson, A.Goth, B. Uvnas,
R. W.Schayer, H. Wetterqvist, N.Chakravarty, M.A.Beaven, Z.Horakova, A. F.Casy,
W. T. Nauta, R. F. Rekker, e. R. Ganellin, F. G. Van den Brink, G. Pelletier, A. Antonio,
F.Hahn, e.G.Van Arman, D.T.Witiak, e.L.Faingold, S.Halevy, E.J.Lien, and
* This Handbook, Volume XVIII, Part I, Preface, 1966.
VI Preface
N.J.Lewis, many of whom gave invaluable suggestions for the organization of
the volume.
The insistence with which we pursued those invited to collaborate with letters,
telephone calls, and telegrams, sometimes so importunately, only meant that we
valued their collaboration so much, that we did not want to lose anyone of them.
This can be compared to Henry V of England, who made war on France because
he admired it so much that he wanted to possess all of it.
Although the time that has elapsed since the publication of Part I has been
long, it has in a way been rather fortunate. In the meantime important developments
have occurred. As far as antihistaminics are concerned the double nature of the
histamine receptors, with the description of HI and H2 antagonists, has widely
expanded the field. Furthermore, the possibility of differentiating histamine from
other endogenous autopharmacologic agents, such as polypeptides, prostaglandins,
acetylcholine, serotonin or IX-or p-sympathomimetics, permit a clear discussion of the
interaction of the receptors of histamine with both kinds of antagonists. I am
furthermore of the opinion that the new contributors were able to develop better
ideas on the basis of the excellent contributions to the first part of this volume.
To both groups, including the general supervisor, Dr. Hanna A.Rothschild, I
address my warm congratulations and thanks.
Acknowledgements,' Thanks are due the Fogarty International Center, National
Institutes of Health, Bethesda, Maryland, for a scholarship-in-residence, where this
book was begun during 1973-1974. It was completed during the second part of the
Scholarship, 1977-1978. We are indebted to colleagues ofN.I.H., and to Dr. Altura,
who recommended many of our collaborators.
