The effect of crude extract of roots of Bredemeyera floribunda Willd., Polygalaceae used by Brazilian popular medicine as a potent diuretic, on renal function in antidiuresis or water diuresis in rats, was studied. During intravenous infusion of the extract (0.05 mg/min/100 g), mean arterial pressure did not change significantly but urine flow, glomerular filtration rate, fractional water and sodium excretion and solute clearance increased significantly, in both groups of animals. In antidiuresis rats the extract significantly increased reabsorption of water by the collecting duct and in water diuresis animals the extract significantly increased free water clearance. Our findings indicate a direct effect of extract on glomerular filtration rate, possibly by detergent like interactions with structural components of glomerular membranes and/or by decreasing renal perfusion pressure. The study on the concentrating and diluting mechanisms suggests preferential action of extract in the proximal tubular cells, possibly on the (Na(+)-K+)-ATPase countertransport system and/or on other proteins components of tubular cell membranes involved with salt transport mechanisms.