Pyrrolidin-2-one derivatives may reduce body weight in rats with diet-induced obesity

Obesity affects an increasing number of individuals in the human population and significant importance is attached to research leading to the discovery of drug which would effectively reduce weight. The search for new drugs with anorectic activity and acting within the adrenergic system has attracte...

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Published in:European journal of pharmacology 2016-04, Vol.776, p.146-155
Main Authors: Dudek, Magdalena, Knutelska, Joanna, Bednarski, Marek, Nowiński, Leszek, Zygmunt, Małgorzata, Kazek, Grzegorz, Mordyl, Barbara, Głuch-Lutwin, Monika, Zaręba, Paula, Kulig, Katarzyna, Sapa, Jacek
Format: Article
Language:English
Subjects:
Adipose Tissue - drug effects
Adipose Tissue - pathology
Animals
Anti-obesity action
Blood Glucose - metabolism
Blood Pressure - drug effects
Body Temperature - drug effects
Body Weight - drug effects
Diet - adverse effects
Diet-induced obese rats
Glycerol - metabolism
Heart Rate - drug effects
Hydrocortisone - metabolism
Lipolysis - drug effects
Locomotion - drug effects
Male
Obesity
Obesity - blood
Obesity - chemically induced
Obesity - drug therapy
Obesity - physiopathology
Pyrrolidin-2-one derivatives
Pyrrolidinones - chemistry
Pyrrolidinones - pharmacology
Pyrrolidinones - therapeutic use
Rats
Rats, Wistar
Thermogenesis - drug effects
α2-Adrenoceptor antagonist
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Summary:Obesity affects an increasing number of individuals in the human population and significant importance is attached to research leading to the discovery of drug which would effectively reduce weight. The search for new drugs with anorectic activity and acting within the adrenergic system has attracted the interest of researchers. This study concerns the experimental effects on body weight of α2-adrenoceptor antagonists from the group of pyrrolidin-2-one derivatives in rats with diet-induced obesity. Methods: The intrinsic activity of the test compounds at the α-adrenoreceptors was tested. Obesity in rats was obtained by the use of fatty diet and then the influence of the test compounds on body weight, food and water intakes, lipid and glucose profiles and glycerol and cortisol levels were determinated. The effects of the compounds on locomotor activity, body temperature, blood pressure and heart rate were tested. Results: One of the test compounds (1-(3-(4-phenylpiperazin-1-yl)propyl)pyrrolidin-2-one) reduces the animal's body weight and the amount of peritoneal adipose tissue during chronic administration, at the same time it does not cause significant adverse effects on the cardiovascular system. This compound decreases temperature and elevates glycerol levels and does not change the locomotor activity and cortisol level at anti-obese dose. Conclusions: Some derivatives of pyrrolidin-2-one that act as antagonists of the α2-adrenoreceptor may reduce body weight. Reducing body weight for 1-(3-(4-phenylpiperazin-1-yl)propyl)pyrrolidin-2-one can be associated with decrease in food intake, body fat reduction, reduction of blood glucose, and increased thermogenesis and lipolysis. This effect cannot be the result of changes in spontaneous activity or stress.
ISSN:0014-2999
1879-0712
DOI:10.1016/j.ejphar.2016.02.047