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The pharmacodynamic profile of bisoprolol, a new beta 1‐selective adrenoceptor antagonist, was investigated in four independent studies including 36 healthy male volunteers. Using the model of exercise‐ induced tachycardia (ET) the beta‐adrenoceptor blocking properties of bisoprolol (2.5‐40 mg) were examined in comparison to metoprolol (50 and 100 mg), propranolol (40 and 80 mg) and atenolol (50 and 100 mg). The maximal reduction of ET was achieved between 1 and 4 h following single oral administration. The dose‐response relationship using individual maximal reduction of ET showed, on a molar basis, that bisoprolol is about 5, 7 and 10 times more effective than propranolol, atenolol and metoprolol, respectively. In the model of insulin‐induced hypoglycaemia bisoprolol behaved as a beta 1‐selective adrenoceptor antagonist. There was a good correlation (r = 0.94) between the log bisoprolol concentration and the reduction in exercise‐induced tachycardia. Bisoprolol is a potent new cardioselective beta‐ adrenoceptor antagonist with a competitive action at beta 1‐ adrenoceptors.

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