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

2-Arachidonoylglycerol Signaling in Forebrain Regulates Systemic Energy Metabolism

(2012) Kwang-Mook Jung 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

Design and Synthesis of Cannabinoid Receptor 1 Antagonists for Peripheral Selectivity

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

Dietary Linoleic Acid Elevates Endogenous 2-AG and Anandamide and Induces Obesity

(2012) Anita R. Alvheim et al.   Obesity

Towards rational design of cannabinoid receptor 1 (CB1) antagonists for peripheral selectivity

(2011) Alan Fulp et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

Central Endocannabinoid Signaling Regulates Hepatic Glucose Production and Systemic Lipolysis

(2011) J. D. O'Hare et al.   DIABETES

Incorporation of EPA and DHA into plasma phospholipids in response to different omega-3 fatty acid formulations - a comparative bioavailability study of fish oil vs. krill oil

(2011) Jan Schuchardt et al.   Lipids in Health and Disease

Krill oil significantly decreases 2-arachidonoylglycerol plasma levels in obese subjects

(2011) Sebastiano Banni et al.   Nutrition & Metabolism

Effect of dietary krill oil supplementation on the endocannabinoidome of metabolically relevant tissues from high-fat-fed mice

(2011) Fabiana Piscitelli et al.   Nutrition & Metabolism

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

Moderate doses of EPA and DHA from re-esterified triacylglycerols but not from ethyl-esters lower fasting serum triacylglycerols in statin-treated dyslipidemic subjects: Results from a six month randomized controlled trial

(2011) J.P. Schuchardt et al.   PROSTAGLANDINS LEUKOTRIENES AND ESSENTIAL FATTY ACIDS

Central mediation and differential blockade by cannabinergics of the discriminative stimulus effects of the cannabinoid CB1 receptor antagonist rimonabant in rats

(2011) Torbjörn U. C. Järbe et al.   PSYCHOPHARMACOLOGY

Peripheral effects of the endocannabinoid system in energy homeostasis: Adipose tissue, liver and skeletal muscle

(2011) Cristoforo Silvestri et al.   REVIEWS IN ENDOCRINE & METABOLIC DISORDERS

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

Evidence for both inverse agonism at the cannabinoid CB1 receptor and the lack of an endogenous cannabinoid tone in the rat and guinea-pig isolated ileum myenteric plexus-longitudinal muscle preparation

(2010) R Makwana et al.   BRITISH JOURNAL OF PHARMACOLOGY

Inverse agonism of cannabinoid CB1 receptors potentiates LiCl-induced nausea in the conditioned gaping model in rats

(2010) CL Limebeer et al.   BRITISH JOURNAL OF PHARMACOLOGY

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

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

Effects of in vitro antagonism of endocannabinoid-1 receptors on the glucose transport system in normal and insulin-resistant rat skeletal muscle

(2010) K. A. Lindborg et al.   DIABETES OBESITY & METABOLISM

Deficiency of CB2 cannabinoid receptor in mice improves insulin sensitivity but increases food intake and obesity with age

(2010) J. Agudo et al.   DIABETOLOGIA

Ligand binding sensitivity of the extracellular loop two of the cannabinoid receptor 1

(2010) Alexander C. Bertalovitz et al.   DRUG DEVELOPMENT RESEARCH

How inverse can a neutral antagonist be? Strategic questions after the rimonabant issue

(2010) Jesús Giraldo   DRUG DISCOVERY TODAY

Structural and pharmacological analysis of O-2050, a putative neutral cannabinoid CB1 receptor antagonist

(2010) Jenny L. Wiley et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Prevalence and Trends in Obesity Among US Adults, 1999-2008

(2010) Katherine M. Flegal   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Pathogenesis of Insulin Resistance in Skeletal Muscle

(2010) Muhammad A. Abdul-Ghani et al.   JOURNAL OF BIOMEDICINE AND BIOTECHNOLOGY

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

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

The Cannabinoid 1–Receptor Silent Antagonist O-2050 Attenuates Preference for High-Fat Diet and Activated Astrocytes in Mice

(2010) Sei Higuchi et al.   JOURNAL OF PHARMACOLOGICAL SCIENCES

Biphasic suppression of appetite by cannabinoid CB1 receptor antagonists with distinct functional activities

(2010) Yinchiu Lin et al.   PHARMACOLOGICAL RESEARCH

The CB1 inverse agonist AM251, but not the CB1 antagonist AM4113, enhances retention of contextual fear conditioning in rats

