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Author: Publisher: Elsevier ISBN: 0443186685 Category : Medical Languages : en Pages : 326
Book Description
Adenosine A2A Receptor Antagonists, Volume 170 in the International Review of Neurobiology series highlights new advances in the field, with this new volume presenting interesting chapters on a variety of timely topics, including A2A Adenosine Receptor Agonists, Antagonists, Inverse Agonists and Partial Agonist, Chemistry – agonists, antagonists, partial agonists, inverse agonists, Functional roles of adenosine receptors – biochemistry and neuronal plasticity, A2A and Depression, A2AR and glial function, The adenosine A2A receptor in the basal ganglia: expression in health and disease, heteromerization, functional selectivity and signaling, How and why A2a receptor become to be a therapeutic target in Parkinson's disease therapy, and much more. - Provides the authority and expertise of leading contributors from an international board of authors - Presents the latest release in the International Review of Neurobiology - Updated release includes the latest information on Adenosine A2A Receptor Antagonists
Author: Publisher: Elsevier ISBN: 0443186685 Category : Medical Languages : en Pages : 326
Book Description
Adenosine A2A Receptor Antagonists, Volume 170 in the International Review of Neurobiology series highlights new advances in the field, with this new volume presenting interesting chapters on a variety of timely topics, including A2A Adenosine Receptor Agonists, Antagonists, Inverse Agonists and Partial Agonist, Chemistry – agonists, antagonists, partial agonists, inverse agonists, Functional roles of adenosine receptors – biochemistry and neuronal plasticity, A2A and Depression, A2AR and glial function, The adenosine A2A receptor in the basal ganglia: expression in health and disease, heteromerization, functional selectivity and signaling, How and why A2a receptor become to be a therapeutic target in Parkinson's disease therapy, and much more. - Provides the authority and expertise of leading contributors from an international board of authors - Presents the latest release in the International Review of Neurobiology - Updated release includes the latest information on Adenosine A2A Receptor Antagonists
Author: Hiroshi Kase Publisher: Elsevier ISBN: 0080525954 Category : Medical Languages : en Pages : 297
Book Description
This book is the first definitive overview on adenosine receptor antagonists and their application to the treatment of Parkinson's Disease. The effect of these novel non-dopamine drugs on vitro and in vivo systems clearly shows their potential for the treatment of this debilitating disease. This book covers how the Parkinson's disease antagonist drug, A2A, has been researched, developed, and tested. It is an essential book for researchers interested in the basal ganglia, purine biology, and Parkinson's Disease. - Discusses the discovery and development of a novel non-dopaminomimetic agent for Parkinson's disease - Provides the first definitive overview of adenosine antagonists and their role in the treatment of Parkinson's disease - Presents a new mechanism of action of adenosine A2A receptor antagonists in motor function Proposes a hypothesis of adenosine A2A receptor function in the striatum - Comprehensive overview of adenosine, its receptor subtypes, their antagonists/agonists from biochemistry, molecular biology, medicinal chemistry, physiology, pharmacology, and neurochemistry viewpoints
Author: Micaela Morelli Publisher: Springer ISBN: 3319202731 Category : Medical Languages : en Pages : 344
Book Description
Adenosine A2A receptor antagonists have shown great promise in the treatment of Parkinson's Disease and alleviation of symptoms. This book addresses various aspects of this class of drugs from their chemical development to their clinical use. Among the many insightful chapters contained in this book, there are three unique reviews that have not previously been published in any format: (1) a history of istradefylline, the first A2A antagonist approved for treatment of Parkinson's Disease, (2) an overview of neuroimaging studies in human death and disease and (3) a study of urate as a possible biomarker and neuroprotectant.
Author: Pier Andrea Borea Publisher: Humana Press ISBN: 3319908081 Category : Medical Languages : en Pages : 603
Book Description
This book traces the history of adenosine receptor research from molecular biology to medicinal chemistry to behavior, including their implications in disease and potential strategies as therapeutic targets. It provides the reader with a comprehensive overview of the adenosine receptors that includes information on all subtypes - A1, A2A, A2B and A3. Aspects addressed include the most up to date information on their functional distribution in the nervous and peripheral systems, behavioral roles in inflammation, cancer, pain and neurological diseases such as Huntington’s disease, Epilepsy, Parkinson’s disease and Alzheimer’s disease.
