Magnetic resonance spectroscopy (MRS) provides a useful method for studying a number of psychotropic medications and metabolites in human brain in vivo. New insights regarding the pharmacokinetic and pharmacodynamic properties of psychotropic medications in the target organ (i.e., brain) have been obtained using lithium-7 MRS and fluorine-19 MRS. Both proton and phosphorus-31 MRS have significantly enhanced our knowledge of the pathophysiology of a number of psychiatric disorders by providing estimates of brain concentrations of several important cerebral metabolites. Efforts are also being made to link MRS measures of cerebral metabolism with neurophysiologic and neurocognitive processes. Ongoing improvement and refinement in MRS techniques, including the installation of scanners with increased magnetic field strength and better methods of data processing, will improve both spatial and temporal resolution. In addition, efforts to develop multisite research studies may result in greater standardization of MRS procedures and methods for interpretation of results. In this review, the current status of MRS applications in psychiatric research is reviewed, and new frontiers and possible future developments are discussed.