Metabolomics, the omics science of biochemistry, is a global approach to understanding regulation of metabolic pathways and metabolic networks of a biological system. Metabolomics complements data derived from genomics, transcriptomics, and proteomics to assist in providing a systems approach to the study of human health and disease. In this review we focus on applications of metabolomics for the study of diseases of the nervous system. We share concepts in metabolomics, tools used in metabolic profiling and early findings from the study of neuropsychiatric diseases, and drugs used to treat these diseases. Metabolomics emerges as another powerful tool in central nervous system research.