Structure Function Studies Of M4 Muscarinic Acetylcholine Receptor Allosteric Modulation

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Allosteric Modulation of G Protein-Coupled Receptors

Author : Robert Laprairie
Publisher : Academic Press
ISBN 13 : 0128197722
Total Pages : 214 pages
Book Rating : 4.1/5 (281 download)

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Book Synopsis Allosteric Modulation of G Protein-Coupled Receptors by : Robert Laprairie

Download or read book Allosteric Modulation of G Protein-Coupled Receptors written by Robert Laprairie and published by Academic Press. This book was released on 2022-02-05 with total page 214 pages. Available in PDF, EPUB and Kindle. Book excerpt: Allosteric Modulation of G Protein-Coupled Receptors reviews fundamental information on G protein-coupled receptors (GPCRs) and allosteric modulation, presenting original research in the area and collectively providing a comprehensive description of key issues in GPCR allosteric modulation. The book provides background on core concepts of molecular pharmacology while also introducing the most important advances and studies in the area. It also discusses key methodologies. This is an essential book for researchers and advanced students engaged in pharmacology, toxicology and pharmaceutical sciences training and research. Many of the GPCR-targeted drugs released in the past decade have specifically worked via allosteric mechanisms. Unlike direct orthosteric-acting compounds that occupy a similar receptor site to that of endogenous ligands, allosteric modulators alter GPCR-dependent signaling at a site apart from the endogenous ligand. Recent methodological and analytical advances have greatly improved our ability to understand the signaling mechanisms of GPCRs. We now know that allostery is a common regulatory mechanism for all GPCRs and not – as we once believed – unique to a few receptor subfamilies. - Introduces background on core concepts of molecular pharmacology, including statistical analyses, non-linear regression, complex models and GPCR-dependent signal transduction as they relate to allosteric modulation - Discusses critical advances and landmark studies, including discoveries in the area of GPCR allosteric modulation, which are reviewed for their importance in positive and negative regulation, protein-protein interactions, and small molecule drug discovery - Includes key methodologies used to study allosteric modulation at the in silico, in vitro, and in vivo levels of drug discovery and characterization

Sensing the Environment: Regulation of Local and Global Homeostasis by the Skin's Neuroendocrine System

Author : Andrzej T. Slominski
Publisher : Springer Science & Business Media
ISBN 13 : 3642196837
Total Pages : 128 pages
Book Rating : 4.6/5 (421 download)

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Book Synopsis Sensing the Environment: Regulation of Local and Global Homeostasis by the Skin's Neuroendocrine System by : Andrzej T. Slominski

Download or read book Sensing the Environment: Regulation of Local and Global Homeostasis by the Skin's Neuroendocrine System written by Andrzej T. Slominski and published by Springer Science & Business Media. This book was released on 2012-06-02 with total page 128 pages. Available in PDF, EPUB and Kindle. Book excerpt: The skin, the body’s largest organ, is strategically located at the interface with the external environment where it detects, integrates and responds to a diverse range of stressors, including solar radiation. It has already been established that the skin is an important peripheral neuroendocrine-immune organ that is closely networked with central regulatory systems. These capabilities contribute to the maintenance of peripheral homeostasis. Specifically, epidermal and dermal cells produce and respond to classical stress neurotransmitters, neuropeptides and hormones, production which is stimulated by ultraviolet radiation (UVR), biological factors (infectious and non-infectious) and other physical and chemical agents. Examples of local biologically active products are cytokines, biogenic amines (catecholamines, histamine, serotonin and N-acetyl-serotonin), melatonin, acetylocholine, neuropeptides including pituitary (proopiomelanocortin-derived ACTH, b-endorphin or MSH peptides, thyroid stimulating hormone) and hypothalamic (corticotropin-releasing factor and related urocortins, thyroid-releasing hormone) hormones, as well as enkephalins and dynorphins, thyroid hormones, steroids (glucocorticoids, mineralocorticoids, sex hormones, 7-δ steroids), secosteroids, opioids and endocannabinoids. The production of these molecules is hierarchical, organized along the algorithms of classical neuroendocrine axes such as the hypothalamic pituitary adrenal axis (HPA), hypothalamic-thyroid axis (HPT), serotoninergic, melatoninergic, catecholaminergic, cholinergic, steroid/secosteroidogenic, opioid and endocannabinoid systems. Disruptions of these axes or of communication between them may lead to skin and/or systemic diseases. These local neuroendocrine networks also serve to limit the effect of noxious environmental agents to preserve local and consequently global homeostasis. Moreover, the skin-derived factors/systems can also activate cutaneous nerve endings to alert the brain to changes in the epidermal or dermal environments, or alternatively to activate other coordinating centers by direct (spinal cord) neurotransmission without brain involvement. Furthermore, rapid and reciprocal communications between epidermal and dermal and adnexal compartments are also mediated by neurotransmission including antidromic modes of conduction. Lastly, skin cells and the skin as an organ coordinate and/or regulate not only peripheral but also global homeostasis.

