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Biased Signaling in Physiology, Pharmacology and Therapeutics

Biased Signaling in Physiology, Pharmacology and Therapeutics
  • Author : Brian J Arey
  • Publisher :Unknown
  • Release Date :2014-06-05
  • Total pages :316
  • ISBN : 9780124115071
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Summary : Biased Signaling in Physiology, Pharmacology and Therapeutics is a unique and essential reference for the scientific community concerning how conformational-dependent activation is a common phenomenon across many classes of receptors or signaling molecules. It discusses the role of conformational dynamics in leading to signaling bias across different classes of receptors and signaling molecules. By providing a broader view of signaling bias, this resource helps to explain common mechanisms shared across receptor classes and how this can be utilized to elucidate their cellular activity and better understand their therapeutic potential. Written for both new and established scientists in pharmacology, cell biology, biochemistry, and signal transduction, as well as physicians, this book clearly illustrates how biased receptor signaling can be utilized to develop and understand complex pharmacology. Chapters are each focused on a specific class of receptor or other important topic and make use of real-world examples illustrating how the latest research in signal transduction has led to a better understanding of pharmacology and cell biology. This structure creates a basis for understanding that physiological signalling bias has been selected by nature in order to provide complex and tissue- specific biological responses in the face of limited receptors and signaling pathways. This book provides a framework to reveal that these physiological mechanisms are not restricted to one receptor type or family and thus presents receptor signaling from a newer, more global perspective. Offers a unique and valuable resource on biased receptor signaling that provides a global view for better understanding pharmacology across many receptor families Integrates biased receptor signaling, physiology, and pharmacology to place this emerging science within the context of treating disease Includes important chapters on both the pharmaceutical and therapeutic implications of biased signaling

Pharmacology and Therapeutics of Constitutively Active Receptors

Pharmacology and Therapeutics of Constitutively Active Receptors
  • Author : Ya-Xiong Tao
  • Publisher :Unknown
  • Release Date :2014-06-11
  • Total pages :440
  • ISBN : 9780124172067
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Summary : Volume 70 of Advances in Pharmacology presents the pharmacology and therapeutics of constitutively active receptors. With a variety of chapters and the best authors in the field, the volume is an essential resource for pharmacologists, immunologists, and biochemists alike. Advances in Pharmacology provides a rich collection of reviews on timely topics. The series places emphasis on the molecular bases of drug action, both applied and experimental. Contributions from the best authors in the field An essential resource for pharmacologists, immunologists, and biochemists

The Physiology and Pharmacology of Leucine-rich Repeat GPCRs

The Physiology and Pharmacology of Leucine-rich Repeat GPCRs
  • Author : Brian J. Arey,James A. Dias
  • Publisher :Unknown
  • Release Date :2016-08-05
  • Total pages :229
  • ISBN : 9782889199587
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Summary : G protein-coupled receptors (GPCRs) represent a large and physiologically important class of cell surface receptors. There are approximately 750 known GPCRs present in the human genome that can be subdivided into general classes based upon sequence homology within their transmembrane domains. Therapeutically, GPCRs represent a fertile source for the development of therapies as they are a significant percentage of our current pharmacopeia. Among the three subclasses of GPCRs, the Class A (rhodopsin-like) receptors are by far the most prevalent and extensively studied. However, within the Class A receptors, sub-families of receptors can be distinguished based upon common sequence motifs within the transmembrane domains as well as extracellular and intracellular domains. One such family of Class A receptors is characterized by multiple leucine- rich repeats within their amino- terminal domains (the Leucine-rich Repeat family (LRR)). This family of GPCRs are best represented by the glycoprotein hormone receptors (LHR, FSHR and TSHR) which have been studied extensively but also includes receptors for the peptide hormone relaxin (RXFP1 and RXFP2 (RXFP2 also binds insulin-like peptide 3)) and three other receptors (LGR4, LGR5 and LGR6). LGR4-6 were, until recently, considered orphan receptors. However, emerging data have revealed that these proteins are the receptors for a family of growth factors called R-spondins. Over the last 20 years much has been learned about LRR receptors, including the development of synthetic agonists and antagonists, new insights into signaling (including signaling bias) and the physiological role these receptors play in regulating the function of many tissues. This topic will focus on what is known concerning the regulation of these receptors, their signaling pathways, functional consequences of activation and pharmacology.

