The cannabinoid CB1 receptor antagonist SR141716A (Rimonabant) enhances the metabolic benefits of long-term treatment with oleoylethanolamide in Zucker rats

Serrano, Antonia; Arco, Ignacio del; Pavón, Francisco Javier; Macías, Manuel; Pérez-Valero, Vidal; Fonseca, Fernando Rodrı́guez de

doi:10.1016/j.neuropharm.2007.03.007

Cited by 74 publications

(71 citation statements)

References 32 publications

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“…In obese Zucker rats, a subchronic treatment with both drugs improves the separate effects of rimonabant and OEA, resulting in a marked decrease on feeding, body weight gain and serum lipid levels [133]. Additionally, this combinational therapy reduces the hepatic steatosis observed in obese rats, decreasing liver fat depots and improving liver function [133]. A similar effect has been observed with the combination of LH-21 and OEA [102].…”

Section: Efficacy Of Combined Therapy For Obesitymentioning

confidence: 77%

“…In this regard, previous studies have described a synergistic effect of both compounds to decrease appetite. A low, non-effective dose of rimonabant potentiates the inhibitory actions of OEA on feeding in fooddeprived rats [57,133]. In obese Zucker rats, a subchronic treatment with both drugs improves the separate effects of rimonabant and OEA, resulting in a marked decrease on feeding, body weight gain and serum lipid levels [133].…”

Section: Efficacy Of Combined Therapy For Obesitymentioning

confidence: 99%

“…A low, non-effective dose of rimonabant potentiates the inhibitory actions of OEA on feeding in fooddeprived rats [57,133]. In obese Zucker rats, a subchronic treatment with both drugs improves the separate effects of rimonabant and OEA, resulting in a marked decrease on feeding, body weight gain and serum lipid levels [133]. Additionally, this combinational therapy reduces the hepatic steatosis observed in obese rats, decreasing liver fat depots and improving liver function [133].…”

Section: Efficacy Of Combined Therapy For Obesitymentioning

confidence: 99%

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Obesity and the Endocannabinoid System: Is There Still a Future for CB1 Antagonists in Obesity?

et al. 2012

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The current epidemic of obesity in western countries is being worsened by the lack of effective pharmacotherapies. The apparent success of a central nervous systemacting cannabinoid CB 1 receptor antagonist-based treatment for obesity was hampered by the appearance of psychiatric side effects in certain patients. These adverse effects forced its withdrawal from the market. However, the discovery that the main beneficial metabolic effects of cannabinoid CB 1 receptor antagonists were derived of its activity in peripheral tissues, including the adipose tissue, opened the possibility of rescuing this type of therapy. This goal might be achieved by differential medicinal chemistry approaches. The present review examines these options that include peripheral-restricted cannabinoid CB 1 receptor antagonists, dual ligands and combinatorial therapies using sub-effective doses of CB 1 receptor antagonists that might be devoid of side effects.

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Section: Efficacy Of Combined Therapy For Obesitymentioning

confidence: 77%

Section: Efficacy Of Combined Therapy For Obesitymentioning

confidence: 99%

Section: Efficacy Of Combined Therapy For Obesitymentioning

confidence: 99%

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Obesity and the Endocannabinoid System: Is There Still a Future for CB1 Antagonists in Obesity?

et al. 2012

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“…For this reason some have suggested the possibility of an association between therapeutic inhibitor of the cannabinoid receptor CB1 produced by adipocytes (rimonobant) and OEA anorectic action for the treatment of severe obesity and dislipemia [107,113,114]. According to others, an enhancement in the production of OAE or its inhibition may represent degradation of the therapy to the treatment of diseases linked to excessive food intake.…”

Section: Sense Of Satietymentioning

confidence: 99%

Virgin olive oil in preventive medicine: From legend to epigenetics

Caramia¹,

Gori

Valli

et al. 2012

Euro J Lipid Sci & Tech

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Among vegetable oils, extra virgin olive oil (EVOO) has nutritional and sensory characteristics that make it unique and a basic component of the Mediterranean diet. EVOO has always been used over the centuries for its preventive and therapeutic properties, as well as precious and valuable dietary lipidic condiment. Benefic effects of a diet rich in EVOO on the human health, especially in prevention and/or reduction of hypercholesterolaemia, serum lipoprotein levels and atherosclerosis, hypertension, cardiovascular diseases and thrombotic risk, oxidation and oxidative stress, obesity and type 2 diabetes, inflammatory processes and cancer are discussed in these review. Recent studies suggest also its role in regulating the sense of satiety. The chemical compounds of EVOO that may contribute to its overall therapeutic characteristics, the epigenetic and physiological mechanisms involved are focused, taking into account the most important studies in the literature of the last years.Practical applications: Many studies on various aspects of nutrition indicated that many human diseases are influenced by lifestyle, in which the diet has an important aspect. The use of extra virgin olive oil is especially important from early childhood and throughout adult life to contribute to hinder the aging process. The importance of preventive and sometimes curative action, carried out by its various components in several pathological conditions has emerged from clinical, experimental, and epidemiological studies which, in many cases, are accompanied by indisputable scientific evidences. Taking into account the most important studies in the literature of the last years, the chemical compounds of extra virgin olive oil and the physiological mechanisms involved in their curative/health effects are the focus of this article.

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“…For example, the combination of OEA (PPARα agonist) with rimonabant (CB1 antagonist) resulted in more effective suppression of feeding and increased weight loss. 12 Another example can be found in the combination of AEA (CB1) and GW7647 (PPARα agonist) leading to synergistic effects on reducing pain behavior. 13 We have previously reported oleylethanolamide analogues as PPARα activators 14 and cannabinoid antagonist derivatives containing a 1,2,4-triazole motif.…”

mentioning

confidence: 99%

Discovery of Potent Dual PPARα Agonists/CB1 Ligands

Pérez-Fernández

Fresno

Macías-González

et al. 2011

ACS Med. Chem. Lett.

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This letter describes the synthesis and in vitro and in vivo evaluation of dual ligands targeting the cannabinoid and peroxisome proliferator-activated receptors (PPAR). These compounds were obtained from fusing the pharmacophores of fibrates and the diarylpyrazole rimonabant, a cannabinoid receptor antagonist. They are the first examples of dual compounds with nanomolar affinity for both PPARα and cannabinoid receptors. Besides, lead compound 2 proved to be CB1 selective. Unexpectedly, the phenol intermediates tested were equipotent (compound 1 as compared to 2) or even more potent (compound 3 as compared with 4). This discovery opens the way to design new dual ligands.

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The cannabinoid CB1 receptor antagonist SR141716A (Rimonabant) enhances the metabolic benefits of long-term treatment with oleoylethanolamide in Zucker rats

Cited by 74 publications

References 32 publications

Obesity and the Endocannabinoid System: Is There Still a Future for CB1 Antagonists in Obesity?

Obesity and the Endocannabinoid System: Is There Still a Future for CB1 Antagonists in Obesity?

Virgin olive oil in preventive medicine: From legend to epigenetics

Discovery of Potent Dual PPARα Agonists/CB1 Ligands

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