Antagonists

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The Antagonist

Author : Lynn Coady
Publisher : Vintage
Page : 286 pages
File Size : 43,9 Mb
Release : 2013-01-22
Category : Fiction
ISBN : 9780307961365

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The Antagonist by Lynn Coady Pdf

A piercing epistolary novel, The Antagonist explores, with wit and compassion, how the impressions of others shape, pervert, and flummox both our perceptions of ourselves and our very nature. Gordon Rankin Jr., aka “Rank,” thinks of himself as “King Midas in reverse”—and indeed misfortune seems to follow him at every turn. Against his will and his nature, he has long been considered—given his enormous size and strength—a goon and enforcer by his classmates, by his hockey coaches, and, not least, by his “tiny, angry” father. He gamely lives up to their expectations, until a vicious twist of fate forces him to flee underground. Now pushing forty, he discovers that an old, trusted friend from his college days has published a novel that borrows freely from the traumatic events of Rank’s own life. Outraged by this betrayal and feeling cruelly misrepresented, he bashes out his own version of his story in a barrage of e-mails to the novelist that range from funny to furious to heartbreaking. With The Antagonist, Lynn Coady demonstrates all of the gifts that have made her one of Canada’s most respected young writers. Here she gives us an astonishing story of sons and fathers and mothers, of the rewards and betrayals of male friendship, and a large-spirited, hilarious, and exhilarating portrait of a man tearing his life apart in order to put himself back together. This ebook edition includes a Reading Group Guide.

Opiate Receptors and Antagonists

Author : Reginald Dean,Edward J. Bilsky,S. Stevens Negus
Publisher : Springer Science & Business Media
Page : 757 pages
File Size : 41,7 Mb
Release : 2009-03-12
Category : Medical
ISBN : 9781597451970

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Opiate Receptors and Antagonists by Reginald Dean,Edward J. Bilsky,S. Stevens Negus Pdf

Comprehensive and authoritative, Opioid Receptors and Antagonists: From Bench to Clinic offers neuroscientists, pharmacologists and interested clinicians a unique survey of the extensive and diverse research efforts currently employed with opioid antagonists to develop novel innovative drug therapies. Summarizes the present understanding of the chemistry, pharmacology and molecular biology of opioid receptors and their subtypes Highlights differences and similarities between the opioid pharmacology of animals and human Describes current and potential therapeutic areas for opioid antagonists, including substance abuse, alcohol and ingestive behaviors, behavioral disorders and other medical indications, supported by nonclinical and clinical evidence Focuses on the development of exciting and innovative drug delivery approaches that are being used with opioid antagonists for the above medical indications

Calcium Antagonists in the Treatment of Hypertension in Pregnancy

Author : C. Romanini,A.L. Tranquilli
Publisher : CRC Press
Page : 174 pages
File Size : 44,7 Mb
Release : 1999-09-15
Category : Medical
ISBN : 1850704686

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Calcium Antagonists in the Treatment of Hypertension in Pregnancy by C. Romanini,A.L. Tranquilli Pdf

This is a clinician's and researcher's reference text on using calcium antagonists - calcium channel blockers - in the treatment of gestational hypertension and pre-eclampsia. It contains twelve chapters covering experimental and clinical studies on the major calcium antagonists, their definition and classification and pharmacological profile, which drugs to use and when and which drugs to avoid. It also describes nifedipine pharmacodynamics and pharmacokinetics and covers nifedipine first-line treatment of gestational hypertension and pre-eclampsia along with chapters on second-line treatment and nifedipine blood cells and blood rheology. The book provides a comparison between two calcium antagonists in treating gestational hypertension and new categories to classify pre-eclampsia. Includes bibliographic references and index.

Nmda Antagonists As Potential Analgesic Drugs

Author : Dalip J.S. Sirinathsinghji,Ray G. Hill
Publisher : Springer Science & Business Media
Page : 212 pages
File Size : 53,6 Mb
Release : 2002
Category : Medical
ISBN : 3764360119

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Nmda Antagonists As Potential Analgesic Drugs by Dalip J.S. Sirinathsinghji,Ray G. Hill Pdf

There is now considerable preclinical evidence that glutamate acting via the NMDA receptor is involved in the transmission of nociceptive information and in the triggering mechanisms for hyperalgesia and allodynia. This evidence allows rational development of a new class of analgesic drugs that act as antagonists of the NMDA receptor, supported by emerging evidence with existing excitatory amino acid antagonists. Leading scientists in excitatory amino acid and analgesia research have compiled in this volume the most recent information on molecular biology, physiology and pharmacology of NMDA receptors, their neuroanatomical localisation within specific neural pathways involved in nociception, and experimental and clinical evidence demonstrating the potential of receptor antagonists of NMDA and other excitatory amino acids in the treatment of pain states.

