Book excerpt: With a focus on functional relationships between drugs and their targets, this book covers basic and general pharmacology, from a cellular and molecular perspective, with particular attention to the mechanisms of drug action – the fundamental basis for proper clinical use- without neglecting clinical application, toxicology and pharmacokinetics. • Covers cell and molecular pharmacology, bringing together current research on regulation of drug targets, at a level appropriate for advanced undergrad and graduate students • Discusses the relevance of pharmacokinetics and drug development for the clinical application of drugs • Presents material from the perspective of drug targets and interaction, the theoretical basis of drug action analysis, and drug properties • Focuses on structure-function relationships of drug targets – informing about their biochemical and physiologic functions and experimental and clinical pathways for drug discovery and development • Has a companion website that offers a host of resources: short additional chapters about methodology, topics at the forefront of research, and all figures and tables from the book