Frontiers in Clinical Drug Research - Anti-Allergy Agents: Volume 3 -  - E-Book

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Frontiers in Clinical Drug Research - Anti-Allergy Agents is a book series comprising of a selection of updated review articles relevant to the recent development of pharmacological agents used for the treatment of allergies. The scope of the reviews incl

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Veröffentlichungsjahr: 2018

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Table of Contents
Welcome
Table of Contents
Title
BENTHAM SCIENCE PUBLISHERS LTD.
End User License Agreement (for non-institutional, personal use)
Usage Rules:
Disclaimer:
Limitation of Liability:
General:
PREFACE
List of Contributors
Developing the Perfect Antihistamine for Use in Allergic Conditions: A Voyage in H1 Selectivity
Abstract
INTRODUCTION
Pharmacology of Histamine
Cellular Sources of Histamine and Mechanisms of Release
Mast Cells and the Inflammatory Environment
Histamine and Body Tissues; Antihistamines for the Treatment of Allergies
Nasal Anatomy and Physiology, Allergic Rhinitis, Allergens and Histamine
Allergens and Allergic Rhinitis
The Eye Conjunctiva; Anatomy and Physiology, Allergic Conjunctivitis and Histamine
Allergens and Allergic Conjunctivitis
The Skin; Anatomy and Physiology, Urticaria and Histamine
Allergens and Urticaria
Histamine and the H1 Receptor
First Generation H1 Antihistamines
A History of First Generation Antihistamine Development
Ethylenediamines and Ethanolamines
Piperazines and Piperidines
Phenothiazines and Doxepin; A New Genre of Antihistamines With Powerful Central Nervous System Effects
Side Effects of The First Generation H1 Antihistamines and Toxicity
Central Nervous System H1 Side Effects
Adverse Effects of First Generation H1 Antihistamines Due to Lack of Selectivity
Toxicity of First Generation Antihistamines
Second Generation H1 Antihistamines; Safer with Less Side Effects
Second Generation Antihistamines With Significant Side Effects: Astemizole, Azelastine and Terfenadine
Second Generation Histamines That are First Generation Analogs; Acrivastine, Cetirizine and Levocetirizine
Cetirizine
Levocetirizine
Second Generation Piperidine Successes; Levocabastine, Loratadine, Desloratadine, Fexofenadine, and Olopatadine
Loratadine
Desloratadine
Fexofenadine
Olopatadine
Clinical Trial Meta-Analysis Data for Extensively Used Second Generation Antihistamines
Conclusion and Further Directions
CONSENT FOR PUBLICATION
CONFLICT OF INTEREST
ACKNOWLEDGEMENTS
REFERENCES
Therapeutics in Chronic Spontaneous Urticaria
Abstract
INTRODUCTION
TREATMENT
Antihistamines
H1-Antihistamines
First-generation H1-antihistamines
Hydroxyzine
Doxepin
Second-generation H1-antihistamines
Cetirizine
Desloratadine
Loratadine
Fexofenadine
Levocetirizine
Rupatadine
H2-Antihistamines
Cimetidine
Ranitidine
Famotidine
Leukotriene Antagonist
Montelukast
Zafirlukast
Immunosuppressive Medications for CSU
Hydroxychloroquine
Colchicine
Dapsone
Sulfasalazine
Methotrexate
Cyclosporine
Immunomodulatory Agents
Omalizumab
Intravenous Immunoglobulin
Corticosteroids
CONSENT FOR PUBLICATION
Conflict of Interest
Acknowledgements
REFERENCES
Research and Development for Anti-Asthmatic Agents with a Focus on Phenotype Changing by Ca2+ Signaling in Airway Smooth Muscle Cells
Abstract
INTRODUCTION
MECHANISM OF AIRWAY SMOOTH MUSCLE TONE
AIRWAY SMOOTH MUSCLE TONE REGULATED BY KCa CHANNELS
Characteristics and Physiological Roles of KCa Channels
Structure of KCa Channels
Electrical Characteristics of KCa Channels
Physiological Role of KCa Channels
Stimulatory Regulation of KCa Channels by β2-Adrenoceptor Agonists
cAMP-Dependent Phosphorylation
Membrane-Delimited Activation by Gs
Dual Regulation by cAMP-Dependent and -Independent Processes
Role in Relaxation by β2-Adrenoceptor Agonists
Inhibitory Regulation of KCa Channels by Muscarinic Receptor Agonists
Membrane-Delimited Inhibition by Gi
Dual Regulation by Gs and Gi
Role in Contraction by Muscarinic Receptor Agonists
Regulation of KCa Channels by Other Factors (cGMP, Protein Kinase C)
NO, cGMP
Protein Kinase C
Redox and ROS
Arachidonic Acid
AIRWAY SMOOTH MUSCLE TONE REGULATED BY Ca2+ DYNAMICS
Membrane Potential-Independent Ca2+ Dynamics
Membrane Potential–dependent Ca2+ Dynamics
Effects of Ca2+ Release from the SR
AIRWAY SMOOTH MUSCLE TONE REGULATED BY Ca2+ SENSITIZATION
Characteristics and Physiological Role of RhoA / Rho-kinase
Role of RhoA / Rho-kinase on Contraction
Role on β2-Adrenergic Relaxation
INTRINSIC EFFICACY OF β2-ADRENOCEPTOR AGONISTS
Characteristics and Measurement
Values of β2-Adrenergic Intrinsic Efficacy for Airway Smooth Muscle Relaxation
Effects of Intrinsic Efficacy on β2-Adrenegic Desensitization
Role of Allosteric GPCR Modulation in Intrinsic Efficacy
ROLE OF Ca2+ SIGNALING IN AIRWAY DISORDERS
Airflow Limitation (Bronchoconstriction)
Airway Hyperresponsiveness
Desensitization of β2- Adrenoceptors
Ca2+ Dynamics
Ca2+ Sensitization
Airway Remodeling
Cell Proliferation
Cell Migration
Interaction between Airway Smooth Muscle and Inflammatory Cells
PHENOTYPE PLASTICITY
Contractile phenotype
Synthetic and Proliferative Phenotypes
Hyper-Contractile Phenotype
Ca2+ Handling
Regulation of Phenotype Switching
Modulation of Cell Phenotype by Cell Culture
RATIONALE USE OF β2-ADRENOCEPTOR AGONISTS BASED ON THEIR INTRINSIC EFFICACY
SYNERGISTIC EFFECTS BETWEEN MUSCARINIC AND β2-ADRENERGIC RECEPTORS
Role of G proteins / KCa Channels Linkage
Role of Allosteric GPCR Modulation in Synergistic Effects
POSSIBLE EFFECTS OF BRONCHODILATORS ON AIRWAY INFLAMMATION
CONCLUSIONS
Abbreviation
CONSENT FOR PUBLICATION
Acknowledgement
Conflict of Interest
REFERENCES
Effects of Allergic Rhinitis on Communication Skills
Abstract
Introduction
Effects of Allergic Rhinitis on Human Relations
Psychological Effects
Physiological Effects
Behavioral Effects
Conclusion
CONSENT FOR PUBLICATION
Conflict of Interest
ACKNOWLEDGEMENTS
References
Endosomal Toll-like Receptors: Rheostats of Inflammation and Diseases
Abstract
AN OVERVIEW
Toll-like Receptors
Structure of Toll-like Receptors
Toll-like Receptor Signaling
ENDOSOMAL TOLL-LIKE RECEPTORS
Ligand Detection by Endosomal TLRs
dsRNA Detection by TLR3
ssRNA Detection by TLR7 and TLR8
CpG DNA Detection by TLR9
Endosomal TLRs in Disease Aggravation
Role of Endosomal TLRs in Inflammatory and Autoimmune Diseases
Systemic Lupus Erythematosus
Type 1 Diabetes
Multiple sclerosis
Inflammatory Bowel Diseases
Crohn’s Disease
Asthma
Rheumatoid Arthritis
Role of Endosomal TLRs in Cancer
Therapeutic Targeting of Endosomal TLRs
Agonists of Endosomal TLRs
Antagonists of Endosomal TLRs
CONCLUSION
CONSENT FOR PUBLICATION
CONFLICT OF INTEREST
ACKNOWLEDGEMENT
REFERENCES

