Hypolipidemic properties of a diphenyl-methylen-ethylamine derivative with affinity for beta 3-adrenoceptors in a model of hypercholesterolemia.
beta 3-Adrenergic agonists have been proposed as potential new drugs for the treatment of diabetes and/or obesity therapy, because of the hypoglycemic and lipolytic effects found with some of these compounds. Moreover, their application in other therapeutic areas such as hypercholesterolemia and atherosclerosis 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 explore a possible beneficial role of these agents in lipid disturbances therapy. 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 compared with hypercholesterolemic non-treated rats. Moreover, Trecadrine produced a significant increase in the oxygen consumption in brown adipose tissue (+154%, P < 0.01). In relation to cholesterolemia, an improvement in total cholesterol (-20%) and total/HDL-cholesterol ratio (-25%) in serum was noted in the animals receiving the pharmacological treatment. In conclusion, the results of this trial support that Trecadrine administration may have a therapeutic potential in disorders associated with hypertriglyceridemia such as obesity and some types of hyperlipidaemias.
Zulet
M A
MA
Department of Physiology and Nutrition, University of Navarra, Pamplona, Spain.
Berraondo
B
B
Milagro
F I
FI
Martínez
J A
JA
D000318:Adrenergic beta-Agonists / Q000627:therapeutic use*; D000818:Animals; D001592:Benzyl Alcohols / Q000627:therapeutic use*; D006937:Hypercholesterolemia / Q000188:drug therapy*; D000960:Hypolipidemic Agents / Q000627:therapeutic use*; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D011943:Receptors, Adrenergic, beta / Q000187:drug effects*; D022702:Receptors, Adrenergic, beta-3
D000318:Adrenergic beta-Agonists; D001592:Benzyl Alcohols; D000960:Hypolipidemic Agents; D011943:Receptors, Adrenergic, beta; D022702:Receptors, Adrenergic, beta-3; C101319:trecadrine