OBJECTIVE This review focuses on the utilization of the effects of general anesthetics on cerebral metabolism as revealed by imaging for therapeutic and preventive purposes, for understanding mechanisms of anesthetic action, and for elucidating mechanisms of cerebral processing in humans. RESULTS General anesthetics suppress cerebral metabolism significantly. This effect has been used for neuroprotection during inadequate cerebral blood flow. With the advent of noninvasive imaging techniques, this suppression has also been used to image and map the sites of anesthetic action in the living human brain. Volatile agents, intravenous anesthetics, and analgesics have all begun to be explored using mostly positron emission tomography. The ability of anesthetics to change global baseline brain metabolism has created the opportunity to examine the relevance of global baseline (resting) brain activity in terms of region-specific cerebral processing. CONCLUSIONS Anesthetics experimentally appear to be useful for neuroprotection, at least during the early post-ischemic period. Identification of the cerebral sites of anesthetic action by in vivo human brain imaging provides new insights into the mechanism of action of these agents. Anesthetic-related manipulation of baseline brain metabolism demonstrates the significant contribution of this global activity to regional cerebral processing.