The Histamine H3 Receptor

Author : R. Leurs,H. Timmerman
Publisher : Elsevier
Page : 290 pages
File Size : 51,7 Mb
Release : 1998-12-09
Category : Medical
ISBN : 0080534007

Get Book

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.

Author : Birgit Schlegel
Publisher : Cuvillier Verlag
Page : 221 pages
File Size : 50,7 Mb
Release : 2005
Category : Electronic
ISBN : 9783865376015

Get Book

The Human Histamine H_1tn3-receptor by Birgit Schlegel Pdf

Author : Divya Vohora
Publisher : CRC Press
Page : 408 pages
File Size : 40,8 Mb
Release : 2008-11-14
Category : Medical
ISBN : 9781000687361

Get Book

The Third Histamine Receptor by Divya Vohora Pdf

Reveals an Emerging Avenue of Potential Treatments for a Host of Challenging Diseases and DisordersThe H3 receptor is known to play a major role in a range of CNS disorders, including those affecting cognitive functions such as ADHD and Alzheimer's disease, as well as sleep disorders, obesity, epilepsy, schizophrenia, depression, and neurodege

Author : Jian-Sheng Lin,Pertti Panula,Maria Beatrice Passani
Publisher : Frontiers Media SA
Page : 100 pages
File Size : 40,7 Mb
Release : 2015-03-18
Category : Brain
ISBN : 9782889194346

Get Book

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.

Author : Kazuhiko Yanai,Maria Beatrice Passani
Publisher : Springer Nature
Page : 463 pages
File Size : 40,9 Mb
Release : 2022-09-28
Category : Medical
ISBN : 9783031169977

Get Book

The Functional Roles of Histamine Receptors by Kazuhiko Yanai,Maria Beatrice Passani Pdf

Research in the field of histamine receptors over the past 100 years went hand-in-hand with the development of modern pharmacology. Advances in histamine research led by outstanding scientists was so incisive that the clinical approach to treat allergies and gastrointestinal ailments was revolutionized. The pharmacological treatment of peptic ulcer and gastroesophageal reflux was indeed a revolution, as it ended the surgical intervention. Interest in histamine pharmacology was resurrected by the discovery of another histamine receptor, number 4, using genomics-based reverse pharmacological approaches for screening orphan GPCRs. This receptor is preferentially expressed by immune cells and its discovery raised hopes for its translational exploitation as a new therapeutic target for unmet medical needs ranging from asthma to cancer. However, several drawbacks emerged and dramatically slowed down research in the field. A better understanding of receptor intra-and interspecies heterogeneity will certainly improve and accelerate the translation of experimental data into clinical practice. Also, the plethora of data on brain histamine is hinting at a fundamental role of this system as a hub that receives internal and peripheral stimuli to allocate the necessary excitation to specific brain circuits that preside the appropriate behavioral responses. The development of new histaminergic ligands is an ongoing process that constantly provide new preclinical tools. The aim of this book is to cover the most important aspects of histamine receptor function and pharmacology in the central nervous system and to provide a comprehensive overview of the preclinical and clinical advances made in recent decades and the exciting prospects for the future. It highlights the clinical areas where there is a great need for new therapeutic approaches and where novel histaminergic agents may be useful for personalized medicine.

Author : Ekaterini Tiligada,Madeleine Ennis
Publisher : Humana
Page : 0 pages
File Size : 53,8 Mb
Release : 2017-03-09
Category : Medical
ISBN : 1493968416

Get Book

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.

Author : Robin Thurmond
Publisher : Springer Science & Business Media
Page : 153 pages
File Size : 40,7 Mb
Release : 2011-06-29
Category : Medical
ISBN : 9781441980564

Get Book

Histamine in Inflammation by Robin Thurmond Pdf

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.

Author : Patrizio Blandina,Maria Beatrice Passani
Publisher : Springer
Page : 378 pages
File Size : 54,7 Mb
Release : 2016-11-07
Category : Medical
ISBN : 9783319403083

Get Book

Histamine Receptors by Patrizio Blandina,Maria Beatrice Passani Pdf

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.

Author : J¿nos Fischer,Christian Klein,Wayne E. Childers
Publisher : John Wiley & Sons
Page : 472 pages
File Size : 48,7 Mb
Release : 2018-06-05
Category : Medical
ISBN : 9783527343034

Get Book

Successful Drug Discovery, Volume 3 by J¿nos Fischer,Christian Klein,Wayne E. Childers Pdf

With its focus on drugs so recently introduced that they have yet to be found in any other textbooks or general references, the information and insight found here makes this a genuinely unique handbook and reference. Following the successful approach of the previous volumes in the series, inventors and primary developers of successful drugs from both industry and academia tell the story of the drug's discovery and describe the sometimes twisted route from the first drug candidate molecule to the final marketed drug. The 11 case studies selected describe recent drugs ranging across many therapeutic fields and provide a representative cross-section of present-day drug developments. Backed by plenty of data and chemical information, the insight and experience of today's top drug creators makes this one of the most useful training manuals that a junior medicinal chemist may hope to find. The International Union of Pure and Applied Chemistry has endorsed and sponsored this project because of its high educational merit.

