Histamine in Inflammation


Robin L. Thurmond
Johnson & Johnson Pharmaceutical Research & Development, LLC

This book is co-published with Springer.
Please click here to purchase this book at the Springer site.


ISBN: 978-1-4419-8055-7
Pub Date: December 7, 2010
Pages: 162
Figures: 24
Tables: 9

About this Book

The year 2010 marks the centennial for the identification of histamine and the first glimpse of its many physiological functions. From these initial findings a rich tapestry of research has uncovered roles for histamine in almost every physiological process with new findings emerging every year. These diverse roles of histamine have made for fertile ground for the discovery of novel therapeutics, and these drugs have been so successful that the term “antihistamine” has entered the common lexicon. This volume is an attempt to give a snapshot in time as to the current understanding of the role of histamine in just one important therapeutic area—inflammation.

The first three chapters provide some background context for the rest of the book starting out with a historical perspective by Figueroa and Shankley. Bongers et al provide an overview of the pharmacology of the four histamine receptors and the chapter by Hiroshi Ohtsu describes how histamine is synthesized as well as the insights derived from mice where this synthesis is disrupted. The next several chapters discuss disease areas where histamine is known to be involved. Chapter 4 by Thomas Taylor‑Clark outlines the role of histamine in allergic rhinitis, an area were antihistamines are commonly used. This is also true for ocular allergy as discussed by Ohbayashi et al. Both of these chapters highlight aspects of these conditions that are still not well‑controlled and suggest the utility of new antihistamines targeting other histamine receptors. A related conclusion can be seen in the chapter by Dunford and Holgate on the role of histamine in asthma. In this case, however, current antihistamines are not considered to be effective, but the circumstantial evidence for a role of histamine in asthma provides evidence that other histamine receptors may be involved. Antihistamines are also useful for the treatment of some dermatological diseases as discussed by Zuberbier and Maurer. However, the chapter by Buddenkotte et al shows that this cannot be generalized since atopic dermatitis is much like asthma in that histamine has been suspected as being involved, but where current antihistamines are not effective. Traditionally histamine has mainly been associated with allergic reactions, but Schneider et al discuss evidence that histamine may have a broader role in immune function and autoimmune disease. While the majority of other contributions focus on inflammatory conditions, two of the concluding chapters touch on other areas. Nuutinen and Panula discuss the important role of histamine in neurotransmission and for the treatment of various neurological disorders. Falus et al takes the same approach with cell proliferation with an emphasis on malignancy.

Finally, the book concludes with the future of antihistamine research and the potential for novel antihistamines targeting newest members of the histamine receptor family—the H3 and H4 receptors. Taken together, I hope that this volume imparts the rich history of histamine research and that it stimulates further interest in uncovering yet to be discovered functions of histamine and the development of new antihistamines for the treatment of human disease.


Table of Contents

1. One Hundred Years of Histamine Research
Katherine Figueroa and Nigel Shankley

2. Molecular Pharmacology of the Four Histamine Receptors
Gerold Bongers, Iwan de Esch and Rob Leurs

3. Histamine Synthesis and Lessons Learned from Histidine Decarboxylase Deficient Mice
Hiroshi Ohtsu

4. Histamine in Allergic Rhinitis
Thomas Taylor‑Clark

5. The Role of Histamine in Ocular Allergy
Masaharu Ohbayashi, Bita Manzouri, Kei Morohoshi, Ken Fukuda and Santa J. Ono

6. The Role of Histamine in Asthma
Paul J. Dunford and Stephen T. Holgate

7. Antihistamines in the Treatment of Urticaria
Torsten Zuberbier and Marcus Maurer

8. Histamine and Antihistamines in Atopic Dermatitis
Jörg Buddenkotte, Marcus Maurer, and Martin Steinhoff

9. Histamine, Immune Cells and Autoimmunity
Elke Schneider, Maria Leite‑de‑Moraes and Michel Dy

10. Histamine in Neurotransmission and Brain Diseases
Saara Nuutinen and Pertti Panula

11. Histamine in Normal and Malignant Cell Proliferation
Andras Falus, Zoltán Pós and Zsuzsanna Darvas

12. The Future Antihistamines: Histamine H3 and H4 Receptor Ligands
Fuqu Yu, Pascal Bonaventure and Robin L. Thurmond


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