Kenakin T.P. A pharmacology primer: theory, applications, and methods

Elsevier, 2009. — 377 p. — ISBN13: 978-0-12-374585-9.This book initially began as a series of lectures at GlaxoSmithKline Research and Development on receptor pharmacology aimed at increasing the communication between pharmacologists and chemists. As these lectures developed it became evident that the concepts were useful to biologists not specifically trained in pharmacology. In return, the exchange between the chemists and biologists furnished new starting points from which to view the pharmacological concepts. It is hoped that this book will somewhat fill what could be a gap in present biological sciences, namely the study of dose-response relationships and how cells react to molecules. It has been an interesting experience as an author and pharmacologist to see the changes that the discipline has experienced through the drug discovery process. While the definition of the human genome has undoubtedly marked pharmacology forever (and advanced it immeasurably), the more we learn, the more we are humbled by nature’s complexity. With the genome, knowing the road map is still a long way from completing the journey and recent experience seems to reinforce the idea that pharmacology must be used to understand integrated systems, not just the pieces they are made of. This edition incorporates a new trend in drug discovery; namely the consideration of pharmacokinetics and ADME properties of drugs (absorption, distribution, metabolism, excretion) early in the process. As prospective new drugs are tested in more complex systems (with concomitantly more complex dependent variable values), the trend in screening is to test fewer compounds of higher (druglike) quality. Finally, this edition also hopefully fills a previous void whereby the ideas and concepts discussed can be applied to actual problems in pharmacological drug discovery in the form of questions with accompanying answers. The expanded version now spans pharmacology from consideration of the independent variable (drug concentration in the form of pharmacokinetics) to the dependent variable (system-independent measurement of drug activity). As with previous editions, the emphasis of this book is still on the chemist–biologist interface with special reference to the use of pharmacology by non-pharmacologists.