Author : Hari Shanker Sharma
Publisher : Elsevier
Page : 623 pages
File Size : 54,6 Mb
Release : 2003-12-21
Category : Medical
ISBN : 9780080528229

Get Book

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

Author : Anonim
Publisher : Elsevier
Page : 418 pages
File Size : 47,6 Mb
Release : 2021-10-22
Category : Science
ISBN : 9780323989282

Get Book

Brain Protection Strategies and Nanomedicine by Anonim Pdf

Brain Protection Strategies and Nanomedicine, Volume 266 in the Progress in Brain Research serial highlights new advances in the field, with this new volume presenting interesting chapters on a variety of topics, including Histamine H3 and H4 receptors modulate Parkinson’s disease induced brain pathology: Neuroprotective effects of nanowired BF-2649 and clobenpropit with anti-histamine-antibody therapy, Ultra Early Molecular Biologic Diagnosis Of Malignant And Neurodegenerative Diseases By The Immunospecific Profiles Of The Proteins Markers Of The Surface Of The Mobilized Autologous Hematopoietic Stem Cells, Neuroprotective effects of Insulin like growth factor-1 on Engineered metal Nanoparticles Ag, Cu and Al induced blood-brain barrier breakdown, and more. Other chapters cover how Methamphetamine exacerbates pathophysiology of traumatic brain injury at high altitude: Neuroprotective effects of nanodelivery of a potent antioxidant compound H-290/51, Effectiveness of bortezomib and temozolomide for eradication of recurrent human glioblastoma cells, resistant to radiation, and more. Provides the authority and expertise of leading contributors from an international board of authors Presents the latest release in Progress in Brain Research serials Includes the latest information on brain protection strategies and nanomedicine

Author : Om Silakari
Publisher : Elsevier
Page : 436 pages
File Size : 46,5 Mb
Release : 2018-06-11
Category : Science
ISBN : 9780081021057

Get Book

Key Heterocycle Cores for Designing Multitargeting Molecules by Om Silakari Pdf

Key Heterocycle Cores for Designing Multitargeting Molecules provides a helpful overview of current developments in the field. Following a detailed introduction to the manipulation of heterocycle cores for the development of dual or multitargeting molecules, the book goes on to describe specific examples of such developments, focusing on compounds such as Benzimidazole, Acridine, Flavones, Thiazolidinedione and Oxazoline. Drawing on the latest developments in the field, this volume provides a valuable guide to current approaches in the design and development of molecules capable of acting on multiple targets. Adapting the heterocyclic core of a single-target molecule can facilitate its development into an agent capable of acting on multiple targets. Such multi-targeting drugs have the potential to become essential components in the design of novel, holistic treatment plans for complex diseases, making the design of such active agents an increasingly important area of research. Emphasizes the chemical development of heterocyclic nuclei, from single to multitargeting molecules Provides chapter-by-chapter coverage of the key heterocyclic compounds used in synthesizing multitargeting agents Outlines current trends and future developments in multitarget molecule design for the treatment of various diseases

Author : Anonim
Publisher : ScholarlyEditions
Page : 24 pages
File Size : 41,5 Mb
Release : 2012-12-26
Category : Medical
ISBN : 9781481633277

Get Book

Histamine Receptors—Advances in Research and Application: 2012 Edition by Anonim Pdf

Histamine Receptors—Advances in Research and Application: 2012 Edition is a ScholarlyPaper™ that delivers timely, authoritative, and intensively focused information about Histamine Receptors in a compact format. The editors have built Histamine Receptors—Advances in Research and Application: 2012 Edition on the vast information databases of ScholarlyNews.™ You can expect the information about Histamine Receptors in this eBook to be deeper than what you can access anywhere else, as well as consistently reliable, authoritative, informed, and relevant. The content of Histamine Receptors—Advances in Research and Application: 2012 Edition has been produced by the world’s leading scientists, engineers, analysts, research institutions, and companies. All of the content is from peer-reviewed sources, and all of it is written, assembled, and edited by the editors at ScholarlyEditions™ and available exclusively from us. You now have a source you can cite with authority, confidence, and credibility. More information is available at http://www.ScholarlyEditions.com/.

Author : Davide Martino,James Leckman
Publisher : Oxford University Press
Page : 577 pages
File Size : 55,5 Mb
Release : 2022
Category : Medical
ISBN : 9780197543214

Get Book

Tourette Syndrome by Davide Martino,James Leckman Pdf

Tourette syndrome (TS) has become increasingly recognised within society and has gained scientific interest worldwide. Knowledge of its clinical presentation, mechanisms of disease, and available treatment approaches has increased remarkably over the last two decades. Likewise, the way clinicians, teachers, social care workers, and families face the problems manifested by patients with TS is rapidly evolving. Tourette Syndrome, edited by Davide Martino and James F. Leckman, offers a unique opportunity to capture this knowledge advance through a comprehensive and up-to-date overview. Tourette Syndrome covers all the main aspects related to TS, analyzing its complex clinical presentation, the novel viewpoints of causes and mechanisms, state-of-the-art assessment techniques, and the diversity of treatment options. Multidisciplinarity is the main asset of this volume, which represents a source of consultation for a wide audience of professionals, integrated with video tutorials related to particularly complex areas of patient management. Medical and PhD students, as well as post-doctoral scientists, will be able to use the volume as a valuable learning source.

Author : C. R. Ganellin,M. E. Parsons
Publisher : Elsevier
Page : 540 pages
File Size : 51,6 Mb
Release : 2013-10-22
Category : Medical
ISBN : 9781483193410

Get Book

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.