Hypolipidemic properties of a diphenyl-methylen-ethylamine derivative withaffinity for beta(3)-adrenoceptors in a model of hypercholesterolemia

beta(3)-Adrenergic agonists have been proposed as potential new drugs for t he treatment of diabetes and/or obesity therapy, because of the hypoglycemi c and lipolytic effects found with some of these compounds. Moreover, their application in other therapeutic areas such as hypercholesterolemia and at herosclerosis has been suggested. This experimental trial was conducted to assess the effects of Trecadrine, a new molecule with affinity for beta(3)- adrenoceptors, on a model of hypercholesterolemia in rats, and also to expl ore a possible beneficial role of these agents in lipid disturbances therap y. The results indicated a marked reduction in serum triglyceride levels (- 40%; P < 0.01) and lipoprotein lipase activity in white fat (- 49%, P < 0. 001) of hypercholesterolemic rats treated with Trecadrine for 16 days as co mpared with hypercholesterolemic non-treated rats. Moreover, Trecadrine pro duced a significant increase in the oxygen consumption in brown adipose tis sue (+ 154%, P < 0.01). In relation to cholesterolemia, an improvement in t otal cholesterol (- 20%) and total/HDL-cholesterol ratio (- 25%) in serum w as noted in the animals receiving the pharmacological treatment. In conclus ion, the results of this trial support that Trecadrine administration may h ave a therapeutic potential in disorders associated with hypertriglyceridem ia such as obesity and some types of hyperlipidaemias. (C) 1999 Elsevier Sc ience S.A. All rights reserved.