Rimonabant hydrochloride: Antiobesity drug aid to smoking cessation treatment of alcohol dependency cannabinoid CB1 antagonist

Drugs of the Future

Volumn 30, Issue 2, 2005, Pages 128-137

  Sorbera, L A ^a   Castaner J ^a   Silvestre, J S ^a  

^a PROUS SCIENCE   (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

4 CHLORO N [[3 (4 CHLOROPHENYL) 4 PHENYL 2 PYRAZOLIN 1 YL](METHYLAMINO)METHYLENE]BENZENESULFONAMIDE; 5 (4 BROMOPHENYL) 1 (2,4 DICHLOROPHENYL) 4 ETHYL N (1 PIPERIDYL) 1H PYRAZOLE 3 CARBOXAMIDE; ANTIOBESITY AGENT; CANNABINOID 1 RECEPTOR; CANNABINOID RECEPTOR; CANNABINOID RECEPTOR ANTAGONIST; DEXFENFLURAMINE; NALOXONE; RIMONABANT; SLV 326; UNCLASSIFIED DRUG;

ALCOHOL CONSUMPTION; ALCOHOLISM; CARDIOVASCULAR RISK; CIGARETTE SMOKING; CLINICAL TRIAL; CORONARY ARTERY DISEASE; DIABETES MELLITUS; DRUG EFFICACY; DRUG TARGETING; FEEDING BEHAVIOR; FOOD INTAKE; HIGH RISK POPULATION; HUMAN; HYPERLIPIDEMIA; HYPERTENSION; MOTIVATION; NONHUMAN; OBESITY; PATHOPHYSIOLOGY; REINFORCEMENT; REVIEW; REWARD; SMOKING CESSATION;

EID: 20044369375     PISSN: 03778282     EISSN: None     Source Type: Journal    
DOI: 10.1358/dof.2005.030.02.880929     Document Type: Review

References (49)

