Histamine Receptors As Drug Targets

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Histamine Receptors as Drug Targets

Author : Ekaterini Tiligada,Madeleine Ennis
Publisher : Unknown
Page : 517 pages
File Size : 40,5 Mb
Release : 2017
Category : Biomedicine
ISBN : 1493968432

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Histamine Receptors as Drug Targets by Ekaterini Tiligada,Madeleine Ennis Pdf

"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." -- OCLC.

Histamine Receptors as Drug Targets

Author : Ekaterini Tiligada,Madeleine Ennis
Publisher : Humana
Page : 0 pages
File Size : 46,6 Mb
Release : 2017-03-09
Category : Medical
ISBN : 1493968416

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Histamine Receptors as Drug Targets by Ekaterini Tiligada,Madeleine Ennis Pdf

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.

The Histamine H3 Receptor

Author : R. Leurs,H. Timmerman
Publisher : Elsevier
Page : 290 pages
File Size : 50,8 Mb
Release : 1998-12-09
Category : Medical
ISBN : 0080534007

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The Histamine H3 Receptor by R. Leurs,H. Timmerman Pdf

In the early eighties when the H3 receptor was identified, many thought that an H3 ligand, an agonist or an antagonist, would become available as a therapeutic agent. This has not occurred. The reason for this could be the fact that many investigators consider histamine mainly, if not only, as a mediator present in for example mast cells being released during allergic events. However, it has become apparent that histamine is an important neurotransmitter. Its role in the nervous system, especially in the central part of it, is rather extensive. The H3 receptor is mainly found as a presynaptic one, both on histaminergic neurons (the auto-type) and on other neuronal systems (the hetero-type). Both the H3 agonist and the H3 antagonist cause important pharmacological effects. Several ligands have become available now, including radiolabelled analogues. In this book, the current state of affairs with regards to the medicinal chemistry and pharmacology of the H3 receptor and the several ligands available are presented by a number of experts in the field. The book presents an extended review of what has happened since the first H3 paper appeared. The editors hope that publication of this work will lead to an increase in interest of both academia and industry for the H3 receptor, especially as a target for drug development.

Histamine H4 receptor

Author : Holger Stark
Publisher : Walter de Gruyter
Page : 368 pages
File Size : 54,7 Mb
Release : 2013-11-20
Category : Science
ISBN : 9788376560564

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Histamine H4 receptor by Holger Stark Pdf

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.

Pharmacology of Histamine Receptors

Author : C. R. Ganellin,M. E. Parsons
Publisher : Elsevier
Page : 540 pages
File Size : 50,8 Mb
Release : 2013-10-22
Category : Medical
ISBN : 9781483193410

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Pharmacology of Histamine Receptors by C. R. Ganellin,M. E. Parsons Pdf

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.

G Protein-Coupled Receptors as Drug Targets

Author : Roland Seifert,Thomas Wieland
Publisher : John Wiley & Sons
Page : 304 pages
File Size : 49,8 Mb
Release : 2006-05-12
Category : Science
ISBN : 9783527606955

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G Protein-Coupled Receptors as Drug Targets by Roland Seifert,Thomas Wieland Pdf

With its particular emphasis on the constitutive activity of G-protein-coupled receptors (GPCRs)s, this book comprehensively discusses an important biological process that has not yet been covered in such depth in any other existing books on GPCRs. The international team of highly distinguished authors addresses in detail current models and concepts, to introduce medicinal chemists, physiologists, pharmacologists, and medical researchers into the advances in the understanding of GPCR activation and constitutive activity. In addition, the book provides an overview on methods of investigating constitutive GPCR activity. The text is well illustrated by selected experimental data and schemes._The chaptes are all cross-referenced with each other and cover general mechnisms, methodological approaches and cover selected important GPCR sysstems, the consequences for drug action, including, side effects, and rational drug design for GPCR targets. A highly recommended reference for researchers in academia and industry. authors addresses in detail current models and concepts, so as to introduce pharmaceutical chemists, physiologists and medical researchers to the advances in the understanding of GPCR activation and constitutive activity, and provides an overview of the methods of investigating GPCR activity. The text is backed by abundant case studies and methodological advice for analyzing GPCRs, covering selected pharmacologically relevant GPCR systems, the consequences for drug action, including unwanted side effects, and rational drug design for GPCR targets. A highly practical reference for researchers in academia and industry.

Histamine in the brain

Author : Jian-Sheng Lin,Pertti Panula,Maria Beatrice Passani
Publisher : Frontiers Media SA
Page : 100 pages
File Size : 55,6 Mb
Release : 2015-03-18
Category : Brain
ISBN : 9782889194346

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Histamine in the brain by Jian-Sheng Lin,Pertti Panula,Maria Beatrice Passani Pdf

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.

Hepatotoxicity

Author : Hyman J. Zimmerman
Publisher : Lippincott Williams & Wilkins
Page : 848 pages
File Size : 50,9 Mb
Release : 1999
Category : Medical
ISBN : 0781719526

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Hepatotoxicity by Hyman J. Zimmerman Pdf

Written by the foremost authority in the field, this volume is a comprehensive review of the multifaceted phenomenon of hepatotoxicity. Dr. Zimmerman examines the interface between chemicals and the liver; the latest research in experimental hepatotoxicology; the hepatotoxic risks of household, industrial, and environmental chemicals; and the adverse effects of drugs on the liver. This thoroughly revised, updated Second Edition features a greatly expanded section on the wide variety of drugs that can cause liver injury. For quick reference, an appendix lists these medications and their associated hepatic injuries. Also included are in-depth discussions of drug metabolism and factors affecting susceptibility to liver injury.