G Protein-Coupled Receptor Signaling

Author : Mario Tiberi
Publisher : Humana Press
ISBN 13 : 9781493991204
Total Pages : 406 pages
Book Rating : 4.9/5 (912 download)

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Book Synopsis G Protein-Coupled Receptor Signaling by : Mario Tiberi

Download or read book G Protein-Coupled Receptor Signaling written by Mario Tiberi and published by Humana Press. This book was released on 2019-03-01 with total page 406 pages. Available in PDF, EPUB and Kindle. Book excerpt: This detailed volume assembles comprehensive protocols to assist with the study of structural, molecular, cell biological, and in vivo facets of GPCRs, and to enable the development of experimental tools for screening novel GPCR drugs. Sections explore the tweaking of ligands, bioluminescence and FRET approaches, specific GPCR signaling properties, as well as visualization of subcellular compartmentalization. Written for the highly successful Methods in Molecular Biology series, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls. Authoritative and practical, G Protein-Coupled Receptor Signaling: Methods and Protocols serves as an ideal reference for life scientists working in a variety of research fields including molecular pharmacology, cell and developmental biology, brain behavior and physiology, drug development and screening. Chapter 4 is available open access under a CC BY 4.0 license via link.springer.com.

Muscarinic Receptors

Author : Allison D. Fryer
Publisher : Springer Science & Business Media
ISBN 13 : 3642232744
Total Pages : 501 pages
Book Rating : 4.6/5 (422 download)

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Book Synopsis Muscarinic Receptors by : Allison D. Fryer

Download or read book Muscarinic Receptors written by Allison D. Fryer and published by Springer Science & Business Media. This book was released on 2012-01-06 with total page 501 pages. Available in PDF, EPUB and Kindle. Book excerpt: Muscarinic acetylcholine receptors have played a key role in the advancement of knowledge of pharmacology and neurotransmission since the inception of studies in these fields, and the effects of naturally occurring drugs acting on muscarinic receptors were known and exploited for both therapeutic and non-therapeutic purposes for hundreds of years before the existence of the receptors themselves was recognized. This volume presents a broad yet detailed review of current knowledge of muscarinic receptors that will be valuable both to long-time muscarinic investigators and to those new to the field. It describes the detailed insights that have been obtained on the structure, function, and cell biology of muscarinic receptors. This volume also describes physiological analyses of muscarinic receptors and their roles in regulating the function of the brain and of a variety of peripheral tissues. This volume shows how the study of muscarinic receptors continues to provide new and surprising insights not just to the cholinergic system but to the broad areas of neurobiology, cell biology, pharmacology, and therapeutics.

Structural Biology in Drug Discovery

Author : Jean-Paul Renaud
Publisher : John Wiley & Sons
ISBN 13 : 1118900502
Total Pages : 1437 pages
Book Rating : 4.1/5 (189 download)

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Book Synopsis Structural Biology in Drug Discovery by : Jean-Paul Renaud

