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Stimulation of choline/Mg 2+ antiport in rat erythrocytes by mefloquine Volume 19, numéro 1, March 2006

Auteurs
Charité-Universitätsmedizin Berlin, Campus Benjamin Franklin, Institut für Klinische Physiologie, Berlin, Germany, Charité-Universitätsmedizin Berlin, Campus Benjamin Franklin, Institut für Molekularbiologie und Biochemie, Berlin, Germany
  • Mots-clés : NPP, new permeation pathway, TCA, trichloroacetic acid
  • Page(s) : 7-11
  • Année de parution : 2006

In non Mg 2+-loaded and non malaria-infected rat erythrocytes, mefloquine (100 μmol·l -1) stimulated choline/Mg 2+ antiport without affecting the Na +/Mg 2+ antiport. The stimulation of the choline/Mg 2+ antiport by mefloquine, found in this study, and by trifluoperazine and fluvoxamine, reported previously [Ebel et al. Biochim Biophys Acta 2004; 1167: 132-40], was associated with CF 3 groups attached to the quinoline or benzene ring. The effect of mefloquine on choline/Mg 2+ antiport in vitro was not related to the antimalarial action of mefloquine in vivo. In rat erythrocytes, the choline/Mg 2+ antiport can be differentiated from the Na +/Mg 2+ antiport through the use of cinchonine that inhibited the choline/Mg 2+ antiport [Ebel et al. Biochim Biophys Acta 2002; 1559: 135-44], and mefloquine that stimulated the choline/Mg 2+ antiport, whereby the Na +/Mg 2+ antiport was not affected by either drug at proper concentrations. The Na +/Mg 2+ antiport and choline/Mg 2+ antiports behave as different molecular entities.