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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.

Includes example-based cases that illustrate how the pharmacological concepts discussed in this book lead to practical outcomes for further research
Provides vignettes on those researchers and scientists who have contributed significantly to the fields of pharmacology and drug discovery throughout history
Offers sample questions throughout the book and an appendix containing answers for self-testing and retention

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1. Pharmacology: The Chemical Control of Physiology 2. Drug Affinity and Efficacy 3. Predicting Agonist Effect 4. Drug Antagonism: Orthosteric Drug Effects 5. Allosteric Drug Effects 6. Enzymes as Drug Targets 7. Pharmacokinetics I: Permeation and Metabolism 8. Pharmacokinetics II: Distribution and Multiple Dosing 9. In Vivo Pharmacology 10. Safety Pharmacology 11. Pharmacology in Drug Discovery

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Kenakin, Terry
Terry P. Kenakin is the recipient of the 2008 Poulsson Medal for Pharmacology awarded by the Norwegian Society of Pharmacology for achievements in basic and clinical pharmacology and toxicology. He has also been awarded the 2011 Ariens Award from the Dutch Pharmacological Society and the 2014 Gaddum Memorial Award from the British Pharmacological Society. Having been involved in drug discovery for over 30 years, his interests include the optimal design of drug activity assays systems and quantitative drug receptor theory. He is a member of numerous editorial boards as well as Editor-in-Chief of the Journal of Receptors and Signal Transduction and Current Opinion in Pharmacology. In addition, Dr. Kenakin has authored numerous articles and has also written a number of books on pharmacology.

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