Distribution volume (Vd$_{ss}$ ) of a model basic drug, tetraethylammonium bromide (TEA) at a steady-state decreased sinificantly in glycerol and uranium-renal failure rats. Assuming carrier-mediated transport of TEA into tissues, the theoretical $Vd_{ss}$ of TEA decreases in an exponential way as the plasmal concentration of TEA increases. The relationship between $Vd_{ss}$ and plasma concentration of TEA in the experimental renal failure (ERF)-rats was similar. Therefore, the decrease in $Vd_{ss}$ of TEA in the ERF-rats seemed to be due to the saturation of the carrier system that are responsible for the tissue distribution of TEA, by the elevated plasma concentration of TEA in the ERF-rats. ERF was induced to rats with glycerol, folate, salicylate, uranium and gentamicin, respectively..