Histamine Receptors as Drug Targets

Histamine Receptors as Drug Targets PDF Author: Ekaterini Tiligada
Publisher: Humana
ISBN: 9781493968411
Category : Medical
Languages : en
Pages : 0

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Book Description
This book illustrates the current state-of-the-art in histamine research, with a focus on the appropriate methodologies to investigate the pharmacological properties and the therapeutic exploitation of HRs and their ligands. In addition, the range of techniques described provides an introduction to complementary cross-methodological disciplines beyond these fields. This multi-disciplinary approach is required to define the ‘decision gates’ that determine the development of more effective and safer therapeutic options for many forms of highly prevalent and debilitating diseases, such as asthma, dementias, dermatitis, and arthritis. Written for the Methods in Pharmacology and Toxicology series, chapters concentrate on practical, hands-on protocols from experts in the techniques. Authoritative and thorough, Histamine Receptors as Drug Targets seeks to aid pharmacologists, biochemists, drug discovery researchers, molecular biologists, chemists, toxicologists, lab scientists, medical doctors, principle investigators, research scientists, lab directors and technicians, as well as graduate students around the world in pursuing the study of this vital scientific area.

Histamine Receptors as Drug Targets

Histamine Receptors as Drug Targets PDF Author: Ekaterini Tiligada
Publisher: Humana
ISBN: 9781493968411
Category : Medical
Languages : en
Pages : 0

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Book Description
This book illustrates the current state-of-the-art in histamine research, with a focus on the appropriate methodologies to investigate the pharmacological properties and the therapeutic exploitation of HRs and their ligands. In addition, the range of techniques described provides an introduction to complementary cross-methodological disciplines beyond these fields. This multi-disciplinary approach is required to define the ‘decision gates’ that determine the development of more effective and safer therapeutic options for many forms of highly prevalent and debilitating diseases, such as asthma, dementias, dermatitis, and arthritis. Written for the Methods in Pharmacology and Toxicology series, chapters concentrate on practical, hands-on protocols from experts in the techniques. Authoritative and thorough, Histamine Receptors as Drug Targets seeks to aid pharmacologists, biochemists, drug discovery researchers, molecular biologists, chemists, toxicologists, lab scientists, medical doctors, principle investigators, research scientists, lab directors and technicians, as well as graduate students around the world in pursuing the study of this vital scientific area.

Histamine H4 receptor

Histamine H4 receptor PDF Author: Holger Stark
Publisher: Walter de Gruyter
ISBN: 8376560565
Category : Science
Languages : en
Pages : 368

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Book Description
H4 R is the newest member of the histamine receptor family, which was discovered about twelve years ago. It is considered a very promising drug target. The effort to improve the pharmacokinetic properties of the currently available H4 R ligands is reflected in a steadily growing number of scientific publications and patent applications. Preclinical data strongly confirms the need for novel potent H4 R ligands to explore their therapeutic value in allergy, inflammation, autoimmune disorders, and possibly, cancer. Readers will be provided with extensive knowledge on histamine metabolism, as well as cellular histamine transport, storage and release, effects of histamine and histamine receptor ligands, with particular attention to the H4 R, on inflammatory cells including mast cells, basophils, eosinophils, neutrophils, macrophages, dendritic cells, and T cells. The present knowledge on the regulatory role of histamine and the therapeutic exploitation of histamine receptor ligands in atopic diseases, with emphasis on human and animal models of asthma, allergic dermatitis and pruritus are discussed.

Histamine in the brain

Histamine in the brain PDF Author: Jian-Sheng Lin
Publisher: Frontiers Media SA
ISBN: 2889194345
Category : Brain
Languages : en
Pages : 100