November, 1977 M.RoCHA E SILVA
Contents
Chapter I: Recent Developments ofthe Histamine Problem
Section A: Pharmacological Actions
1. Cardiovascular Actions of Histamine. B. M. ALTURA and S. HALEVY. With 3 Figures
I. Introduction . . . . . . . . . . . 1
II. Systemic Vascular Effects of Histamine 2
A. Rat 2
B. Guinea-Pig 2
C. Rabbit 3
D. Dog ... 3
E. Cat 3
F. Calf, Horse, and Sheep 7
G. Man ....... . 7
III. Cardiac Actions of Histamine 7
A. Intact Animals. . . . 11
1. Inotropic Action 11
2. Chronotropic Action 11
3. Dromotropic Action 11
4. Cardiac Output . . 11
B. Isolated Heart Preparations 12
1. Inotropic Action 12
2. Chronotropic Action 12
3. Dromotropic Action 12
4. Coronary Flow . . 13
IV. Effects of Histamine on Regional Vasculatures 13
A. Coronary . . . 13
B. Pulmonary Lung 21
C. Splanchnic 21
D. Liver-Portal . . 22
E. Renal ..... 22
F. Musculo-Cutaneous 22
G. Cerebral . . . . . 22
H. Miscellaneous . . . 22
V. Microcirculatory Actions of Histamine 22
A. Direct In-Vivo Microcirculatory Actions of Histamine. 24
B. Hi Versus H -Receptors in Microcirculation ..... 25
2
C. Effects of Histamine on Vascular Permeability and Endothelial Cells 26
VIII Contents
VI. Isolated Vascular Smooth Muscle and Histamine 27
VII. Conclusions 29
References 30
2. Histamine and Gastric Secretion. L.R.JOHNSON. With 7 Figures
I. Introduction 41
II. Historical Review . . . . . . . . . 41
III. Physiologic Evidence . . . . . . . . 43
A. Histidine Decarboxylase Activation 43
B. Histamine Release and Gastric Secretion 46
IV. H -Receptor Antagonists: Gastric Secretion and the Role of Histamine 49
2
V. Conclusions . 54
References 55
Section B: Histamine Release
1. On the General Problem of the Release of Histamine. A. GOTH
I. Introduction . . . . . . . . . . . . . . . . . 57
II. The Noncytotoxic Nature of Histamine Secretion 58
III. Histamine Release and Complement. . . 60
IV. The IgE Receptor ......... . 60
V. Control Mechanisms of Histamine Release 61
Cyclic Nucleotides and Histamine Release 61
VI. Enhancers and Inhibitors of Histamine Release 62
A. Enhancers of Histamine Release . 62
1. Phosphatidyl Serine . . 63
2. Deuterium Oxide (0 0) . . 63
2
3. Cholinergic Stimulation . . 64
B. Inhibitors of Histamine Release 64
1. The Role of Calcium in Histamine Release . 65
2. Desensitization . . . . . . . . . . . . . 66
VII. Histamine Release from Tissues and Platelets . . . 67
A. Histamine Release from Isolated Tissues and Organs 67
B. Histamine Release from Platelets 67
VIII. Concluding Remarks 68
References 69
2. The Mechanism of Histamine Release from Mast Cells. B. UVNAs. With 9 Figures
I. Introduction . . . . . 75
II. The Normal Mast Cells . 75
A. Morphology 75
B. Contents. . . . . . 78
Contents IX
III. The Degranulating Mast Cell . . . . . . . . . . . . 78
A. Degranulating Agents . . . . . . . . . . . . . . 78
B. Noncytotoxic Character of the Degranulation Process 79
C. Electron-Microscopic Changes . . . 79
IV. Storage Properties of Basophil Granules 82
A. Role of Heparin . . . . . . . . . 82
B. Role of Zinc . . . . . . . . . . . 83
C. Role of the Granule Protein-Heparin Complex 84
V. Relationship Between Degranulation and Histamine Release 87
References 90
3. Metabolic Changes in Mast Cells Associated with Histamine Release.
N. CHAKRAVARTY. With 8 Figures
I. Energy Dependence of Anaphylactic Histamine Release . . . . . 93
II. Energy Metabolism of Mast Cells . . . . . . . . . . . . . . 95
III. Changes in Mast Cell Respiration in Relation to Histamine Release. 97
IV. Changes in Glucose Metabolism in Mast Cells Associated with Histamine
Release . . . . . . . . . . . . . . . . . . . . . . . . . 98
V. Changes in Adenosine Triphosphate Content of Mast Cells Associated
with Histamine Release 10 1
VI. Conclusion 105
References 106
Section C: Metabolism and Excretion of Histamine
1. Biogenesis of Histamine. R. W. SCHAYER
I. Introduction . . . . . . . . . . . . . . . . . . . . . . . 109
II. Methods for Determination of Histidine Decarboxylase Activity of
Mammalian Tissues. . . . . 109
III. Histamine Formation in vitro 110
IV. Histamine Formation in vivo. . . . . . . . 113
V. Inhibition of Histamine Formation in vitro. 115
VI. Inhibition of Histamine Formation in vivo. . 117
VII. Histidine Decarboxylase Activation and Deactivation; Role of
Protein and RNA Synthesis . . . . . . . . 118
VIII. Effect of Hormones on Histamine Formation 119
IX. Histamine Formation in Brain . . . . . 119
X. Histamine Formation and Antihistamines 121
XI. Conclusion 122
References 122
x
Contents
2. Histamine Metabolism and Excretion. H. WETTERQVIST
I. Histamine Metabolism in Tissues . . . . . . . . 132
II. Changes in Histamine Metabolism in Tissues. . 133
III. Histamine Metabolism and Excretion in Animals 134
A. Rat . . . 134
B. Mouse. . . 135
C. Guinea Pig . 135
D. Hamster . 136
E. Rabbit . 136
F. Sheep . 136
G. Goat . 136
H. Pig . . 137
I. Cow. . 137
J. Horse 137
K. Cat . 137
L. Toad, Tortoise, Terrapin 137
IV. Changes in Histamine Metabolism and Excretion in Animals. 137
V. Histamine Metabolism in Human Tissues. . . . . . . . 139
VI. Histamine Metabolism and Excretion in Man. . . . . . 139
VII. Changes in Histamine Metabolism and Excretion in Man. 140
VIII. Blood Diseases. 142
IX. Allergy . . . 142
X. Burns. . . . 142
XI. Miscellaneous 143
XII. Comments. 143
References . 143
3. The Enzymatic Isotopic Assay of Histamine. M.A.BEAVEN and Z.HORAKOVA.
With 3 Figures
I. Introduction 151
A. Principle of Isotope Derivative Dilution Assays. . . . . . . . . . 151
B. Applications ofIsotope Derivative Dilution Analysis in Biological Work 152
C. Enzymatic Isotope Derivative Dilution Assays. . . . . . . 153
II. Double Isotope Assay (with /PH-Histamine as Internal Standard) 154
A. Principle ................ . 154
B. Chemicals . . . . . . . . . . . . . . . . . 154
C. Preparation of /PH-(side-chain label)-Histamine . 155
D: Preparation of Histamine-N-Methyltransferase . 155
E. Storage and Preparation of Samples for Analysis · 156
F. Reagents and Stock Solutions (in Order of Use) . · 157
G. Incubation Procedure . . . . . . . . . . . . . · 157
H. Extraction and Measurement of Labeled Methylhistamine . · 158
I. Calculation · 159
J. Comments . . . . . . . . . . . . . . . . . . . . . · 160