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Open AccessReview

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

by 1,2 and 1,2,3,4,5,6,7,*
1
Translational Addiction Research Laboratory, Centre for Addiction and Mental Health, University of Toronto, 33 Russell Street, Toronto, ON M5S 2S1, Canada
2
Department of Pharmacology and Toxicology, University of Toronto, Toronto, ON M5S 1A8, Canada
3
Acute Care Program, Centre for Addiction and Mental Health, Toronto, ON M6J 1H4, Canada
4
Campbell Family Mental Health Research Institute, Centre for Addiction and Mental Health, Toronto, ON M5S 2S1, Canada
5
Department of Family and Community Medicine, University of Toronto, Toronto, ON M5G 1V7, Canada
6
Department of Psychiatry, Division of Brain and Therapeutics, University of Toronto, Toronto, ON M5T 1R8, Canada
7
Institute of Medical Sciences, University of Toronto, Toronto, ON M5S 1A8, Canada
*
Author to whom correspondence should be addressed.
Biomolecules 2020, 10(6), 855; https://doi.org/10.3390/biom10060855
Received: 20 April 2020 / Revised: 29 May 2020 / Accepted: 1 June 2020 / Published: 4 June 2020
(This article belongs to the Special Issue The Endocannabinoid System in Health and Disease)
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. View Full-Text
Keywords: obesity; cannabinoid; cannabis; weight loss; BMI; preclinical; clinical obesity; cannabinoid; cannabis; weight loss; BMI; preclinical; clinical
MDPI and ACS Style

Murphy, T.; Le Foll, B. 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. Biomolecules 2020, 10, 855. https://doi.org/10.3390/biom10060855

AMA Style

Murphy T, Le Foll B. 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. Biomolecules. 2020; 10(6):855. https://doi.org/10.3390/biom10060855

Chicago/Turabian Style

Murphy, Thomas; Le Foll, Bernard. 2020. "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" Biomolecules 10, no. 6: 855. https://doi.org/10.3390/biom10060855

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Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

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