Download or read book Structural Biology in Drug Discovery written by Jean-Paul Renaud and published by John Wiley & Sons. This book was released on 2020-01-09 with total page 1437 pages. Available in PDF, EPUB and Kindle. Book excerpt: With the most comprehensive and up-to-date overview of structure-based drug discovery covering both experimental and computational approaches, Structural Biology in Drug Discovery: Methods, Techniques, and Practices describes principles, methods, applications, and emerging paradigms of structural biology as a tool for more efficient drug development. Coverage includes successful examples, academic and industry insights, novel concepts, and advances in a rapidly evolving field. The combined chapters, by authors writing from the frontlines of structural biology and drug discovery, give readers a valuable reference and resource that: Presents the benefits, limitations, and potentiality of major techniques in the field such as X-ray crystallography, NMR, neutron crystallography, cryo-EM, mass spectrometry and other biophysical techniques, and computational structural biology Includes detailed chapters on druggability, allostery, complementary use of thermodynamic and kinetic information, and powerful approaches such as structural chemogenomics and fragment-based drug design Emphasizes the need for the in-depth biophysical characterization of protein targets as well as of therapeutic proteins, and for a thorough quality assessment of experimental structures Illustrates advances in the field of established therapeutic targets like kinases, serine proteinases, GPCRs, and epigenetic proteins, and of more challenging ones like protein-protein interactions and intrinsically disordered proteins

Protein Allostery in Drug Discovery

Author : Jian Zhang
Publisher : Springer Nature
ISBN 13 : 9811387192
Total Pages : 386 pages
Book Rating : 4.8/5 (113 download)

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Book Synopsis Protein Allostery in Drug Discovery by : Jian Zhang

Download or read book Protein Allostery in Drug Discovery written by Jian Zhang and published by Springer Nature. This book was released on 2019-11-09 with total page 386 pages. Available in PDF, EPUB and Kindle. Book excerpt: The book focuses on protein allostery in drug discovery. Allosteric regulation, ʹthe second secret of lifeʹ, fine-tunes virtually most biological processes and controls physiological activities. Allostery can both cause human diseases and contribute to development of new therapeutics. Allosteric drugs exhibit unparalleled advantages compared to conventional orthosteric drugs, rendering the development of allosteric modulators as an appealing strategy to improve selectivity and pharmacodynamic properties in drug leads. The Series delineates the immense significance of protein allostery—as demonstrated by recent advances in the repertoires of the concept, its mechanistic mechanisms, and networks, characteristics of allosteric proteins, modulators, and sites, development of computational and experimental methods to predict allosteric sites, small-molecule allosteric modulators of protein kinases and G-protein coupled receptors, engineering allostery, and the underlying role of allostery in precise medicine. Comprehensive understanding of protein allostery is expected to guide the rational design of allosteric drugs for the treatment of human diseases. The book would be useful for scientists and students in the field of protein science and Pharmacology etc.

Drug-Acceptor Interactions

Author : Niels Bindslev
Publisher : CRC Press
ISBN 13 : 1351660578
Total Pages : 847 pages
Book Rating : 4.3/5 (516 download)

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Book Synopsis Drug-Acceptor Interactions by : Niels Bindslev

Download or read book Drug-Acceptor Interactions written by Niels Bindslev and published by CRC Press. This book was released on 2017-02-10 with total page 847 pages. Available in PDF, EPUB and Kindle. Book excerpt: Drug-Acceptor Interactions: Modeling theoretical tools to test and evaluate experimental equilibrium effects suggests novel theoretical tools to test and evaluate drug interactions seen with combinatorial drug therapy. The book provides an in-depth, yet controversial, exploration of existing tools for analysis of dose-response studies at equilibrium or steady state. The book is recommended reading for post-graduate students and researchers engaged in the study of systems biology, networks, and the pharmacodynamics of natural or industrial drugs, as well as for medical clinicians interested in drug application and combinatorial drug therapy. Even people without mathematical skills will be able to follow the pros and cons of reaction schemes and their related distribution equations. Chapter 9 is a hands-on guide for software to plot, fit and analyze one’s own data.

Tourette Syndrome

Author : Davide Martino
Publisher : Oxford University Press
ISBN 13 : 0197543219
Total Pages : 577 pages
Book Rating : 4.1/5 (975 download)

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Book Synopsis Tourette Syndrome by : Davide Martino

