Next Article in Journal
Acute MDPV Binge Paradigm on Mice Emotional Behavior and Glial Signature
Next Article in Special Issue
Etanercept Ameliorates Cardiac Fibrosis in Rats with Diet-Induced Obesity
Previous Article in Journal
Plant Phenolics and Extracts in Animal Models of Preeclampsia and Clinical Trials—Review of Perspectives for Novel Therapies
Article

Effects of GPR18 Ligands on Body Weight and Metabolic Parameters in a Female Rat Model of Excessive Eating

1
Department of Pharmacological Screening, Faculty of Pharmacy, Jagiellonian University, Medical College, 9 Medyczna Street, 30-688 Kraków, Poland
2
Department of Pharmacokinetics and Physical Pharmacy, Jagiellonian University Medical College, 9 Medyczna Street, 30-688, Krakow, Poland
3
Pharmaceutical & Medicinal Chemistry, Pharmaceutical Institute, PharmaCenter Bonn, University of Bonn, An der Immenburg 4, D-53121 Bonn, Germany
4
Department of Technology and Biotechnology of Drugs, Faculty of Pharmacy, Jagiellonian University, Medical College, 9 Medyczna Street, 30-688 Kraków, Poland
*
Author to whom correspondence should be addressed.
Academic Editor: Félix Carvalho
Pharmaceuticals 2021, 14(3), 270; https://doi.org/10.3390/ph14030270
Received: 2 February 2021 / Revised: 11 March 2021 / Accepted: 13 March 2021 / Published: 16 March 2021
(This article belongs to the Special Issue Searching for New Therapeutic Targets with Anti-obesity Potential)
GPR18 has been proposed to play a role in the progression of metabolic disease and obesity. Therefore, the aim of this study was to determine the effects of selective GRP18 ligands (the antagonists PSB-CB5 and PSB-CB27 and the agonist PSB-KK1415) on body mass and the development of metabolic disorders commonly accompanying obesity. Experiments were carried out on female Wistar rats. In order to determine the anorectic activity of the investigated ligands, their effect on food and water intake in a model of excessive eating was assessed. Lipid profile, glucose and insulin levels as well as alanine aminotransferase, aspartate aminotransferase, and γ-glutamyl transpeptidase activity in plasma were also evaluated. Potential side effects were examined in rat models of pica behavior and conditioned taste aversion. Animals treated with different ligands gained significantly less weight than rats from the obese control group. Effects of GPR18 antagonists on food intake and body weight were specific and unrelated to visceral illness, stress or changes in spontaneous activity. However, the GPR18 agonist is likely to affect body weight by inducing gastrointestinal disorders such as nausea. The presented preliminary data support the idea that the search for selective GPR18 antagonists for the treatment of obesity might be promising. View Full-Text
Keywords: GPR18 ligands; anorectic activity; palatable diet; excessive eating model; PSB-CB5 GPR18 ligands; anorectic activity; palatable diet; excessive eating model; PSB-CB5
Show Figures

Figure 1

MDPI and ACS Style

Kotańska, M.; Mika, K.; Szafarz, M.; Kubacka, M.; Müller, C.E.; Sapa, J.; Kieć-Kononowicz, K. Effects of GPR18 Ligands on Body Weight and Metabolic Parameters in a Female Rat Model of Excessive Eating. Pharmaceuticals 2021, 14, 270. https://doi.org/10.3390/ph14030270

AMA Style

Kotańska M, Mika K, Szafarz M, Kubacka M, Müller CE, Sapa J, Kieć-Kononowicz K. Effects of GPR18 Ligands on Body Weight and Metabolic Parameters in a Female Rat Model of Excessive Eating. Pharmaceuticals. 2021; 14(3):270. https://doi.org/10.3390/ph14030270

Chicago/Turabian Style

Kotańska, Magdalena, Kamil Mika, Małgorzata Szafarz, Monika Kubacka, Christa E. Müller, Jacek Sapa, and Katarzyna Kieć-Kononowicz. 2021. "Effects of GPR18 Ligands on Body Weight and Metabolic Parameters in a Female Rat Model of Excessive Eating" Pharmaceuticals 14, no. 3: 270. https://doi.org/10.3390/ph14030270

Find Other Styles
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop