The endocannabinoid system: Potential for reducing cardiometabolic risk

Obesity

Volumn 17, Issue 10, 2009, Pages 1821-1829

  Ginsberg, Henry N ^a   Woods, Stephen C ^b  

^a Surgeons of Columbia University ^*  (United States)

^b UNIVERSITY OF CINCINNATI COLLEGE OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CANNABINOID RECEPTOR; ENDOCANNABINOID; PIPERIDINE DERIVATIVE; PYRAZOLE DERIVATIVE; RIMONABANT;

ANIMAL; DRUG ANTAGONISM; HUMAN; METABOLISM; MOUSE; OBESITY; REVIEW;

ANIMALS; ENDOCANNABINOIDS; HUMANS; MICE; OBESITY; PIPERIDINES; PYRAZOLES; RECEPTORS, CANNABINOID;

EID: 70349488868     PISSN: 19307381     EISSN: 1930739X     Source Type: Journal    
DOI: 10.1038/oby.2009.107     Document Type: Review

References (95)

1. Clinical Guidelines on the Identification, Evaluation, and Treatment of Overweight and Obesity in Adults - The Evidence Report. National Institutes of Health. National Institutes of Health. Obes Res 1998;6(Suppl 2):51S-209S.
2. Leibel RL, Rosenbaum M, Hirsch J. Changes in energy expenditure resulting from altered body weight. N Engl J Med 1995;332:621-628.
3. Rosenbaum M, Vandenborne K, Goldsmith R et al. Effects of experimental weight perturbation on skeletal muscle work efficiency in human subjects. Am J Physiol Regul Integr Comp Physiol 2003;285:R183-R192.
4. Gong Y, Ishida-Takahashi R, Villanueva EC et al. The long form of the leptin receptor regulates STAT5 and ribosomal protein S6 via alternate mechanisms. J Biol Chem 2007;282:31019-31027.
5. Morton GJ, Cummings DE, Baskin DG, Barsh GS, Schwartz MW. Central nervous system control of food intake and body weight. Nature 2006;443:289-295.
6. Woods SC, D'Alessio DA. Central control of body weight and appetite. J Clin Endocrinol Metab 2008;93:S37-S50.
7. Cota D. Role of the endocannabinoid system in energy balance regulation and obesity. Front Horm Res 2008;36:135-145.
8. Pi-Sunyer FX. Use of lifestyle changes treatment plans and drug therapy in controlling cardiovascular and metabolic risk factors. Obesity (Silver Spring) 2006;14(Suppl 3):135S-142S.
9. Aronne LJ, Thornton-Jones ZD. New targets for obesity pharmacotherapy. Clin Pharmacol Ther 2007;81:748-752.
10. Di Marzo V. The endocannabinoid system in obesity and type 2 diabetes. Diabetologia 2008;51:1356-1367.
11. Devane WA, Hanus L, Breuer A et al. Isolation and structure of a brain constituent that binds to the cannabinoid receptor. Science 1992;258:1946-1949.
12. Sugiura T, Kondo S, Sukagawa A et al. 2-Arachidonoylglycerol: a possible endogenous cannabinoid receptor ligand in brain. Biochem Biophys Res Commun 1995;215:89-97.
13. Di Marzo V. Endocannabinoids: synthesis and degradation. Rev Physiol Biochem Pharmacol 2008;160:1-24.
14. Placzek EA, Okamoto Y, Ueda N, Barker EL. Membrane microdomains and metabolic pathways that define anandamide and 2-arachidonyl glycerol biosynthesis and breakdown. Neuropharmacology 2008;55:1095-1104.
15. Sugiura T, Kodaka T, Nakane S et al. Evidence that the cannabinoid CB1 receptor is a 2-arachidonoylglycerol receptor. Structure-activity relationship of 2-arachidonoylglycerol, ether-linked analogues, and related compounds. J Biol Chem 1999;274:2794-2801.
16. Heimann AS, Gomes I, Dale CS et al. Hemopressin is an inverse agonist of CB1 cannabinoid receptors. Proc Natl Acad Sci USA 2007;104:20588-20593.
17. Kunos G, Osei-Hyiaman D. Endocannabinoids and liver disease. I V. Endocannabinoid involvement in obesity and hepatic steatosis. Am J Physiol Gastrointest Liver Physiol 2008;294:G1101-G1104.
