The endocannabinoid system and the treatment of obesity

Annals of Medicine

Volumn 37, Issue 4, 2005, Pages 270-275

  Pagotto, Uberto ^a   Vicennati, Valentina ^a   Pasquali, Renato ^a  

^a UNIVERSITY OF BOLOGNA   (Italy)

Author keywords

CB1 receptor; Endocannabinoid system; Obesity; Rimonabant

Indexed keywords

1 (2,4 DICHLOROPHENYL) 5 (4 IODOPHENYL) 4 METHYL N (1 PIPERIDYL) 1H PYRAZOLE 3 CARBOXAMIDE; 5 (4 BROMOPHENYL) 1 (2,4 DICHLOROPHENYL) 4 ETHYL N (1 PIPERIDYL) 1H PYRAZOLE 3 CARBOXAMIDE; ADIPONECTIN; CANNABINOID 1 RECEPTOR; CANNABINOID 2 RECEPTOR; CANNABINOID RECEPTOR ANTAGONIST; CANNABIS; DOPAMINE; ENDOCANNABINOID; FATTY ACID; G PROTEIN COUPLED RECEPTOR; PLACEBO; RIMONABANT; TETRAHYDROCANNABINOL; UNCLASSIFIED DRUG;

ADIPOCYTE; ADIPOSE TISSUE; BINDING AFFINITY; BODY MASS; BODY WEIGHT; CARDIOVASCULAR RISK; CLINICAL TRIAL; DOPAMINE RELEASE; DRUG RECEPTOR BINDING; ENERGY BALANCE; FATTY ACID METABOLISM; FATTY ACID OXIDATION; FOOD INTAKE; GASTROINTESTINAL TRACT; HUMAN; HYPOTHALAMUS; LIMBIC SYSTEM; LIPOGENESIS; MEDIATOR RELEASE; NONHUMAN; NUCLEUS ACCUMBENS; OBESITY; PATHOGENESIS; PRIORITY JOURNAL; PROTEIN FAMILY; PROTEIN LOCALIZATION; PROTEIN SYNTHESIS; RECEPTOR BLOCKING; RECEPTOR INTRINSIC ACTIVITY; RECEPTOR UPREGULATION; REVIEW; THERMOGENESIS; TREATMENT OUTCOME;

ADIPOCYTES; APPETITE DEPRESSANTS; EATING; ENDOCANNABINOIDS; HUMANS; OBESITY; RECEPTOR, CANNABINOID, CB1;

EID: 21344453761     PISSN: 07853890     EISSN: None     Source Type: Journal    
DOI: 10.1080/07853890510037419     Document Type: Review

References (59)