Frontiers in Clinical Drug Research – Anti Allergy Agents

(Volume 3)

Edited by

Atta-ur-Rahman, FRS

Kings College,University of Cambridge,
Cambridge,
UK

BENTHAM SCIENCE PUBLISHERS LTD.

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PREFACE

Frontiers in Clinical Drug Research - Anti Allergy Agents (Volume 3) comprises five comprehensive chapters on various treatment strategies for allergic conditions. In chapter 1, Cundell and Mickle focus on the existing different generations of drugs and the development of more potent anti-histamines. In the second chapter, Gonzalez-Estrada and Fernandez discuss the common drugs used for managing Chronic Spontaneous Urticaria, their side effects, and monitoring parameters. Both Ca2+ dynamics and Ca2+ sensitization are responsible for alterations in contractility in airway smooth muscle cells that lead to conditions of asthma and chronic obstructive pulmonary disease (COPD). Hiroaki Kume in chapter 3 of this book explain that the Ca2+ dynamics and Ca2+ sensitization may be the therapeutic approaches for treating asthma and COPD, and research in these areas may provide novel strategies for the development of bronchodilators for these diseases that will be effective for both bronchoconstriction and airway inflammation. In the next chapter Cingi et al. review the effects of Allergic Rhinitis on communication skills mainly in three categories: physiological, psychological and behavioral. In the last chapter, Bajpai et al. present the role of Endosomal Toll-like Receptors in inflammation and related diseases. They focus on the structural features of Toll-like Receptors, specific ligands, intracellular signaling and the role of Endosomal TLRs in the aggravation of diseases.