(2010) K.S. Sink et al.   PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR

The novel cannabinoid CB1 antagonist AM6545 suppresses food intake and food-reinforced behavior

(2010) P.A. Randall et al.   PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR

The neutral cannabinoid CB1 receptor antagonist AM4113 regulates body weight through changes in energy intake in the rat

(2010) Nina L. Cluny et al.   PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR

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

Delta(9)-tetrahydrocannabinol Enhances an Increase of Plasma Corticosterone Levels Induced by Forced Swim-Stress

(2009) Kazunori Sano et al.   BIOLOGICAL & PHARMACEUTICAL BULLETIN

Novel thioamide derivatives as neutral CB1 receptor antagonists

(2009) Jonas Boström et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

Synthesis and Pharmacological Activity of a Potent Inhibitor of the Biosynthesis of the Endocannabinoid 2-Arachidonoylglycerol

(2009) Tiziana Bisogno et al.   ChemMedChem

Regulation of MAP Kinase-Directed Mitogenic and Protein Kinase B-Mediated Signaling by Cannabinoid Receptor Type 1 in Skeletal Muscle Cells

(2009) C. Lipina et al.   DIABETES

Potential anxiogenic effects of cannabinoid CB1 receptor antagonists/inverse agonists in rats: Comparisons between AM4113, AM251, and the benzodiazepine inverse agonist FG-7142

(2009) K.S. Sink et al.   EUROPEAN NEUROPSYCHOPHARMACOLOGY

Dietary krill oil increases docosahexaenoic acid and reduces 2-arachidonoylglycerol but not N-acylethanolamine levels in the brain of obese Zucker rats

(2009) Vincenzo Di Marzo et al.   INTERNATIONAL DAIRY JOURNAL

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

Endocannabinoids May Mediate the Ability of (n-3) Fatty Acids to Reduce Ectopic Fat and Inflammatory Mediators in Obese Zucker Rats

(2009) Barbara Batetta et al.   JOURNAL OF NUTRITION

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

Cannabinoid CB2 Receptor Potentiates Obesity-Associated Inflammation, Insulin Resistance and Hepatic Steatosis

(2009) Vanessa Deveaux et al.   PLoS One

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

Paracrine Activation of Hepatic CB1 Receptors by Stellate Cell-Derived Endocannabinoids Mediates Alcoholic Fatty Liver

(2008) Won-il Jeong et al.   Cell Metabolism

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

(2008) L. Tedesco et al.   DIABETES

Peripheral, but Not Central, CB1 Antagonism Provides Food Intake-Independent Metabolic Benefits in Diet-Induced Obese Rats

(2008) R. Nogueiras et al.   DIABETES

Changes in plasma endocannabinoid levels in viscerally obese men following a 1 year lifestyle modification programme and waist circumference reduction: associations with changes in metabolic risk factors

(2008) V. Di Marzo et al.   DIABETOLOGIA

Adipose tissue dysfunction in obesity, diabetes, and vascular diseases

(2008) G. R. Hajer et al.   EUROPEAN HEART JOURNAL

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

Bioisosteric Replacement of the Pyrazole 5-Aryl Moiety ofN-(Piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716A). A Novel Series of Alkynylthiophenes as Potent and Selective Cannabinoid-1 Receptor Antagonists

(2008) Shi-Liang Tseng et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Dysregulation of peripheral endocannabinoid levels in hyperglycemia and obesity: Effect of high fat diets

(2008) Isabel Matias et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

The Cannabinoid CB1 Receptor Antagonist Rimonabant Stimulates 2-Deoxyglucose Uptake in Skeletal Muscle Cells by Regulating the Expression of Phosphatidylinositol-3-kinase

(2008) I. Esposito et al.   MOLECULAR PHARMACOLOGY

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

(2008) Christoph Buettner et al.   NATURE MEDICINE

Oral bioavailability of the novel cannabinoid CB1 antagonist AM6527: Effects on food-reinforced behavior and comparisons with AM4113

(2008) K.S. Sink et al.   PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR

Overactive endocannabinoid signaling impairs apolipoprotein E-mediated clearance of triglyceride-rich lipoproteins

(2008) M. A. Ruby et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Effect of polyunsaturated fatty acids on endocannabinoid and N-acyl-ethanolamine levels in mouse adipocytes

(2007) I MATIAS   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS