UPTAKE MECHANISM OF TRIENTINE BY RAT INTESTINAL BRUSH-BORDER MEMBRANE-VESICLES

Citation
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
Citations number
12
Categorie Soggetti
Pharmacology & Pharmacy
ISSN journal
00223573
Volume
48
Issue
5
Year of publication
1996
Pages
517 - 521
Database
ISI
SICI code
0022-3573(1996)48:5<517:UMOTBR>2.0.ZU;2-W
Abstract
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.