T. Orsiere et al., IN-VITRO INFLUENCE OF BENFLUOREX AND ITS MAIN METABOLITES ON RAT-LIVER MICROSOMAL MEMBRANE-PROPERTIES, Chemico-biological interactions, 97(3), 1995, pp. 297-306
Benfluorex and its three main metabolites at 30 mu M have been shown t
o inhibit Acyl CoA cholesterol acyl transferase activity in rat liver
microsome preparations and to fluidize these membranes, as reflected b
y a decrease in the lipid order parameter. When drug concentrations we
re higher (60-200 mu M), the compounds differed in their enzymatic inh
ibition properties but retained the same fluidizing effects. Only the
parent compound had a dose-dependent inhibiting effect. These results
are discussed with regard to the chemical properties of compounds, in
particular their electric charges and their lipophilic characters.