Controlled downregulation of the cannabinoid CB1 receptor provides a promising approach for the treatment of obesity and obesity-derived type 2 diabetes

LTB4 promotes insulin resistance in obese mice by acting on macrophages, hepatocytes and myocytes

(2015) Pingping Li et al.   NATURE MEDICINE

Mitochondria: a possible nexus for the regulation of energy homeostasis by the endocannabinoid system?

(2014) Christopher Lipina et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

The pathogenic mechanism of diabetes varies with the degree of overexpression and oligomerization of human amylin in the pancreatic islet β cells

(2014) Shaoping Zhang et al.   FASEB JOURNAL

Targeting inflammation in the treatment of type 2 diabetes: time to start

(2014) Marc Y. Donath   NATURE REVIEWS DRUG DISCOVERY

Peripherally restricted CB1 receptor blockers

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

Circadian Disruption Leads to Insulin Resistance and Obesity

(2013) Shu-qun Shi et al.   CURRENT BIOLOGY

Abdominal obesity and low-grade systemic inflammation as markers of subclinical organ damage in type 2 diabetes

(2013) E.M. Dahlén et al.   DIABETES & METABOLISM

Global estimates of diabetes prevalence for 2013 and projections for 2035

(2013) L. Guariguata et al.   DIABETES RESEARCH AND CLINICAL PRACTICE

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

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

Diabetes Mellitus and the β Cell: The Last Ten Years

(2012) Frances M. Ashcroft et al.   CELL

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

(2012) Joseph Tam et al.   Cell Metabolism

Ibipinabant attenuates β-cell loss in male Zucker diabetic fatty rats independently of its effects on body weight

(2012) K. Rohrbach et al.   DIABETES OBESITY & METABOLISM

Second generation CB1 receptor blockers and other inhibitors of peripheral endocannabinoid overactivity and the rationale of their use against metabolic disorders

(2012) Cristoforo Silvestri et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

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

(2012) Jie Liu et al.   GASTROENTEROLOGY

Cannabinoids Induce Pancreatic  -Cell Death by Directly Inhibiting Insulin Receptor Activation

(2012) W. Kim et al.   Science Signaling

Adverse Metabolic Consequences in Humans of Prolonged Sleep Restriction Combined with Circadian Disruption

(2012) O. M. Buxton et al.   Science Translational Medicine

Design of a Potent CB1 Receptor Antagonist Series: Potential Scaffold for Peripherally-Targeted Agents

(2012) Robert L. Dow et al.   ACS Medicinal Chemistry Letters

Obesity and endoplasmic reticulum (ER) stresses

(2012) Yamini B. Tripathi et al.   Frontiers in Immunology

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

The case for peripheral CB1receptor blockade in the treatment of visceral obesity and its cardiometabolic complications

(2011) George Kunos et al.   BRITISH JOURNAL OF PHARMACOLOGY

A New Perspective of Cannabinoid 1 Receptor Antagonists: Approaches Toward Peripheral CB1R Blockers without Crossing the Blood-Brain Barrier

(2011) Yen-Ku Wu et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Antagonism of peripheral hepatic cannabinoid receptor-1 improves liver lipid metabolism in mice: Evidence from cultured explants

(2011) Tony Jourdan et al.   HEPATOLOGY

The Major Plant-derived Cannabinoid Δ9-Tetrahydrocannabinol Promotes Hypertrophy and Macrophage Infiltration in Adipose Tissue

(2011) A. Wong et al.   HORMONE AND METABOLIC RESEARCH

Mitochondria and endoplasmic reticulum: Mitochondria–endoplasmic reticulum interplay in type 2 diabetes pathophysiology

(2011) Jennifer Rieusset   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

Obesity and Type 2 Diabetes: What Can Be Unified and What Needs to Be Individualized?

