Recent advances in the development and applications of neurochemical brain imaging methods have improved the ability to study the neurochemistry of the living brain in normal processes as well as psychiatric disorders. In particular, positron emission tomography (PET) and single photon emission computed tomography (SPECT) have been used to determine neurochemical substrates of schizophrenia and to uncover the mechanism of action of antipsychotic medications. The growing availability of radiotracers for monoaminergic neurotransmitter synthesis, transporters and receptors, has enabled the evaluation of hypotheses regarding neurotransmitter function in schizophrenia derived from preclinical and clinical observations. This chapter reviews the studies using neurochemical brain imaging methods for (1) detection of abnormalities in indices of dopamine and serotonin transmission in patients with schizophrenia compared to controls, (2) development of new tools to study other neurotransmitters systems, such as gamma-aminobutyric acid (GABA) and glutamate, and (3) characterization of target occupancy by antipsychotic drugs, as well as its relationship to efficacy and side effects. As more imaging tools become available, this knowledge will expand and will lead to better detection of disease, as well as better therapeutic approaches.