This report describes a new approach to the evaluation of neuroleptic effects on regional brain function. Using Tc-99m HMPAO SPECT imaging, consecutive brain perfusion studies before and after acute haloperidol administration were performed on three schizophrenic patients and two normal volunteers. The antipsychotic drug ameliorated the hypoactivity in the frontal lobe and suppressed the hyperactivity in the temporo-occipito-parietal lobe selectively in the dominant hemisphere in the schizophrenic patients. It did not exert a significant influence on the brain perfusion pattern in normal volunteers. This nuclear medicine technique seems to be useful for the evaluation of drug effects in psychiatric diseases.