The aim of the study was to evaluate the effects of a beta 1-selective (atenolol 50 mg q.d.) and a non-selective (propranolol 80 mg b.i.d.) beta-adrenoceptor antagonists on human stimulated parotid and submandibular-sublingual (SM-SL) gland secretion. A randomized double-blind, placebo-controlled cross-over ("Latin square") design was used in 19 healthy male volunteers. Stimulated parotid and SM-SL saliva were sampled immediately before and 7 days after the start of each treatment period. Stimulation of salivary secretion was achieved by use of a 3% citric acid solution. Plasma concentrations of propranolol and atenolol were determined from blood samples. The salivary secretion of both glands was assessed for flow rate, amylase, lysozyme, and salivary peroxidase activity and for concentrations of total protein, hexosamine, sialic acid, Ca2+, Cl-, K+, Mg2+, Na+, and PO4(3-). In both parotid and SM-SL secretions, the total protein and phosphate concentrations and amylase activity were significantly decreased during the two active treatment periods. In SM-SL gland secretion, there were significant changes in potassium and calcium concentrations during active treatment as compared with baseline, with potassium showing a decreased and calcium an increased concentration. During atenolol treatment, salivary peroxidase activity decreased significantly in SM-SL secretion. In parotid secretion, the hexosamine/total protein ratio decreased and the sialic acid/hexosamine ratio increased during atenolol treatment, which may indicate an effect on protein synthesis. No significant effects on salivary secretion rates were disclosed.