GPCRs

GPCRs
  • Author : Beata Jastrzebska,Paul S.-H. Park
  • Publisher :Unknown
  • Release Date :2019-09-11
  • Total pages :500
  • ISBN : 9780128167281
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Summary : GPCRS: Structure, Function, and Drug Discovery provides a comprehensive overview of recent discoveries and our current understanding of GPCR structure, signaling, physiology, pharmacology and methods of study. In addition to the fundamental aspects of GPCR function and dynamics, international experts discuss crystal structures, GPCR complexes with partner proteins, GPCR allosteric modulation, biased signaling through protein partners, deorphanization of GPCRs, and novel GPCR-targeting ligands that could lead to the development of new therapeutics against human diseases. GPCR association with, and possible therapeutic pathways for, retinal degenerative diseases, Alzheimer’s disease, Parkinson’s disease, cancer and diabetic nephropathy, among other illnesses, are examined in-depth. Addresses our current understanding and novel advances in the GPCR field, directing readers towards recent finding of key significance for translational medicine Combines a thorough discussion of structure and function of GPCRs with disease association and drug discovery Features chapter contributions from international experts in GPCR structure, signaling, physiology and pharmacology

The Molecular Biology of Arrestins

The Molecular Biology of Arrestins
  • Author : Anonim
  • Publisher :Unknown
  • Release Date :2013-06-10
  • Total pages :536
  • ISBN : 9780123947895
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Summary : This special volume of Progress in Molecular Biology and Translational Science focuses on the molecular biology of arrestins, with contributions from leaders in the field. Arrestins have emerged as central players in the regulation of many facets of G protein-coupled receptor signaling. This volume covers a variety of topics with reviews written by experts in the field. Contributions from leading authorities Informs and updates on all the latest developments in the field

Physiology of Neurons

Physiology of Neurons
  • Author : Anne Feltz
  • Publisher :Unknown
  • Release Date :2020-04-09
  • Total pages :458
  • ISBN : 9781000761559
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Summary : Thanks to tremendous technical advances in molecular biology and cellular imaging after those in electrophysiology, there is now a deep understanding of the physiology of nerve cells and their synaptic interconnections. The complexity of the brain emerges from the communication and interaction between billions of these elements. This book explores systematically and didactically the details of neuronal physiology, covering membrane biophysics, receptor physiology, sensory transduction and synaptic transmission with its selective pharmacology. Readers of the book will be fully equipped to understand the functions and possibilities of the key units of the brain’s parallel computations.

Cannabinoid Pharmacology

Cannabinoid Pharmacology
  • Author : Anonim
  • Publisher :Unknown
  • Release Date :2017-08-18
  • Total pages :492
  • ISBN : 9780128112335
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Summary : Cannabinoid Pharmacology, Volume 80 is a new volume in the Advances in Pharmacology that presents reviews of recent breakthroughs. This volume aims to present current knowledge of the endogenous cannabinoid system, and looks at molecular, cellular, tissue and organismal effects of endogenous and exogenous cannabinoids. Topics of note in this new volume include Endocannabinoids and their congeners, Endocannabinoid turnover, Plant cannabinoids, Synthetic cannabinoids and ‘legal highs’, CB1 and CB2 cannabinoid receptors, Novel signaling modalities, Novel cannabinoid receptors, and Ion channel regulation by cannabinoids. There is a broad coverage of the essential elements associated with the cannabinoid system. The Editors have sought to include authors who represent authoritative voices on these themes, but have not previously worked together to allow a fresh approach to the individual aspects covered. Presents reviews of recent breakthroughs in the cannabinoid system Features chapters from the best authors in the field Provides an essential resource for scientists, advanced undergraduate students through to established faculty members

