Literature DB >> 17112304

Rimonabant.

Sheridan Henness1, Dean M Robinson, Katherine A Lyseng-Williamson.   

Abstract

Rimonabant is the first of a new class of selective cannabinoid receptor-1 blockers. It reduces the overactivity of the endocannabinoid system, improving lipid and glucose metabolism and regulating food intake and energy balance. In four randomised, double-blind clinical trials in overweight or obese adults with or without type 2 diabetes and/or dyslipidaemia, oral rimonabant 20mg once daily reduced weight and waist circumference to a significantly greater extent than placebo. A significantly greater proportion of rimonabant than placebo recipients achieved the clinically significant weight-loss target of > or =5% or > or =10% of initial weight. Rimonabant was associated with significant improvements in glycaemic control relative to placebo, with approximately equal to 57% of the reduction in glycosylated haemoglobin being independent of the effects of weight loss in one trial. Improvements in other cardiometabolic risk factors (i.e. increases in high-density lipoprotein-cholesterol [HDL-C] and decreases in triglyceride [TG] levels) were significantly greater with rimonabant than with placebo. The improvement in lipid profile also demonstrated a weight-independent effect, with approximately equal to 47-58% of the improvement in HDL-C and TG being beyond that expected through weight loss alone. Rimonabant was generally well tolerated, with most adverse events considered mild to moderate in severity.

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Year:  2006        PMID: 17112304     DOI: 10.2165/00003495-200666160-00006

Source DB:  PubMed          Journal:  Drugs        ISSN: 0012-6667            Impact factor:   9.546


  29 in total

1.  Regulation, function, and dysregulation of endocannabinoids in models of adipose and beta-pancreatic cells and in obesity and hyperglycemia.

Authors:  Isabel Matias; Marie-Paule Gonthier; Pierangelo Orlando; Vassilis Martiadis; Luciano De Petrocellis; Cristina Cervino; Stefania Petrosino; Laurence Hoareau; Franck Festy; Renato Pasquali; Regis Roche; Mario Maj; Uberto Pagotto; Palmiero Monteleone; Vincenzo Di Marzo
Journal:  J Clin Endocrinol Metab       Date:  2006-05-09       Impact factor: 5.958

2.  Effects of the cannabinoid-1 receptor blocker rimonabant on weight reduction and cardiovascular risk factors in overweight patients: 1-year experience from the RIO-Europe study.

Authors:  Luc F Van Gaal; Aila M Rissanen; André J Scheen; Olivier Ziegler; Stephan Rössner
Journal:  Lancet       Date:  2005 Apr 16-22       Impact factor: 79.321

3.  Endocannabinoid activation at hepatic CB1 receptors stimulates fatty acid synthesis and contributes to diet-induced obesity.

Authors:  Douglas Osei-Hyiaman; Michael DePetrillo; Pál Pacher; Jie Liu; Svetlana Radaeva; Sándor Bátkai; Judith Harvey-White; Ken Mackie; László Offertáler; Lei Wang; George Kunos
Journal:  J Clin Invest       Date:  2005-05       Impact factor: 14.808

4.  Potential modulation of plasma ghrelin and glucagon-like peptide-1 by anorexigenic cannabinoid compounds, SR141716A (rimonabant) and oleoylethanolamide.

Authors:  Patrice D Cani; Maite Lasa Montoya; Audrey M Neyrinck; Nathalie M Delzenne; Didier M Lambert
Journal:  Br J Nutr       Date:  2004-11       Impact factor: 3.718

5.  Effects of the cannabinoid CB1 receptor antagonist SR141716 on oxygen consumption and soleus muscle glucose uptake in Lep(ob)/Lep(ob) mice.

Authors:  Y L Liu; I P Connoley; C A Wilson; M J Stock
Journal:  Int J Obes (Lond)       Date:  2005-02       Impact factor: 5.095

6.  Efficacy and tolerability of rimonabant in overweight or obese patients with type 2 diabetes: a randomised controlled study.

Authors:  André J Scheen; Nick Finer; Priscilla Hollander; Michael D Jensen; Luc F Van Gaal
Journal:  Lancet       Date:  2006-11-11       Impact factor: 79.321

7.  The cannabinoid CB1 receptor antagonist SR141716 increases Acrp30 mRNA expression in adipose tissue of obese fa/fa rats and in cultured adipocyte cells.

