Toliprolol is beta-adrenergic blocker. It was developed as antianginal and antihypertensive agent. Toliprolol is moderately lipophilic. It appears to have the appropriate characteristics for cerebral beta-adrenoreceptor imaging. However, tissue uptake of toliprolol was dominated by the nonspecific binding, both in the brain and in peripheral target organs, such as heart and lung. Toliprolol seems unsuitable for visualization of cerebral beta-adrenoceptors. After application of ethanol to mice, the content of glycogen of the liver and the brain decreased. By pretreatment with the beta-sympatholytic agent toliprolol, the ethanol-induced break-down of glycogen was partially blocked in the liver and completely abolished in the brain. In contrast, mainly synergistic effects of ethanol and toliprolol on the glycolysis of the liver and the brain were found. Toliprolol reduced the greater variance during the emotionally stressful situation in doses insufficient to diminish the mean increase in forearm blood flow.