The ability of cardioselective and nonselective beta-adrenoceptor blocking drugs, with and without partial agonist activity, to control increases in blood pressure associated with mental and physical activity was compared in 35 subjects with hypertension. Direct measurements of blood pressure and radioenzymatic determinations of plasma norepinephrine were obtained before, during and after four activities, and were repeated after random allocation to treatment with atenolol, metoprolol, pindolol or propranolol. Cardioselective and nonselective drugs modestly reduced the pressor response to reaction time testing, but not to mental arithmetic or isometric exercise. The increase in systolic blood pressure during bicycling was attenuated significantly by the cardioselective drugs atenolol (by 23 mm Hg, or 38%) and metoprolol (21 mm Hg, or 41%), but not by the nonselective agents pindolol (with partial agonist activity) (13 mm Hg, or 20%) and propranolol (10 mm Hg, or 17%) (p less than 0.02 cardioselective versus nonselective; p = NS pindolol versus propranolol). Only bicycle exercise increased plasma norepinephrine concentrations (by 80%). These results suggest that beta-adrenoceptor blocking drugs will not attenuate increases in blood pressure during mental or physical activities unless intense sympathoadrenal activation also occurs. Marked elevations in circulating epinephrine, with or without norepinephrine, and peripheral beta 2-blockade appear necessary for alpha-mediated vasoconstriction to predominate and for the contrasting effects of cardioselective and nonselective drugs to be appreciated.