The effect of labetalol, a combined alpha- and beta-adrenoceptor antagonist, on the cerebral circulation was investigated in 7 normotensive subjects. Cerebral blood flow (CBF) was measured with the intravenous 133Xe method and mean flow velocity (Vmean) in the middle cerebral artery was determined using transcranial Doppler (TCD) ultrasound. Examination was performed before and then 15, 60 and 120 min after 0.75 mg/kg i.v. labetalol. Reactivity to inhalation of 5% CO2 in air was studied before, and again 90 min after labetalol administration. Neither CBF nor Vmean changed following labetalol administration, whereas a marked increase occurred during inhalation of CO2. The median CO2 reactivity was 3.2%/mmHg (range: 1.8-4.0) for CBF and 4.4%/mmHg (1.5-5.6) for Vmean. These results indicate that labetalol, given in moderate but clinically relevant doses, does not affect the cerebral circulation in normotensive subjects. Neither does it affect CO2 reactivity. The uniform results obtained with the two methods suggest TCD as a usable alternative to conventional CBF technique in the assessment of cerebral vasoactivity of various drugs in subjects with a normal cerebral circulation.