Thiopental and pentobarbital induced dose-dependent vasodilations in human cerebral arteries previously contracted with noradrenaline (NA), serotonin (5-HT) and KCl. Preincubation with both barbiturates decreased the contractions evoked by the three agents. Pentobarbital and thiopental reduced the Ca2+-induced contractile effects in K+-depolarized arteries and 5-HT-Ca2+ and NA-Ca2+ contractions dose-dependently. The tritium release evoked by K+ from these vessels prelabelled with [3H]NA was significantly reduced by both barbiturates at 10(-3) M and by Ca2+ removal. These results indicate that pentobarbital and thiopental essentially produce a similar interference with Ca2+ influx inhibiting the contractile responses induced by the three vasoactive agents and the exocytotic NA release evoked by K+.