The effect of antiestrogen U23,469 administration in vivo on the concentration of dopamine, norepinephrine and epinephrine in the plasma, cerebral cortex and hypothalamus in ovariectomized rats was investigated. Rats were treated with estradiol benzoate, progesterone and U23,469 in different doses, s.c., daily for 6 days. Control group was injected with sesame oil. Catecholamines were estimated by radioenzymatic assay. Six days of U23,469, estradiol benzoate, progesterone or its combination altered the catecholamine levels compared to the control. Dopamine decreased in plasma with progesterone and U23,469. In the cerebral cortex, progesterone and U23,469 increased significantly and in the hypothalamus all the treatments produced a decrease of catecholamines. The levels of NE were reduced with estradiol benzoate, progesterone and U23,469; there was no significant difference in the norepinephrine levels after different treatments in the cerebral cortex, but the NE levels were significantly decreased in the hypothalamus. Epinephrine showed differences related to the treatment, as in plasma, as in cerebral cortex and hypothalamus. These results suggest that antiestrogen treatment compared with the estradiol benzoate or progesterone may affect the catecholamine levels of the central nervous system and plasma and support the idea that AE could have an indirect effect on the catecholaminergic system.