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

In vitro and in vivo pharmacology of CP-945,598, a potent and selective cannabinoid CB 1 receptor antagonist for the management of obesity

(2010) John R. Hadcock et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

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

Combination Drugs for Treating Obesity

(2010) Frank L. Greenway et al.   Current Diabetes Reports

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

(2010) Jesús Giraldo   DRUG DISCOVERY TODAY

The endocannabinoid system: Its roles in energy balance and potential as a target for obesity treatment

(2010) Aurore André et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

A clinical trial assessing the safety and efficacy of taranabant, a CB1R inverse agonist, in obese and overweight patients: a high-dose study

(2010) L J Aronne et al.   INTERNATIONAL JOURNAL OF OBESITY

A clinical trial assessing the safety and efficacy of the CB1R inverse agonist taranabant in obese and overweight patients: low-dose study

(2010) J Proietto et al.   INTERNATIONAL JOURNAL OF OBESITY

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

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

Depression-like phenotype following chronic CB1 receptor antagonism

(2010) Chad E. Beyer et al.   NEUROBIOLOGY OF DISEASE

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

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

Modulation of anxiety by acute blockade and genetic deletion of the CB1 cannabinoid receptor in mice together with biogenic amine changes in the forebrain

(2009) Gunnar Thiemann et al.   BEHAVIOURAL BRAIN RESEARCH

Novel thioamide derivatives as neutral CB1 receptor antagonists

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

The Current Status and Future Perspectives of Studies of Cannabinoid Receptor 1 Antagonists as Anti-Obesity Agents

(2009) Hyeon-Kyu Lee et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

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

The future of endocannabinoid-oriented clinical research after CB1 antagonists

(2009) Bernard Le Foll et al.   PSYCHOPHARMACOLOGY

The cannabinoid CB1 receptor inverse agonist AM 251 and antagonist AM 4113 produce similar effects on the behavioral satiety sequence in rats

(2008) Janel Hodge et al.   BEHAVIOURAL BRAIN RESEARCH

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

The Acyclic CB1R Inverse Agonist Taranabant Mediates Weight Loss by Increasing Energy Expenditure and Decreasing Caloric Intake

(2008) Carol Addy et al.   Cell Metabolism

Medications for Weight Reduction

(2008) George A. Bray   ENDOCRINOLOGY AND METABOLISM CLINICS OF NORTH AMERICA

Additive subthreshold dose effects of cannabinoid CB1 receptor antagonist and selective serotonin reuptake inhibitor in antidepressant behavioral tests

(2008) Eiki Takahashi et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

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

Δ9-tetrahydrocannabinol prolongs the immobility time in the mouse forced swim test: Involvement of cannabinoid CB1 receptor and serotonergic system

(2008) Nobuaki Egashira et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Emerging role of cannabinoids in gastrointestinal and liver diseases: basic and clinical aspects

(2008) A A Izzo et al.   GUT

Effect of Rimonabant on Progression of Atherosclerosis in Patients With Abdominal Obesity and Coronary Artery Disease

(2008) Steven E. Nissen et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

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

Conformational Analysis and Receptor Docking ofN-[(1S,2S)-3-(4-Chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-{[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (Taranabant, MK-0364), a Novel, Acyclic Cannabinoid-1 Receptor Inverse Agonist

(2008) Linus S. Lin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of 1-[9-(4-Chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic Acid Amide Hydrochloride (CP-945,598), a Novel, Potent, and Selective Cannabinoid Type 1 Receptor Antagonist

(2008) David A. Griffith et al.   JOURNAL OF MEDICINAL CHEMISTRY

Effects of a Cannabinoid1 Receptor Antagonist and Serotonin2C Receptor Agonist Alone and in Combination on Motivation for Palatable Food: A Dose-Addition Analysis Study in Mice

(2008) S. J. Ward et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

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

(2008) Dan Jones   NATURE REVIEWS DRUG DISCOVERY

Intrinsic effects of AM4113, a putative neutral CB1 receptor selective antagonist, on open-field behaviors in rats

(2008) T JARBE et al.   PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR

Cannabinoid receptor antagonism increases female sexual motivation

(2008) Hassan H. López et al.   PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR

Bioisosteric replacement of dihydropyrazole of 4S-(−)-3-(4-chlorophenyl)-N-methyl-N′-[(4-chlorophenyl)-sulfonyl]-4-phenyl-4,5-dihydro-1H-pyrazole-1-caboxamidine (SLV-319) a potent CB1 receptor antagonist by imidazole and oxazole

(2007) Brijesh Kumar Srivastava et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Pharmacotherapeutic targeting of the endocannabinoid signaling system: Drugs for obesity and the metabolic syndrome

(2007) V. Kiran Vemuri et al.   PHYSIOLOGY & BEHAVIOR

Antidepressant-like behavioral effects of impaired cannabinoid receptor type 1 signaling coincide with exaggerated corticosterone secretion in mice

(2007) Michel A. Steiner et al.   PSYCHONEUROENDOCRINOLOGY