Cannabimimetic Activity, Binding, and Degradation of Stearoylethanolamide within the Mouse Central Nervous System

Maccarrone, Mauro; Cartoni, Antonella; Parolaro, Daniela; Margonelli, Andrea; Massi, Paola; Bari, Monica; Battista, Natalia; Finazzi‐Agrò, Alessandro

doi:10.1006/mcne.2002.1164

Cited by 66 publications

(46 citation statements)

References 38 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Recent work has shown that PEA reduces inflammation in a PPAR-a-dependent manner [68]. Is this true also for other FAEs such as stearoylethanolamide, or do these molecules interact with additional members of the nuclear transcription factor family [69,70]? As these questions are progressively unraveled, we may not only gain insight on the OEA signaling system, but also identify new potential drug targets for the treatment of appetite disorders and obesity.…”

Section: Discussionmentioning

confidence: 99%

Regulation of food intake by oleoylethanolamide

Verme

Gaetani

et al. 2005

CMLS, Cell. Mol. Life Sci.

157

130

View full text Add to dashboard Cite

Abstract. Oleoylethanolamide (OEA), the naturally occurring amide of ethanolamine and oleic acid, is an endogenous lipid that modulates feeding, body weight and lipid metabolism by binding with high affinity to the ligand-activated transcription factor, peroxisome proliferator-activated receptor-alpha (PPAR-a). In the CMLS, Cell. Mol. Life Sci. 62 (2005) 708 -716 1420-682X/05/060708-09 DOI 10.1007/s00018-004-4494-0 © Birkhäuser Verlag, Basel, 2005 CMLS Cellular and Molecular Life Sciencespresent article, we describe the biochemical pathways responsible for the initiation and termination of OEA signaling, and outline the pharmacological properties of this compound in relation to its ability to activate PPARa. Finally, we discuss the possible role of OEA as a peripheral satiety hormone.

show abstract

Section: Discussionmentioning

confidence: 99%

Regulation of food intake by oleoylethanolamide

Verme

Gaetani

et al. 2005

CMLS, Cell. Mol. Life Sci.

157

130

View full text Add to dashboard Cite

show abstract

“…Reduced locomotor activity, ataxia, and catalepsy are indeed commonly observed after administration of cannabinoid agonists (35). Interestingly, stearoylethanolamide is another member of the fatty acid ethanolamide family that does not activate cannabinoid receptors but that causes cannabimimetic effects, including catalepsy (21).…”

Section: Discussionmentioning

confidence: 99%

Mechanisms of oleoylethanolamide-induced changes in feeding behavior and motor activity

Proulx

Cota²,

Castañeda³

et al. 2005

American Journal of Physiology-Regulatory, Integrative and Comp

View full text Add to dashboard Cite

, a lipid synthesized in the intestine, reduces food intake and stimulates lipolysis through peroxisome proliferator-activated receptor-␣. OEA also activates transient receptor potential vanilloid type 1 (TRPV1) in vitro. Because the anorexigenic effect of OEA is associated with delayed feeding onset and reduced locomotion, we examined whether intraperitoneal administration of OEA results in nonspecific behavioral effects that contribute to the anorexia in rats. Moreover, we determined whether circulating levels of other gut hormones are modulated by OEA and whether CCK is involved in OEA-induced anorexia. Our results indicate that OEA reduces food intake without causing a conditioned taste aversion or reducing sodium appetite. It also failed to induce a conditioned place aversion. However, OEA induced changes in posture and reduced spontaneous activity in the open field. This likely underlies the reduced heat expenditure and sodium consumption observed after OEA injection, which disappeared within 1 h. The effects of OEA on motor activity were similar to those of the TRPV1 agonist capsaicin and were also observed with the peroxisome proliferator-activated receptor-␣ agonist Wy-14643. Plasma levels of ghrelin, peptide YY, glucagon-like peptide 1, and apolipoprotein A-IV were not changed by OEA. Finally, antagonism of CCK-1 receptors did not affect OEA-induced anorexia. These results suggest that OEA suppresses feeding without causing visceral illness and that neither ghrelin, peptide YY, glucagon-like peptide 1, apolipoprotein A-IV, nor CCK plays a critical role in this effect. Despite that OEA-induced anorexia is unlikely to be due to impaired motor activity, our data raise a cautionary note in how specific behavioral and metabolic effects of OEA should be interpreted.peroxisome proliferator-activated receptor-␣; transient receptor potential vanilloid type 1; cholecystokinin; satiety; obesity ENERGY HOMEOSTASIS IN MAMMALS is tightly regulated by complex neuroendocrine systems matching caloric intake to energy expenditure. In addition to hormones, fatty acids (18, 28) and fatty acid derivatives (6a, 11, 37) also signal to central nervous system pathways that control body weight regulation. Recent evidence suggests that oleoylethanolamide (OEA), the amide of oleic acid and ethanolamine, could play a significant role in the regulation of energy balance (34). This lipid is synthesized in astrocytes (39) and neurons (6, 10), as well as in cells of the small intestine, where its levels are reduced by fasting and increased on refeeding (34).

show abstract

“…OEA is also associated with both analgesic properties which has been suggested to occur independently of PPAR-α activation [9], and induction of visceral pain via TRPV 1 activation [10]. SEA has a cannabimimetic activity partly similar to AEA [11]. The in energy homeostasis role of the endocannabinoid system in adipose tissue, liver and skeletal muscle has been reviewed [12].…”

Section: Introductionmentioning

confidence: 99%

Identification of Lipid Mediators in Peripheral Human Tissues Using an Integrative In Vivo Microdialysis Approach

2016

J Anal Bioanal Tech

View full text Add to dashboard Cite

Endocannabinoids and related N-acylethanolamines (NAEs) are lipid mediators involved in a number of physiological and pathological mechanisms in peripheral tissues. Microdialysis (MD) technique allows continues sampling of endogenous substances in the interstitial fluids of the tissues. The main limitation of MD sampling of lipophilic compounds is low recovery due to adsorption to the MD system and particularly to the catheter membranes. In this in vivo study microdialysate samples were collected from human trapezius muscle and forearm skin. The levels of arachidonoylethanolamide (AEA), 2-arachidonoylglycerol (2-AG), oleoylethanolamide (OEA), palmitoylethanolamide (PEA), and stearoylethanolamide (SEA) were analyzed in both microdialysate and in catheter membrane samples using liquid chromatography tandem mass spectrometry. OEA, PEA and SEA were identified in all microdialysate and catheter membrane samples from trapezius and skin. 2-AG was found in all catheter membrane samples from both tissues but not in the actual microdialysate. In conclusion sampling of OEA, PEA and SEA was achievable from trapezius and skin with the presented MD set-up. 2-AG is present in both trapezius muscle and skin tissue but adsorbs to the membranes in a higher extent than the NAEs. Furthermore, consideration of data conserved in the membrane during an MD experiment could be a relevant and more broadly applicable extension of MD sampling methodology which could fill an "information gap" and enhance an adequate interpretation of microdialysate data outcomes

show abstract

Cannabimimetic Activity, Binding, and Degradation of Stearoylethanolamide within the Mouse Central Nervous System

Cited by 66 publications

References 38 publications

Regulation of food intake by oleoylethanolamide

Regulation of food intake by oleoylethanolamide

Mechanisms of oleoylethanolamide-induced changes in feeding behavior and motor activity

Identification of Lipid Mediators in Peripheral Human Tissues Using an Integrative In Vivo Microdialysis Approach

Contact Info

Product

Resources

About