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A Pharmacology Primer,

Edition 2 Theory, Applications, and Methods

Editors: By Terry Kenakin

Publication Date: 30 Oct 2006

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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.

Key Features

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

About the author

By Terry Kenakin, GlaxoSmithKline Research & Development, Research Triangle Park, North Carolina, U.S.A.

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

A Pharmacology Primer,

Editors: By Terry Kenakin

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About the author

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