ENP11, a potential CB1R antagonist, induces anorexia in rats

Méndez-Dı́az, Mónica; Amancio-Belmont, Octavio; Hernández‐Vázquez, Eduardo; Ruiz-Contreras, Alejandra E.; Hernández‐Luis, Francisco; Prospéro-Garcı́a, Oscar

doi:10.1016/j.pbb.2015.06.007

Cited by 5 publications

(2 citation statements)

References 24 publications

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“…This proof of concept was followed by the development of other peripherally restricted CB1 inverse agonists. The most promising molecules of this group were TM38837 [157], AJ5012 [158], AJ5018 [159], JD5037 [160], BPR0912 [161], BPR697 [162], TXX-522 [163], ENP11 [164], Compound6a [165], BMS-725519, BMS-811064, and BMS-812204 [166]. All these molecules showed a significant reduction of body weight, food intake, or metabolic activity and were characterized by a low brain/plasma concentration ratio.…”

Section: Endocannabinoid System As a Pharmacological Target For Obesity And Food Addictionmentioning

confidence: 99%

Obesity as a Condition Determined by Food Addiction: Should Brain Endocannabinoid System Alterations Be the Cause and Its Modulation the Solution?

et al. 2021

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Obesity is a complex disorder, and the number of people affected is growing every day. In recent years, research has confirmed the hypothesis that food addiction is a determining factor in obesity. Food addiction is a behavioral disorder characterized by disruptions in the reward system in response to hedonic eating. The endocannabinoid system (ECS) plays an important role in the central and peripheral control of food intake and reward-related behaviors. Moreover, both obesity and food addiction have been linked to impairments in the ECS function in various brain regions integrating peripheral metabolic signals and modulating appetite. For these reasons, targeting the ECS could be a valid pharmacological therapy for these pathologies. However, targeting the cannabinoid receptors with inverse agonists failed when used in clinical contexts as a consequence of the induction of affective disorders. In this context, new classes of drugs acting either on CB1 and/or CB2 receptors or on synthetic and degradation enzymes of endogenous cannabinoids are being studied. However, further investigation is necessary to find safe and effective treatments that can exert anti-obesity effects, normalizing reward-related behaviors without causing important adverse mood effects.

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Section: Endocannabinoid System As a Pharmacological Target For Obesity And Food Addictionmentioning

confidence: 99%

Obesity as a Condition Determined by Food Addiction: Should Brain Endocannabinoid System Alterations Be the Cause and Its Modulation the Solution?

et al. 2021

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“…TXX-522 (IC 50 = 10.33 ± 6.08 nM), an analog of rimonabant, exhibited approximately 2% blood-brain barrier penetrance, and dose-dependently decreased body weight and fat mass in DIO mice, with levels comparable to rimonabant [ 71 ]. ENP11 is another rimonabant analog that decreases food intake in rats as early as two hours post-administration ( p = 0.049 and p = 0.048; 1 and 3 mg/kg, respectively) [ 72 ]. The decreased food intake following the acute administration of ENP11 is comparable to AM251, and more pronounced than that of rimonabant.…”

Section: Exploring the Direct Effects Of Cannabinoid Drugs On Bodymentioning

confidence: 99%

Targeting the Endocannabinoid CB1 Receptor to Treat Body Weight Disorders: A Preclinical and Clinical Review of the Therapeutic Potential of Past and Present CB1 Drugs

Murphy

Foll

2020

Biomolecules

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Obesity rates are increasing worldwide and there is a need for novel therapeutic treatment options. The endocannabinoid system has been linked to homeostatic processes, including metabolism, food intake, and the regulation of body weight. Rimonabant, an inverse agonist for the cannabinoid CB1 receptor, was effective at producing weight loss in obese subjects. However, due to adverse psychiatric side effects, rimonabant was removed from the market. More recently, we reported an inverse relationship between cannabis use and BMI, which has now been duplicated by several groups. As those results may appear contradictory, we review here preclinical and clinical studies that have studied the impact on body weight of various cannabinoid CB1 drugs. Notably, we will review the impact of CB1 inverse agonists, agonists, partial agonists, and neutral antagonists. Those findings clearly point out the cannabinoid CB1 as a potential effective target for the treatment of obesity. Recent preclinical studies suggest that ligands targeting the CB1 may retain the therapeutic potential of rimonabant without the negative side effect profile. Such approaches should be tested in clinical trials for validation.

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Variability in cannabinoid receptor genes is associated with psychiatric comorbidities in anorexia nervosa

et al. 2021

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ENP11, a potential CB1R antagonist, induces anorexia in rats

Cited by 5 publications

References 24 publications

Obesity as a Condition Determined by Food Addiction: Should Brain Endocannabinoid System Alterations Be the Cause and Its Modulation the Solution?

Obesity as a Condition Determined by Food Addiction: Should Brain Endocannabinoid System Alterations Be the Cause and Its Modulation the Solution?

Targeting the Endocannabinoid CB1 Receptor to Treat Body Weight Disorders: A Preclinical and Clinical Review of the Therapeutic Potential of Past and Present CB1 Drugs

Variability in cannabinoid receptor genes is associated with psychiatric comorbidities in anorexia nervosa

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