A Pharmacology Primer: Techniques for More Effective and Strategic Drug Discovery, Sixth Edition features the latest research surrounding the application of pharmacology in drug discovery in an effort to equip readers with a deeper understanding of complex and rapid changes in this field. Written by well-respected pharmacologist, Terry P. Kenakin, this primer is an indispensable resource for anyone involved in drug discovery. This edition has been reorganized for better flow and clarity and includes material on new technologies for screening (virtual, DNA encoded libraires, fragment-based) and a major section on phenotypic (target agnostic) screening for new leads and determination of drug targets.
With full color illustrations as well as new examples throughout, this book remains a top reference for all industry and academic scientists and students directly involved in drug discovery or pharmacologic research. New material includes a discussion of the determination of target engagement, including numerous new ways to demonstrate the physical interaction of molecules with drug targets and new drug candidates such a mRNA, gene therapy, antibodies and information on CRISPR and genomics.
1. 7.1: Introduction - p. 189 2. 7.2: Kinetics of drug–receptor interaction - p. 189 3. 7.3: Surmountable competitive antagonism - p. 192 4. 7.4: Noncompetitive antagonism - p. 204 5. 7.5: Agonist–antagonist hemiequilibria - p. 208 6. 7.6: Resultant analysis - p. 210 7. 7.7: Antagonism in vivo - p. 210 8. 7.8: Blockade of indirectly acting agonists - p. 219 9. 7.9: Irreversible antagonism - p. 220 10. 7.10: Chemical antagonism - p. 222 11. 7.11: Chapter summary and conclusions - p. 226 12. 7.12: Derivations - p. 227 13. Chapter 8 Allosteric modulation - p. 233 14. Chapter 9 The optimal design of pharmacological experiments - p. 269 15. Chapter 10 Pharmacokinetics - p. 307 16. 10.1: Introduction - p. 307 17. 10.2: Biopharmaceutics - p. 307 18. 10.3: The chemistry of “drug-like” character - p. 308 19. 10.4: Pharmacokinetics - p. 313 20. 10.5: Nonlinear pharmacokinetics - p. 342 21. 10.6: Multiple dosing - p. 343 22. 10.7: Modifying pharmacokinetics through medicinal chemistry - p. 345 23. 10.8: Practical pharmacokinetics - p. 347 24. 10.9: Placement of pharmacokinetic assays in discovery and development - p. 350 25. 10.10: The pharmacokinetics of biologics - p. 352 26. 10.11: Summary and conclusions - p. 355 27. Chapter 11 Safety pharmacology - p. 359 28. Chapter 12 The drug-discovery process - p. 383 29. Chapter 13 Selected pharmacological methods - p. 423 30. Appendix 1 Statistics - p. 453 31. Index - p. 483
A Pharmacology Primer: Techniques for More Effective and Strategic Drug Discovery, Sixth Edition features the latest research surrounding the application of pharmacology in drug discovery in an effort to equip readers with a deeper understanding of complex and rapid changes in this field. Written by well-respected pharmacologist, Terry P. Kenakin, this primer is an indispensable resource for anyone involved in drug discovery. This edition has been reorganized for better flow and clarity and includes material on new technologies for screening (virtual, DNA encoded libraires, fragment-based) and a major section on phenotypic (target agnostic) screening for new leads and determination of drug targets.
With full color illustrations as well as new examples throughout, this book remains a top reference for all industry and academic scientists and students directly involved in drug discovery or pharmacologic research. New material includes a discussion of the determination of target engagement, including numerous new ways to demonstrate the physical interaction of molecules with drug targets and new drug candidates such a mRNA, gene therapy, antibodies and information on CRISPR and genomics.
1. 7.1: Introduction - p. 189 2. 7.2: Kinetics of drug–receptor interaction - p. 189 3. 7.3: Surmountable competitive antagonism - p. 192 4. 7.4: Noncompetitive antagonism - p. 204 5. 7.5: Agonist–antagonist hemiequilibria - p. 208 6. 7.6: Resultant analysis - p. 210 7. 7.7: Antagonism in vivo - p. 210 8. 7.8: Blockade of indirectly acting agonists - p. 219 9. 7.9: Irreversible antagonism - p. 220 10. 7.10: Chemical antagonism - p. 222 11. 7.11: Chapter summary and conclusions - p. 226 12. 7.12: Derivations - p. 227 13. Chapter 8 Allosteric modulation - p. 233 14. Chapter 9 The optimal design of pharmacological experiments - p. 269 15. Chapter 10 Pharmacokinetics - p. 307 16. 10.1: Introduction - p. 307 17. 10.2: Biopharmaceutics - p. 307 18. 10.3: The chemistry of “drug-like” character - p. 308 19. 10.4: Pharmacokinetics - p. 313 20. 10.5: Nonlinear pharmacokinetics - p. 342 21. 10.6: Multiple dosing - p. 343 22. 10.7: Modifying pharmacokinetics through medicinal chemistry - p. 345 23. 10.8: Practical pharmacokinetics - p. 347 24. 10.9: Placement of pharmacokinetic assays in discovery and development - p. 350 25. 10.10: The pharmacokinetics of biologics - p. 352 26. 10.11: Summary and conclusions - p. 355 27. Chapter 11 Safety pharmacology - p. 359 28. Chapter 12 The drug-discovery process - p. 383 29. Chapter 13 Selected pharmacological methods - p. 423 30. Appendix 1 Statistics - p. 453 31. Index - p. 483
