This paper analyses the effects of antipsychotic drug treatment on cerebral structure and function in schizophrenia reviewing qualitatively some of the relevant literature on the issue. Magnetic resonance imaging (MRI) studies of brain morphology in patients at different stages of illness and after varying times of neuroleptic exposure and longitudinal studies show possible different effects of first and second generation antipsychotics. This is true also for functional parameters, such as regional cerebral blood flow and metabolism, analysed, both in resting condition and after specific activation paradigms, with such diverse techniques as positron emission tomography (PET), single photon emission computed tomography (SPECT), functional MRI and MR spectroscopy. The possible molecular mechanisms underlying such differences and whether they represent direct drug effects or indirect consequences of their different and specific interactions with the 'natural' pathophysiological trajectory of brain abnormalities in schizophrenia are matter of present research and debate.