Download or read book Tourette Syndrome written by Davide Martino and published by Oxford University Press. This book was released on 2022 with total page 577 pages. Available in PDF, EPUB and Kindle. Book excerpt: Tourette syndrome (TS) has become increasingly recognised within society and has gained scientific interest worldwide. Knowledge of its clinical presentation, mechanisms of disease, and available treatment approaches has increased remarkably over the last two decades. Likewise, the way clinicians, teachers, social care workers, and families face the problems manifested by patients with TS is rapidly evolving. Tourette Syndrome, edited by Davide Martino and James F. Leckman, offers a unique opportunity to capture this knowledge advance through a comprehensive and up-to-date overview. Tourette Syndrome covers all the main aspects related to TS, analyzing its complex clinical presentation, the novel viewpoints of causes and mechanisms, state-of-the-art assessment techniques, and the diversity of treatment options. Multidisciplinarity is the main asset of this volume, which represents a source of consultation for a wide audience of professionals, integrated with video tutorials related to particularly complex areas of patient management. Medical and PhD students, as well as post-doctoral scientists, will be able to use the volume as a valuable learning source.

Receptor-Receptor Interactions

Author : Kjell Fuxe
Publisher : Springer Science & Business Media
ISBN 13 : 1468454153
Total Pages : 577 pages
Book Rating : 4.4/5 (684 download)

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Book Synopsis Receptor-Receptor Interactions by : Kjell Fuxe

Download or read book Receptor-Receptor Interactions written by Kjell Fuxe and published by Springer Science & Business Media. This book was released on 2013-03-13 with total page 577 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Molecular Pharmacology

Author : John Dickenson
Publisher : John Wiley & Sons
ISBN 13 : 1118451953
Total Pages : 675 pages
Book Rating : 4.1/5 (184 download)

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Book Synopsis Molecular Pharmacology by : John Dickenson

Download or read book Molecular Pharmacology written by John Dickenson and published by John Wiley & Sons. This book was released on 2012-11-30 with total page 675 pages. Available in PDF, EPUB and Kindle. Book excerpt: This textbook provides a fresh, comprehensive and accessible introduction to the rapidly expanding field of molecular pharmacology. Adopting a drug target-based, rather than the traditional organ/system based, approach this innovative guide reflects the current advances and research trend towards molecular based drug design, derived from a detailed understanding of chemical responses in the body. Drugs are then tailored to fit a treatment profile, rather than the traditional method of ‘trial and error’ drug discovery which focuses on testing chemicals on animals or cell cultures and matching their effects to treatments. Providing an invaluable resource for advanced under-graduate and MSc/PhD students, new researchers to the field and practitioners for continuing professional development, Molecular Pharmacology explores; recent advances and developments in the four major human drug target families (G-protein coupled receptors, ion channels, nuclear receptors and transporters), cloning of drug targets, transgenic animal technology, gene therapy, pharmacogenomics and looks at the role of calcium in the cell. Current - focuses on cutting edge techniques and approaches, including new methods to quantify biological activities in different systems and ways to interpret and understand pharmacological data. Cutting Edge - highlights advances in pharmacogenomics and explores how an individual’s genetic makeup influences their response to therapeutic drugs and the potential for harmful side effects. Applied - includes numerous, real-world examples and a detailed case-study based chapter which looks at current and possible future treatment strategies for cystic fibrosis. This case study considers the relative merits of both drug therapy for specific classes of mutation and gene therapy to correct the underlying defect. Accessible - contains a comprehensive glossary, suggestions for further reading at the end of each chapter and an associated website that provides a complete set of figures from within the book.

Conn's Translational Neuroscience

Author : P. Michael Conn
Publisher : Academic Press
ISBN 13 : 0128025964
Total Pages : 778 pages
Book Rating : 4.1/5 (28 download)

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Book Synopsis Conn's Translational Neuroscience by : P. Michael Conn