18. Svízenská I, Dubový P, Sulcová A. Cannabinoid receptors 1 and 2 (CB1 and CB2), their distribution, ligands and functional involvement in nervous system structures - a short review. Pharmacol Biochem Behav 2008;90:501-511.
19. Juan-Picó P, Fuentes E, Bermúdez-Silva FJ et al. Cannabinoid receptors regulate Ca(2+) signals and insulin secretion in pancreatic beta-cell. Cell Calcium 2006;39:155-162.
20. Klein TW. Cannabinoid-based drugs as anti-inflammatory therapeutics. Nat Rev Immunol 2005;5:400-411.
21. Shimizu T. Lipid mediators in health and disease: enzymes and receptors as therapeutic targets for the regulation of immunity and inflammation. Annu Rev Pharmacol Toxicol 2009;49:123-150.
22. Basavarajappa BS. Critical enzymes involved in endocannabinoid metabolism. Protein Pept Lett 2007;14:237-246.
23. Kano M, Ohno-Shosaku T, Hashimotodani Y, Uchigashima M, Watanabe M. Endocannabinoid-mediated control of synaptic transmission. Physiol Rev 2009;89:309-380.
24. Kawamura Y, Fukaya M, Maejima T et al. The CB1 cannabinoid receptor is the major cannabinoid receptor at excitatory presynaptic sites in the hippocampus and cerebellum. J Neurosci 2006;26:2991-3001.
25. Tasker JG. Rapid glucocorticoid actions in the hypothalamus as a mechanism of homeostatic integration. Obesity (Silver Spring) 2006;14(Suppl 5):259S-265S.
26. Kirkham TC, Williams CM, Fezza F, Di Marzo V. Endocannabinoid levels in rat limbic forebrain and hypothalamus in relation to fasting, feeding and satiation: stimulation of eating by 2-arachidonoyl glycerol. Br J Pharmacol 2002;136:550-557.
27. Colombo G, Agabio R, Diaz G et al. Appetite suppression and weight loss after the cannabinoid antagonist SR 141716. Life Sci 1998;63:PL113-PL117.
28. Di Marzo V, Goparaju SK, Wang L et al. Leptin-regulated endocannabinoids are involved in maintaining food intake. Nature 2001;410:822-825.
29. Osei-Hyiaman D, DePetrillo M, Pacher P et al. Endocannabinoid activation at hepatic CB1 receptors stimulates fatty acid synthesis and contributes to diet-induced obesity. J Clin Invest 2005;115:1298-1305.
30. Pavon FJ, Bilbao A, Hernández-Folgado L et al. Antiobesity effects of the novel in vivo neutral cannabinoid receptor antagonist 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-hexyl-1H-1,2,4-triazole--LH 21. Neuropharmacology 2006;51:358-366.
31. Gary-Bobo M, Elachouri G, Gallas JF et al. Rimonabant reduces obesity-associated hepatic steatosis and features of metabolic syndrome in obese Zucker fa/fa rats. Hepatology 2007;46:122-129.
32. Bensaid M, Gary-Bobo M, Esclangon A 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;63:908-914.
33. Wiley JL, Burston JJ, Leggett DC et al. CB1 cannabinoid receptor-mediated modulation of food intake in mice. Br J Pharmacol 2005;145:293-300.
34. Solinas M, Goldberg SR, Piomelli D. The endocannabinoid system in brain reward processes. Br J Pharmacol 2008;154: 369-383.
35. Salamone JD, McLaughlin PJ, Sink K, Makriyannis A, Parker LA. Cannabinoid CB1 receptor inverse agonists and neutral antagonists: effects on food intake, food-reinforced behavior and food aversions. Physiol Behav 2007;91:383-388.
36. Verty AN, McGregor IS, Mallet PE. Consumption of high carbohydrate, high fat, and normal chow is equally suppressed by a cannabinoid receptor antagonist in non-deprived rats. Neurosci Lett 2004;354: 217-220.
37. Mathes CM, Ferrara M, Rowland NE. Cannabinoid-1 receptor antagonists reduce caloric intake by decreasing palatable diet selection in a novel dessert protocol in female rats. Am J Physiol Regul Integr Comp Physiol 2008;295:R67-R75.