Inner Thoughtz

Inner Thoughtz
  • Author : Innerthoughtz Publishing
  • Publisher :Unknown
  • Release Date :2019-10-21
  • Total pages :102
  • ISBN : 1701587572
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Summary : This is a 100 page lined notebook with an inspiring thought on the cover.No fluff and nonsense. Just a simple notebook.6" x 9" in size.To view more InnerThoughtz notebooks, simply type "innerthoughtz" into the search bar. (don't forget the z)

Receptor-Receptor Interactions

Receptor-Receptor Interactions
  • Author : Kjell Fuxe,Luigi F. Agnati
  • Publisher :Unknown
  • Release Date :2013-03-13
  • Total pages :580
  • ISBN : 9781468454154
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Summary :

Free Fatty Acid Receptors

Free Fatty Acid Receptors
  • Author : Graeme Milligan,Ikuo Kimura
  • Publisher :Unknown
  • Release Date :2017-02-08
  • Total pages :256
  • ISBN : 9783319506937
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Summary : This book highlights the important role free fatty acids (FFA) play as potential drug targets. While FFA have long been considered byproducts of cell metabolism, they are now recognized as ligands that regulate cell and tissue function via G-protein-coupled receptors. At least three receptors have been identified for which FFA appear to be the endogenous ligands.

Pharmacology of G Protein Coupled Receptors

Pharmacology of G Protein Coupled Receptors
  • Author : Anonim
  • Publisher :Unknown
  • Release Date :2011-09-08
  • Total pages :408
  • ISBN : 9780123859532
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Summary : G protein coupled receptors remain the most important class of therapeutic targets in medicine. In the last 5 years, tremendous advances have been made in our understanding of the structure and mechanism of this critical family of drug targets. The present volume explores the modern experimental and conceptual framework for drug discovery for G protein coupled receptors. It explores advances in structure determination and structure-based drug design as well as new concepts of allosteric modulation, functional selectivity/biased agonism, and pharmacological chaperones. In addition, emerging drug targets such as receptor families for fatty acids, carboxylic acids, lipid mediators, etc. are included. Final chapters cover novel mechanisms of signal regulation through PDZ domains and RGS proteins. This volume will bring an up-to-date perspective on the G protein coupled receptor field to both academic and industry scientists. The present volume explores the modern experimental and conceptual framework for drug discovery for G protein coupled receptors It explores advances in structure determination and structure-based drug design as well as new concepts of allosteric modulation, functional selectivity/biased agonism, and pharmacological chaperones This volume will bring an up-to-date perspective on the G protein coupled receptor field to both academic and industry scientists

Medical Pharmacology and Therapeutics E-Book

Medical Pharmacology and Therapeutics E-Book
  • Author : Derek G. Waller,Tony Sampson
  • Publisher :Unknown
  • Release Date :2013-08-07
  • Total pages :744
  • ISBN : 9780702055034
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Summary : This book covers all the pharmacology you need, from basic science pharmacology and pathophysiology, through to clinical pharmacology to therapeutics, in line with the integrated approach of new medical curricula. The first section covers the basic principles, and the rest is organised by body systems. The book ends with sections on toxicity and prescribing practice. Integrates basic science pharmacology, clinical pharmacology and therapeutics Brief review of pathophysiology of major diseases Case histories and multiple choice questions (and answers) Tabular presentation of all common drugs within each class Section on further reading Kinetics chapter simplified with more practical examples Includes more on genetic issues Drug tables made more concise to make information more accessible Fully updated to reflect current clinical practice

