This book summarizes 20 years of work on the kinetics of blood-brain transfer and metabolism mechanisms in mammalian brain. The substances affiliated with these mechanisms include glucose, amino acids, monocarboxylic acids, and oxygen. These substances are important to energy metabolism and neurotransmission in the mammalian brain at rest and during activation. To understand the processes addressed by these mechanisms, the book examines the kinetics of compartmentation and compartmental analysis, particularly as they relate to transporter, enzyme, and receptor function. Compartments are subsets of substances separated by transporters and receptors in membranes, and enzymes in cells. This book is divided in six major chapters covering compartmental analysis, kinetic analysis of transport and metabolism, blood-brain transfer and metabolism of glucose, amino acids, and oxygen, and amino acid metabolism and interaction of amino acid metabolites with receptors.