1. Abel EL. Cannabis: effects on hunger and thirst. Behav Biol. 1975;15:255-81.
2. Gaoni Y, Mechoulam R. Isolation, structure and partial synthesis of an active constituent of hashish. J Am Chem Soc. 1964;86:1646-7.
3. Matsuda LA, Lolait SJ, Brownstein MJ, Young AC, Bonner TI. Structure of a cannabinoid receptor and functional expression of the cloned cDNA. Nature. 1990;346:561-4.
4. 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;258:1946-9.
5. Munro S, Thomas KL, Abu-Shaar M. Molecular characterization of a peripheral receptor for cannabinoids. Nature. 1993;365:61-5.
6. Hewlett AC, Glass M, Dragunow M, Faull RL. Cannabinoid receptors in the human brain: a detailed anatomical and quantitative autoradiographic study in the fetal, neonatal and adult human brain. Neuroscience. 1997;77:299-318.
7. Batkai S, Jarai Z, Wagner JA, Goparaju SK, Varga K, Liu J, et al. Endocannabinoids acting at vascular CB1 receptors mediate the vasodilated state in advanced liver cirrhosis. Nat Med. 2001;7:827-32.
8. Pagotto U, Marsicano G, Fezza F, Theodoropoulou M, Grübler Y, Stalla J, et al. Normal human pituitary gland and pituitary adenomas express cannabinoid receptor type 1 and synthesize endogenous cannabinoids: first evidence for a direct role of cannabinoids on hormone modulation at the human pituitary level. J Clin Endocrinol Metab. 2001;86:2687-96.
9. Hewlett AC, Barth F, Bonner TI, Cabral G, Casellas P, Devane WA, et al. International Union of Pharmacology. XXVII. Classification of cannabinoid receptors. Pharmacol Rev. 2002;54:161-202.
10. Cota D, Marsicano G, Tschoep M, Gruebler 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;112:423-31.
11. Bensaid M, Gary-Bobo M, Esclangon A, Maffrand JP, Le Fur G, Oury-Donat F, Soubrié P. 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;63:908-14.
12. Pertwee RG. Pharmacology of cannabinoid CB1 and CB2 receptors. Pharmacol Ther. 1997;74:129-80.
13. Hanus L, Gopher A, Almog S, Mechoulam R. Two new unsaturated fatty acid ethanolamides in brain that bind to the cannabinoid receptor. J Med Chem. 1993;36:3032-4.
14. Sugiura T, Kondo S, Sukagawa A, Nakane S, Shinoda A, Itoh K, et al. 2-Arachidonoylglycerol: a possible endogenous cannabinoid receptor ligand in brain. Biochem Biophys Res Commun. 1995;215:89-97.
15. Mechoulam R, Ben Shabat S, Hanus L, Ligumsky M, Kaminski NE, Schatz AR, et al. Identification of an endogenous 2-monoglyceride, present in canine gut, that binds to cannabinoid receptors. Biochem Pharmacol. 1995;50:83-90.
16. Di Marzo V, Fontana A, Cadas H, Schinelli S, Cimino G, Schwartz JC, et al. Formation and inactivation of endogenous cannabinoid anandamide in central neurons. Nature. 1994;372:686-91.
17. Dinh TP, Carpenter D, Leslie FM, Freund TF, Katona I, Sensi SL, et al. Brain monoglyceride lipase participating in endocannabinoid inactivation. Proc Natl Acad Sci U S A. 2002;99:10819-24.
18. Di Marzo V, Melck D, Bisogno T, De Petrocellis L. Endocannabinoids: endogenous cannabinoid receptor ligands with neuromodulatory action. Trends Neurosci. 1998;21:521-8.
19. Piomelli D, Giuffrida A, Calignano A, Rodriguez De Fonseca F. The endocannabinoid system as a target for therapeutic drugs. Trends Pharmacol Sci. 2000;21:218-24.
20. De Petrocellis L, Cascio MG, Di Marzo V. The endocannabinoid system: a general view and latest additions. Br J Pharmacol. 2004;141:765-74.
21. Hanus L, Avraham Y, Ben-Shushan D, Zolotarev O, Berry EM, Mechoulam R. Short-term fasting and prolonged semistarvation have opposite effects on 2-AG levels in mouse brain. Brain Res. 2003;983:144-51.
22. Plasse TF, Gorter RW, Krasnow SH, Lane M, Shepard KV, Wadleigh RG. Recent clinical experience with dronabinol. Pharmacol Biochem Behav. 1991;40:695-700.
23. Gorter R, Seefried M, Volberding P. Dronabinol effects on weight in patients with HIV infection. AIDS. 1992;6:127.
24. Beal JE, Olson R, Lefkowitz L, Laubenstein L, Bellman P, Yangco B, et al. Long-term efficacy and safety of dronabinol for acquired immunodeficiency syndrome-associated anorexia. J Pain Symptom Manage. 1997;14:7-14.
25. Rinaldi-Carmona M, Barth F, Héaulme M, Shire D, Calandra B, Congy C, et al. SR141716A, a potent and selective antagonist of the brain cannabinoid receptor. FEBS Lett. 1994;350:240-4.
26. Berridge KC. Food reward: brain substrates of wanting and liking. Neurosci Biobehav Rev. 1996;20:1-25.
27. Herkenham M, Lynn AB, Johnson MR, Melvin LD, de Costa BR, Rice KC. Characterization and localization of cannabinoid receptors in rat brain: a quantitative in vitro autoradiographic study. J Neurosci. 1991;11:563-83.
28. Kirkham TC, Williams C. Synergistic effects of opioid and cannabinoid antagonists on food intake. Psychopharmacology (Berl). 2001;153:267-70.
