Summary
The accumulation ofD-galactose by rings of hamster small intestine shows a Michaelis-Menten kinetics with an apparent Km of 5.5 mM and a maximum rate of net penetration of 0.35 micromoles/100 mg tissue w.w./min. Dicoumarol when present in the medium at concentrations 10−5 to 10−4 M, markedly inhibits (40–72%) galactose accumulation, behaving as a noncompetitive inhibitor with an apparent Ki of 5.5×10−5 M. The drug also inhibits the oxygen uptake by the tissue in the absence of added substrate.
Inhibition of galactose active transport by dicoumarol was also observed if the incubation was carried out after a preincubation with the drug. This effect could not be eliminated by repeated washings of the rings after preincubation.
The effects of dicoumarol are explained as due to binding to cellular constituents and to inhibition of cell metabolism. Aesculine up to 10−4 M concentration does not affect galactose accumulation.
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Bolufer, J., Larralde, J. & Ponz, F. The effect of dicoumarol and aesculine on the accumulation ofD-galactose by the intestinal rings of hamsters. Pflugers Arch. 338, 159–167 (1973). https://doi.org/10.1007/BF00592750
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DOI: https://doi.org/10.1007/BF00592750