Cannabis: From a Plant That Modulates Feeding Behaviors toward Developing Selective Inhibitors of the Peripheral Endocannabinoid System for the Treatment of Obesity and Metabolic Syndrome

Crystal Structure of the Human Cannabinoid Receptor CB2

(2019) Xiaoting Li et al.   CELL

Lower circulating endocannabinoid levels in children with autism spectrum disorder

(2019) Adi Aran et al.   Molecular Autism

Muscle cannabinoid 1 receptor regulates Il-6 and myostatin expression, governing physical performance and whole-body metabolism

(2019) Isabel González-Mariscal et al.   FASEB JOURNAL

Peripheral cannabinoid 1 receptor blockade mitigates adipose tissue inflammation via NLRP3 inflammasome in mouse models of obesity

(2018) Ji H. Han et al.   DIABETES OBESITY & METABOLISM

Absence of cannabinoid 1 receptor in beta cells protects against high-fat/high-sugar diet-induced beta cell dysfunction and inflammation in murine islets

(2018) Isabel González-Mariscal et al.   DIABETOLOGIA

The therapeutic potential of targeting the peripheral endocannabinoid/CB 1 receptor system

(2018) Joseph Tam et al.   European Journal of Internal Medicine

Cannabinoid Receptors and the Endocannabinoid System: Signaling and Function in the Central Nervous System

(2018) et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Peripheral CB1 Receptor Neutral Antagonist, AM6545, Ameliorates Hypometabolic Obesity and Improves Adipokine Secretion in Monosodium Glutamate Induced Obese Mice

(2018) Haiming Ma et al.   Frontiers in Pharmacology

Dronabinol oral solution in the management of anorexia and weight loss in AIDS and cancer

(2018) Melissa Badowski et al.   Therapeutics and Clinical Risk Management

Synthesis and pharmacological characterization of functionalized 6-piperazin-1-yl-purines as cannabinoid receptor 1 (CB1) inverse agonists

(2018) George S. Amato et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Cannabinoid-1 receptor regulates mitochondrial dynamics and function in renal proximal tubular cells

(2018) Adi Drori et al.   DIABETES OBESITY & METABOLISM

Circulating Endocannabinoids Are Reduced Following Bariatric Surgery and Associated with Improved Metabolic Homeostasis in Humans

(2018) Shahar Azar et al.   OBESITY SURGERY

A new ESI-LC/MS approach for comprehensive metabolic profiling of phytocannabinoids in Cannabis

(2018) Paula Berman et al.   Scientific Reports

A novel peripheral cannabinoid 1 receptor antagonist, AJ5012, improves metabolic outcomes and suppresses adipose tissue inflammation in obese mice

(2018) Ji Hye Han et al.   FASEB JOURNAL

6-Benzhydryl-4-amino-quinolin-2-ones as Potent Cannabinoid Type 1 (CB1) Receptor Inverse Agonists and Chemical Modifications for Peripheral Selectivity

(2018) Yue-Mei Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

MECHANISMS IN ENDOCRINOLOGY: Endocannabinoids and metabolism: past, present and future

(2017) Vincent Simon et al.   EUROPEAN JOURNAL OF ENDOCRINOLOGY

Antidiabetic, antidyslipidemic and toxicity profile of ENV-2: A potent pyrazole derivative against diabetes and related diseases

(2017) Eduardo Hernández-Vázquez et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Cannabinoid CB 1 receptor inverse agonist MJ08 stimulates glucose production via hepatic sympathetic innervation in rats

(2017) Wei Chen et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Metabolic side effects induced by olanzapine treatment are neutralized by CB1 receptor antagonist compounds co-administration in female rats

(2017) P. Lazzari et al.   EUROPEAN NEUROPSYCHOPHARMACOLOGY

Adipocyte cannabinoid receptor CB1 regulates energy homeostasis and alternatively activated macrophages

(2017) Inigo Ruiz de Azua et al.   JOURNAL OF CLINICAL INVESTIGATION

Proximal Tubular Cannabinoid-1 Receptor Regulates Obesity-Induced CKD

(2017) Shiran Udi et al.   JOURNAL OF THE AMERICAN SOCIETY OF NEPHROLOGY

Modulation of Renal GLUT2 by the Cannabinoid-1 Receptor: Implications for the Treatment of Diabetic Nephropathy

