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With publication of the human genome has come an experiment in reductionism for drug discovery. With the evaluation of the number and quality of new drug treatments from this approach has come a reevaluation of target-based versus systems-based strategies. Pharmacology, historically rooted in systems-based approaches and designed to give systems-independent measures of drug activity, is suitably poised to be a major (if not the major) tool in this new environment of drug discovery. Compared to the first edition, this book now expands discussion of tools and ideas revolving around allosteric drug action. This is an increasingly therapeutically relevant subject in pharmacology as new drug screening utilizes cell function for discovery of new drug entities | Foreword to Second Edition With publication of the human genome has come an experiment in reductionism for drug discovery. With the evaluation of the number and quality of new drug treatments from this approach has come a reevaluation of target-based versus systems-based strategies. Pharmacology historically rooted in systems-based approaches and designed to give systems-independent measures of drug activity is suitably poised to be a major if not the major tool in this new environment of drug discovery. Compared to the first edition this book now expands discussion of tools and ideas revolving around allosteric drug action. This is an increasingly therapeutically relevant subject in pharmacology as new drug screening utilizes cell function for discovery of new drug entities. In addition discussion of system-based approaches drug development pharmacokinetics therapeutics sources of chemicals for new drugs and elements of translational medicine have been added. As with the first edition the emphasis of this volume is the gaining of understanding of pharmacology by the nonpharmacologist. Terry P. Kenakin Ph.D. Research Triangle Park 2006 xi Foreword to First Edition If scientific disciplines can be said to go in and out of vogue pharmacology is exemplary in this regard. The flourishing of receptor theory in the 1950s the growth of biochemical binding technology in the 1970s and the present resurgence of interest in defining cellular phenotypic sensitivity to drugs has been interspersed with troughs such as that brought on by the promise of the human genome and a belief that this genetic roadmap may make classical pharmacology redundant. The fallacy in this belief has been found in experimental data showing the importance of phenotype over genotype which underscores a common finding with roadmaps they are not as good as a guide who knows the way. Pharmacology is now more relevant to the drug discovery process than ever as the genome furnishes a wealth of new targets .