38. Melis T, Succu S, Sanna F et al. The cannabinoid antagonist SR 141716A (Rimonabant) reduces the increase of extracellular dopamine release in the rat nucleus accumbens induced by a novel high palatable food. Neurosci Lett 2007;419:231-235.
39. DiPatrizio NV, Simansky KJ. Activating parabrachial cannabinoid CB1 receptors selectively stimulates feeding of palatable foods in rats. J Neurosci 2008;28:9702-9709.
40. Dipatrizio N V, Simansky KJ. Inhibiting parabrachial fatty acid amide hydrolase activity selectively increases the intake of palatable food via cannabinoid CB1 receptors. Am J Physiol Regul Integr Comp Physiol 2008;295:R1409-R1414.
41. Cota D, Marsicano G, Tschöp M et al. The endogenous cannabinoid system affects energy balance via central orexigenic drive and peripheral lipogenesis. J Clin Invest 2003;112:423-431.
42. Ravinet Trillou C, Delgorge C, Menet C, Arnone M, Soubrié 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;28:640-648.
43. Thornton-Jones ZD, Kennett GA, Benwell KR et al. The cannabinoid CB1 receptor inverse agonist, rimonabant, modifies body weight and adiponectin function in diet-induced obese rats as a consequence of reduced food intake. Pharmacol Biochem Behav 2006;84:353-359.
44. Vickers S P, Webster LJ, Wyatt A, Dourish CT, Kennett GA. Preferential effects of the cannabinoid CB1 receptor antagonist, SR 141716, on food intake and body weight gain of obese (fa/fa) compared to lean Zucker rats. Psychopharmacology (Berl) 2003;167:103-111.
45. Matias I, Gonthier M P, Orlando P et al. Regulation, function, and dysregulation of endocannabinoids in models of adipose and beta-pancreatic cells and in obesity and hyperglycemia. J Clin Endocrinol Metab 2006;91:3171-3180.
46. Viveros M P, de Fonseca FR, Bermudez-Silva FJ, McPartland JM. Critical role of the endocannabinoid system in the regulation of food intake and energy metabolism, with phylogenetic, developmental, and pathophysiological implications. Endocr Metab Immune Disord Drug Targets 2008;8:220-230.
47. Burdyga G, Lal S, Varro A et al. Expression of cannabinoid CB1 receptors by vagal afferent neurons is inhibited by cholecystokinin. J Neurosci 2004;24:2708-2715.
48. Cummings DE, Weigle DS, Frayo RS et al. Plasma ghrelin levels after diet-induced weight loss or gastric bypass surgery. N Engl J Med 2002;346:1623-1630.
49. Kola B, Farkas I, Christ-Crain M et al. The orexigenic effect of ghrelin is mediated through central activation of the endogenous cannabinoid system. PLoS ONE 2008;3:e1797.
50. Tucci SA, Rogers EK, Korbonits M, Kirkham TC. The cannabinoid CB1 receptor antagonist SR141716 blocks the orexigenic effects of intrahypothalamic ghrelin. Br J Pharmacol 2004;143:520-523.
51. Gary-Bobo M, Elachouri G, Scatton B et al. The cannabinoid CB1 receptor antagonist rimonabant (SR141716) inhibits cell proliferation and increases markers of adipocyte maturation in cultured mouse 3T3 F442A preadipocytes. Mol Pharmacol 2006;69:471-478.
52. Pagano C, Pilon C, Calcagno A et al. The endogenous cannabinoid system stimulates glucose uptake in human fat cells via phosphatidylinositol 3-kinase and calcium-dependent mechanisms. J Clin Endocrinol Metab 2007;92:4810-4819.
53. Pagano C, Rossato M, Vettor R. Endocannabinoids, adipose tissue and lipid metabolism. J Neuroendocrinol 2008;20(Suppl 1):124-129.
54. Jbilo O, Ravinet-Trillou C, Arnone M 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: 1567-1569.
55. Kunz I, Meier MK, Bourson A, Fisseha M, Schilling W. Effects of rimonabant, a cannabinoid CB1 receptor ligand, on energy expenditure in lean rats. Int J Obes (Lond) 2008;32:863-870.