Download or read book Conn's Translational Neuroscience written by P. Michael Conn and published by Academic Press. This book was released on 2016-09-28 with total page 778 pages. Available in PDF, EPUB and Kindle. Book excerpt: Conn's Translational Neuroscience provides a comprehensive overview reflecting the depth and breadth of the field of translational neuroscience, with input from a distinguished panel of basic and clinical investigators. Progress has continued in understanding the brain at the molecular, anatomic, and physiological levels in the years following the 'Decade of the Brain,' with the results providing insight into the underlying basis of many neurological disease processes. This book alternates scientific and clinical chapters that explain the basic science underlying neurological processes and then relates that science to the understanding of neurological disorders and their treatment. Chapters cover disorders of the spinal cord, neuronal migration, the autonomic nervous system, the limbic system, ocular motility, and the basal ganglia, as well as demyelinating disorders, stroke, dementia and abnormalities of cognition, congenital chromosomal and genetic abnormalities, Parkinson's disease, nerve trauma, peripheral neuropathy, aphasias, sleep disorders, and myasthenia gravis. In addition to concise summaries of the most recent biochemical, physiological, anatomical, and behavioral advances, the chapters summarize current findings on neuronal gene expression and protein synthesis at the molecular level. Authoritative and comprehensive, Conn's Translational Neuroscience provides a fully up-to-date and readily accessible guide to brain functions at the cellular and molecular level, as well as a clear demonstration of their emerging diagnostic and therapeutic importance. - Provides a fully up-to-date and readily accessible guide to brain functions at the cellular and molecular level, while also clearly demonstrating their emerging diagnostic and therapeutic importance - Features contributions from leading global basic and clinical investigators in the field - Provides a great resource for researchers and practitioners interested in the basic science underlying neurological processes - Relates and translates the current science to the understanding of neurological disorders and their treatment

Gaba

Author : Chikako Tanaka
Publisher : Springer Science & Business Media
ISBN 13 : 9783764352844
Total Pages : 354 pages
Book Rating : 4.3/5 (528 download)

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Book Synopsis Gaba by : Chikako Tanaka

Download or read book Gaba written by Chikako Tanaka and published by Springer Science & Business Media. This book was released on 1996 with total page 354 pages. Available in PDF, EPUB and Kindle. Book excerpt: Highlighting the current developments and future directions in GABA research, the ambitious aim of this topical volume is to cover GABA from the molecular mechanisms of its transmission to new targets for pharmaceutical research. Distinguished scientists at the forefront of GABA research were invited to contribute reviews on glutamate decarboxylase and autoimmunity, molecular structure and functional regulation of GABA transporters, transmitter release and GABA receptor regulation, GABA receptor subtypes and functional regulation, and GABA receptor ligands and their therapeutic application. Describing the latest advances in what has become a rapidly-evolving field, this volume will prove immensely valuable to neuroscientists, pharmacologists, biochemists, and physiologists working in the field of GABA research.

Elements of Molecular Neurobiology

Author : C. U. M. Smith
Publisher : John Wiley & Sons
ISBN 13 : 047085717X
Total Pages : 630 pages
Book Rating : 4.4/5 (78 download)

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Book Synopsis Elements of Molecular Neurobiology by : C. U. M. Smith

Download or read book Elements of Molecular Neurobiology written by C. U. M. Smith and published by John Wiley & Sons. This book was released on 2003-06-13 with total page 630 pages. Available in PDF, EPUB and Kindle. Book excerpt: This edition of the popular text incorporates recent advances in neurobiology enabled by modern molecular biology techniques. Understanding how the brain works from a molecular level allows research to better understand behaviours, cognition, and neuropathologies. Since the appearance six years ago of the second edition, much more has been learned about the molecular biology of development and its relations with early evolution. This "evodevo" (as it has come to be known) framework also has a great deal of bearing on our understanding of neuropathologies as dysfunction of early onset genes can cause neurodegeneration in later life. Advances in our understanding of the genomes and proteomes of a number of organisms also greatly influence our understanding of neurobiology. * Well known and widely used as a text throughout the UK, good reviews from students and lecturers. * Good complement to Fundementals of Psychopharmacology by Brian Leonard. This book will be of particular interest to biomedical undergraduates undertaking a neuroscience unit, neuroscience postgraduates, physiologists, pharmacologists. It is also a useful basic reference for university libraries. Maurice Elphick, Queen Mary, University of London "I do like this book and it is the recommended textbook for my course in Molecular Neuroscience. The major strength of the book is the overall simplicity of the format both in terms of layout and diagrams."

