Machine generated contents note: 1. Pharmacology: The Chemical Control of Physiology -- Pharmacology and Cellular Drug Response -- New Terminology -- Pharmacological Targets -- Dose -- Response Curves -- Linking Observed Pharmacology With Molecular Mechanism -- Descriptive Pharmacology: I -- Summary -- Questions -- References -- 2. Drug Affinity and Efficacy -- Introduction -- New Terminology -- Agonist Selectivity -- Affinity -- Efficacy -- Drugs With Multiple Efficacies -- Quantifying Agonist Activity -- Descriptive Pharmacology: II -- Summary -- Questions -- References -- 3. Predicting Agonist Effect -- Agonist Response in Different Tissues -- New Terminology -- Black -- Leff Operational Model of Agonism Applying the Black -- Leff Model to Predict Agonism -- Receptor Selectivity -- Biased Agonist Signaling -- Descriptive Pharmacology: III -- Summary -- Questions -- References -- 4. Drug Antagonism: Orthosteric Drug Effects -- Bimolecular Systems -- New Terminology -- What Is Drug Antagonism? -- Antagonist Potency -- Mechanism(s) of Receptor Antagonism -- Orthosteric (Competitive and Noncompetitive) Antagonism -- Slow Dissociation Kinetics and Noncompetitive Antagonism -- Partial and Inverse Agonists -- Antagonist Effects In Vivo -- Descriptive Pharmacology: IV -- Summary -- Questions -- References -- 5. Allosteric Drug Effects -- Introduction -- New Terminology -- Protein Allosterism -- Allosteric Phenotypes -- Unique Effects of Allosteric Modulators -- Detecting Allosterism -- Quantifying Allosteric Effect -- Descriptive Pharmacology: V -- Summary -- Questions -- References -- 6. Enzymes as Drug Targets -- Introduction -- New Terminology -- Enzyme Kinetics -- Enzymes as Drug Targets -- Reversible Enzyme Inhibition -- Irreversible Enzyme Inhibition -- Allosteric Enzyme Modulation -- Enzyme Activation -- Intracellular Effects of Enzyme-Active Drugs -- Summary -- Questions -- References -- 7. Pharmacokinetics I: Permeation and Metabolism -- Importance of Drug Concentration -- New Terminology -- "Drug-Like" Properties of Molecules -- Drug Absorption -- Drug Metabolism -- Oral Bioavailability -- Summary -- Questions -- References -- 8. Pharmacokinetics II: Distribution and Multiple Dosing -- Drugs in Motion: In Vivo Pharmacokinetics -- New Terminology -- Central Compartment and In vivo Clearance -- Renal Excretion -- Drug Distribution -- In Vivo PK -- Oral Bioavailability -- Drug -- Drug Interactions -- Nonlinear Pharmacokinetics -- Scaling Data to Predict Human Pharmacokinetic Behavior -- Summary -- Questions -- References -- 9. In Vivo Pharmacology -- Whole Body Drug Response -- New Terminology -- "Dose" in Dose -- Response -- What Constitutes Drug Response? -- Importance of Kinetics In Vivo -- Summary -- Questions -- References -- 10. Safety Pharmacology -- Introduction -- New Terminology -- Safety Versus Toxicity -- Safety Pharmacology -- Early Safety Tests -- Hepatic Toxicity -- Summary -- Questions -- References -- 11. Pharmacology in Drug Discovery -- Introduction -- Unique Aspects of Pharmacology in the Discovery Process -- Target-Versus System-Based Discovery Strategies -- Progression Scheme for Drug Discovery -- Libraries and Molecules as Drug Sources -- Pharmacological Assay Design -- High-Throughput Screening -- Lead Optimization -- Drug Development -- Summary -- Questions -- References.

Pharmacology in Drug Discovery and Development: Understanding Drug Response, Second Edition, is an introductory resource illustrating how pharmacology can be used to furnish the tools necessary to analyze different drug behavior and trace this behavior to its root cause or molecular mechanism of action. The concepts discussed in this book allow for the application of more predictive pharmacological procedures aimed at increasing therapeutic efficacy that will lead to more successful drug development. Chapters logically build upon one another to show how to characterize the pharmacology of any given molecule and allow for more informed predictions of drug effects in all biological systems. New chapters are dedicated to the interdisciplinary drug discovery environment in both industry and academia, and special techniques involved in new drug screening and lead optimization. This edition has been fully revised to address the latest advances and research related to real time kinetic assays, pluridimensional efficacy, signaling bias, irreversible and chemical antagonism, allosterically-induced bias, pharmacokinetics and safety, target and pathway validation, and much more. With numerous valuable chapter summaries, detailed references, practical examples and case studies throughout, Dr. Kenakin successfully navigates a highly complex subject, making it accessible for students, professors, and new researchers working in pharmacology and drug discovery.