(2011) Robert H. Eckel et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

Energy balance regulation by endocannabinoids at central and peripheral levels

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

Endoplasmic reticulum stress, obesity and diabetes

(2011) Miriam Cnop et al.   TRENDS IN MOLECULAR MEDICINE

Rational design of a novel peripherally-restricted, orally active CB1 cannabinoid antagonist containing a 2,3-diarylpyrrole motif

(2010) Laurent Hortala et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

Endoplasmic Reticulum Stress and the Inflammatory Basis of Metabolic Disease

(2010) Gökhan S. Hotamisligil   CELL

Cannabinoid Receptor Stimulation Impairs Mitochondrial Biogenesis in Mouse White Adipose Tissue, Muscle, and Liver: The Role of eNOS, p38 MAPK, and AMPK Pathways

(2010) L. Tedesco et al.   DIABETES

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

Genetics of type 2 diabetes: pathophysiologic and clinical relevance

(2010) Christian Herder et al.   EUROPEAN JOURNAL OF CLINICAL INVESTIGATION

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

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

An overview of the metabolic effects of rimonabant in randomized controlled trials: potential for other cannabinoid 1 receptor blockers in obesity

(2010) F. D. Christopoulou et al.   JOURNAL OF CLINICAL PHARMACY AND THERAPEUTICS

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

Biomarkers of Endocannabinoid System Activation in Severe Obesity

(2010) Jack C. Sipe et al.   PLoS One

Effects of the cannabinoid CB1 antagonist rimonabant on hepatic mitochondrial function in rats fed a high-fat diet

(2009) Mélissa Flamment et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

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

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

Cannabinoid type 1 receptor blockade induces transdifferentiation towards a brown fat phenotype in white adipocytes

(2009) N. Perwitz et al.   DIABETES OBESITY & METABOLISM

Endocannabinoids and Their Receptors as Targets for Obesity Therapy

(2009) Annette D. de Kloet et al.   ENDOCRINOLOGY

Beneficial effect of a chronic treatment with rimonabant on pancreatic function and β-cell morphology in Zucker Fatty rats

(2009) Valérie F. Duvivier et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Inflammation and endoplasmic reticulum stress in obesity and diabetes

(2009) G S Hotamisligil   INTERNATIONAL JOURNAL OF OBESITY

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

GRP78 expression inhibits insulin and ER stress–induced SREBP-1c activation and reduces hepatic steatosis in mice

(2009) Hélène L. Kammoun et al.   JOURNAL OF CLINICAL INVESTIGATION

The CB1 Antagonist Rimonabant Decreases Insulin Hypersecretion in Rat Pancreatic Islets

(2009) Lisa Getty-Kaushik et al.   Obesity

The psychiatric side-effects of rimonabant

(2009) Fabrício A. Moreira et al.   REVISTA BRASILEIRA DE PSIQUIATRIA

Adipose Macrophage Infiltration Is Associated With Insulin Resistance and Vascular Endothelial Dysfunction in Obese Subjects

(2008) Caroline M. Apovian et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

Coupling mitochondrial dysfunction to endoplasmic reticulum stress response: A molecular mechanism leading to hepatic insulin resistance

(2008) J LIM et al.   CELLULAR SIGNALLING

Cannabinoid Type 1 Receptor Blockade Promotes Mitochondrial Biogenesis Through Endothelial Nitric Oxide Synthase Expression in White Adipocytes

(2008) L. Tedesco et al.   DIABETES

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

The endocannabinoid system in obesity and type 2 diabetes

(2008) V. Di Marzo   DIABETOLOGIA

Cannabinoid type 1 receptors in human skeletal muscle cells participate in the negative crosstalk between fat and muscle

(2008) K. Eckardt et al.   DIABETOLOGIA

Long-term effect of CB1 blockade with rimonabant on cardiometabolic risk factors: two year results from the RIO-Europe Study †

(2008) Luc F. Van Gaal et al.   EUROPEAN HEART JOURNAL

Dysregulation of the Endocannabinoid System in Obesity

(2008) S. Engeli   JOURNAL OF NEUROENDOCRINOLOGY

From endoplasmic-reticulum stress to the inflammatory response

(2008) Kezhong Zhang et al.   NATURE

PSNCBAM-1, a novel allosteric antagonist at cannabinoid CB1 receptors with hypophagic effects in rats

(2007) J G Horswill et al.   BRITISH JOURNAL OF PHARMACOLOGY

The role of adipose tissue dysfunction in the pathogenesis of obesity-related insulin resistance

(2007) Gijs H. Goossens   PHYSIOLOGY & BEHAVIOR