Cognitive Enhancing Drugs

Author : Jerry J. Buccafusco
Publisher : Birkhäuser
Page : 213 pages
File Size : 53,9 Mb
Release : 2012-12-06
Category : Medical
ISBN : 9783034878678

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Cognitive Enhancing Drugs by Jerry J. Buccafusco Pdf

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.

Itch

Author : E. Carstens,Tasuku Akiyama
Publisher : CRC Press
Page : 482 pages
File Size : 50,9 Mb
Release : 2014-02-25
Category : Science
ISBN : 9781466505438

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Itch by E. Carstens,Tasuku Akiyama Pdf

Advances in itch research have elucidated differences between itch and pain but have also blurred the distinction between them. There is a long debate about how somatic sensations including touch, pain, itch, and temperature sensitivity are encoded by the nervous system. Research suggests that each sensory modality is processed along a fixed, direct-line communication system from the skin to the brain. Itch: Mechanisms and Treatment presents a timely update on all aspects of itch research and the clinical treatment of itch that accompanies many dermatological conditions including psoriasis, neuropathic itch, cutaneous t-cells lymphomas, and systemic diseases such as kidney and liver disease and cancer. Composed of contributions from distinguished researchers around the world, the book explores topics such as: Neuropathic itch Peripheral neuronal mechanism of itch The role of PAR-2 in neuroimmune communication and itch Mrgprs as itch receptors The role of interleukin-31 and oncostatin M in itch and neuroimmune communication Spinal coding of itch and pain Spinal microcircuits and the regulation of itch Examining new findings on cellular and molecular mechanisms, the book is a compendium of the most current research on itch, its prevalence in society, and the problems associated with treatment.

Biomedical Aspects of Histamine

Author : Nancy Khardori,Rahat Ali Khan,Trivendra Tripathi
Publisher : Springer Science & Business Media
Page : 451 pages
File Size : 46,7 Mb
Release : 2010-09-30
Category : Medical
ISBN : 9789048193493

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Biomedical Aspects of Histamine by Nancy Khardori,Rahat Ali Khan,Trivendra Tripathi Pdf

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.

Human Drug Targets

Author : Edward D. Zanders
Publisher : John Wiley & Sons
Page : 456 pages
File Size : 41,7 Mb
Release : 2015-12-14
Category : Science
ISBN : 9781118849835

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Human Drug Targets by Edward D. Zanders Pdf

The identification of drug targets in a given disease has been central to pharmaceutical research from the latter half of the 20th century right up to the modern genomics era. Human Drug Targets provides an essential guide to one of the most important aspects of drug discovery – the identification of suitable protein and RNA targets prior to the creation of drug development candidates. The first part of the book consists of introductory chapters that provide the background to drug target discovery and highlight the way in which these targets have been organised into online databases. It also includes a user’s guide to the list of entries that forms the bulk of the book. Since this is not designed to be a compendium of drugs, the emphasis will be on the known (or speculated) biological role of the targets and not on the issues associated with pharmaceutical development. The objective is to provide just enough information to be informative and prompt further searches, while keeping the amount of text for each of the many entries to a minimum. Human Drug Targets will prove invaluable to those drug discovery professionals, in both industry and academia, who need to make some sense of the bewildering array of online information sources on current and potential human drug targets. As well as creating order out of a complex target landscape, the book will act as an ideas generator for potentially novel targets that might form the basis of future discovery projects.

Blood-Spinal Cord and Brain Barriers in Health and Disease

Author : Hari Shanker Sharma
Publisher : Elsevier
Page : 605 pages
File Size : 48,6 Mb
Release : 2003-12-21
Category : Science
ISBN : 9780080528229

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Blood-Spinal Cord and Brain Barriers in Health and Disease by Hari Shanker Sharma Pdf

Recent research into the anatomy and pathophysiology of the blood-brain and blood-spinal cord barriers suggests that a breakdown in these barriers can result in several diseases affecting the central nervous system (CNS). This book presents new findings in the area of blood-brain barrier research that suggest barriers play important roles in health and disease conditions. It also discusses the development of new drugs that can modulate the barrier function in the CNS and may provide new approaches to treating neurological diseases such as Alzheimer's disease and other motor neuron diseases, as well as spinal cord trauma. Key Features * Presents the recent progress made in the research on the blood-brain and spinal cord barrier * Contains numerous illustrations of light and electron micrographs * Includes Foreword written by two eminent researchers in the field, Milton Brightman and Jorge Cervos-Navarro

Receptor - Based Drug Design

Author : Paul Leff
Publisher : CRC Press
Page : 816 pages
File Size : 53,7 Mb
Release : 1998-04-10
Category : Medical
ISBN : 1420001132

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Receptor - Based Drug Design by Paul Leff Pdf

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.

Parasite Neuromusculature and Its Utility as a Drug Target

Author : Aaron G. Maule,T. A. Day,L. H. Chappell
Publisher : Cambridge University Press
Page : 208 pages
File Size : 45,9 Mb
Release : 2006-10-19
Category : Science
ISBN : 0521691788

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Parasite Neuromusculature and Its Utility as a Drug Target by Aaron G. Maule,T. A. Day,L. H. Chappell Pdf

Nerve and muscle systems in helminth parasites interact in a highly co-ordinated manner to control movements associated with alimentation, reproduction, locomotion and attachment. All metazoan parasites rely on some or all of these activities for their survival. For a long time it has been known that neuromuscular function in parasites is susceptible to chemotherapeutic attack, and that compromising this aspect of parasite biology is sufficient to cure many parasite infections. This volume outlines the latest research in this area, showing why this system is so amenable to drug intervention and outlining potential targets for new treatments. Written by experts in the field, this volume will be invaluable to anyone interested in the molecular biology, physiology and biochemistry of parasites as well as those looking to exploit these for the creation of new treatments.