The effect of methimazole on bile flow and composition was studied in male Wistar rats. Administration of methimazole as a single bolus (175-700 mumol/kg body wt) or infusion over three hours (1 mumol/100 g body wt/min) significantly increased bile flow and the biliary output of bile acids and inorganic electrolytes. Choleresis was a transient phenomenon and at the end of the experiments bile flow had returned to control values, although bile acid output was significantly lowered. When the amounts of bile acids arriving into the liver were increased by taurocholate infusion or decreased by cholestyramine pretreatment, a transitory enhancement was also found in bile flow and bile acid output, but the amounts of bile acid secreted and the choleretic effect induced were different according to the bile acid secretory rate found before methimazole administration. The bile acid content in the liver of taurocholate-infused rats was reduced during methimazole-induced choleresis. Our data indicate that the higher bile flow in methimazole-treated rats is related to an enhanced biliary secretion of bile acids probably due to a transitory stimulating effect on the transport into bile of the intrahepatocytary bile acid pool. The choleretic effect is not apparently shared by other thiocarbamide compounds.