Author: Manuela Jorg Publisher: ISBN: Category : Languages : en Pages : 490
Book Description
In this project, the adenosine A2A receptor and the dopamine D2 receptor were studied as potential targets for the treatment of Parkinson's disease. Investigated were both targets individually as well as the approach to target both receptors simultaneously with just one single molecule.Herein, present is the synthesis, characterization and pharmacological evaluation of the literature compound ZM 241385 and a series of structurally related adenosine A2A receptor antagonists. Further determined was a chemically and biologically suitable attachment position for linkers on the parent pharmacophores. From this research a triazolotriazine carboxylic acid congener with inhibitory potency equivalent to ZM 241385 has been established, allowing further functionalization towards the extracellular space of the adenosine A2A receptor. At the dopamine D2 receptor, a chemically and biologically suitable attachment position on the chemical structure of the dopamine D2 receptor agonist ropinirole was determined, allowing the development of an oxindole carboxylic acid and an oxindole amine congener. Based on these results a series of homobivalent ligands was synthesized, characterized and pharmacologically evaluated. The homobivalent ligands with a spacer length of 22 to 30 atoms exhibited up to an 80-fold increase in potency compared to the parent molecule ropinirole. Docking of the synthesized molecules in a dopamine D2 receptor dimer model indicated that the increase in potency of the homobivalent ligands was most likely due to an additional allosteric interaction and very unlikely due to interactions at two orthosteric sites across a homodimer. The research results from targeting each receptor individually formed the pillars for the synthesis, characterization and pharmacological evaluation of our dual acting ligands targeting the dopamine D2 and adenosine A2A receptors with just one molecule. A library of compounds ranging from classical heterobivalent ligands to more drug-like merged molecules was synthesized. The most encouraging higher integrated "drug-like" molecules exhibited promising initial blood-brain barrier permeability results and maintained similar EC50 values to the dopamine D2 receptor agonist ropinirole but showed a slight decrease in inhibitory potency compared to the adenosine A2A receptor antagonist ZM 241385. Conversely, the pharmacological evaluation of the dual acting ligands revealed that the most potent classical heterobivalent ligands showed comparable affinities to both original pharmacophores.
Author: Publisher: Academic Press ISBN: 0128013184 Category : Science Languages : en Pages : 523
Book Description
This well-established international series examines major areas of basic and clinical research within neuroscience, as well as emerging and promising subfields. This volume concentrates on adenosine receptor science, providing insights useful for actual drug discovery/development in neurology and psychiatry areas. - Expertise of contributors - Subject including practical drug development from basic science, as translational research taste - Structure of contents focusing on two CNS areas for diseases (neurology and psychiatry)
Author: Publisher: Academic Press ISBN: 0123739616 Category : Medical Languages : en Pages : 1853
Book Description
As a truly translational area of biomedical investigation, epilepsy research spans an extraordinary breadth of subjects and involves virtually every tool that modern neuroscience has at its disposal. The Encyclopedia of Basic Epilepsy Research provides an up to date, comprehensive reference for all epilepsy researchers. With an expert list of authors, the encyclopedia covers the full spectrum of research activities from genes and molecules to animal models and human patients. The encyclopedia's electronic format also provides unparalleled access to frequent updates and additions, while the limited edition print version provides another option for owning this content. The Encyclopedia of Basic Epilepsy Research is an essential resource for researchers of all levels and clinicians who study epilepsy. The only comprehensive reference for basic research and current activities in epilepsy Electronic format provides fast and easy access to updates and additions, with limited print version available as well Contains over 85 articles, all written by experts in epilepsy research
Author: Constance N. Wilson Publisher: Springer Science & Business Media ISBN: 3540896155 Category : Medical Languages : en Pages : 656
Book Description
Since their discovery approximately 25 years ago, adenosine receptors have now emerged as important novel molecular targets in disease and drug discovery. These proteins play important roles in the entire spectrum of disease from inflammation to immune suppression. Because of their expression on a number of different cell types and in a number of different organ systems they play important roles in specific diseases, including asthma, rheumatoid arthritis, Parkinson’s disease, multiple sclerosis, Alzheimer’s disease, heart disease, stroke, cancer, sepsis, and obesity. As a result of intense investigations into understanding the molecular structures and pharmacology of these proteins, new molecules have been synthesized that have high specificity for these proteins and are now entering clinical trials. These molecules will define the next new classes of drugs for a number of diseases with unmet medical needs.
Author: Gyorgy Hasko Publisher: CRC Press ISBN: 1420005774 Category : Medical Languages : en Pages : 377
Book Description
After a century of research, several lines of evidence now indicate that the ability of adenosine to directly control inflammatory cells has a major impact on the functions of the inflammatory and immune systems. Consequently, many promising therapeutic approaches are beginning to emerge that focus on the modulation of adenosine, including the deve
Author: Publisher: Academic Press ISBN: 0128137444 Category : Science Languages : en Pages : 756
Book Description
Handbook of Sleep Research, Volume 30, provides a comprehensive review of the current status of the neuroscience of sleep research. It begins with an overview of the neural, hormonal and genetic mechanisms of sleep and wake regulation before outlining the various proposed functions of sleep and the role it plays in plasticity, and in learning and memory. Finally, the book discusses disorders of sleep and waking, covering both lifestyle factors that cause disrupted sleep and psychiatric and neurological conditions that contribute to disorders. Emphasizes a comparative and multidisciplinary approach to the topic of sleep Covers the neurobiology and physiology of sleep stages, mechanisms of waking, and dreaming Discusses in detail the proposed functions of sleep, from health and rest, to memory consolidation and synaptic plasticity Examines the current state of research in mammalian and non-mammalian species, ranging from primates to invertebrates
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Author: Hiroshi Kase
Author: Micaela Morelli
Author: Pier Andrea Borea
Author: Manuela Jorg
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Author: Constance N. Wilson
Author: Gyorgy Hasko
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