R. Tanabe et al., UPTAKE MECHANISM OF TRIENTINE BY RAT INTESTINAL BRUSH-BORDER MEMBRANE-VESICLES, Journal of Pharmacy and Pharmacology, 48(5), 1996, pp. 517-521
The uptake characteristics of trientine by rat intestinal brush-border
membrane vesicles were studied. The uptake characteristics of trienti
ne were similar to those of the physiological polyamines with respect
to the excessive accumulation in vesicles, the pH dependency, the temp
erature dependency and the ineffectiveness of K+ diffusion potential (
inside negative). The initial uptake of trientine was saturable with a
K-m value of 1.13 mM, which was larger than that of spermine and sper
midine. Furthermore, the uptake rate of trientine was dose-dependently
inhibited by spermine and spermidine. Spermine competitively inhibite
d the uptake of trientine with a K-i value of 18.6 mu M, and it was cl
ose to the K-m value for spermine (30.4 mu M). These data suggested th
at the uptake of trientine was similar to that of spermine and spermid
ine in rat small intestinal brush-border membrane vesicles, and these
polyamines seem to inhibit the absorption of trientine from the gastro
intestinal tract.