Stimulation of choline/Mg2+ antiport in rat erythrocytes by mefloquine.
In non Mg(2+)-loaded and non malaria-infected rat erythrocytes, mefloquine (100 micromol x l (-1)) stimulated choline/Mg2+ antiport without affecting the Na+/Mg2+ antiport. The stimulation of the choline/Mg2+ 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 CF3 groups attached to the quinoline or benzene ring. The effect of mefloquine on choline/Mg2+ antiport in vitro was not related to the antimalarial action of mefloquine in vivo. In rat erythrocytes, the choline/Mg2+ antiport can be differentiated from the Na+/Mg2+ antiport through the use of cinchonine that inhibited the choline/Mg2+ antiport [Ebel et al. Biochim Biophys Acta 2002; 1559: 135-44], and mefloquine that stimulated the choline/Mg2+ antiport, whereby the Na+/Mg2+ antiport was not affected by either drug at proper concentrations. The Na+/Mg2+ antiport and choline/Mg2+ antiports behave as different molecular entities.
Ebel
H
H
Charité-Universitätsmedizin Berlin, Campus Benjamin Franklin, Institut für Klinische Physiologie, Berlin, Germany. hans.ebel@charite.de
Günther
T
T
D000818:Animals; D000962:Antimalarials / Q000494:pharmacology*; D017920:Antiporters / Q000378:metabolism; D002794:Choline / Q000378:metabolism*; D004912:Erythrocytes / Q000187:drug effects / Q000378:metabolism; D017136:Ion Transport / Q000187:drug effects* / Q000502:physiology; D008274:Magnesium / Q000378:metabolism*; D008297:Male; D015767:Mefloquine / Q000494:pharmacology*; D015394:Molecular Structure; D051381:Rats; D017207:Rats, Sprague-Dawley
D000962:Antimalarials; D017920:Antiporters; D008274:Magnesium; D002794:Choline; D015767:Mefloquine