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Targeting Adenosine A2a Receptors In Parkinsons Disease And Other Cns Disorders
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Book Synopsis The Adenosinergic System by : Micaela Morelli
Download or read book The Adenosinergic System written by Micaela Morelli and published by Springer. This book was released on 2015-10-01 with total page 344 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Book Synopsis Targeting Adenosine A2A Receptors in Parkinson's Disease and Other CNS Disorders by : Michael A. Schwarzschild
Download or read book Targeting Adenosine A2A Receptors in Parkinson's Disease and Other CNS Disorders written by Michael A. Schwarzschild and published by . This book was released on 2007 with total page 86 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis Targeting Adenosine A2A Receptors in Parkinson's Disease by :
Download or read book Targeting Adenosine A2A Receptors in Parkinson's Disease written by and published by . This book was released on 2006 with total page 101 pages. Available in PDF, EPUB and Kindle. Book excerpt: In pursuit of an improved understanding and treatment of Parkinson's disease (PD) and related neuropsychiatric disease we have held a translational research conference entitled, "Targeting Adenosine A2A Receptors in ParkThson's Disease and other CNS Disorders" in Boston, May 17-19, 2006. Recent insights into the ONS functions of the adenosine A2A receptor, A2A receptor neurotoxicology, and intriguing environmental clues have all converged to markedly enhance the potential of A2A antagonists as a therapeutic strategy for PD. The goal of this conference was to facilitate the translation of advances in A2A receptor biology into improved therapy for PD by promoting the exchange of ideas on the basic science and clinical study of this molecular target.
Book Synopsis Adenosine A2A Receptor Antagonists by :
Download or read book Adenosine A2A Receptor Antagonists written by and published by Elsevier. This book was released on 2023-09-25 with total page 326 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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
Book Synopsis Adenosine Receptors and Parkinson's Disease by : Hiroshi Kase
Download or read book Adenosine Receptors and Parkinson's Disease written by Hiroshi Kase and published by Elsevier. This book was released on 1999-10-27 with total page 297 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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
Book Synopsis The Adenosine Receptors by : Pier Andrea Borea
Download or read book The Adenosine Receptors written by Pier Andrea Borea and published by Humana Press. This book was released on 2018-07-28 with total page 593 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Book Synopsis Novel Therapeutic Approaches to the Treatment of Parkinson’s Disease by : Corey R. Hopkins
Download or read book Novel Therapeutic Approaches to the Treatment of Parkinson’s Disease written by Corey R. Hopkins and published by Springer. This book was released on 2016-06-23 with total page 158 pages. Available in PDF, EPUB and Kindle. Book excerpt: Medicinal chemistry is both science and art. The science of medicinal chemistry offers mankind one of its best hopes for improving the quality of life. The art of medicinal chemistry continues to challenge its practitioners with the need for both intuition and experience to discover new drugs. Hence sharing the experience of drug research is uniquely beneficial to the field of medicinal chemistry. Drug research requires interdisciplinary team-work at the interface between chemistry, biology and medicine. Therefore, the topic-related series Topics in Medicinal Chemistry covers all relevant aspects of drug research, e.g. pathobiochemistry of diseases, identification and validation of (emerging) drug targets, structural biology, drugability of targets, drug design approaches, chemogenomics, synthetic chemistry including combinatorial methods, bioorganic chemistry, natural compounds, high-throughput screening, pharmacological in vitro and in vivo investigations, drug-receptor interactions on the molecular level, structure-activity relationships, drug absorption, distribution, metabolism, elimination, toxicology and pharmacogenomics. In general, special volumes are edited by well known guest editors.
Book Synopsis Investigations of Adenosine A2A Receptor Antagonists, Dopamine D2 Receptor Agonists and Dual Acting Ligands for the Treatment of Parkinson's Disease by : Manuela Jorg
Download or read book Investigations of Adenosine A2A Receptor Antagonists, Dopamine D2 Receptor Agonists and Dual Acting Ligands for the Treatment of Parkinson's Disease written by Manuela Jorg and published by . This book was released on 2014 with total page 490 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Book Synopsis The Adenosinergic System by : Micaela Morelli
Download or read book The Adenosinergic System written by Micaela Morelli and published by . This book was released on 2015 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: 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 health and disease, and (3) a study of urate as a possible biomarker and neuroprotectant.
Book Synopsis GPR37-ADENOSINE A2A Receptor-receptor Interaction as a New Pharmacological Target for Parkinson's Disease Treatment by : Xavier Morató Arús
Download or read book GPR37-ADENOSINE A2A Receptor-receptor Interaction as a New Pharmacological Target for Parkinson's Disease Treatment written by Xavier Morató Arús and published by . This book was released on 2017 with total page 254 pages. Available in PDF, EPUB and Kindle. Book excerpt: GPR37 is an orphan GPCR that belongs to the Rodhopsin family. GPR37 is highly expressed in the Central Nervous System (CNS), while little peripheral expression has been found in humans and rodents. GPR37 is highly distributed in the brain, particularly at the cerebellum, corpus callosum, substantia nigra, striatum and hippocampus with a predominantly neuronal distribution. However, the function of this receptor in the CNS remains unknown. The interest on GPR37 biology was bolstered when it was described as a Parkin substrate. GPR37 was isolated from a human brain library in a yeast 2-hybrid screen for novel interacting partners of Parkin, and thus rebaptized as “Parkin-associated endothelin-like receptor” (Pael-R). Parkin is of great interest because mutations in this gene are directly linked to autosomal recessive juvenile Parkinsonism (AR-JP).