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Book Description
Brain aminergic pathways are organized in parallel and interacting systems, which support a range of functions, from homoeostatic regulations to cognitive, and motivational processes. Despite overlapping functional influences, dopamine, serotonin, noradrenaline and histamine systems provide different contributions to these processes. The histaminergic system, long ignored as a major regulator of the sleep-wake cycle, has now been fully acknowledged also as a major coordinator of attention, learning and memory, decision making. Although histaminergic neurons project widely to the whole brain, they are functionally heterogeneous, a feature which may provide the substrate for differential regulation, in a region-specific manner, of other neurotransmitter systems. Neurochemical preclinical studies have clearly shown that histamine interacts and modulates the release of neurotransmitters that are recognized as major modulators of cognitive processing and motivated behaviours. As a consequence, the histamine system has been proposed as a therapeutic target to treat sleep-wake disorders and cognitive dysfunctions that accompany neurodegenerative and neuroinflammatory pathologies. Last decades have witnessed an unexpected explosion of interest in brain histamine system, as new receptors have been discovered and selective ligands synthesised. Nevertheless, the complete picture of the histamine systems fine-tuning and its orchestration with other pathways remains rather elusive. This Research Topic is intended to offer an inter-disciplinary forum that will improve our current understanding of the role of brain histamine and provide the fundamentals necessary to drive innovation in clinical practice and to improve the management and treatment of neurological disorders.

Pharmacology of Histamine Receptors

Pharmacology of Histamine Receptors PDF Author: C. R. Ganellin
Publisher: Elsevier
ISBN: 1483193411
Category : Medical
Languages : en
Pages : 540

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Book Description
Pharmacology of Histamine Receptors presents a summary of the pharmacology of histamine receptors. It discusses the research and developments made in the use of histamine. It addresses the biological actions of the drug in various pathological instances. Some of the topics covered in the book are the classification of histamine receptors; mepyramine and related histamine antagonists; activity relationships of drugs acting at histamine receptors; chemical structure of histamine; effects of methyl substituents in histamine; enzymes involved in histamine metabolism; and histamine in body fluids. The cellular sources of histamine in tissues and blood are fully covered. The relationship of the mast cell to basophil is discussed in detail. The text describes in depth the urinary excretion of histamine and metabolites. The pathological conditions in man are presented completely. A chapter is devoted to the fundamental properties of adenylate cyclase and its measurement. The book can provide useful information to pharmacists, doctors, chemists, students, and researchers.

Histamine Receptors

Histamine Receptors PDF Author: Patrizio Blandina
Publisher: Springer
ISBN: 3319403087
Category : Medical
Languages : en
Pages : 378

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Book Description
A comprehensive and detailed overview of the current state of preclinical research on histamine and histamine receptors. Part of the book focuses on novel approaches to the study of histamine receptors such as polymorphism, genetic linkage, and computational analysis, and on the use of new histaminergic ligands in diseases such as asthma and dermatitis. Several chapters will be devoted to the role of histamine in the control of homeostatic and behavioral responses such as the sleep-wake cycle, regulation of the blood brain barrier, food intake, alertness, itch, and memory formation and consolidation.

Receptor - Based Drug Design

Receptor - Based Drug Design PDF Author: Paul Leff
Publisher: CRC Press
ISBN: 9781420001136
Category : Medical
Languages : en
Pages : 816

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Book Description
Employing a wide range of examples from G-protein-coupled receptors and ligand-gated ion channels, this detailed, single-source reference illustrates the principles of pharmacological analysis and receptor classification that are the basis of rational drug design. Explains the experimental and theoretical methods used to characterize interactions between ligands and receptors-providing the pharmacological information needed to solve treatment problems and facilitate the drug design process! Demonstrating the achievements of the receptor-based approach in therapeutics and indicating future directions, Receptor-Based Drug Design introduces novel computer-assisted strategies for the design of new agonists, antagonists, and inverse agonists for G-protein-coupled receptors shows how to assess agonist concentration-effect curve data discusses radioligand binding assays presents new in vitro multiarray assays for G-protein-coupled receptors explains the use of individual second messenger signaling responses in analyzing drug-receptor interactions examines the role of electrophysiology in finding new drugs and drug targets describes selectively acting b-adrenoceptor agonists and glucocorticoid steroids for asthma treatment outlines the rationale for using angiotensin receptor antagonists and more! Written by over 25 international authorities and containing nearly 1200 bibliographic citations, Receptor-Based Drug Design is a practical resource for pharmacologists, pharmacists, and pharmaceutical scientists; organic and medicinal chemists and biochemists; molecular biologists; biomedical researchers; and upper-level undergraduate and graduate students in these disciplines.