A Pharmacology Primer

A Pharmacology Primer
  • Author : Terry Kenakin
  • Publisher :Unknown
  • Release Date :2018-10-26
  • Total pages :488
  • ISBN : 9780128139585
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Summary : A Pharmacology Primer: Techniques for More Effective and Strategic Drug Discovery, Fifth Edition features the latest ideas and research regarding the application of pharmacology to the process of drug discovery. Written by well-respected pharmacologist, Terry P. Kenakin, this primer is an indispensable resource for all those involved in drug discovery. This updated edition has been thoroughly revised to include material on quantifying drug efficacy through bias and cluster analysis, the impact of molecular dynamics and protein structural analysis, the real time kinetic analysis of drug effect, virtual screening for new drug chemical scaffolds, and much more. With full color illustrations and new examples throughout, this book remains a top reference for all industry and academic scientists that is also ideal for students directly involved in drug discovery or pharmacologic research. Highlights changes surrounding strategies for drug discovery, providing a comprehensive reference and featuring advances in the methods involved Includes multiple new sections, such as development and utilization of models in pharmacology, de-orphanization of new drug targets, predicting impact of disease on drug pharmacokinetics, and the impact of enzyme kinetics on drug-drug interactions Illustrates the application of rapid inexpensive assays to predict activity in the therapeutic setting, showing data outcomes and the limitations inherent in interpreting this data

Handbook of Cannabis and Related Pathologies

Handbook of Cannabis and Related Pathologies
  • Author : Victor R. Preedy
  • Publisher :Unknown
  • Release Date :2016-12-31
  • Total pages :1170
  • ISBN : 9780128008270
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Summary : Handbook of Cannabis and Related Pathologies: Biology, Pharmacology, Diagnosis, and Treatment is the first book to take an interdisciplinary approach to the understanding of cannabis use and misuse. Recent worldwide trends toward decriminalizing marijuana for medical use have increased legal use of the drug and recreational use remains high, making cannabis one of the most commonly used drugs. Cannabis has a wide range of adverse neurological effects, and use and abuse can lead to physical, social, and psychopathological issues that are multifarious and complex. Effective understanding and treatment requires knowledge of the drug’s effects from across scientific disciplines. This book provides an overview of the biological and pharmacological components of the cannabis plant, outlines its neurological, social, and psychopathological effects, assists in the diagnosis and screening for use and dependency, and aids researchers in developing effective treatments for cannabis-related issues and disorders. Fully illustrated, with contributions from internationally recognized experts, it is the go-to resource for neuroscientists, pharmacologists, pathologists, public-health workers, and any other researcher who needs an in-depth and cross-disciplinary understanding of cannabis and its effects. Comprehensive chapters include an abstract, key facts, mini dictionary of terms, and summary points Presents illustrations with at least six figures, tables, and diagrams per chapter Provides a one-stop-shopping synopsis of everything to do with cannabis and its related pathology, from chemicals and cells, individuals and communities, and diagnosis and treatment Offers an integrated and informed synopsis of the complex issues surrounding cannabis as a substance, its use, and its misuse

Adhesion G Protein-coupled Receptors

Adhesion G Protein-coupled Receptors
  • Author : Tobias Langenhan,Torsten Schöneberg
  • Publisher :Unknown
  • Release Date :2016-11-09
  • Total pages :403
  • ISBN : 9783319415239
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Summary : Latest research on Adhesion GPCRs has unearthed surprising revelations about the events that govern the signal transduction of these receptor molecules and the cellular and organ requirements for these signals. Unexpected and unprecedented findings suggest that Adhesion GPCRs constitute a group of receptors that sense mechanical stimuli and transcode them into metabotropic signals through the action of a novel activation paradigm. Interdisciplinary efforts transcending many areas of biomedical research including pharmacology, physiology, genetics, cell biology, structural biology, biochemistry and bioinformatics were necessary to unveil these fundamental properties. The scientific leaders in the field that carried this research effort have teamed up here to provide a comprehensive overview of our current understanding, how Adhesion GPCRs signal and how these receptors shape organ structure and function.

