Pharmacology in drug discovery : understanding drug response / Terry P. Kenakin.

Includes bibliographical references and index.

Front Cover -- Pharmacology in Drug Discovery -- Copyright Page -- Contents -- Foreword -- Acknowledgements -- 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 -- References -- 2. Drug Affinity and Efficacy -- Introduction -- New Terminology -- Agonist Selectivity -- Affinity -- Efficacy -- Drugs with Multiple Efficacies -- Quantifying Agonist Activity -- Descriptive Pharmacology: II -- Summary -- Reference. 3. Predicting Agonist EffectAgonist Response in Different Tissues -- New Terminology -- The Black-Leff Operational Model of Agonism -- Applying the Black-Leff Model to Predict Agonism -- Descriptive Pharmacology: III -- Summary -- References -- 4. Drug Antagonism: Orthosteric Drug Effects -- Bi-Molecular Systems -- New Terminology -- What is Drug Antagonism? -- Antagonist Potency -- Mechanism(S) of Receptor Antagonism -- Orthosteric (Competitive and Non-Competitive) Antagonism -- Slow Dissociation Kinetics and Non-Competitive Antagonism -- Partial and Inverse Agonists -- Antagonist Effects in Vivo. Descriptive Pharmacology: IV Summary -- References -- 5. Allosteric Drug Effects -- Introduction -- New Terminology -- Protein Allosterism -- Types of Allosteric Modulators -- Unique Effects of Allosteric Modulators -- Detecting Allosterism -- Quantifying Allosteric Effect -- Descriptive Pharmacology: V -- Summary -- References -- 6. Enzymes as Drug Targets -- Introduction -- New Terminology -- Enzyme Kinetics -- Enzymes as Drug Targets -- Reversible Enzyme Inhibition -- Irreversible Enzyme Inhibition -- Intracellular Effects of Enzyme-Active Drugs -- Summary -- References -- 7. Pharmacokinetics I: Permeation and Metabolism. The Importance of Drug Concentration New Terminology -- "Drug-Like" Properties of Molecules -- Drug Absorption -- Drug Metabolism -- Oral Bioavailability -- Summary -- References -- 8. Pharmacokinetics II: Distribution and Multiple Dosing -- Drugs in Motion: in vivo Pharmacokinetics -- New Terminology -- The Central Compartment and in vivo Clearance -- Renal Excretion -- Drug Distribution -- Pharmacokinetics in vivo -- Scaling Data to Predict Human Pharmacokinetic Behavior -- Summary -- References -- 9. In Vivo Pharmacology -- Whole Body Drug Response -- New Terminology -- The "Dose" in Dose-Response -- What Constitutes Drug Response? The Importance of Kinetics in vivo Summary -- References -- 10. Safety Pharmacology -- Introduction -- New Terminology -- Safety Versus Toxicity -- Safety Pharmacology -- Early Safety Tests -- Hepatic Toxicity -- Summary -- References -- Appendix A: Answers to Chapter Questions -- Appendix B: Derivations and Proofs -- Index.