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Cyclic nucleotide phosphodiesterases (PDEs) are promising targets for pharmacological intervention. Multiple PDE genes, isoform diversity, selective expression and compartmentation of the isoforms, and an array of conformations of PDE proteins are properties that challenge development of drugs that selectively target this class of enzymes. Novel characteristics of PDEs are viewed as unique opportunities to increase specificity and selectivity when designing novel compounds for certain therapeutic indications. This chapter provides a summary of the major concepts related to the design and use of PDE inhibitors.
Since the last major compendium dedicated to cyclic nucleotide phosphodiesterases (PDEs) was published over 15 years ago, an enormous amount of progress has occurred in the field. There is great need for a centralized source for key information in this burgeoning and therapeutically important area of medical research. Cyclic Nucleotide Phosph
Focused on central nervous system (CNS) drug discovery efforts, this book educates drug researchers about the blood-brain barrier (BBB) so they can affect important improvements in one of the most significant – and most challenging – areas of drug discovery. • Written by world experts to provide practical solutions to increase brain penetration or minimize CNS side-effects • Reviews state-of-the-art in silico, in vitro, and in vivo tools to assess brain penetration and advanced CNS drug delivery strategies • Covers BBB physiology, medicinal chemistry design principles, free drug hypothesis for the BBB, and transport mechanisms including passive diffusion, uptake/efflux transporters, and receptor-mediated processes • Highlights the advances in modelling BBB pharmacokinetics and dynamics relationships (PK/PD) and physiologically-based pharmacokinetics (PBPK) • Discusses case studies of successful CNS and non-CNS drugs, lessons learned and paths to the market
"Mechanisms of Neuroinflammation" book explains how the neuronal cells become swollen at the moment of the blood-brain barrier disruption and how they lose their immunological isolation. A cascade of cytokines and immune cells from the bloodstream enters the nervous system, inflaming neurons and activating the glia. This produces a neuroinflammatory process that can generate different neurodegenerative diseases. Better understanding of mechanisms that are activated at the time when the damage to the brain occurs could lead to the development of suitable therapies that revert the neuronal inflammation and thus prevent further damage to the nervous system.
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.
This book reviews current science and applications in fields including thrombosis and hemostasis, signal transduction, and non-thrombotic conditions such as inflammation, allergy and tumor metastasis. It is a detailed, up-to-date, highly referenced text for clinical scientists and physicians, including recent developments in this rapidly expanding field. More than a scientific resource, this is also an authoritative reference and guide to the diagnosis.
Written by the foremost authority in the field, this volume is a comprehensive review of the multifaceted phenomenon of hepatotoxicity. Dr. Zimmerman examines the interface between chemicals and the liver; the latest research in experimental hepatotoxicology; the hepatotoxic risks of household, industrial, and environmental chemicals; and the adverse effects of drugs on the liver. This thoroughly revised, updated Second Edition features a greatly expanded section on the wide variety of drugs that can cause liver injury. For quick reference, an appendix lists these medications and their associated hepatic injuries. Also included are in-depth discussions of drug metabolism and factors affecting susceptibility to liver injury.
Written by leading experts in the field and designed for dermatologists and residents, this book includes evidence-based medicine that underscores the clinical data, as well as practical tips on how to use both biologic and systemic agents in the field of dermatology. In the past decade, there have been several groundbreaking advances in medical dermatology. Novel biologic and systemic agents have been developed to treat inflammatory disorders, including psoriasis and atopic dermatitis, as well as skin malignancies such as melanoma. Biologic and Systemic Agents in Dermatology encompasses these developments by describing the mechanism of action of these various agents and the clinical efficacy and safety to treating these respective disorders. The utilization of biologic and systemic agents in other dermatologic conditions, pharmacoeconomics, pharmacovigilance, and clinical trials outcomes are discussed as well as topics including tumor necrosis, conventional systemic agents for psoriatic disease, and oral agents for atopic dermatitis.
Lower Urinary Tract Symptoms and Benign Prostatic Hyperplasia: From Research to Bedside offers full acknowledgment of the basic research of lower urinary tract symptoms (LUTS) and benign prostatic hyperplasia (BPH), also connecting the clinical and practice management of the disease. It provides a full comprehension of LUTS and BPH from several aspects, allowing for a schematic interpretation of the disease and subsequent medical management. Going beyond the guidelines in the field, this title enhances the knowledge of BPH onset, allowing for the advancement of research, beneficial clinical implication and treatment. Perfect for researchers, urologists, pathologists and endocrinologists, this must-have reference provides what is needed to understand LUTS and BPH in one easy to reference place. - Provides a clear understanding of the pathological mechanisms that are present in lower urinary tract symptoms (LUTS) and benign prostatic hyperplasia (BPH) - Incorporates research with the clinical aspects of LUTS and BPH, including surgical techniques - Presents an overview of LUTS and BPH in one easy to reference place