Biomedical Aspects of Histamine

Biomedical Aspects of Histamine PDF Author: Nancy Khardori
Publisher: Springer Science & Business Media
ISBN: 9048193494
Category : Medical
Languages : en
Pages : 451

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Book Description
Since its identification by Sir Henry H. Dale a century ago, histamine has become one of the most important multifunctional biogenic amines in the field of biomedicine. The pharmacological effects of histamine are mediated through four types of membrane histamine receptors; H1R, H2R, H3R and H4R, which are all heptahelical G-protein-coupled receptors. It has been known to play the broadest spectrum of activities in various physiological and pathological conditions including cell proliferation, differentiation, hematopoiesis, embryonic development, regeneration, wound healing, aminergic neurotransmission and numerous brain functions, secretion of pituitary hormones, regulation of gastrointestinal and circulatory functions, cardiovascular system, as well as inflammatory reactions, modulation of the immune response, endocrine function and homeostasis, and other important areas. This book is a compendium of the current state of established and investigational literature on Histamine, its receptors and their Agonists and antagonists. It provides a comprehensive overview of histamine biology in the field of biochemistry, cell biology, molecular biology, immunology, allergy, neurobiology, pharmacology, microbiology and reproductive biology. The first section on Histamine biology and physiology leads into subsequent sections on enzymology, pharmacology, regulation of the immune system and cell proliferation and role in allergic and other diseases including acid peptic diseases, inflammatory diseases, autoimmune and cancer diseases, nervous system, reproductive functions and hematopoiesis. The compilation of chapters in the book presents the most recent advances in histamine research and bridges the basic and clinical aspects of histamine biology.

Cognitive Enhancing Drugs

Cognitive Enhancing Drugs PDF Author: Jerry J. Buccafusco
Publisher: Birkhäuser
ISBN: 3034878672
Category : Medical
Languages : en
Pages : 213

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Book Description
During the past decade research into the pharmacology of cognition, particularly regarding learning and memory, has supported the concept that many potential neural targets exist for the development of cognitive-enhancing drugs. Whereas the main impetus for this research has been the ever growing population of individuals with dementing disorders such as Alzheimer`s disease, attention is also being focused on issues relating to cognitive impairment associated with "normal" aging. This book is useful as a source of information for making informed decisions regarding the relative utility and attributes of the various neural targets that have been studied to date.

Pharmacoepigenetics

Pharmacoepigenetics PDF Author: Ramón Cacabelos
Publisher: Academic Press
ISBN: 0128139404
Category : Medical
Languages : en
Pages : 986

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Book Description
Pharmacoepigenetics provides a comprehensive volume on the role of epigenetics and epigenomics in drug discovery and development, providing a detailed, but accessible, view of the field, from basic principles, to applications in disease therapeutics. Leading international researchers from across academia, clinical settings and the pharmaceutical industry discuss the influence of epigenetics and epigenomics in human pathology, epigenetic biomarkers for disease prediction, diagnosis, and treatment, current epigenetic drugs, and the application of epigenetic procedures in drug development. Throughout the book, chapter authors offer a balanced and objective discussion of the future of pharmacoepigenetics and its crucial contribution to the growth of precision and personalized medicine. - Fully examines the influence of epigenetics and epigenomics in human pathology, epigenetic biomarkers for disease prediction, diagnosis, treatment, current epigenetic drugs and the application of epigenetic procedures in drug development - Features chapter contributions from leading international researchers in academia, clinical settings and the pharmaceutical industry - Instructs researchers, students and clinicians on how to better interpret and employ pharmacoepigenetics in drug development, efficiency and safety - Provides a balanced and objective discussion of the future of pharmacoepigenetics and its crucial role in precision medicine

Textbook of Drug Design and Discovery, Third Edition

Textbook of Drug Design and Discovery, Third Edition PDF Author: Tommy Liljefors
Publisher: CRC Press
ISBN: 9780415282888
Category : Medical
Languages : en
Pages : 596

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Book Description
Building on the success of the previous editions, Textbook of Drug Design and Discovery has been thoroughly revised and updated to provide a complete source of information on all facets of drug design and discovery for students of chemistry, pharmacy, pharmacology, biochemistry, and medicine. The book follows drug design from the initial lead identification through optimization and structure-activity relationship with reference to the final processes of clinical evaluation and registration. Chapters investigate the design of enzyme inhibitors and drugs for particular cellular targets such as ion channels and receptors, and also explore specific classes of drug such as peptidomimetics, antivirals and anticancer agents. The use of gene technology in pharmaceutical research, computer modeling techniques, and combinatorial approaches are also included.