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Müller, G. ; Wied, S.* ; Herling, A.W.*

Analysis of direct effects of the CB1 receptor antagonist rimonabant on fatty acid oxidation and glycogenolysis in liver and muscle cells in vitro.

Biochemistry 84, 954-962 (2019)
DOI PMC
Open Access Green as soon as Postprint is submitted to ZB.
Recent pharmacological findings regarding rimonabant, an anorectic and cannabinoid type 1 receptor (CB1R) antagonist, strongly suggest that some of its effects on the metabolic parameters and energy balance in rats are not related to the centrally mediated reduction in caloric intake. Instead, they may be associated with acute induction of glycogenolysis in the liver, in combination with transient increase in glucose oxidation and persistent increase in fat oxidation. It is possible that rimonabant produced direct short- or long-term stimulatory effect on these processes in primary and cultured rat cells. Rimonabant slightly stimulated β-oxidation of long-chain fatty acids in cultured rat myocytes overexpressing glucose transporter isoform 4, as well as activated phosphorylation of adenosine monophosphate-dependent protein kinase (AMPK) in primary rat hepatocytes upon long-term incubation. However, short-term action of rimonabant failed to stimulate β-oxidation in myocytes, myotubes, and hepatocytes, as well as to upregulate AMPK phosphorylation, glycogenolysis, and cAMP levels in hepatocytes. As a consequence, the acute effects of rimonabant on hepatic glycogen content (reduction) and total energy expenditure (increase) in rats fed with a standard diet cannot be explained by direct stimulation of glycogenolysis and fatty acid oxidation in muscles and liver. Rather, these effects seem to be centrally mediated.
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Publication type Article: Journal article
Document type Scientific Article
Corresponding Author
Keywords Amp ; And Camp-dependent Signaling ; Cannabinoid Receptor 1 ; Glucose And Lipid Metabolism ; Obesity; Diet-induced Obesity; Lipid Droplets; Food-intake; Endocannabinoids; Cannabinoids; Mechanisms; Sr141716a; Potent; Rats; Mice
ISSN (print) / ISBN 0006-2960
e-ISSN 1520-4995
Journal Biochemistry
Quellenangaben Volume: 84, Issue: 8, Pages: 954-962 Article Number: , Supplement: ,
Publisher American Chemical Society (ACS)
Publishing Place 233 Spring St, New York, Ny 10013-1578 Usa
Non-patent literature Publications
Reviewing status Peer reviewed
Institute(s) Institute of Diabetes and Obesity (IDO)