Encyclopedia of Inflammatory Diseases

Encyclopedia of Inflammatory Diseases
  • Author : Michael J. Parnham
  • Publisher :Unknown
  • Release Date :2021-01-14
  • Total pages :1600
  • ISBN : 3034806205
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Summary :

Pharmacology of Itch

Pharmacology of Itch
  • Author : Alan Cowan,Gil Yosipovitch
  • Publisher :Unknown
  • Release Date :2015-04-10
  • Total pages :382
  • ISBN : 9783662446058
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Summary : Basic research on the pharmacology of itch has exploded in the wake of two very influential papers that were published in Nature (2007) and Science (2009). Long overlooked as a milder form of pain, itching has rapidly gained a new appreciation in both research and clinical communities because of its complexity and its negative effects on the quality of life of the distressed patients. Like pain, not all itches are the same. Unlike pain, there are no standard drugs equivalent to aspirin and morphine. Epidemiological studies emphasize the high incidence and economic costs of itch (pruritus). It is the most prevalent symptom of a wide variety of allergic and inflammatory skin conditions (e.g., psoriasis, atopic dermatitis), is associated with several systemic diseases (e.g., chronic kidney and liver disease), and occurs in patients undergoing hemodialysis, spinal administration of opioids, and in those suffering from AIDS. The reader will learn about the multiple pathways for itch and their interactions with pain. The relationship between these closely related, yet distinct sensory phenomena, will be emphasized. Both itch and pain use several common molecules to send signals to the brain. Thus, drugs that have been, and are being, developed as analgesics may also attenuate intractable itch. This has been an exciting and very necessary turn of events since traditional H-1 receptor antagonists are ineffective in blocking the pruritus associated with kidney failure and cholestasis. The clinical chapters will provide insights into contemporary treatment regimens for pruritus in different human scenarios.

Affinity and Efficacy

Affinity and Efficacy
  • Author : Frederick J. Ehlert
  • Publisher :Unknown
  • Release Date :2014-09-15
  • Total pages :739
  • ISBN : 9814322563
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Summary : The interaction of a drug with a receptor encodes a vector of information having components of affinity and efficacy. How this information is translated into a response depends on the unique cells, tissue, organ or system in which the receptor resides. This book describes how to analyze various responses to estimate the affinity and efficacy components of the initial drugreceptor interaction. More specifically, it describes how to measure the affinity and efficacy of drugs through the analysis of single receptor activity, the activation state of a population of receptors, and responses downstream from receptor activation. More light is shed on ligand-gated ion channels and G protein-coupled receptors in this book. The topics discussed include radioligand binding, estimation of agonist affinity and efficacy, competitive antagonism, inverse agonism, allosteric agonists and modulators, ligand-directed signaling, modulation of pathway selectivity, and the analysis of the loss of function in tissues from receptor knockout mice. The natural history and structure of ligand-gated ion channels, G proteins, and G protein-coupled receptors are also discussed.

The American Psychiatric Association Practice Guidelines for the Psychiatric Evaluation of Adults, Third Edition