Hormone antagonists

Author : M.K. Agarwal
Publisher : Walter de Gruyter GmbH & Co KG
Page : 744 pages
File Size : 43,7 Mb
Release : 2019-05-20
Category : Medical
ISBN : 9783111506753

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Hormone antagonists by M.K. Agarwal Pdf

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Calcium Antagonists

Author : T. Godfraind,S. Govoni,Rodolfo Paoletti,Paul M. Vanhoutte
Publisher : Springer Science & Business Media
Page : 382 pages
File Size : 46,9 Mb
Release : 2013-03-14
Category : Medical
ISBN : 9789401117258

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Calcium Antagonists by T. Godfraind,S. Govoni,Rodolfo Paoletti,Paul M. Vanhoutte Pdf

Although the importance of calcium (Ca2+) in the maintenance of cardiac contractility was recognized as early as 1880, the critical role of the ion in the contractile process in skeletal, cardiac, and smooth muscle has only been established within the last three decades. As the complexity of the pharmacological actions of the Ca2+ channel inhibitors grows, there is a continued need to further clarify the inhibitors, both chemically and functionally. This volume provides an update of the field based on the work presented at the 5th International Symposium on Calcium Antagonists: Pharmacology and Clinical Research. It reviews the current state of the growing area of molecular biology of Ca2+ channels. In the cardiovascular area, in addition to the well-established clinical uses of Ca2+ channel inhibitors, exciting new work pointing to an application in atherosclerosis is described. The book also includes important uses of Ca2+ antagonists in novel areas of interest such as the gastrointestinal tract, renal protection and multi-drug resistance.

Narcotic Antagonists

Author : National Institute on Drug Abuse. Division of Research
Publisher : Unknown
Page : 290 pages
File Size : 46,9 Mb
Release : 1981
Category : Drugs
ISBN : PURD:32754081426151

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Narcotic Antagonists by National Institute on Drug Abuse. Division of Research Pdf

Myocardial Protection by Calcium Antagonists

Author : Lionel H. Opie
Publisher : John Wiley & Sons
Page : 220 pages
File Size : 48,9 Mb
Release : 1994-08-16
Category : Medical
ISBN : 0471076694

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Myocardial Protection by Calcium Antagonists by Lionel H. Opie Pdf

About the Book There are vast amounts of new data emerging in the study of calcium antagonist drugs. The major issues involved are no longer just the effects of calcium antagonist drugs in angina or hypertension but their possible postinfarct protective effects, both to provide prophylaxis and to improve left ventricular function. New trials have also changed our thinking. One major trial suggested that the use of one of these agents in postinfarct patients with no history of heart failure in the acute infarct stage was not only safe but could confer positive protection from reinfarction and possibly from sudden death. Another study, also in postinfarct patients but with a different agent, has drawn attention to a further unexpected benefit, namely improvement of mechanical diastolic function. In the area of hypertension, the emphasis has shifted to the regression of left ventricular hypertrophy, now recognized as an independent risk factor for cardiovascular mortality, and to diastolic dysfunction. Looking to the future, calcium antagonists may exert protection against end-stage heart failure by limiting left ventricular hypertrophy and by vascular beneficial effects. There is emerging interest that the combination with ACE inhibitors may exert additive effects on control of hypertension and on diabetic hypertensive renal lesions. Reviews of Other Books by the Author Drugs for the Heart--"A gem" (New England Journal of Medicine) The Heart--"The subjects are brilliantly illuminated and made exciting by excellent line diagrams" (The Lancet) Angiotensin-Converting Enzyme Inhibitors: Scientific Basis for Clinical Use--"A milestone" (British Medical Journal)

Handbook of PAF and PAF Antagonists

Author : lPierre Braquet
Publisher : CRC Press
Page : 307 pages
File Size : 48,6 Mb
Release : 2019-06-13
Category : Medical
ISBN : 9780429556449

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Handbook of PAF and PAF Antagonists by lPierre Braquet Pdf

Published in 1991: Since its characterization in the 1970s from antigen-stimulated rabbit basophils, platelet-activating factor (PAF) has been demonstrated to be produced by, and act upon, a variety of cell types. PAF antagonists, which have been obtained from both natural sources and chemical synthesis, now represent a new class of therapeutic agents and may provide new prospects for treating several major pathologies, particularly shock, ischemia and asthma. This book provides a unique overview of the chemistry, molecular modeling, pharmacology, and clinical potential of the major classes of natural and synthetic PAF antagonists. Compounds reviewed include the ginkgolides, diketopiperazines, neolignans, hetrazepines, cyclic and 1,3-dioxolan derived PAF analogs, pyrrolo[1,2-c]thiazoles, imidazo[2,1-a]isoquinolines and pyridoquinazoline carboxamides. Consisting of 12 chapters written by leading experts in PAF antagonist research, this book is essential reading for students, researchers, clinicians, and medical practitioners involved in this rapidly developing field of biomedical research.