Snake Venoms

Author : P. Gopalakrishnakone
Publisher : Springer
ISBN 13 : 9789400764095
Total Pages : 0 pages
Book Rating : 4.7/5 (64 download)

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Book Synopsis Snake Venoms by : P. Gopalakrishnakone

Download or read book Snake Venoms written by P. Gopalakrishnakone and published by Springer. This book was released on 2017-02-14 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: In recent years, the field of Toxinology has expanded substantially. On the one hand it studies venomous animals, plants and micro organisms in detail to understand their mode of action on targets. While on the other, it explores the biochemical composition, genomics and proteomics of toxins and venoms to understand their three interaction with life forms (especially humans), development of antidotes and exploring their pharmacological potential. Therefore, Toxinology has deep linkages with biochemistry, molecular biology, anatomy and pharmacology. In addition, there is a fast developing applied subfield, clinical toxinology, which deals with understanding and managing medical effects of toxins on human body. Given the huge impact of toxin-based deaths globally, and the potential of venom in generation of drugs for so-far incurable diseases (for example, Diabetes, Chronic Pain), the continued research and growth of the field is imminent. This has led to the growth of research in the area and the consequent scholarly output by way of publications in journals and books. Despite this ever growing body of literature within biomedical sciences, there is still no all-inclusive reference work available that collects all of the important biochemical, biomedical and clinical insights relating to Toxinology. The Handbook of Toxinology aims to address this gap and cover the field of Toxinology comprehensively.

Anesthetic Pharmacology

Author : Alex S. Evers
Publisher : Cambridge University Press
ISBN 13 : 1139497022
Total Pages : 2902 pages
Book Rating : 4.1/5 (394 download)

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Book Synopsis Anesthetic Pharmacology by : Alex S. Evers

Download or read book Anesthetic Pharmacology written by Alex S. Evers and published by Cambridge University Press. This book was released on 2011-03-10 with total page 2902 pages. Available in PDF, EPUB and Kindle. Book excerpt: In recent years our understanding of molecular mechanisms of drug action and interindividual variability in drug response has grown enormously. Meanwhile, the practice of anesthesiology has expanded to the preoperative environment and numerous locations outside the OR. Anesthetic Pharmacology: Basic Principles and Clinical Practice, 2nd edition, is an outstanding therapeutic resource in anesthesia and critical care: Section 1 introduces the principles of drug action, Section 2 presents the molecular, cellular and integrated physiology of the target organ/functional system and Section 3 reviews the pharmacology and toxicology of anesthetic drugs. The new Section 4, Therapeutics of Clinical Practice, provides integrated and comparative pharmacology and the practical application of drugs in daily clinical practice. Edited by three highly acclaimed academic anesthetic pharmacologists, with contributions from an international team of experts, and illustrated in full colour, this is a sophisticated, user-friendly resource for all practitioners providing care in the perioperative period.

Textbook of Receptor Pharmacology

Author : John C. Foreman
Publisher : CRC Press
ISBN 13 : 1420052551
Total Pages : 314 pages
Book Rating : 4.4/5 (2 download)

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Book Synopsis Textbook of Receptor Pharmacology by : John C. Foreman

Download or read book Textbook of Receptor Pharmacology written by John C. Foreman and published by CRC Press. This book was released on 2010-09-10 with total page 314 pages. Available in PDF, EPUB and Kindle. Book excerpt: For the past four decades, University College London has offered a renowned course on receptor pharmacology. Originating from this course, the perennially bestselling Textbook of Receptor Pharmacology has presented in-depth coverage of this rapidly expanding area of research. This third edition continues to combine current understanding of classica

Neuroscientific Foundations of Anesthesiology

Author : George A. Mashour
Publisher : Oxford University Press
ISBN 13 : 0190453303
Total Pages : 296 pages
Book Rating : 4.1/5 (94 download)

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Book Synopsis Neuroscientific Foundations of Anesthesiology by : George A. Mashour

Download or read book Neuroscientific Foundations of Anesthesiology written by George A. Mashour and published by Oxford University Press. This book was released on 2011-10-05 with total page 296 pages. Available in PDF, EPUB and Kindle. Book excerpt: Although the perioperative care of patients by anesthesiologists draws on diverse clinical skills, the principles of anesthesiology and pain management are rooted in the neurosciences. The Neuroscientific Foundations of Anesthesiology thoroughly examines the anesthetic modulation of the central, peripheral, and autonomic nervous systems and will help redefine anesthesiology as a fundamentally neuroscientific field. The book is organized by sections, with each focusing on a different part of the nervous system. State-of-the-art chapters written by thought-leaders in anesthesiology and neuroscience provide a novel and invaluable resource.