A Pharmacology Primer
Theory, Applications, and Methods
- 2nd Edition - October 30, 2006
- Author: Terry P. Kenakin
- Language: English
The Second Edition will continue this tradition of better preparing researchers in the basics of pharmacology. In addition, new human interest material including historical facts… Read more
The Second Edition will continue this tradition of better preparing researchers in the basics of pharmacology. In addition, new human interest material including historical facts in pharmacology will be added. A new section on therapeutics will help readers identify with diseases and drug treatments.
- Over 30 new figures and tables
- More human interest information to provide readers with historical facts on pharmacology research
- New section on therapeutics to help identify diseaes and drug treatments
- New section on new biological concepts relevant to pharmacological research (i.e., systems biology)
- New study sections organized with ASPET and other international pharmacology organizations
- New coverage of pharmacokinetics and drug disposition
Researchers in all areas of molecular biology who need the background basics of pharmacology. This list includes pharmaceutical companies, drug disocvery professionals, and researchers in pharmacology, biochemistry, cell biology, and molecular biology. Also can be used for upper-level undergrad textbook.
- Foreword to Second Edition
- Foreword to First Edition
- Chapter 1: What Is Pharmacology?
- Publisher Summary
- 1.1 About This Book
- 1.2 What Is Pharmacology?
- 1.3 The Receptor Concept
- 1.4 Pharmacological Test Systems
- 1.5 The Nature of Drug Receptors
- 1.6 Pharmacological Intervention and the Therapeutic Landscape
- 1.7 System-independent Drug Parameters: Affinity and Efficacy
- 1.8 What Is Affinity?
- 1.9 The Langmuir Adsorption Isotherm
- 1.10 What Is Efficacy?
- 1.11 Dose-response Curves
- 1.12 Chapter Summary and Conclusions
- 1.13 Derivations: Conformational Selections as a Mechanism of Efficacy
- Chapter 2: How Different Tissues Process Drug Response
- Publisher Summary
- 2.1 Drug Response as Seen Through the “Cellular Veil”
- 2.2 The Biochemical Nature of Stimulus-response Cascades
- 2.3 The Mathematical Approximation of Stimulus-response Mechanisms
- 2.4 System Effects on Agonist Response: Full and Partial Agonists
- 2.5 Differential Cellular Response to Receptor Stimulus
- 2.6 Receptor Desensitization and Tachyphylaxis
- 2.7 The Measurement of Drug Activity
- 2.8 Advantages and Disadvantages of Different Assay Formats
- 2.9 Drug Concentration as an Independent Variable
- 2.10 Chapter Summary and Conclusions
- 2.11 Derivations
- Chapter 3: Drug-Receptor Theory
- Publisher Summary
- 3.1 About This Chapter
- 3.2 Drug-Receptor Theory
- 3.3 The Use of Mathematical Models in Pharmacology
- 3.4 Some Specific Uses of Models in Pharmacology
- 3.5 Classical Model of Receptor Function
- 3.6 The Operational Model of Receptor Function
- 3.7 Two-state Theory
- 3.8 The Ternary Complex Model
- 3.9 The Extended Ternary Model
- 3.10 Constitutive Receptor Activity
- 3.11 The Cubic Ternary Complex Model
- 3.12 Chapter Summary and Conclusions
- 3.13 Derivations
- Chapter 4: Pharmacological Assay Formats: Binding
- Publisher Summary
- 4.1 The Structure of This Chapter
- 4.2 Binding Theory and Experiment
- 4.3 Complex Binding Phenomena: Agonist Affinity from Binding Curves
- 4.4 Experimental Prerequisites for Correct Application of Binding Techniques
- 4.5 Chapter Summary and Conclusions
- 4.6 Derivations
- Chapter 5: Agonists: The Measurement of Affinity and Efficacy in Functional Assays
- Publisher Summary
- 5.1 Functional Pharmacological Experiments
- 5.2 The Choice of Functional Assays