Adenosine A2A Receptor Antagonists

Author : Anonim
Publisher : Elsevier
Page : 326 pages
File Size : 54,8 Mb
Release : 2023-09-25
Category : Medical
ISBN : 9780443186684

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Adenosine A2A Receptor Antagonists by Anonim Pdf

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

Calmodulin Antagonists and Cellular Physiology

Author : Hiroyoshi Hidaka
Publisher : Elsevier
Page : 568 pages
File Size : 51,8 Mb
Release : 2012-12-02
Category : Medical
ISBN : 9780323145732

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Calmodulin Antagonists and Cellular Physiology by Hiroyoshi Hidaka Pdf

Calmodulin Antagonists and Cellular Physiology focuses on the biochemistry of calmodulin antagonists as regulators of cellular physiology. Emphasis is placed on the use of calmodulin antagonists as an indicator of calmodulin function. The mechanism of action of calmodulin antagonists and their interactions with calmodulin are explored. This book is comprised of 33 chapters and begins with an introduction to the biochemical aspects of calmodulin as well as its distribution and functions, followed by a discussion on how calmodulin antagonists and other agents modulate Ca2+-dependent regulatory systems. The next section is devoted to the mechanism of action of calmodulin antagonists and includes chapters that examine the interaction of various drugs with calmodulin and the structure-activity relationships of calmodulin antagonists. The effects of calmodulin antagonists on cell proliferation and growth are then discussed. The remaining chapters deal with the role of calmodulin antagonists in cell function and the contractile process, along with their effect on protein kinase C. This monograph will be a useful resource for biochemists as well as students and researchers in biochemistry.

Structure–Activity Relationships for Development of Neurokinin-3 Receptor Antagonists

Author : Koki Yamamoto
Publisher : Springer Nature
Page : 86 pages
File Size : 44,7 Mb
Release : 2020-01-23
Category : Science
ISBN : 9789811529658

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Structure–Activity Relationships for Development of Neurokinin-3 Receptor Antagonists by Koki Yamamoto Pdf

This book explores the possible development of neurokinin-3 receptor (NK3R) antagonists with reduced environmental impact. Pharmaceuticals are used to cure diseases and to alleviate symptoms in humans and animals. However, the stable, bioactive substances excreted by patients have unfavorable effects on non-target species. To overcome these disadvantages of these highly stable, potent substances, drug design to turn off bioactivity after release into the environment is needed. The book describes the development of eco-friendly NK3R antagonists by introducing a labile functional moiety and substituting a scaffold. This resulted in a novel NK3R antagonist that oxidized into its inactive form when exposed to air. Further, the book presents an efficient and easily achievable synthetic method of creating triazolopiperazine scaffolds, as well as a structure–activity relationship study involving scaffold hopping for decomposable motifs, which led to a novel photodegradable NK3R antagonist. Demonstrating that it is possible to develop compounds that convert into their inactive forms under environmental conditions, this book is useful for anyone interested in therapeutic agents with reduced environmental impact.

Insomnia and beyond - Exploring the therapeutic potential of orexin receptor antagonists

Author : Michel Alexander Steiner,Christopher J Winrow
Publisher : Frontiers E-books
Page : 220 pages
File Size : 49,8 Mb
Release : 2014-11-11
Category : Medicine (General)
ISBN : 9782889193301

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Insomnia and beyond - Exploring the therapeutic potential of orexin receptor antagonists by Michel Alexander Steiner,Christopher J Winrow Pdf