56. Addy C, Wright H, Van Laere K et al. The acyclic CB1R inverse agonist taranabant mediates weight loss by increasing energy expenditure and decreasing caloric intake. Cell Metab 2008;7:68-78.
57. Côté M, Matias I, Lemieux I et al. Circulating endocannabinoid levels, abdominal adiposity and related cardiometabolic risk factors in obese men. Int J Obes (Lond) 2007;31: 692-699.
58. Di Marzo V, Côté M, Matias I et al. 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. Diabetologia 2009;52:213-217.
59. Engeli S, Böhnke J, Feldpausch M et al. Activation of the peripheral endocannabinoid system in human obesity. Diabetes 2005;54:2838-2843.
60. Sipe JC, Waalen J, Gerber A, Beutler E. Overweight and obesity associated with a missense polymorphism in fatty acid amide hydrolase (FAAH). Int J Obes (Lond) 2005;29:755-759.
61. Jensen D P, Andreasen CH, Andersen MK et al. The functional Pro129Thr variant of the FAAH gene is not associated with various fat accumulation phenotypes in a population-based cohort of 5,801 whites. J Mol Med 2007;85:445-449.
62. Russo P, Strazzullo P, Cappuccio FP et al. Genetic variations at the endocannabinoid type 1 receptor gene (CNR1) are associated with obesity phenotypes in men. J Clin Endocrinol Metab 2007;92:2382-2386.
63. Monteleone P, Matias I, Martiadis V et al. Blood levels of the endocannabinoid anandamide are increased in anorexia nervosa and in binge-eating disorder, but not in bulimia nervosa. Neuropsychopharmacology 2005;30:1216-1221.
64. Kunos G, Osei-Hyiaman D. Endocannabinoids and liver disease. IV. Endocannabinoid involvement in obesity and hepatic steatosis. Am J Physiol Gastrointest Liver Physiol 2008;294:G1101-G1104.
65. Muñoz-Luque J, Ros J, Fernández-Varo G et al. Regression of fibrosis after chronic stimulation of cannabinoid CB2 receptor in cirrhotic rats. J Pharmacol Exp Ther 2008;324:475-483.
66. Jeong WI, Osei-Hyiaman D, Park O et al. Paracrine activation of hepatic CB1 receptors by stellate cell-derived endocannabinoids mediates alcoholic fatty liver. Cell Metab 2008;7:227-235.
67. Osei-Hyiaman D, Liu J, Zhou L et al. Hepatic CB1 receptor is required for development of diet-induced steatosis, dyslipidemia, and insulin and leptin resistance in mice. J Clin Invest 2008;118:3160-3169.
68. Kunos G, Osei-Hyiaman D, Bátkai S, Sharkey KA, Makriyannis A. Should peripheral CB(1) cannabinoid receptors be selectively targeted for therapeutic gain? Trends Pharmacol Sci 2009;30:1-7.
69. Bergman RN, Kim SP, Hsu IR et al. Abdominal obesity: role in the pathophysiology of metabolic disease and cardiovascular risk. Am J Med 2007;120(2 Suppl 1):S3-S8; discussion S29-S32.
70. Ravinet Trillou C, Arnone M, Delgorge C 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:R345-R353.
71. Liu YL, Connoley IP, Wilson CA, Stock MJ. Effects of the cannabinoid CB1 receptor antagonist SR141716 on oxygen consumption and soleus muscle glucose uptake in Lep(ob)/Lep(ob) mice. Int J Obes (Lond) 2005;29:183-187.
72. Trujillo ME, Scherer PE. Adiponectin--journey from an adipocyte secretory protein to biomarker of the metabolic syndrome. J Intern Med 2005;257:167-175.
73. Combs T P, Berg AH, Obici S, Scherer PE, Rossetti L. Endogenous glucose production is inhibited by the adipose-derived protein Acrp30. J Clin Invest 2001;108: 1875-1881.
74. Poirier B, Bidouard J P, Cadrouvele C et al. The anti-obesity effect of rimonabant is associated with an improved serum lipid profile. Diabetes Obes Metab 2005;7:65-72.
