This study examined the extent of mammary excretion and placental transfer of bisphenol A in rats. Bisphenol A was given by simultaneous i.v. bolus injection plus infusion to steady-state at low, medium and high doses. The steady-state serum levels of bisphenol A were linearly increased with increasing the dosing rate. The systemic clearance (mean range, 119.2-154.1 ml/min/kg) remained unaltered over the dosing rate studied. The levels of bisphenol A in milk exceeded those in serum, with the steady-state milk to serum concentration ratio being 2.4-2.7. The steady-state milk levels of bisphenol A were also increased linearly with increasing the infusion rate. In a separate study, the kinetic disposition of bisphenol A in the rat maternal-fetal unit was studied in pregnant rats. After i.v. injection, bisphenol A concentration in the maternal serum declined biexponentially. Bisphenol A was rapidly distributed into placenta, fetus and amniotic fluid, with maximum concentrations in these tissues achieved within 1 hr of injection. The decline of bisphenol A in placenta, fetus and amniotic fluid paralleled that of maternal serum. A simultaneous computer simulation showed that the observed concentrations were well represented by a 5-compartmental model consisting of the maternal central, placenta, fetus, amniotic fluid, and maternal tissue compartments.