Premium
THE KINETICS OF UPTAKE OF 5‐FLUOROURACIL BY RAT LIVER
Author(s) -
HSU LORNA S.F.
Publication year - 1982
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1982.tb09313.x
Subject(s) - incubation , kinetics , fluorouracil , intracellular , extracellular , 2,4 dinitrophenol , chemistry , dinitrophenol , metabolism , efflux , incubation period , biochemistry , medicine , chemotherapy , physics , quantum mechanics
1 Slices of rat liver weighing 15–30 mg were incubated at 37°C in 5‐fluorouracil (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 K t and V max equal to 15.39 mmol l −1 and 1.96 μmol 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.