The effect of salbutamol (SB) on the cerebral levels of serotonin (5-HT) and 5-hydroxyindolacetic acid (5-HIAA) was determined as well as the effect on the uptake and turnover of 5-HT in rat brain. SB failed to inhibit the cerebral uptake of 5-HT and did not change 5-HT and 5-HIAA levels in the brain; however, it significantly increased the cerebral turnover of 5-HT. The latter effect may partly be responsible for the antidepressant properties of the compounds.