Paraquat and diquat, bipyridilium herbicides, have been shown to be accumulated into pneumocytes of three species in culture. Paraquat at 10(-3) M was accumulated to a maximum of 3-7 nmol/mg protein for 20 min. Diquat accumulated more slowly but reached a concentration of 1-6 nmol/mg protein for 60 min. Differences in the ability of various pneumocytes to accumulate paraquat and diquat appear to exist. It was found that the cations, Ca++, Na+ and K+, reduced the accumulation of paraquat. Valinomycin stimulated paraquat accumulation significantly. On the other hand, paraquat accumulation was inhibited by 2, 4-dinitrophenol. These results indicate that paraquat may be accumulated, in part, as cation species into pneumocytes and also by a energy-dependent process regulated by cellular ATP.