(2017) Liad Hinden et al.   JOURNAL OF THE AMERICAN SOCIETY OF NEPHROLOGY

Crystal structures of agonist-bound human cannabinoid receptor CB1

(2017) Tian Hua et al.   NATURE

Peripheral endocannabinoid signaling controls hyperphagia in western diet-induced obesity

(2017) Donovan A. Argueta et al.   PHYSIOLOGY & BEHAVIOR

Novel Peripherally Restricted Cannabinoid 1 Receptor Selective Antagonist TXX-522 with Prominent Weight-Loss Efficacy in Diet Induced Obese Mice

(2017) Wei Chen et al.   Frontiers in Pharmacology

Peripheral cannabinoid-1 receptor blockade restores hypothalamic leptin signaling

(2017) Joseph Tam et al.   Molecular Metabolism

Pyrazole antagonists of the CB1 receptor with reduced brain penetration

(2016) Alan Fulp et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Tetrahydroindazole derivatives as potent and peripherally selective cannabinoid-1 (CB1) receptor inverse agonists

(2016) Jay M. Matthews et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Crystal Structure of the Human Cannabinoid Receptor CB 1

(2016) Tian Hua et al.   CELL

Phytocannabinoids: a unified critical inventory

(2016) Lumír Ondřej Hanuš et al.   NATURAL PRODUCT REPORTS

High-resolution crystal structure of the human CB1 cannabinoid receptor

(2016) Zhenhua Shao et al.   NATURE

Serum levels of endocannabinoids are independently associated with nonalcoholic fatty liver disease

(2016) Shira Zelber-Sagi et al.   Obesity

Targeting the endocannabinoid/CB1 receptor system for treating obesity in Prader–Willi syndrome

(2016) Ibrahim Knani et al.   Molecular Metabolism

A novel peripheral cannabinoid receptor 1 antagonist, BPR0912, reduces weight independently of food intake and modulates thermogenesis

(2015) W.-C. Hsiao et al.   DIABETES OBESITY & METABOLISM

Exploring structural requirements for peripherally acting 1,5-diaryl pyrazole-containing cannabinoid 1 receptor antagonists for the treatment of obesity

(2015) Mayank Kumar Sharma et al.   MOLECULAR DIVERSITY

Safety and Toxicology of Cannabinoids

(2015) Jane Sachs et al.   Neurotherapeutics

The Endocannabinoid System and its Modulation by Phytocannabinoids

(2015) Vincenzo Di Marzo et al.   Neurotherapeutics

Prospective therapeutic agents for obesity: Molecular modification approaches of centrally and peripherally acting selective cannabinoid 1 receptor antagonists

(2014) Mayank Kumar Sharma et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Peripheral cannabinoid 1 receptor blockade activates brown adipose tissue and diminishes dyslipidemia and obesity

(2014) Mariëtte R. Boon et al.   FASEB JOURNAL

Care and Feeding of the Endocannabinoid System: A Systematic Review of Potential Clinical Interventions that Upregulate the Endocannabinoid System

(2014) John M. McPartland et al.   PLoS One

Regular Cocaine Use Is Associated with Increased Systolic Blood Pressure, Aortic Stiffness and Left Ventricular Mass in Young Otherwise Healthy Individuals

(2014) Rebecca Kozor et al.   PLoS One

A peripheral endocannabinoid mechanism contributes to glucocorticoid-mediated metabolic syndrome

(2014) Nicole P. Bowles et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

[18F]MK-9470 PET measurement of cannabinoid CB1receptor availability in chronic cannabis users

(2013) Jenny Ceccarini et al.   ADDICTION BIOLOGY

Peripherally restricted CB1 receptor blockers

(2013) Robert J. Chorvat   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Peripheral selectivity of the novel cannabinoid receptor antagonist TM38837 in healthy subjects

(2013) Linda E. Klumpers et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Parsing the players: 2-arachidonoylglycerol synthesis and degradation in the CNS