- 5.3 Recombinant Functional Systems
- 5.4 Functional Experiments: Dissimulation in Time
- 5.5 Experiments in Real Time Versus Stop Time
- 5.6 The Measurement of Agonist Affinity in Functional Experiments
- 5.7 Estimates of Relative Efficacy of Agonists in Functional Experiments
- 5.8 Chapter Summary and Conclusions
- 5.9 Derivations
- Chapter 6: Orthosteric Drug Antagonism
- Publisher Summary
- 6.1 Introduction
- 6.2 Kinetics of Drug-Receptor Interaction
- 6.3 Surmountable Competitive Antagonism
- 6.4 Noncompetitive Antagonism
- 6.5 Agonist-Antagonist Hemi-equilibria
- 6.6 Resultant Analysis
- 6.7 Chapter Summary and Conclusions
- 6.8 Derivations
- Chapter 7: Allosteric Drug Antagonism
- Publisher Summary
- 7.1 Introduction
- 7.2 The Nature of Receptor Allosterism
- 7.3 Properties of Allosteric Modulators
- 7.4 Functional Study of Allosteric Modulators
- 7.5 Measurement of the Potency of Allosteric Insurmountable Antagonists
- 7.6 Methods for Detecting Allosterism
- 7.7 Chapter Summary and Conclusions
- 7.8 Derivations
- Chapter 8: The Process of Drug Discovery
- Publisher Summary
- 8.1 Pharmacology in Drug Discovery
- 8.2 Chemical Sources for Potential Drugs
- 8.3 Pharmacodynamics and High-throughput Screening
- 8.4 Pharmacokinetics
- 8.5 Pharmaceutical Development
- 8.6 Adverse Drug Effects
- 8.7 Chapter Summary and Conclusions
- Chapter 9: Target- and System-based Strategies for Drug Discovery
- Publisher Summary
- 9.1 Some Challenges for Modern Drug Discovery
- 9.2 Target-based Drug Discovery
- 9.3 Systems-based Drug Discovery
- 9.4 In Vivo Systems, Biomarkers, and Clinical Feedback
- 9.5 Types of Therapeutically Active Ligands
- 9.6 Summary and Conclusions
- Chapter 10: “Hit” to Drug: Lead Optimization
- Publisher Summary
- 10.1 Tracking SARs and Determining Mechanism of Action: Data-driven Drug-based Pharmacology
- 10.2 Drug Initiation of Response: Agonism
- 10.3 Inhibition of Agonist Response: Antagonism
- 10.4 “Short-form” Measures of Antagonism for Following Structure-activity Relationship
- 10.5 Summary and Conclusions
- 10.6 Derivations
- Chapter 11: Statistics and Experimental Design
- Publisher Summary
- 11.1 Structure of This Chapter
- 11.2 Introduction
- 11.3 Descriptive Statistics: Comparing Sample Data
- 11.4 How Consistent Is Experimental Data with Models?
- 11.5 Comparison of Samples to “Standard Values”
- 11.6 Experimental Design and Quality Control
- 11.7 Chapter Summary and Conclusions
- Chapter 12: Selected Pharmacological Methods
- Publisher Summary
- 12.1 Binding Experiments
- 12.2 Functional Experiments
- Glossary of Pharmacological Terms
- Appendices
- Index
- Edition: 2
- Published: October 30, 2006
- Language: English
TK
Terry P. Kenakin
Dr. Terry Kenakin is Professor of Pharmacology at the University of North Carolina School of Medicine. Prior to this, he spent 7 years in drug discovery at Burroughs-Wellcome. He then moved to GlaxoSmithKline for 25 years. Dr. Kenakin has written 11 books on Pharmacology, is the Editor in Chief of the Journal of Receptors and Signal Transduction, is on numerous Editorial Boards. He is the Editor-in-Chief of Comprehensive Pharmacology (Elsevier, 2022). He is the recipient of the 2008 Poulsson Medal for Pharmacology awarded by the Norwegian Society of Pharmacology for achievements in basic and clinical pharmacology and toxicology. He has also been awarded the 2011 Ariens Award from the Dutch Pharmacological Society and the 2014 Gaddum Memorial Award from the British Pharmacological Society, and the 2020 Goodman and Gilman Award in Receptor Pharmacology from ASPET.
Affiliations and expertise
Professor, Pharmacology, University of North Carolina, USARead A Pharmacology Primer on ScienceDirect