Responses to estrogen differ between the sexes, yet sex differences in specific binding of estradiol (E2) to its receptor are not observed consistently. Dopaminergic treatment has been shown to increase binding of 3H-E2 in selected brain areas and anterior pituitary in the female rat, and the dopaminergic system is sexually differentiated. In order to determine whether or not dopaminergic stimulation might induce sex differences in 3H-E2 binding, male and female gonadectomized-adrenalectomized rats were pretreated either with bromocriptine, a dopamine agonist, or with diethyldithiocarbamate (DDC), an inhibitor of dopamine β-hydroxylase. DDC was used in order to increase endogenous release of dopamine. After such acute dopaminergic treatment, specific binding of 3H-E2 in nuclear and extranuclear fractions of 6 brain areas and pituitary in vivo was determined 1 h after intravenous injection of Η-E2 (1 µg/kg body weight). Administration of either bromocriptine or DDC increased specific 3H-E2 binding to nuclear and extranuclear fractions of basal hypothalamus and anterior pituitary from female but not from male rats, thus inducing sex differences in binding in these two tissues. Bromocriptine also increased specific binding in the pineal in females. Total binding was increased in a crude membrane fraction (P2) from pituitary of female but not of male rats after administration of DDC, but the percent of extranuclear specific binding found in the P2 fraction was decreased after DDC in both males and females. The findings suggest that dopaminergic stimulation may induce sex differences in 3H-E2 binding by increasing binding in some brain areas and anterior pituitary in females but not in mal