(2013) N Murataeva et al.   BRITISH JOURNAL OF PHARMACOLOGY

Endocannabinoid signaling in the gut mediates preference for dietary unsaturated fats

(2013) Nicholas V. DiPatrizio et al.   FASEB JOURNAL

Dronabinol in severe, enduring anorexia nervosa: A randomized controlled trial

(2013) Alin Andries et al.   INTERNATIONAL JOURNAL OF EATING DISORDERS

6-Alkoxy-5-aryl-3-pyridinecarboxamides, a New Series of Bioavailable Cannabinoid Receptor Type 1 (CB1) Antagonists Including Peripherally Selective Compounds

(2013) Stephan Röver et al.   JOURNAL OF MEDICINAL CHEMISTRY

Activation of the Nlrp3 inflammasome in infiltrating macrophages by endocannabinoids mediates beta cell loss in type 2 diabetes

(2013) Tony Jourdan et al.   NATURE MEDICINE

Circulating endocannabinoids in insulin sensitive vs. Insulin resistant obese postmenopausal women. A MONET group study

(2013) Joseph Abdulnour et al.   Obesity

NESS06SM reduces body weight with an improved profile relative to SR141716A

(2013) Andrea Mastinu et al.   PHARMACOLOGICAL RESEARCH

Low brain CB1 receptor occupancy by a second generation CB1 receptor antagonist TM38837 in comparison with rimonabant in nonhuman primates: A PET study

(2013) Akihiro Takano et al.   SYNAPSE

Opioid-induced respiratory depression in paediatrics: a review of case reports

(2012) M. Niesters et al.   BRITISH JOURNAL OF ANAESTHESIA

Peripheral Cannabinoid-1 Receptor Inverse Agonism Reduces Obesity by Reversing Leptin Resistance

(2012) Joseph Tam et al.   Cell Metabolism

Design and Synthesis of Cannabinoid Receptor 1 Antagonists for Peripheral Selectivity

(2012) Alan Fulp et al.   JOURNAL OF MEDICINAL CHEMISTRY

Why do cannabinoid receptors have more than one endogenous ligand?

(2012) V. Di Marzo et al.   PHILOSOPHICAL TRANSACTIONS OF THE ROYAL SOCIETY B-BIOLOGICAL SCIENCES

Novel selective cannabinoid CB1 receptor antagonist MJ08 with potent in vivo bioactivity and inverse agonistic effects

(2011) Wei Chen et al.   ACTA PHARMACOLOGICA SINICA

Anti-obesity efficacy of LH-21, a cannabinoid CB1 receptor antagonist with poor brain penetration, in diet-induced obese rats

(2011) Mónica Alonso et al.   BRITISH JOURNAL OF PHARMACOLOGY

Reversible and regionally selective downregulation of brain cannabinoid CB1 receptors in chronic daily cannabis smokers

(2011) J Hirvonen et al.   MOLECULAR PSYCHIATRY

Rimonabant Redux and Strategies to Improve the Future Outlook of CB1 Receptor Neutral-Antagonist/Inverse-Agonist Therapies

(2011) Sara Jane Ward et al.   Obesity

Endocannabinoid signal in the gut controls dietary fat intake

(2011) N. V. DiPatrizio et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Defining Desirable Central Nervous System Drug Space through the Alignment of Molecular Properties, in Vitro ADME, and Safety Attributes

(2010) Travis T. Wager et al.   ACS Chemical Neuroscience

A novel peripherally restricted cannabinoid receptor antagonist, AM6545, reduces food intake and body weight, but does not cause malaise, in rodents

(2010) NL Cluny et al.   BRITISH JOURNAL OF PHARMACOLOGY

CB1 Signaling in Forebrain and Sympathetic Neurons Is a Key Determinant of Endocannabinoid Actions on Energy Balance

(2010) Carmelo Quarta et al.   Cell Metabolism

Discovery of 1-(2,4-Dichlorophenyl)-4-ethyl-5-(5-(2-(4-(trifluoromethyl)phenyl)ethynyl)thiophen-2-yl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide as a Potential Peripheral Cannabinoid-1 Receptor Inverse Agonist

