Opiate Receptors And Antagonists

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

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

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.

The Essence of Analgesia and Analgesics is an invaluable practical resource for clinicians giving pain relief in any clinical setting, describing the pharmacologic principles and clinical use of all available pain medications. As well as detailed overviews of pain processing and analgesic theory, sections are dedicated to oral and panteral opioid analgesics, neuraxial opioids, NSAIDs, local anesthetics, anticonvulsant type analgesics, NMDA antagonists, alpha adrenergic analgesics, antidepressant analgesics, muscle relaxants, adjuvant medications, and new and emerging analgesics. The concise format of the chapters allows for quick and easy reading and assimilation of information. Enhanced by summary tables and figures, each chapter provides an overview of a particular drug, covering chemical structure, mode of activity, indications, contraindications, common doses and uses, advantages and disadvantages, and drug related adverse events. Key references are also provided. Edited by leading experts in pain management, this is essential reading for any clinician involved in pain management.

Endogenous and Exogenous Opiate Agonists and Antagonists documents the proceedings of the International Narcotic Research Club Conference, held in North Falmouth, Massachusetts, USA, on 11-15 June 1979. The volume begins with a discussion of the programs of the World Health Organization, with an emphasis on the components of its drug dependence program. The 139 papers discussed at the conference are then presented. These papers are organized into 10 parts. The papers in Part I examine structure-activity relationships. Part II contains studies on receptor binding while Part III deals with the localization and characterization of active sites. Part IV focuses on ligands and receptor isolation. Part 5 examines neurochemical interactions. Part VI presents papers on disposition and metabolism. Parts VII and VIII take up analgetic mechanisms and neuroendocrine relationships, respectively. Part IX focuses on behavioral effects while the studies in Part X cover tolerance and physical dependence.

The rapidly burgeoning research of the past two decades on agonist-antagonist analgesics and opioid receptors makes this exhaustive review of opioid anal gesics particularly relevant and timely. After an introductory chapter the additional 12 chapters begin logically with morphine and congeners (4- epoxymorphinans) and end with opioid receptors. All principal chemical types of centrally acting analgesics (including endogenous opioid-like substances) and their antagonists as well as the mixed agonist-antagonists are treated thoroughly, although not always (and for good reason) in historical (chrono logical) order. A chapter on miscellaneous types (atypical structures for the most part) includes the benzimidazoles (etonitazene), aminotetralins (dezocine), tetrahydroisoquinolines (methopholine), and so on. Important aspects and correlations of chemistry, pharmacology, and biochemistry are discussed in depth. Literature citations are numerous. For educators, practicing laboratory scientists, and physicians, this scholarly review by two authors well of opioid analgesics versed in the chemistry, pharmacology, and biochemistry will be informative, stimulating, and thought-provoking. Everette L. May Medical College of Virginia Richmond, VA 23298 v Preface The history of opium predates the written word, although knowledge of its constituents dates back less than 200 years. Over the centuries its popularity for the relief of pain has waxed and waned, until today the opiates are widely recognized as excellent analgesics but with disadvantages that have impaired their use seriously. There is a clear need for a potent analgesic with minimal effects on the respiratory centers and gastrointestinal tract and preferably devoid of dependence liability.

This book covers the latest knowledge in structure, signaling, and biochemical pharmacology of KOR as well as preclinical research and clinical applications (including clinical phase studies and approved for human use) of KOR compounds. It is divided up into the three parts: Molecular aspects of KOR, Preclinical research on pharmacology of KOR agonists and antagonists in animals and KOR agonists and antagonists in clinical use and in past and present clinical trials. The chapters "Biosensors monitor ligand-selective effects at kappa opioid receptors" and "The role of dynorphin and the kappa opioid receptor in schizophrenia and major depressive disorder: a translational approach" of this book are available open access under a Creative Commons Attribution 4.0 International License via link.springer.com.

Animal and Translational Models for CNS Drug Discovery combines the experience of academic, clinical and pharmaceutical neuroscientists in a unique collaborative approach to provide a greater understanding of the relevance of animal models of neuropsychiatric disorders and their role as translational tools for the discovery of CNS drugs being developed for the treatment of these disorders. The focus of this three-volume series of essays is to present a consensual picture of the translational value of animal models from leading experts actively involved in the use of animal models for understanding fundamental neurobiology of CNS disorders and the application of this knowledge to CNS drug discovery, and clinical investigators involved in clinical trials, drug development and eventual registration of novel pharmaceuticals. Each volume of the Animal and Translational Models for CNS Drug Discovery series is dedicated to the development and use of animal models in key therapeutic areas in psychiatric, neurologic and reward deficit disorders. Each volume has introductory chapters expressing the view of the role and relevance of animal models for CNS drug discovery and development from the perspective of (a) academic basic neuroscientific research, (b) applied pharmaceutical drug discovery and development, and (c) issues of clinical trial design and regulatory agencies limitations. Each volume examines the rationale, use, robustness and limitations of animal models in relevant therapeutic areas and discusses the use of animal models for target identification and validation. The clinical relevance of animal models is discussed in terms of major limitations in cross-species comparisons, clinical trial design of drug candidates, and how clinical trial endpoints could be improved. The aim of this series of volumes on Animal and Translational Models for CNS Drug Discovery is to identify and provide common endpoints between species that can serve to inform both the clinic and the bench with the information needed to accelerate clinically-effective CNS drug discovery. - Provides clinical, academic, government and industry perspectives fostering integrated communication between principle participants at all stages of the drug discovery process - Critical evaluation of animal and translational models improving transition from drug discovery and clinical development - Emphasizes what results mean to the overall drug discovery process - Explores issues in clinical trial design and conductance in each therapeutic area - Each volume is available for purchase individually.