29. Verty ANA, Singh ME, McGregor IS, Mallet PE. The cannabinoid receptor anatgonist SR141716 attenuates overfeeding induced by systemic or intracranial morphine. Psychopharmacology (Berl). 2003;168:314-23.
30. Verty ANA, McGregor IS, Mallet PE. The dopamine receptor antagonist SCH 23390 attenuates feeding induced by Δ9-tetrahydrocannabinol. Brain Res. 2004;1020:188-95.
31. Higgs S, Williams CM, Kirkham TC. Cannabinoid influences on palatability: microstructural analysis of sucrose drinking after delta(9)- tetrahydrocannabinol, anandamide, 2-arachidonoyl glycerol and SR141716. Psychopharmacology (Berl). 2003;165:370-7.
32. Kirkham TC, Williams CM. Endogenous cannabinoids and food appetite. Nutr Res Rev. 2001;14:65-86.
33. Freedland CS, Poston JS, Porrino LJ. Effects of SR141716, a central cannabinoid receptor antagonist, on food-maintained responding. Pharmacol Biochem Behav. 2000;67:265-70.
34. Perio A, Barnouin MC, Poncelet M, Soubrié P. Activity of SR141716 on post-reinforcement pauses in operant responding for sucrose reward in rats. Behav Pharmacol. 1998;12:641-6.
35. Arnone M, Maruani J, Chaperon F, Thiebot MH, Poncelet M, Soubrié P, et al. Selective inhibition of sucrose and ethanol intake by SR141716, an antagonist of central cannabinoid (CB1) receptors. Psychopharmacology (Berl). 1997;132:104-6.
36. Simiand J, Keane M, Keane PE, Soubrié P. CB1 cannabinoid receptor antagonist, selectively reduces sweet food intake in marmoset. Behav Pharmacol. 2001;9:179-81.
37. Sanchis-Segura C, Cline BH, Marsicano G, Lutz B, Spanagel R. Reduced sensitivity to reward in CB1 knockout mice. Psychopharmacology (Berl). 2004;176:223-32.
38. 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;136:550-7.
39. Flier JS. Obesity wars: molecular progress confronts an expanding epidemic. Cell. 2004;116:337-50.
40. Jamshidi N, Taylor DA. Anandamide administration into the ventromedial hypothalamus stimulates appetite in rats. Br J Pharmacol. 2001;134:1151-4.
41. 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;410:822-5.
42. Ravinet Trillou C, Delgorge C, Mener 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. 2004;28:640-8.
43. 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:R345-53.
44. Gil-Campos M, Canete R, Gil A. Adiponectin, the missing link in insulin resistance and obesity. Clin Nutr. 2004;23:963-74.
45. Chandran M, Phillips SA, Ciaraldi T, Henry RR. Adiponectin: more than just another fat cell hormone? Diabetes Care. 2003;26:2442-50.
46. ob mice. Int J Obes. 2005;29:183-7.
47. Tzavara ET, Perry KW, Rodriguez DE, Bymaster FP, Nomikos GG. The cannabinoid CB1 receptor antagonist SR141716A increases norepinephrine outflow in the rat anterior hypothalamus. Eur J Pharmacol. 2001;426:R3-4.
48. 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;22:9612-7.
49. Burdyga G, Lal S, Varro A, Dimaline R, Thompson DG, Dockray GJ. Expression of cannabinoid CB1 receptors by vagal afferent neurons is inhibited by cholecystokinin. J Neurosci. 2004;24:2708-11.
50. Hildebrandt AL, Kelly-Sullivan DM, Black SC. Antiobesity effects of chronic cannabinoid CB1 receptor antagonist treatment in diet-induced obese mice. Eur J Pharmacol. 2003;462:125-32.
51. Zhou D, Shearman LP. Voluntary exercise augments acute effects of CB1-receptor inverse agonist on body weight loss in obese and lean mice. Pharmacol Biochem Behav. 2004;77:117-25.
52. Chambers AP, Sharkey KA, Koopmans HS. Cannabinoid (CB) 1 receptor antagonist, AM 251, causes a sustained reduction of daily food intake in the rat. Physiol Behav. 2004;82:863-9.
53. Rinaldi-Carmona M, Barth F, Congy C, Martinez S, Oustric D, Perio A, et al. SR147778, a new potent and selective antagonist of the CB1 cannabinoid receptor. Biochemical and pharmacological characterization. J Pharmacol Exp Ther. 2004;310:905-14.
54. Lange JHM, Coolen HKAC, von Stuivenburg HH, Dijksman JAR, Herremans AHJ, Ronken E, et al. Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolmes as potent and selective CB1 cannabinoid receptor antagonists. J Med Chem. 2004;427:627-43.
55. Lange JHM, Kruse CG. Recent advances in CB1 cannabinoid receptor antagonists. Curr Opin Drug Discov Devel. 2004;7:498-506.
56. Fernandez JR, Allison DB. Rimonabant. Curr Opin Invest Drug. 2004;5:430-5.
57. Cota D, Marsicano G, Lutz B, Vicennati V, Stalla GK, Pasquali R, Pagotto U. Endogenous cannabinoid system as a modulator of food intake. Int J Obes. 2003;27:289-301.
58. Cota D, Genghini S, Pasquali R, Pagotto U. Antagonizing the cannabinoid receptor type 1: a dual way to fight obesity. J Endocrinol Invest. 2003;26:1041-4.
59. Marsicano G, Cota D, Stalla GK, Pasquali R, Pagotto U, Lutz B. Cannabinoids in energy balance and prospectives in the therapy of obesity. Curr Med Chem. 2003;3:81-7.