Authors:  M Bensaid; M Gary-Bobo; A Esclangon; J P Maffrand; G Le Fur; F Oury-Donat; P Soubrié
Journal:  Mol Pharmacol       Date:  2003-04       Impact factor: 4.436

Review 8.  Rimonabant--a selective CB1 antagonist.

Authors:  Steven Thomas Boyd; Brad Allen Fremming
Journal:  Ann Pharmacother       Date:  2005-03-08       Impact factor: 3.154

9.  The endogenous cannabinoid system affects energy balance via central orexigenic drive and peripheral lipogenesis.

Authors:  Daniela Cota; Giovanni Marsicano; Matthias Tschöp; Yvonne Grübler; Cornelia Flachskamm; Mirjam Schubert; Dorothee Auer; Alexander Yassouridis; Christa Thöne-Reineke; Sylvia Ortmann; Federica Tomassoni; Cristina Cervino; Enzo Nisoli; Astrid C E Linthorst; Renato Pasquali; Beat Lutz; Günter K Stalla; Uberto Pagotto
Journal:  J Clin Invest       Date:  2003-08       Impact factor: 14.808

10.  Endocannabinoid levels in rat limbic forebrain and hypothalamus in relation to fasting, feeding and satiation: stimulation of eating by 2-arachidonoyl glycerol.

Authors:  Tim C Kirkham; Claire M Williams; Filomena Fezza; Vincenzo Di Marzo
Journal:  Br J Pharmacol       Date:  2002-06       Impact factor: 8.739

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  12 in total

1.  AM-251 and rimonabant act as direct antagonists at mu-opioid receptors: implications for opioid/cannabinoid interaction studies.

Authors:  Kathryn A Seely; Lisa K Brents; Lirit N Franks; Maheswari Rajasekaran; Sarah M Zimmerman; William E Fantegrossi; Paul L Prather
Journal:  Neuropharmacology       Date:  2012-07-04       Impact factor: 5.250

2.  Development of Quinazoline/Pyrimidine-2,4(1H,3H)-diones as Agonists of Cannabinoid Receptor Type 2.

Authors:  Hai-Yan Qian; Zhi-Long Wang; You-Lu Pan; Li-Li Chen; Xin Xie; Jian-Zhong Chen
Journal:  ACS Med Chem Lett       Date:  2017-05-01       Impact factor: 4.345

3.  Effects of CB1 receptor blockade on monosodium glutamate induced hypometabolic and hypothalamic obesity in rats.

Authors:  Wei Chen; Zhenhua Chen; Nina Xue; Zhibing Zheng; Song Li; Lili Wang
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2013-04-26       Impact factor: 3.000

Review 4.  Pharmacotherapeutic targeting of the endocannabinoid signaling system: drugs for obesity and the metabolic syndrome.

Authors:  V Kiran Vemuri; David R Janero; Alexandros Makriyannis
Journal:  Physiol Behav       Date:  2007-11-21

Review 5.  Rimonabant: new data and emerging experience.

Authors:  Suzanne M Wright; Carolien Dikkers; Louis J Aronne
Journal:  Curr Atheroscler Rep       Date:  2008-02       Impact factor: 5.113

Review 6.  Targeted modulators of the endogenous cannabinoid system: future medications to treat addiction disorders and obesity.

Authors:  David R Janero; Alexandros Makriyannis
Journal:  Curr Psychiatry Rep       Date:  2007-10       Impact factor: 5.285

Review 7.  Cytotoxic edema: mechanisms of pathological cell swelling.

Authors:  Danny Liang; Sergei Bhatta; Volodymyr Gerzanich; J Marc Simard
Journal:  Neurosurg Focus       Date:  2007-05-15       Impact factor: 4.047

8.  The cannabinoid receptor-1 antagonist rimonabant inhibits platelet activation and reduces pro-inflammatory chemokines and leukocytes in Zucker rats.

Authors:  A Schäfer; J Pfrang; J Neumüller; S Fiedler; G Ertl; J Bauersachs
Journal:  Br J Pharmacol       Date:  2008-05-12       Impact factor: 8.739

Review 9.  Non-selective cation channels, transient receptor potential channels and ischemic stroke.

Authors:  J Marc Simard; Kirill V Tarasov; Volodymyr Gerzanich
Journal:  Biochim Biophys Acta       Date:  2007-03-19

Review 10.  Prejunctional and peripheral effects of the cannabinoid CB(1) receptor inverse agonist rimonabant (SR 141716).

Authors:  Hester van Diepen; Eberhard Schlicker; Martin C Michel
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2008-07-25       Impact factor: 3.000

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