We investigated whether the LLC-PK1 epithelial cell line (which shows many characteristics of proximal tubular cells) also is capable of transporting an organic ion. Suspended LLC-PK1 cells accumulated tetraethylammonium (TEA). The uptake showed characteristics of a facilitated mechanism; TEA uptake was saturable and temperature-dependent and was inhibited by other organic cations. Quinine and mepiperphenidol were the most potent inhibitors, whereas N1-methylnicotinamide and morphine inhibited the transport system only slightly at doses of 10(-3) M. Basolateral-to-apical TEA flux through LLC-PK1 monolayers was five to six times larger than that of mannitol, a nontransported compound, whereas apical-to-basolateral TEA and mannitol fluxes were equal. Only the basolateral-to-apical TEA flux was inhibited by quinine. Under similar experimental conditions, no transport of p-aminohippuric acid was observed. It is concluded that LLC-PK1 cells are able to transport TEA, as do cells of the proximal tubule.