Book Synopsis Neuroprotection by : Raymond Chuen-Chung Chang
Download or read book Neuroprotection written by Raymond Chuen-Chung Chang and published by BoD – Books on Demand. This book was released on 2019-08-28 with total page 104 pages. Available in PDF, EPUB and Kindle. Book excerpt: Neuroprotection is a strategy to prevent or delay the progression of chronic neurodegenerative diseases, acute neurological disorders, or even mental disorders. The major aim of this book is to focus on different approaches to achieve neuroprotection. In this book, there are chapters discussing imidazoline ligands and opioid ligands in Alzheimer's disease, the beneficial effects of adenosine A2A receptor antagonist, adrenergic receptor agonists and antagonists modulating microglial responses, and different approaches to achieve neuroprotection against aging-associated macular degeneration. This book will give insights to scientists in the field to stimulate their research, medical professionals to review their clinical practices, and others who would like to learn more about different neuroprotective approaches.
Book Synopsis Atlas of Neuroactive Substances and Their Receptors in the Rat by : Masaya Tohyama
Download or read book Atlas of Neuroactive Substances and Their Receptors in the Rat written by Masaya Tohyama and published by . This book was released on 1998 with total page 364 pages. Available in PDF, EPUB and Kindle. Book excerpt: The rat is probably the most widely used experimental system in neurobiology. Several anatomical atlases of the rat's nervous system already exist, but this atlas is unique in that it maps the distribution of all neuroactive substances--transmitters, growth factors, modulators, hormones, and peptides--and their receptors by brain region. It begins with a useful overview of neurotransmission mechanisms. The entire brain is then presented in highly visual three-color sections. The atlas covers the synthesis, distribution, and functions of each class of substances in intricate detail. The authors follow this with an analysis of the structure, subtypes, and distribution of receptors. The volume will be an invaluable reference work for all researchers in neuropharmacology, neurobiology, and neuropathology.
Book Synopsis Adenosine Receptors in Health and Disease by : Constance N. Wilson
Download or read book Adenosine Receptors in Health and Disease written by Constance N. Wilson and published by Springer Science & Business Media. This book was released on 2009-07-28 with total page 656 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Book Synopsis Adenosine Receptors in Neurology and Psychiatry by :
Download or read book Adenosine Receptors in Neurology and Psychiatry written by and published by Academic Press. This book was released on 2014-08-28 with total page 523 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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)
Book Synopsis Adenosine Receptors by : Gyorgy Hasko
Download or read book Adenosine Receptors written by Gyorgy Hasko and published by CRC Press. This book was released on 2006-07-20 with total page 377 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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
Book Synopsis Homeostatic Control of Brain Function by : Detlev Boison
Download or read book Homeostatic Control of Brain Function written by Detlev Boison and published by Oxford University Press. This book was released on 2016 with total page 657 pages. Available in PDF, EPUB and Kindle. Book excerpt: Homeostatic Control of Brain Function offers a broad view of brain health and diverse perspectives for potential treatments, targeting key areas such as mitochondria, the immune system, epigenetic changes, and regulatory molecules such as ions, neuropeptides, and neuromodulators. Loss of homeostasis becomes expressed as a diverse array of neurological disorders. Each disorder has multiple comorbidities - with some crossing over several conditions - and often disease-specific treatments remain elusive. When current pharmacological therapies result in ineffective and inadequate outcomes, therapies to restore and maintain homeostatic functions can help improve brain health, no matter the diagnosis. Employing homeostatic therapies may lead to future cures or treatments that address multiple comorbidities. In an age where brain diseases such as Alzheimer's or Parkinson's are ever present, the incorporation of homeostatic techniques could successfully promote better overall brain health. Key Features include · A focus on the homeostatic controls that significantly depend on the way one lives, eats, and drinks. · Highlights from emerging research in non-pharmaceutical therapies including botanical medications, meditation, diet, and exercise. · Incorporation of homeostatic therapies into existing basic and clinical research paradigms. · Extensive scientific basic and clinical research ranging from molecules to disorders. · Emerging practical information for improving homeostasis. · Examples of homeostatic therapies in preventing and delaying dysfunction. Both editors, Detlev Boison and Susan Masino, bring their unique expertise in homeostatic research to the overall scope of this work. This book is accessible to all with an interest in brain health; scientist, clinician, student, and lay reader alike.
Book Synopsis Adenosine Receptors in Neurodegenerative Diseases by : David Blum
Download or read book Adenosine Receptors in Neurodegenerative Diseases written by David Blum and published by Academic Press. This book was released on 2017-03-30 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: Adenosine Receptors in Neurodegenerative Diseases covers the role of adenosine receptors in brain function, also focusing on related methodologies and perspectives in therapeutics. The book provides an up-to-date overview by the best specialists in the field, helping readers consider the importance of adenosine and expand the global impact and visibility of adenosine research in the CNS field. Chapters include adenosine biology and signaling, gene regulation, control of motor function, and novel adenosine-based therapies in the CNS. It is an ideal resource for researchers, advanced graduate students, clinicians, and industry scientists working in the fields of clinical neuroscience and molecular and cellular neuroscience.