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Central versus peripheral antagonism of cannabinoid CB1 receptor in obesity: effects of LH-21, a peripherally acting neutral cannabinoid receptor antagonist, in Zucker rats.

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The endogenous cannabinoid system plays an important modulatory role in feeding behaviour and metabolism, acting at both central and peripheral levels. Chronic administration of cannabinoid CB(1) receptor antagonists has been found to be effective in experimental obesity. However, clinically

Lifetime marijuana use in relation to insulin resistance in lean, overweight, and obese US adults.

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Obese individuals are more likely to show insulin resistance (IR). However, limited population studies on marijuana use with markers of IR have yielded mixed results. The aim of this study was to examine the association of marijuana use with IR in US adults with different body mass

Cannabis use in relation to obesity and insulin resistance in the Inuit population.

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OBJECTIVE To ascertain the relationship between cannabis use, obesity, and insulin resistance. METHODS Data on 786 Inuit adults from the Nunavik Inuit Health Survey (2004) were analyzed. Information on cannabis use was obtained from a self-completed, confidential questionnaire. Fasting blood glucose

Benzodioxoles: novel cannabinoid-1 receptor inverse agonists for the treatment of obesity.

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The application of the evolutionary fragment-based de novo design tool TOPology Assigning System (TOPAS), starting from a known CB1R (CB-1 receptor) ligand, followed by further refinement principles, including pharmacophore compliance, chemical tractability, and drug likeness, allowed the

Cannabinoid 1 G protein-coupled receptor (periphero-)neutral antagonists: emerging therapeutics for treating obesity-driven metabolic disease and reducing cardiovascular risk.

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BACKGROUND Obesity and related cardiometabolic derangements are spiraling global health problems urgently in need of safe, effective and durable pharmacotherapy. METHODS As an orexigenic and anabolic biosignaling network, the endocannabinoid system interacts with other information-transducing

Childhood obesity and the role of dopamine D2 receptor and cannabinoid receptor-1 gene polymorphisms.

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OBJECTIVE The dopaminergic and endocannabinoid systems are involved in regulation of feeding behavior. The aim of the study is to examine the possible relation between polymorphisms of the dopamine D2 receptor (DRD2) and cannabinoid receptor-1 (CNR1) genes and childhood obesity. METHODS A hundred

Chronic treatment with the cannabinoid 1 antagonist rimonabant altered vasoactive cyclo-oxygenase-derived products on arteries from obese Zucker rats.

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To investigate the effect of chronic cannabinoid 1 antagonism on vascular prostanoid production, obese Zucker rats were treated with rimonabant (10 mg/kg per day) during 20 weeks and then vascular and endothelial reactivity were assessed in aortic rings by analyzing response to phenylephrine and

Mice Expressing a "Hyper-Sensitive" Form of the Cannabinoid Receptor 1 (CB1) Are Neither Obese Nor Diabetic.

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Multiple lines of evidence implicate the endocannabinoid signaling system in the modulation of metabolic disease. Genetic or pharmacological inactivation of CB1 in rodents leads to reduced body weight, resistance to diet-induced obesity, decreased intake of highly palatable food, and increased

1-Sulfonyl-4-acylpiperazines as selective cannabinoid-1 receptor (CB1R) inverse agonists for the treatment of obesity.

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A novel series of 1-sulfonyl-4-acylpiperazines as selective cannabinoid-1 receptor (CB1R) inverse agonists was discovered through high throughput screening (HTS) and medicinal chemistry lead optimization. Potency and in vivo properties were systematically optimized to afford orally bioavailable,

Targeted modulators of the endogenous cannabinoid system: future medications to treat addiction disorders and obesity.

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The endogenous endocannabinoid system encompasses a family of natural signaling lipids ("endocannabinoids") functionally related to (9)-tetrahydrocannabinol, the psychoactive ingredient of marijuana (cannabis), along with proteins that modulate the endocannabinoids, including enzymes, transporters,

Cannabis exposure associated with weight reduction and β-cell protection in an obese rat model.

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The aim of this study was to investigate the effect of an organic cannabis extract on β-cell secretory function in an in vivo diet-induced obese rat model and determine the associated molecular changes within pancreatic tissue. Diet-induced obese Wistar rats and rats fed on standard pellets were

Impact of lifetime marijuana use on fasting plasma insulin levels and HOMA-IR score in obese adults with and without insulin resistance.

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To explore the association of marijuana use with mean plasma fasting insulin levels and homeostasis model assessment of insulin resistance (HOMA-IR) score in obese adults with different HOMA-IR.The National Health and Nutrition Examination Survey (NHANES)

Diet-Induced Obesity in Cannabinoid-2 Receptor Knockout Mice and Cannabinoid Receptor 1/2 Double-Knockout Mice.

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Evidence suggests that cannabinoid-1 receptor (CB1R) activation is associated with increased food intake and body weight gain. Human epidemiological studies, however, show decreased prevalence of obesity in cannabis users. Given the overlapping and complementary functions of the

Cannabinoid receptor antagonists and obesity.

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The cannabinoid-1 (CB1) receptor plays a role in the regulation of appetitive behavior. Exogenously administered cannabinoid receptor agonists stimulate food consumption in animals and humans. Endogenous cannabinoid receptor agonists are present in the brain, and the brain level of these agonists

Reduced cannabinoid receptor 1 protein in subcutaneous adipose tissue of obese.

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BACKGROUND Cannabinoid 1 receptors are identified in various tissues involved in the internal metabolism including adipose tissue and the endocannabinoid system is claimed to be overactive in the obese state. To study the potential involvement of cannabinoid receptor 1 in the endocannabinoid system

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