Title Fundamentals of receptor, enzyme, and transport kinetics / John C. Matthews

Published Boca Raton : CRC Press, 2018

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Description 1 online resource Series CRC revivals CRC revivals. Contents Cover -- Title Page -- Copyright Page -- Preface -- The Author -- Acknowledgment -- Table of Contents -- Part I: Receptors -- Chapter 1 Introduction to Receptors -- I. Receptor-Ligand Complexes -- II. Affinity, Intrinsic Activity, and Effect -- III. Receptor Stimulation and Physiological Effect -- IV. Fundamentals of Receptor-Ligand Interaction -- V. Antagonists and Activators -- Chapter 2 Simple Receptor-Ligand Interactions -- I. Ligand Binding -- II. RL Lifetimes and Reaction Rate Constants -- III. Chemical Equilibrium -- IV. Equilibrium and Affinity Constants -- V. Receptor-Ligand Interaction Energies -- VI. The Langmuir Binding Isotherm -- VII. The Practical Meaning of Affinity -- VIII. Fractional Receptor Occupancy -- IX. Linear Transformations -- A. Double-Reciprocal or Lineweaver-Burk Equation -- B. The Rosenthal-Scatchard Equation -- C. The Eadie-Hofstee Equation -- D. The Woolf Equation -- X. Weighting Errors -- Chapter 3 Overview of Techniques for Direct Measurement of Receptor-Ligand Interactions -- I. Receptor Preparations -- II. Choosing Receptor Ligands and Radioisotopes -- III. Quantification of Radioactivity -- IV. Equilibrium and Dynamic Binding Measurements -- V. Fast and Slow Receptor-Ligand Interactions -- VI. General Considerations in Receptor Binding Methods -- A. Relationship between Receptor and Ligand Concentrations -- B. Nonspecific Binding -- C. Affinity -- D. Choice of Isotope for Radiolabeling -- E. Weighting Errors Inherent in the Use of Radioisotopes -- VII. Calorimetry -- Chapter 4 Receptor-Ligand Interactions That Generate Proportional Physiological Effects -- I. Relationship between Ligand Binding and Effect -- II. The Value pL[sub(2)] -- III. pH Equations and Receptor-Ligand Interactions -- IV. Relative Intrinsic Activity Chapter 5 Overview of Mechanisms for Coupling of Receptor-Agonist Interactions with Physiological Effects -- I. Introduction -- II. Ion Channel-Linked Signal Transduction -- III. Cyclic Nucleotide-Linked Signal Transduction -- A. Stimulatory Receptors -- B. Inhibitory Receptors -- IV. Phosphatidyl Inositol-Linked Signal Transduction -- V. Steroid Receptors -- Chapter 6 Overview of Techniques for Measuring Receptor-Agonist Interactions Through Their Physiological Effects -- I. Introduction -- II. Effects on Whole Animals -- III. Isolated Organs and Tissues -- IV. Tissue Slices, Cell Cultures, and Membrane Vesicles -- V. Receptor-Effector Systems at the Molecular Level -- Chapter 7 Receptor-Ligand Interactions that are Disproportionate with Their Physiological Effects -- I. Introduction -- II. Spare Receptors -- III. Homotropic Cooperativity and the Hill Equation -- IV. Discrepancies in and Alternatives for the Hill Equation -- V. Physiological Advantages of Homotropic Cooperativity -- A. Hemoglobin -- B. Calmodulin -- VI. Heterotropic Cooperativity -- VII. Receptor Desensitization -- Chapter 8 Antagonism -- I. Introduction -- II. Types of Antagonism -- A. Chemical Antagonism -- B . Physical Antagonism -- C. Functional Antagonism -- D. Irreversible Antagonists -- E. Reversible Antagonists -- 1. Simple Competitive Antagonism -- a. Slope Replots of Double-Reciprocal Data -- b. The Schild Equation -- c. The Value pI[sub(2)] -- 2. Partial Agonists as Competitive Inhibitors of Full Agonists -- 3. Simple Noncompetitive Antagonism -- 4. Heterotropic-Cooperative Noncompetitive Inhibition -- 5. Allosteric Competitive Inhibition -- 6. Allosteric Competitive Stimulation -- 7. Noncompetitive Stimulation -- 8. Homotropic Noncompetitive Inhibition -- 9. Uncompetitive Antagonism -- III. Conclusion -- Part II: Enzymes -- Chapter 9 Introduction to Enzymes I. Enzyme Catalysis and Specificity -- II. Reaction Rates -- III. Analysis of Enzyme Catalyzed Reactions -- Chapter 10 Simple Enzyme-Substrate Interactions -- I. Noncatalyzed Reaction Kinetics -- II. Enzyme Catalyzed Reaction Kinetics -- Chapter 11 Complex Enzyme-Substrate Interactions -- I. Introduction -- II. Sequential, Random Addition Bi-Uni Mechanism -- III. Sequential, Ordered Bi-Uni Mechanism -- IV. Ping-Pong Mechanisms -- V. Cooperativity in Enzyme Kinetics -- Part III: Transport Systems -- Chapter 12 Transport Kinetics -- I. Introduction -- II. Channels and Pores -- III. Carriers -- IV. Membrane Fusion -- V. Active Transport -- A. Ion Pumps -- B. Symport and Antiport Systems -- VI. Measurement of Transport -- VII. Analysis of Transport Data -- References -- Appendices -- Appendix 1 Table of Equations and Their Uses -- Appendix 2 Sample Calculations -- Part 1. Problems -- Part 2. Solutions -- Index Summary Fundamentals of Receptor, Enzyme, and Transport Kinetics is the first book to pull together the most important topics in receptor, enzyme, and transport kinetics into a concise, easy-to-use format. Numerous equations are included, and key equations are graphed. For each graphed equation, important features are carefully explained. The book is organized so that simple material is presented first, providing a firm foundation on which to cover the advanced topics which appear later. Terminology used throughout the book is consistent with that used in scientific literature, and concepts are explained using analogies from daily life. The book also features two important appendices that will be particularly useful learning tools. The first appendix outlines all of the key equations from the text and indicates their use. The second appendix is a set of sample calculation problems and their solutions. Fundamentals of Receptor, Enzyme, and Transport Kinetics is an excellent text/reference for pharmacologists, biological chemists, experimental biologists, neurochemists, neurotoxicologists, physiologists, and toxicologists. It is also suitable as a graduate-level text in pharmacology and medical pharmacology Bibliography Includes bibliographical references and index Notes Online resource; title from PDF title page (EBSCO, viewed February 12, 2018) Subject Ligand binding (Biochemistry) Enzyme kinetics. Biological transport. Cell receptors. Pharmacokinetics. Biological Transport Receptors, Cell Surface Pharmacokinetics MEDICAL -- Pharmacology. SCIENCE -- Life Sciences -- Cytology. Biological transport Cell receptors Enzyme kinetics Ligand binding (Biochemistry) Pharmacokinetics Form Electronic book ISBN 9780203713433 0203713435 9781351364584 1351364588 9781351364577 135136457X 9781351364560 1351364561

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