The kinetics of uptake of 5-fluorouracil by rat liver.
1 Slices of rat liver weighing 15-30 mg were incubated at 37 degrees C in 5-fluorourecil (5-FU) solution. 2 The 5-FU taken up was measured by high pressure liquid chromatography. 3 Uptake of 5-FU was found to approximate to Michaelis-Menton kinetics with the values of Kt and Vmax equal to 15.39 mmol 1-1 and 1.96 mumol g-1 min-1 respectively. 4 Transport of 5-FU was saturable with the uptake being much greater in the non-fasting rats. 5 Intracellular concentration of 5-FU after 24 min incubation approached but did not significantly exceed that in the extracellular fluid. 6 Enzymatic destruction of 5-FU at 2 min was negligible but substantial after a long incubation period. 7 2,4-Dinitrophenol was found to inhibit transport of 5-FU significantly. 8 Results suggested that the mechanism of uptake of 5-FU by rat liver is an energy requiring process.
D019297:2,4-Dinitrophenol; D000818:Animals; D004140:Dinitrophenols / Q000494:pharmacology; D005472:Fluorouracil / Q000378:metabolism*; D066298:In Vitro Techniques; D007700:Kinetics; D008099:Liver / Q000378:metabolism*; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains
D004140:Dinitrophenols; D019297:2,4-Dinitrophenol; D005472:Fluorouracil