Rimonabant: A cannabinoid receptor blocker for the treatment of metabolic and cardiovascular risk factors

Nutrition, Metabolism and Cardiovascular Diseases

Volumn 16, Issue 2, 2006, Pages 156-162

  Tonstad, Serena ^a  

^a ULLEVÅL UNIVERSITY HOSPITAL   (Norway)

Author keywords

Cardiometabolic; Cardiovascular; Endocannabinoid system; Obesity; Rimonabant; Smoking cessation

Indexed keywords

ANIMALIA; NICOTIANA TABACUM;

EID: 33644928428     PISSN: 09394753     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.numecd.2005.10.011     Document Type: Short Survey

References (45)

1. Matsuda LA, Lolait SJ, Brownstein MJ, Young AC, Bonner TI. Structure of a cannabinoid receptor and functional expression of the cloned cDNA. Nature 1990;346(6284):561-4.
2. Devane WA, Hanus L, Breuer A, Pertwee RG, Stevenson LA, Griffin G, et al. Isolation and structure of a brain constituent that binds to the cannabinoid receptor. Science 1992; 258(5090):1946-9.
3. Salzet M, Breton C, Bisogno T, Di Marzo V. Comparative biology of the endocannabinoid system possible role in the immune response. Eur J Biochem 2000;267(16):4917-27.
4. Di Marzo V, Melck D, Bisogno T, De Petrocellis L. Endocannabinoids: endogenous cannabinoid receptor ligands with neuromodulatory action. Trends Neurosci 1998;21(12):521-8.
5. Di Marzo V, Bifulco M, De Petrocellis L. The endocannabinoid system and its therapeutic exploitation. Nat Rev Drug Discov 2004;3(9):771-84.
6. Marsicano G, Wotjak CT, Azad SC, Bisogno T, Rammes G, Cascio MG, et al. The endogenous cannabinoid system controls extinction of aversive memories. Nature 2002; 418(6897):530-4.
7. Herkenham M, Lynn AB, Little MD, Johnson MR, Melvin LS, de Costa BR, et al. Cannabinoid receptor localization in brain. Proc Natl Acad Sci U S A 1990;87(5):1932-6.
8. Cota D, Marsicano G, Tschop M, Grubler Y, Flachskamm C, Schubert M, et al. The endogenous cannabinoid system affects energy balance via central orexigenic drive and peripheral lipogenesis. J Clin Invest 2003;112(3):423-31.
9. Kirkham TC, Williams CM. Endogenous cannabinoids and appetite. Nutr Res Rev 2001;14(1):65-86.
10. Rinaldi-Carmona M, Barth F, Heaulme M, Shire D, Calandra B, Congy C, et al. SR141716A, a potent and selective antagonist of the brain cannabinoid receptor. FEBS Lett 1994;350(2-3):240-4.
11. Pertwee RG. Pharmacology of cannabinoid CB1 and CB2 receptors. Pharmacol Ther 1997;74(2): 129-80. doi:10.1016/S0163-7258(97)82001-3.
12. Howlett AC, Barth F, Bonner TI, Cabrai G, Casellas P, Devane WA, et al. International Union of Pharmacology. XXVII. Classification of cannabinoid receptors. Pharmacol Rev 2002;54(2):161-202.
13. Massa F, Storr M, Lutz B. The endocannabinoid system in the physiology and pathophysiology of the gastrointestinal tract. J Mol Med 2005 (e-pub ahead of print).
14. Pagotto U, Pasquali R. Fighting obesity and associated risk factors by antagonising cannabinoid type 1 receptors. Lancet 2005;365(9468):1363-4. doi:10.1016/S0140-6736(05)66348-9.
15. Jbilo O, Ravinet-Trillou C, Arnone M, Buisson I, Bribes E, Peleraux A, et al. The CB1 receptor antagonist rimonabant reverses the diet-induced obesity phenotype through the regulation of lipolysis and energy balance. FASEB J 2005; 19(11):1567-9.