The American Psychiatric Association Practice Guidelines for the Psychiatric Evaluation of Adults, Third Edition
  • Author : American Psychiatric Association
  • Publisher :Unknown
  • Release Date :2015-07-29
  • Total pages :170
  • ISBN : 9780890424650
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Summary : Since the publication of the Institute of Medicine (IOM) report Clinical Practice Guidelines We Can Trust in 2011, there has been an increasing emphasis on assuring that clinical practice guidelines are trustworthy, developed in a transparent fashion, and based on a systematic review of the available research evidence. To align with the IOM recommendations and to meet the new requirements for inclusion of a guideline in the National Guidelines Clearinghouse of the Agency for Healthcare Research and Quality (AHRQ), American Psychiatric Association (APA) has adopted a new process for practice guideline development. Under this new process APA's practice guidelines also seek to provide better clinical utility and usability. Rather than a broad overview of treatment for a disorder, new practice guidelines focus on a set of discrete clinical questions of relevance to an overarching subject area. A systematic review of evidence is conducted to address these clinical questions and involves a detailed assessment of individual studies. The quality of the overall body of evidence is also rated and is summarized in the practice guideline. With the new process, recommendations are determined by weighing potential benefits and harms of an intervention in a specific clinical context. Clear, concise, and actionable recommendation statements help clinicians to incorporate recommendations into clinical practice, with the goal of improving quality of care. The new practice guideline format is also designed to be more user friendly by dividing information into modules on specific clinical questions. Each module has a consistent organization, which will assist users in finding clinically useful and relevant information quickly and easily. This new edition of the practice guidelines on psychiatric evaluation for adults is the first set of the APA's guidelines developed under the new guideline development process. These guidelines address the following nine topics, in the context of an initial psychiatric evaluation: review of psychiatric symptoms, trauma history, and treatment history; substance use assessment; assessment of suicide risk; assessment for risk of aggressive behaviors; assessment of cultural factors; assessment of medical health; quantitative assessment; involvement of the patient in treatment decision making; and documentation of the psychiatric evaluation. Each guideline recommends or suggests topics to include during an initial psychiatric evaluation. Findings from an expert opinion survey have also been taken into consideration in making recommendations or suggestions. In addition to reviewing the available evidence on psychiatry evaluation, each guideline also provides guidance to clinicians on implementing these recommendations to enhance patient care.

Major Depressive Disorder

Major Depressive Disorder
  • Author : Yong-Ku Kim
  • Publisher :Unknown
  • Release Date :2015-06-11
  • Total pages :156
  • ISBN : 9789535121299
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Summary : Major depressive disorder (MDD) is a complex and heterogeneous disorder, phenotypically and biologically. MDD may be caused by complex interaction between genes and environment in susceptible individuals. Thus, a combination of certain genetic polymorphism, environmental stress, and personal susceptibility ultimately may induce MDD. Gene-environment interactions in the pathophysiology of MDD lead to advancement in personalized medicine by means of genotyping for inter-individual variability in drug action and metabolism. Gene-environment interactions may explain why some subjects become depressed while others remain unaffected. The aim of this book is to describe current knowledge of MDD from the point of view of neurobiology, molecular genetics and cognition. The authors address a deep understanding of cognitive and neurobiological mechanisms involved in MDD.

The Oxford Handbook of the Neurobiology of Pain

The Oxford Handbook of the Neurobiology of Pain
  • Author : Professor John N. Wood
  • Publisher :Unknown
  • Release Date :2020-06-17
  • Total pages :512
  • ISBN : 9780190860523
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Summary : The Oxford Handbook of the Neurobiology of Pain represents a state of the art overview of the rapidly developing field of pain research. As populations age, the number of people in pain is growing dramatically, with half the population living with pain. The opioid crisis has highlighted this problem. The present volume is thus very timely, providing expert overviews of many complex topics in pain research that are likely to be of interest not just to pain researchers, but also to pain clinicians who are seeking new therapeutic opportunities to develop analgesics. Many of the topics covered are of interest to neuroscientists, as pain is one of the most amenable sensations for mechanistic dissection. The present volume covers all aspects of the topic, from a history of pain through invertebrate model systems to the human genetics of pain and functional imaging. Chapters include the role of ion channels, the opioid system, the immune and sympathetic systems, as well as the mechanisms that transform acute to chronic pain. Migraine and the interplay between sleep and pain are also discussed. New technology in the form of transgenic animals, chemogenetics, optogenetics, and proteomic analyses are providing significant advances in our research and are covered as well. Demystifying pain through an understanding of its fundamental biology, as outlined in this volume, is the most direct route to ameliorating this vast human problem.