Anti-obesity therapy with peripheral CB1 blockers: from promise to safe(?) practice

Multiple endocannabinoid-mediated mechanisms in the regulation of energy homeostasis in brain and peripheral tissues

(2019) Inigo Ruiz de Azua et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

The Cannabinoid CB1 Antagonist TM38837 With Limited Penetrance to the Brain Shows Reduced Fear-Promoting Effects in Mice

(2019) Vincenzo Micale et al.   Frontiers in Pharmacology

Semaglutide as a promising antiobesity drug

(2019) Georgios A. Christou et al.   Obesity Reviews

Dyslipidemia in nonalcoholic fatty liver disease

(2019) Antonio J. Amor et al.   Current Opinion in Endocrinology Diabetes and Obesity

Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor

(2019) George Amato et al.   JOURNAL OF MEDICINAL CHEMISTRY

Dual Inhibition of Cannabinoid‐1 Receptor and iNOS Attenuates Obesity‐induced Chronic Kidney Disease

(2019) Shiran Udi et al.   BRITISH JOURNAL OF PHARMACOLOGY

Glucose Increase DAGLα Levels in Tanycytes and Its Inhibition Alters Orexigenic and Anorexigenic Neuropeptides Expression in Response to Glucose

(2019) Alejandra Palma-Chavez et al.   Frontiers in Endocrinology

Partial Leptin Reduction as an Insulin Sensitization and Weight Loss Strategy

(2019) Shangang Zhao et al.   Cell Metabolism

Preclinical toxicity evaluation of JD5037, a peripherally restricted CB1 receptor inverse agonist, in rats and dogs for treatment of nonalcoholic steatohepatitis

(2019) Vijay Pralhad Kale et al.   REGULATORY TOXICOLOGY AND PHARMACOLOGY

Endocannabinoids in Islets of Langerhans: The Ugly, the Bad and the Good Facts

(2018) Isabel González-Mariscal et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

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

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

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

Blocking Alcoholic Steatosis in Mice with a Peripherally Restricted Purine Antagonist of the Type 1 Cannabinoid Receptor

(2018) George S. Amato et al.   JOURNAL OF MEDICINAL CHEMISTRY

Anti-Obesity Therapy: from Rainbow Pills to Polyagonists

(2018) T. D. Müller et al.   PHARMACOLOGICAL REVIEWS

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

Cannabinoid-1 Receptor Antagonism Improves Glycemic Control and Increases Energy Expenditure via Sirt1/mTORC2 and AMPK Signaling

(2018) Jie Liu et al.   HEPATOLOGY

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

Adipocyte cannabinoid receptor CB1 regulates energy homeostasis and alternatively activated macrophages

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

Design, Synthesis, and Biological Evaluation of Novel, Non-Brain-Penetrant, Hybrid Cannabinoid CB1R Inverse Agonist/Inducible Nitric Oxide Synthase (iNOS) Inhibitors for the Treatment of Liver Fibrosis

(2017) Malliga R. Iyer et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Current pharmacotherapy for obesity

(2017) Gitanjali Srivastava et al.   Nature Reviews Endocrinology

The CB1 Receptor as the Cornerstone of Exostasis

(2017) Pier Vincenzo Piazza et al.   NEURON

Health Effects of Overweight and Obesity in 195 Countries over 25 Years

(2017)   NEW ENGLAND JOURNAL OF MEDICINE

Cannabinoid type 1 receptor-containing axons innervate NPY/AgRP neurons in the mouse arcuate nucleus

(2017) Yury M. Morozov et al.   Molecular Metabolism

Plasma 2-arachidonoylglycerol is a biomarker of age and menopause related insulin resistance and dyslipidemia in lean but not in obese men and women

(2017) Flaminia Fanelli et al.   Molecular Metabolism

Peripheral cannabinoid-1 receptor blockade restores hypothalamic leptin signaling

(2017) Joseph Tam et al.   Molecular Metabolism

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

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

Blockade of cannabinoid 1 receptor improves GLP-1R mediated insulin secretion in mice

(2016) Isabel González-Mariscal et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

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

(2016) Shira Zelber-Sagi et al.   Obesity

Management and Prevention of Surgical and Nutritional Complications After Bariatric Surgery

(2016) Eric Marcotte et al.   SURGICAL CLINICS OF NORTH AMERICA

Cannabinoid CB1 Receptors Are Localized in Striated Muscle Mitochondria and Regulate Mitochondrial Respiration

(2016) Juan Mendizabal-Zubiaga et al.   Frontiers in Physiology

Human CB1 Receptor Isoforms, present in Hepatocytes and β-cells, are Involved in Regulating Metabolism

(2016) Isabel González-Mariscal et al.   Scientific Reports

Leptin Keeps Working, Even in Obesity

(2015) Martin G. Myers   Cell 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

The Endocannabinoid System: Pivotal Orchestrator of Obesity and Metabolic Disease

(2015) Wilfrid Mazier et al.   TRENDS IN ENDOCRINOLOGY AND METABOLISM

Ghrelin

(2015) T.D. Müller et al.   Molecular Metabolism

Deranged endocannabinoid responses to hedonic eating in underweight and recently weight-restored patients with anorexia nervosa

(2014) Alessio Maria Monteleone et al.   AMERICAN JOURNAL OF CLINICAL NUTRITION

Cannabinoid receptor 1 antagonist treatment induces glucagon release and shows an additive therapeutic effect with GLP-1 agonist in diet-induced obese mice

(2014) Kartikkumar Navinchandra Patel et al.   CANADIAN JOURNAL OF PHYSIOLOGY AND PHARMACOLOGY

Hypothalamic Tanycytes Are an ERK-Gated Conduit for Leptin into the Brain

(2014) Eglantine Balland et al.   Cell Metabolism

Neurobiology of food intake in health and disease

(2014) Gregory J. Morton et al.   NATURE REVIEWS NEUROSCIENCE

Thyroid Hormone Regulation of Metabolism

(2014) Rashmi Mullur et al.   PHYSIOLOGICAL REVIEWS

Is fat taste ready for primetime?