16. Bensaid M, Gary-Bobo M, Esclangon A, Maffrand JP, Le Fur G, Oury-Donat F, et al. The cannabinoid CB1 receptor antagonist SR141716 increases Acrp30 mRNA expression in adipose tissue of obese fa/fa rats and in cultured adipocyte cells. Mol Pharmacol 2003;63(4):908-14.
17. Després JP, Golay A, Sjöström L, for the RIO-Lipids study group. Effect of rimonabant on body weight and the metabolic syndrome in overweight patients. N Engl J Med 2005;353:2121-34.
18. Kanamaluru V, Lockwood G, Bonnet D, Newton J. Lack of effect of rimonabant on the pharmacokinetics of digoxin. J Clin Pharmacol 2005;49(9):1081.
19. Kanamaluru V, Lockwood G, Bonnet D, Newton J. Lack of effect of rimonabant on the pharmacokinetics of oral contraceptives. J Clin Pharmacol 2005;45(9):1081.
20. Grandison M, Kanamaluru V, Lockwood G, Bonnet D, Newton J. Lack of rimonabant on the pharmacokinetics and pharmacodynamics of warfarin. J Clin Pharmacol 2005;45(9):1082.
21. Grandison M, Kanamaluru V, Lockwood G, Bonnet D, Newton J. Lack of effect of rimonabant on the pharmacokinetics of midazolam. J Clin Pharmacol 2005;45(9):1082.
22. Di Marzo V, Goparaju SK, Wang L, Liu J, Batkai S, Jarai Z, et al. Leptin-regulated endocannabinoids are involved in maintaining food intake. Nature 2001;410(6830):822-5.
23. Hilairet S, Bouaboula M, Carriere D, Le Fur G, Casellas P. Hypersensitization of the Orexin 1 receptor by the CB1 receptor: evidence for cross-talk blocked by the specific CB1 antagonist, SR141716. J Biol Chem 2003;278(26):23731-7.
24. Gomez R, Navarro M, Ferrer B, Trigo JM, Bilbao A, Del Arco I, et al. A peripheral mechanism for CB1 cannabinoid receptor-dependent modulation of feeding. J Neurosci 2002;22(21):9612-7.
25. Lichtman AH, Cravatt BF. Food for thought: endocannabinoid modulation of lipogenesis. J Clin Invest 2005;115(5): 1130-3.
26. Liu Y, Connoley I, Wilson C, Stock M. Effects of the cannabinoid CB1 receptor antagonist SR141716 on oxygen consumption and soleus muscle glucose uptake in Lepob/Lepob mice. Int J Obes Relat Metab Disord 2005;29(2):183-7.
27. Ravinet Trillou C, Delgorge C, Menet C, Arnone M, Soubrie P. CB1 cannabinoid receptor knockout in mice leads to leanness, resistance to diet-induced obesity and enhanced leptin sensitivity. Int J Obes Relat Metab Disord 2004;28(4):640-8.
28. Osei-Hyiaman D, DePetrillo M, Pacher P, Liu J, Radaeva S, Batkai S, et al. Endocannabinoid activation at hepatic CB1 receptors stimulates fatty acid synthesis and contributes to diet-induced obesity. J Clin Invest 2005;115(5):1298-305.
29. Harrold JA, Williams G. The cannabinoid system: a role in both the homeostatic and hedonic control of eating? Br J Nutr 2003;90(4):729-34.
30. Ravinet Trillou C, Arnone M, Delgorge C, Gonalons N, Keane P, Maffrand JP, et al. Anti-obesity effect of SR141716, a CB1 receptor antagonist, in diet-induced obese mice. Am J Physiol Regul Integr Comp Physiol 2003;284(2):R345-53.
31. Corrigall WA, Franklin KB, Coen KM, Clarke PB. The mesolimbic dopaminergic system is implicated in the reinforcing effects of nicotine. Psychopharmacology (Berl) 1992;107(2-3):285-9.
