TY  - BOOK
AU  - Kenakin,Terrence P.
TI  - Pharmacology in drug discovery: understanding drug response 
SN  - 9780123848567 (pbk.)
AV  - RM301.35 .K46 2012
U1  - 615.1 23
PY  - 2012///
CY  - Amsterdam
PB  - Academic Press
KW  - Developmental pharmacology
KW  - Pharmacology
KW  - Drug development
KW  - Drug Discovery
KW  - Dose-Response Relationship, Drug
KW  - history
KW  - Pharmacological Processes
N1  - 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
ER  -