I hope that this volume will be of great interest to the scientific community and will play a vital role in the development of more effective therapeutic agents to combat various pulmonary ailments.

I would like to thank all the authors and the excellent team of Bentham Science Publishers, especially Dr. Faryal Sami, Mr. Shehzad Naqvi and Mr. Mahmood Alam for their support and hardwork.

Prof. Atta-ur-Rahman, FRS Honorary Life Fellow, Kings College, University of Cambridge, Cambridge, UK

List of Contributors

Alexei Gonzalez-EstradaDepartment of Allergy and Clinical Immunology, Respiratory Institute, Cleveland Clinic Foundation, Cleveland, OH, USACan Cemal CingiDepartment of Communication Design and Management, Faculty of Communication Sciences, Anadolu University, Eskişehir, TurkeyChhedi Lal GuptaDepartment of Biosciences, Integral University, Lucknow-226026, UP, IndiaDiana R. CundellDivision of Health Professions, College of Science, Health and the Liberal Arts, Philadelphia University, Philadelphia, PA, USAErkan YükselDepartment of Journalism, Faculty of Communication Sciences, Anadolu University, Eskişehir, TurkeyHiroaki KumeFaculty of Medicine, Department of Respiratory Medicine and Allergology, Kindai University, 377-2 Ohnohigashi, Osakasayama, Osaka 589-8511, Japan Department of Respiratory Medicine, Rinku General Medical Center, 2-23 Rinkuohraikita, Izumisano, Osaka 598-8577, JapanJames FernandezDepartment of Allergy and Clinical Immunology, Respiratory Institute, Cleveland Clinic Foundation, Cleveland, OH, USAKathryn E. MickleDivision of Health Professions, College of Science, Health and the Liberal Arts, Philadelphia University, Philadelphia, PA, USANeelam PathakDepartment of Biosciences, Integral University, Lucknow-226026, UP, IndiaNuray Bayar MulukDepartment of ENT, Faculty of Medicine, Kirikkale University, Kirikkale, TurkeyPreeti BajpaiDepartment of Biosciences, Integral University, Lucknow-226026, UP, IndiaRohit Kumar TiwariDepartment of Biosciences, Integral University, Lucknow-226026, UP, India

Developing the Perfect Antihistamine for Use in Allergic Conditions: A Voyage in H1 Selectivity

Diana R. Cundell*,Kathryn E. Mickle
Division of Health Professions, College of Science, Health and the Liberal Arts, Philadelphia University, 4201, Henry Avenue, Philadelphia, PA 19144, USA

Abstract

Histamine is a potent chemical mast cell and basophil messenger able to stimulate vasodilatation, gastrointestinal, respiratory and cardiac muscle contractions.At least four types of histamine receptors exist with varying physiological effects including vasodilatation, gastric acid secretion, brain chemistry and the cardiovascular system. Pharmacological antagonists are in common usage to at least two types of these receptors, H1 and H2; H1 being the classical “antihistamine” used in allergic conditions and H2 antagonism primarily associated with the prevention of gastric acid secretions. The first use of antihistamines to treat allergies was made over seventy years ago and these agents have undergone many chemical derivations since in order to maximize their H1 selectivity. In order to fully understand the underlying biochemistry of allergic disease, physiological roles of mast cells and basophils will be discussed together with a review of the mechanism through which histamine stimulates the H1 receptor. This chapter will delve into the history of the discovery of histamine, development of the antihistamines and the different pharmacological generations of drugs that have occurred since. Finally, we will conclude with a discussion of the new H1antihistamines currently under development together with potential future directions for this class of pharmaceuticals.

Keywords: Combinatorial chemistry, Drug repurposing, H1, Histamine, Mast cells, Metabolomics, Urticaria and Rhinoconjunctivitis.
*Corresponding author Diana R. Cundell: Division of Health Professions, College of Science, Health and the Liberal Arts, Philadelphia University, 4201, Henry Avenue, Philadelphia, PA 19144, USA; Tel: 215-951-2664; Fax: 215-951-6812; Email: [email protected]