PMID: 9178186May 1, 1997Paper

A structure-relationship study of the uptake of aliphatic polyamine compounds by rat intestinal brush-border membrane vesicles

The Journal of Pharmacy and Pharmacology
M KobayashiK Miyazaki

Abstract

The effects of lipophilicity, ion-diffusion potential and membrane surface potential on the uptake of various aliphatic polyamine compounds by rat intestinal brush-border membrane vesicles (BBMV) have been investigated. A valinomycin-induced potassium-diffusion potential (inside-negative) stimulated the initial uptake of diamine compounds, and good correlation was observed between lipophilicity and the amount of diffusion-potential-dependent transport of the diamines. In contrast, because of their much lower lipophilicity, tri- and tetraamine compounds were not affected by the diffusion potential. Tetracaine, which can make the membrane surface potential more positive, inhibited the transport rate of 1,9-nonanediamine, spermidine and spermine by the BBMV. These data suggest that the transport mechanism of diamines is similar to that of monoamine compounds in respect to its dependence on ion-diffusion potential and on the membrane surface potential. The extent of the effect of ion-diffusion potential on the rate of transport of the diamines was closely related to the lipophilicity of the diamine. In contrast, only the surface potential contributed to the transport mechanism of lower lipophilic tri- and tetraamine compounds.

References

Sep 1, 1992·The Journal of Pharmacy and Pharmacology·K IsekiK Miyazaki
Mar 23, 1992·Biochimica Et Biophysica Acta·M KobayashiK Miyazaki
Sep 10, 1991·Biochimica Et Biophysica Acta·K IsekiK Miyazaki
May 15, 1989·The Biochemical Journal·F Schuber
Nov 15, 1986·Biochemical Pharmacology·M W Yung, C Green
Jan 1, 1984·Annual Review of Biochemistry·C W Tabor, H Tabor
May 1, 1996·The Journal of Pharmacy and Pharmacology·R TanabeK Miyazaki

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Citations

Sep 19, 2002·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Michiya Kobayashi

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