(2010) Ming-Shiu Hung et al.   ChemMedChem

CB1 Antagonism Exerts Specific Molecular Effects on Visceral and Subcutaneous Fat and Reverses Liver Steatosis in Diet-Induced Obese Mice

(2010) T. Jourdan et al.   DIABETES

Peripheral CB1 cannabinoid receptor blockade improves cardiometabolic risk in mouse models of obesity

(2010) Joseph Tam et al.   JOURNAL OF CLINICAL INVESTIGATION

International Union of Basic and Clinical Pharmacology. LXXIX. Cannabinoid Receptors and Their Ligands: Beyond CB1 and CB2

(2010) R. G. Pertwee et al.   PHARMACOLOGICAL REVIEWS

Conversion of 4-cyanomethyl-pyrazole-3-carboxamides into CB1 antagonists with lowered propensity to pass the blood–brain-barrier

(2009) Jean-Marie Receveur et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Chronic toxicology of cannabis

(2009) Albert Stuart Reece   CLINICAL TOXICOLOGY

Effect of Rimonabant on Glycemic Control in Insulin-Treated Type 2 Diabetes: The ARPEGGIO Trial

(2009) P. A. Hollander et al.   DIABETES CARE

Role of insulin as a negative regulator of plasma endocannabinoid levels in obese and nonobese subjects

(2009) Vincenzo Di Marzo et al.   EUROPEAN JOURNAL OF ENDOCRINOLOGY

Peripherally acting CB1-receptor antagonist: the relative importance of central and peripheral CB1 receptors in adiposity control

(2009) M-H Son et al.   INTERNATIONAL JOURNAL OF OBESITY

The endocannabinoid system as a link between homoeostatic and hedonic pathways involved in energy balance regulation

(2009) V Di Marzo et al.   INTERNATIONAL JOURNAL OF OBESITY

Cannabinoid CB1 receptor expression in relation to visceral adipose depots, endocannabinoid levels, microvascular damage, and the presence of the Cnr1 A3813G variant in humans

(2009) Marica Bordicchia et al.   METABOLISM-CLINICAL AND EXPERIMENTAL

Effect of Rimonabant on the High-Triglyceride/ Low–HDL-Cholesterol Dyslipidemia, Intraabdominal Adiposity, and Liver Fat

(2008) Jean-Pierre Després et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

Synthesis and characterization of a peripherally restricted CB1 cannabinoid antagonist, URB447, that reduces feeding and body-weight gain in mice

(2008) Jesse LoVerme et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

SERENADE: The Study Evaluating Rimonabant Efficacy in Drug-Naive Diabetic Patients: Effects of monotherapy with rimonabant, the first selective CB1 receptor antagonist, on glycemic control, body weight, and lipid profile in drug-naive type 2 diabetes

(2008) J. Rosenstock et al.   DIABETES CARE

Therapeutic use ofCannabis sativaon chemotherapy-induced nausea and vomiting among cancer patients: systematic review and meta-analysis

(2008) F.C. MACHADO ROCHA et al.   EUROPEAN JOURNAL OF CANCER CARE

Pharmacological evaluation of LH-21, a newly discovered molecule that binds to cannabinoid CB1 receptor

(2008) Richard Z. Chen et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Hepatic CB1 receptor is required for development of diet-induced steatosis, dyslipidemia, and insulin and leptin resistance in mice

(2008) Douglas Osei-Hyiaman et al.   JOURNAL OF CLINICAL INVESTIGATION

Central Versus Peripheral Antagonism of Cannabinoid CB1 Receptor in Obesity: Effects of LH-21, a Peripherally Acting Neutral Cannabinoid Receptor Antagonist, in Zucker Rats

(2008) F. J. Pavón et al.   JOURNAL OF NEUROENDOCRINOLOGY

Pharmacological and therapeutic secrets of plant and brain (endo)cannabinoids

(2008) Lumír Ondřej Hanuš   MEDICINAL RESEARCH REVIEWS

End of the line for cannabinoid receptor 1 as an anti-obesity target?

(2008) Dan Jones   NATURE REVIEWS DRUG DISCOVERY