75. Lofgren P, Sjolin E, Wahlen K, Hoffstedt J. Human adipose tissue cannabinoid receptor 1 gene expression is not related to fat cell function or adiponectin level. J Clin Endocrinol Metab 2007;92:1555-1559.
76. Watanabe T, Kubota N, Ohsugi M et al. Rimonabant ameliorates insulin resistance via both adiponectin-dependent and adiponectin-independent pathways. J Biol Chem 2009;284:1803-1812.
77. Boyd ST, Fremming BA. Rimonabant - a selective CB1 antagonist. Ann Pharmacother 2005;39:684-690.
78. Pi-Sunyer FX, Aronne LJ, Heshmati HM, Devin J, Rosenstock J. Effect of rimonabant, a cannabinoid-1 receptor blocker, on weight and cardiometabolic risk factors in overweight or obese patients: RIO-North America: a randomized controlled trial. JAMA 2006;295:761-775.
79. Després J P, Golay A, Sjöström L. Effects of rimonabant on metabolic risk factors in overweight patients with dyslipidemia. N Engl J Med 2005;353:2121-2134.
80. Scheen AJ, Finer N, Hollander P, Jensen MD, Van Gaal L F. Efficacy and tolerability of rimonabant in overweight or obese patients with type 2 diabetes: a randomised controlled study. Lancet 2006;368:1660-1672.
81. 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;365:1389-1397. (Pubitemid 40523733)
82. Gadde KM, Allison DB. Cannabinoid-1 receptor antagonist, rimonabant, for management of obesity and related risks. Circulation 2006;114:974-984.
83. Van Gaal L, Pi-Sunyer X, Després JP, McCarthy C, Scheen A. Efficacy and safety of rimonabant for improvement of multiple cardiometabolic risk factors in overweight/ obese patients: pooled 1-year data from the Rimonabant in Obesity (RIO) program. Diabetes Care 2008;31(Suppl 2):S229-S240.
84. Bray GA. Etiology and pathogenesis of obesity. Clin Cornerstone 1999;2:1-15.
85. Finer N, Pagotto U. The endocannabinoid system: a new therapeutic target for cardiovascular risk factor management. Br J Diabetes Vasc Dis 2005;5:121-124.
86. Food and Drug Administration. FDA Briefing Document. NDA 21-888. Zimulti (rimonabant) tablets, 20 mg. Sanofi Aventis. Advisory Committee, 13 June 2007. http://www.fda. gov/ohrms/dockets/AC/07/briefing/2007-4306b1-fda-backgrounder. pdf. Accessed 9 August 2007.
87. Curioni C, André C. Rimonabant for overweight or obesity. Cochrane Database Syst Rev 2006:CD006162.
88. Carr R, Erondu N, Gonzalez C et al. Effects of taranabant, a novel cannabinoid 1 receptor (CB-1R) inverse agonist, on weight reduction in obese patients over 12 weeks. Atherosclerosis Suppl 2008;9:209.
89. Carr R, Gantz I, Erondu N et al. A two-year study to assess the efficacy, safety, and tolerability of taranabant in obese patients: 52 week results. Atherosclerosis Suppl 2008;9:12.
90. European Medicines Agency recommends acomplia must not be used in patients on antidepressants or with major depression. Medical News Today, 21 July 2007. http://www.medicalnewstoday.com.
91. European Medicines Agency. The committee for medicinal products for human use: summary of product characteristics (acomplia). Approved 19 July 2007.
92. Jones D. End of the line for cannabinoid receptor 1 as an anti-obesity target? Nat Rev Drug Discov 2008;7:961-962.
93. Nissen SE, Nicholls SJ, Wolski K et al. Effect of rimonabant on progression of atherosclerosis in patients with abdominal obesity and coronary artery disease: the STRADIVARIUS randomized controlled trial. JAMA 2008;299:1547-1560.
94. Di Marzo V. Play an ADAGIO with a STRADIVARIUS: the right patient for CB1 receptor antagonists? Nat Clin Pract Cardiovasc Med 2008;5:610-612.
95. Di Marzo V, Bifulco M, De Petrocellis L. The endocannabinoid system and its therapeutic exploitation. Nat Rev Drug Discov 2004;3:771-784.