(2014) Nicholas V. DiPatrizio   PHYSIOLOGY & BEHAVIOR

Cardiorespiratory Anomalies in Mice Lacking CB1 Cannabinoid Receptors

(2014) Alessandro Silvani et al.   PLoS One

Overactive cannabinoid 1 receptor in podocytes drives type 2 diabetic nephropathy

(2014) Tony Jourdan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

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

Endocannabinoid signaling in the gut mediates preference for dietary unsaturated fats

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

Hepatic cannabinoid-1 receptors mediate diet-induced insulin resistance by increasingde novosynthesis of long-chain ceramides

(2013) Resat Cinar et al.   HEPATOLOGY

Discovery of 1-(2,4-Dichlorophenyl)-N-(piperidin-1-yl)-4-((pyrrolidine-1-sulfonamido)methyl)-5-(5-((4-(trifluoromethyl)phenyl)ethynyl)thiophene-2-yl)-1H-pyrazole-3-carboxamide as a Novel Peripherally Restricted Cannabinoid-1 Receptor Antagonist with Significant Weight-Loss Efficacy in Diet-Induced Obese Mice

(2013) Chun-Ping Chang 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

Activation of the sympathetic nervous system mediates hypophagic and anxiety-like effects of CB1 receptor blockade

(2013) L. Bellocchio et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

JD-5006 and JD-5037: Peripherally restricted (PR) cannabinoid-1 receptor blockers related to SLV-319 (Ibipinabant) as metabolic disorder therapeutics devoid of CNS liabilities

(2012) Robert J. Chorvat et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

(2012) Joseph Tam et al.   Cell Metabolism

Hepatic Cannabinoid Receptor-1 Mediates Diet-Induced Insulin Resistance via Inhibition of Insulin Signaling and Clearance in Mice

(2012) Jie Liu et al.   GASTROENTEROLOGY

Hedonic Eating Is Associated with Increased Peripheral Levels of Ghrelin and the Endocannabinoid 2-Arachidonoyl-Glycerol in Healthy Humans: A Pilot Study

(2012) Palmiero Monteleone et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

Role of ceramides in nonalcoholic fatty liver disease

(2012) Mangesh Pagadala et al.   TRENDS IN ENDOCRINOLOGY AND METABOLISM

Some cannabinoid receptor ligands and their distomers are direct-acting openers of SUR1 KATP channels

(2011) Christopher J. Lynch et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

Induction of fatty acid oxidation resists weight gain, ameliorates hepatic steatosis and reduces cardiometabolic risk factors

(2011) R S Vijayakumar et al.   INTERNATIONAL JOURNAL OF OBESITY

Simultaneous postprandial deregulation of the orexigenic endocannabinoid anandamide and the anorexigenic peptide YY in obesity

(2011) B Gatta-Cherifi et al.   INTERNATIONAL JOURNAL OF OBESITY

Estimation of reference intervals of five endocannabinoids and endocannabinoid related compounds in human plasma by two dimensional-LC/MS/MS

(2011) Flaminia Fanelli et al.   JOURNAL OF LIPID RESEARCH

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

Energy balance regulation by endocannabinoids at central and peripheral levels

(2011) Carmelo Quarta et al.   TRENDS IN MOLECULAR MEDICINE

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

Splanchnic Balance of Free Fatty Acids, Endocannabinoids, and Lipids in Subjects With Nonalcoholic Fatty Liver Disease

(2010) Jukka Westerbacka et al.   GASTROENTEROLOGY

Endocannabinoid system in the adult rat circumventricular areas: An immunohistochemical study

(2010) Juan Suárez et al.   JOURNAL OF COMPARATIVE NEUROLOGY

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

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

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

Expression and Function of Endocannabinoid Receptors in the Human Adrenal Cortex

(2009) C. G. Ziegler et al.   HORMONE AND METABOLIC RESEARCH

Male–female differences in the effects of cannabinoids on sexual behavior and gonadal hormone function

(2009) Boris B. Gorzalka et al.   HORMONES AND BEHAVIOR

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

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

Blocking cannabinoid CB1 receptors for the treatment of nicotine dependence: insights from pre-clinical and clinical studies

(2008) Bernard Le Foll et al.   ADDICTION BIOLOGY

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

Modulation of the Endocannabinoid System in Cardiovascular Disease

(2008) Pál Pacher et al.   HYPERTENSION

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

Acute effects of endocannabinoid anandamide and CB1 receptor antagonist, AM251 in the regulation of thyrotropin secretion

(2008) Marco Aurélio Liberato Costa da Veiga et al.   JOURNAL OF ENDOCRINOLOGY

Leptin controls adipose tissue lipogenesis via central, STAT3–independent mechanisms

(2008) Christoph Buettner et al.   NATURE MEDICINE

Genetic variation in cannabinoid receptor 1 (CNR1) is associated with derangements in lipid homeostasis, independent of body mass index

(2008) Tes M Baye et al.   PHARMACOGENOMICS