Functional neuroimaging provides a direct way of investigating the pathophysiology of schizophrenia in vivo. The function of neurotransmitters implicated in schizophrenia, such as dopamine and glutamate, can be assessed using molecular imaging techniques such as positron emission tomography (PET), single-photon emission tomography (SPET) and magnetic resonance spectroscopy (MRS). Regional brain activity, particularly that associated with the cognitive processes and symptoms associated with the disorder, can be studied using functional magnetic resonance imaging (fMRI). Here, we focus on the potential for the use of these techniques in the diagnosis of schizophrenia and in the development of new drugs for its treatment.