Orexin/hypocretin neuropeptides, produced by a few thousand neurons in the lateral hypothalamus, are of critical importance for the control of vigilance and arousal of vertebrates, from fish to amphibians, birds and mammals. Two orexin peptides, called orexin-A and orexin-B, exist in mammals. They bind with different affinities to two distinct, widely distributed, excitatory G-protein- coupled receptors, orexin receptor type 1 and type 2 (OXR-1/2). The discovery of an OXR mutation causing canine narcolepsy, the narcolepsy-like phenotype of orexin peptide knockout mice, and the orexin neuron loss associated with human narcoleptic patients laid the foundation for the discovery of small molecule OXR antagonists as novel treatments for sleep disorders. Proof of concept studies from Glaxo Smith Kline, Actelion Pharmaceuticals Ltd. and Merck have now consistently demonstrated the efficacy of dual OXR antagonists (DORAs) in promoting sleep in rodents, dogs, non-human primates and humans. Some of these antagonists have completed late stage clinical testing in primary insomnia. Orexin drug discovery programs have also been initiated by other large pharmaceutical companies including Hoffmann La Roche, Novartis, Eli Lilly and Johnson & Johnson. Orexins are increasingly recognized for orchestrating the activity of the organism’s arousal system with appetite, reward and stress processing pathways. Therefore, in addition to models of insomnia, pharmacological effects of DORAs have begun to be investigated in rodent models of addiction, depression and anxiety. The first clinical trials in diabetic neuropathy, migraine and depression have been initiated with Merck’s MK-6096 (www.clinicaltrials.gov). Whereas the pharmacology of DORAs is established for their effects on wakefulness, pharmacological effects of selective OXR-1 or OXR-2 antagonists (SORAs) have remained less clear. From an evolutionary point of view, the OXR-2 was expressed first in most vertebrate lineages, whereas the OXR-1 is believed to result from a gene duplication event, when mammals emerged. Yet, both receptors do not have redundant function. Their brain expression pattern, their intracellular signaling, as well as their affinity for orexin-A and orexin-B differs. During the past decade most preclinical research on selective OXR-1 antagonism was performed with SB-334867. Only in recent years, other selective OXR-1 and OXR-2 antagonists with optimized selectivity profiles and pharmacokinetic properties have been discovered, and phenotypes of OXR-1 and OXR-2 knockout mice were described. The present Research Topic (referred to in the Editorial as “special topics issue”) comprises submissions of original research manuscripts as well as reviews, directed towards the neuropharmacology of OXR antagonists. The submissions are preclinical papers dealing with dual and/or selective OXR antagonists that shed light on the differential contribution of endogenous orexin signaling through both OXRs for cellular, physiological and behavioral processes. Some manuscripts also report on convergence or divergence of DORA vs. SORA effects with phenotypes expressed by OXR-1 or OXR-2 knockout animals. Ultimately these findings may help further define the potential of DORAs and SORAs in particular therapeutic areas in insomnia and beyond insomnia.

Cholecystokinin and Its Antagonists in Pain Management

Author : Gary McCleane
Publisher : CRC Press
Page : 162 pages
File Size : 42,6 Mb
Release : 2006-06-22
Category : Health & Fitness
ISBN : 078902893X

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Cholecystokinin and Its Antagonists in Pain Management by Gary McCleane Pdf

Examine the strong evidence of this unrealized pain management tool Cholecystokinin (CCK), the regulatory peptide hormone found primarily in the gastrointestinal tract that works as a neurotransmitter throughout the nervous system, has been researched for years. CCK antagonists in conjunction with opioids are beginning to be seen as having possible major therapeutic benefits in pain management. Cholecystokinin and Its Antagonists in Pain Management is an extensive examination that gathers the mounting compelling evidence into one comprehensive source. Here researchers, neuroscientists, physicians, and pharmacy professionals are given the research and findings they need to explore the possible applications of CCK antagonists for a variety of illnesses. Cholecystokinin and Its Antagonists in Pain Management extensively describes opioids in pain management, CCK and the body’s uses for the chemical, CCK receptor antagonists, and the evidence that points to its being a possible breakthrough application in pain management. Various animal studies are offered that present a convincing view of what may be the future of chronic pain management, with less side effects and a reduction in analgesic tolerance than when opioids are used alone. Potential uses of CCK antagonists are clearly discussed. The book is comprehensively referenced and provides several tables and graphs to fully illustrate the research findings. Topics in Cholecystokinin and Its Antagonists in Pain Management include: in vivo localization of CCK CCK as a gut and nervous system peptide factors that increase CCK anti-opioid effects CCK receptor antagonists pro-analgesic effect of CCK antagonists CCK antagonists reducing analgesic tolerance to opioids safety of combining opioids and CCK antagonists human clinical application of CCK antagonists Cholecystokinin and Its Antagonists in Pain Management is a crucial source of the latest information and research results on CCK that is certain to be important for neuroscientists, clinicians, and pharmaceutical industry professionals.

Cardiovascular Effects of Dihydropyridine-Type Calcium Antagonists and Agonists

Author : A. Fleckenstein,C. Van Breemen,R. Groß,F. Hoffmeister
Publisher : Springer Science & Business Media
Page : 520 pages
File Size : 42,7 Mb
Release : 2013-03-12
Category : Medical
ISBN : 9783642704994

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Cardiovascular Effects of Dihydropyridine-Type Calcium Antagonists and Agonists by A. Fleckenstein,C. Van Breemen,R. Groß,F. Hoffmeister Pdf

Held at Boppard, Germany, October 3-6, 1984