IN-VITRO INFLUENCE OF BENFLUOREX AND ITS MAIN METABOLITES ON RAT-LIVER MICROSOMAL MEMBRANE-PROPERTIES

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.