32. Pontieri FE, Tanda G, Orzi F, Di Chiara G. Effects of nicotine on the nucleus accumbens and similarity to those of addictive drugs. Nature 1996;382(6588):255-7.
33. Cohen C, Perrault G, Voltz C, Steinberg R, Soubrie P. SR141716, a central cannabinoid (CB(1)) receptor antagonist, blocks the motivational and dopamine-releasing effects of nicotine in rats. Behav Pharmacol 2002;13(5-6):451-63.
34. Mascia MS, Obinu MC, Ledent C, Parmentier M, Bohme GA, Imperato A, et al. Lack of morphine-induced dopamine release in the nucleus accumbens of cannabinoid CB(1) receptor knockout mice. Eur J Pharmacol 1999;383(3):R1-2. doi:10.1016/S0014-2999(99)00656-1.
35. Castane A, Valjent E, Ledent C, Parmentier M, Maldonado R, Valverde O. Lack of CB1 cannabinoid receptors modifies nicotine behavioural responses, but not nicotine abstinence. Neuropharmacology 2002;43(5):857-67. doi:10.1016/S0028-3908(02)00118-1.
36. Ledent C, Valverde O, Cossu G, Petitet F, Aubert JF, Beslot F, et al. Unresponsiveness to cannabinoids and reduced addictive effects of opiates in CB1 receptor knockout mice. Science 1999;283(5400):401-4.
37. Gonzalez S, Cascio MG, Fernandez-Ruiz J, Fezza F, Di Marzo V, Ramos JA. Changes in endocannabinoid contents in the brain of rats chronically exposed to nicotine, ethanol or cocaine. Brain Res 2002;954(1):73-81. doi:10.1016/S0006- 8993(02)03344-9).
38. Cohen C, Perrault G, Griebel G, Soubrie P. Nicotine-associated cues maintain nicotine-seeking behavior in rats several weeks after nicotine withdrawal: reversal by the cannabinoid (CB1) receptor antagonist, rimonabant (SR141716). Neuropsychopharmacology 2005;30(1):145-55.
39. Fernandez JR, Allison DB. Rimonabant Sanofi-Synthelabo. Curr Opin Investig Drugs 2004;5(4):430-5.
40. Pi-Sunyer F.X., Marbury T.C., Garland W.T., et al., The selective CB1-receptor antagonist rimonabant reduces body weight and waist circumference in obese subjects. In: 86th Annual Meeting of the Endocrine Society 2004. New Orleans, USA; 2004.
41. Van Gaal LF, Rissanen AM, Scheen AJ, Ziegler O, Rössner S. 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. Lancet 2005;365(9468): 1389-97. doi:10.1016/S0140-6736(05) 66374-X.
42. Scheen A. Rimonabant in patients with type 2 diabetes: results from the RIO-Diabetes Trial. In: In: 65th Scientific Sessions of the American Diabetes Association. San Diego, CA, USA.: American Diabetes Congress (ADA); June 2005. p. 10-4.
43. Anthenelli R, Dale L. Rimonabant helps cigarette smokers stop smoking and prevents post cessation weight gain: results from the STRATUS-US trial. In: Final Program and Abstracts of 6th Annual Conference of the SRNT Europe; Tübingen, Germany; 2004. p. 35.
44. Lakka HM, Laaksonen DE, Lakka TA, Niskanen LK, Kumpusalo E, Tuomilehto J, et al. The metabolic syndrome and total and cardiovascular disease mortality in middle-aged men. JAMA 2002;288(21):2709-16.
45. Koh-Banerjee P, Chu NF, Spiegelman D, Rosner B, Colditz G, Willett W, et al. Prospective study of the association of changes in dietary intake, physical activity, alcohol consumption, and smoking with 9-y gain in waist circumference among 16587 US men. Am J Clin Nutr 2003;78(4):719-27.