1. Barth, F., Casellas, P., Congy, C., Martinez, S., Rinaldi, M., Anne-Archard, G. (Sanofi-Aventis). Substd. N-piperidino 3-pyrazolecarboxamide. CA 2136893, EP 0576357, EP 0656354, FR 2692575, FR 2713224, FR 2713225, JP 1994073014, JP 1995309841, JP 2001026541, US 5624941.
2. Barth, F., Casellas, P., Congy, C., Martinez, S., Rinaldi, M. (Sanofi-Aventis). Novel 3-pyrazolecarboxamide derivs. with cannabioid receptor affinity. EP 0658546, FR 2714057, JP 1995324076, US 5462960.
3. Seltzman, H.H., Carroll, F.I., Burgess, J.P., Wyrick, C.D., Burch, D.F. Synthesis, spectral studies and tritiation of the cannabinoid antagonist SR141716A. J Chem Soc Chem Commun 1995, (15): 1549-50.
4. Dutta, A.K., Sard, H., Ryan, W., Razdan, R.K., Compton, D.R., Martin, B.R. The synthesis and pharmacological evaluation of the cannabinoid antagonist SR 141716A. Med Chem Res 1994, 5: 54-62.
5. Prous Science Drug R&D Backgrounders: Obesity (online publication). Updated February 28, 2005.
6. World Health Organization. Obesity: preventing and managing the global epidemic. Report of a WHO Consultation Technical Report Series 894, Geneva, Switzerland 2000.
7. Bonow, R.O., Eckel, R.H. Diet, obesity, and cardiovascular risk. New Engl J Med 2003, 348: 2057-8.
8. National Task Force on the Prevention and Treatment of Obesity. Overweight, obesity, and health risk. Arch Intern Med 2000, 160: 898-904.
9. Deckelbaum, R.J., Williams, C.L. Childhood obesity: The health issue. Obes Res 2001, 9(Suppl. 4): 239S-43S.
10. US Department of Health and Human Services. The Surgeon General's call to action to prevent and decrease overweight and obesity in 2001. US Department of Health and Human Services, Public Health Service, Office of the Surgeon General, Rockville, MD, 2001.
11. Pi-Sunyer, F.X. Medical hazards of obesity. Ann Int Med 1993, 119: 655-60.
12. Calle, E.E., Rodriguez, C., Walker-Thurmond, K., Thun, M.J. Overweight, obesity, and mortality from cancer in a prospectively studied cohort of U.S. adults. New Engl J Med 2003, 348: 1625-38.
13. 9-THC. Physiol Behav 1998, 65: 343-6.
14. 9-THC stimulates food intake in Lewis rats: Effects on chow, high-fat and sweet high-fat diets. Pharmacol Biochem Behav 2001, 68: 539-43.
15. Bays, H.E. Current and investigational antiobesity agents and obesity therapeutic treatment targets. Obes Res 2004, 12: 1197-211.
16. Rinaldi-Carmona, M., Barth, F., Heaulme, M. et al. SR141716A, a potent and selective antagonist of the brain cannabinoid receptor. FEBS Lett 1994, 350: 240-4.
17. Colombo, G., Agabio, R., Diaz, G., Lobina, C., Reali, R., Gessa, G.L. Appetite suppression and weight loss after the cannabinoid antagonist SR 141716. Life Sci 1998, 63: PL113-7.
18. Di Marzo, V., Goparaju, S.K., Wang, L. et al. Leptin-regulated endocannabinoids are involved in maintaining food intake. Nature 2001, 410: 822-5.
19. 1 cannabinoid receptor knockout in mice leads to leanness, resistance to diet-induced obesity and enhanced leptin sensitivity. Int J Obes 2004, 28: 640-8.
20. Verty, A.N.A., McGregor, I.S., Mallet, P.E. 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: 217-20.
21. 1 antagonists SR 141716A and AM 251 suppress food intake and food reinforced behavior in a variety of tasks in rats. Behav Pharmacol 2003, 14: 583-8.
22. Freedland, C.S., Poston, J.S., Porrino, L.J. Effects of SR141716A, a central cannabinoid receptor antagonist, on food-maintained responding. Pharmacol Biochem Behav 2000, 67: 265-70.
23. Rowland, N.E., Mukherjee, M., Robertson, K. Effects of the cannabinoid receptor antagonist SR 141716, alone and in combination with dexfenfluramine or naloxone, on food intake in rats. Psychopharmacology (Berlin) 2001, 159: 111-6.
24. 1 receptor antagonist, in diet-induced obese mice. Am J Physiol - Regul Integr Comp Physiol 2003, 284: R345-53.
25. 1 receptor antagonist, SP 141716, on food intake and body weight gain of obese (fa/fa) compared to lean Zucker rats. Psychopharmacology (Berlin) 2003, 167: 103-11.
26. Poirier, B., Bidouard, J.-P., Cadrouvele, C., Marniquet, X., Staels, B., O'Connor, S.E., Janiak, P., Herbert, J.M. The antiobesity effect of rimonabant is associated with an improved serum lipid profile. Diabetes Obes Metab 2005, 7: 65-72.
27. 1 cannabinoid receptor antagonist, selectively reduces sweet food intake in marmoset. Behav Pharmacol 1998, 9: 179-81.
28. Gallate, J.E., Mallet, P.E., McGregor, I.S. Combined low dose treatment with opioid and cannabinoid receptor antagonists synergistically reduces the motivation to consume alcohol in rats. Psychopharmacology (Berlin) 2004, 173: 210-6.
29. 1 receptor antagonist, SR 141716, on alcohol's motivational properties in alcohol-preferring rats. Eur J Pharmacol 2004, 498: 119-23.
30. 1 receptor antagonist, SR 141716, of alcohol deprivation effect in alcohol-preferring rats. Eur J Pharmacol 2002, 443: 95-7.
31. 1) receptor antagonist, blocks the motivational and dopamine-releasing effects of nicotine in rats. Behav Pharmacol 2002, 13: 451-63.
32. 1) receptor antagonist, rimonabant (SR141716). Neuropsychopharmacology 2005, 30: 145-55.
33. 1 antagonist, blocks nicotine-conditioned place preferences. NeuroReport 2004, 15: 2139-43.
34. 1-receptor antagonist rimonabant reduces body weight and waist circumference in obese subjects. Int J Obes 2004, 28(Suppl. 1): Abst T5:O2-001.
35. Després, J.P., Golay, A., Sjöström, L. Effect of rimonabant on metabolic markers and CHD risk in overweight/obese dyslipidemic subjects: The RIO-Lipids trial. 15th Int Symp Drugs Affect Lipid Metab (Oct 24-27, Venice) 2004, 129.
36. Després, J.-P. Selective cannabinoid receptor antagonism and its role in the management of obesity/metabolic syndrome. Metab Syndr Type II Diabetes Atheroscler Congr (May 19-23, Marrakesh) 2004, Abst P-42.
37. Van Gaal, L. Effect of rimonabant on weight reduction and weight maintenance: RIO-Europe (RIO-EU) trial. 15th Int Symp Drugs Affect Lipid Metab (Oct 24-27, Venice) 2004, 30.
38. Van Gaal, L., Pi-Sunyer, X. Effect of rimonabant on weight reduction, weight maintenance and prevention of weight regain: Design of RIO-North America & RIO-Europe trials. Int J Obes 2004, 28(Suppl. 1): Abst T5:P5b-034.
39. Anthenelli, R.M. Using a cannabinoid receptor antagonist as an aid to smoking cessation. Metab Syndr Type II Diabetes Atheroscler Congr (May 19-23, Marrakesh) 2004, Abst P-39.
40. 1 receptor to stimulation of cAMP accumulation. J Pharmacol Exp Ther 1998, 284: 291-7.
41. Lange, J.H., Coolen, H.K., van Stuivenberg, H.H. et al. Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB1 cannabinoid receptor antagonists. J Med Chem 2004, 47: 627-43.
42. 2 receptors. Br J Pharmacol 1998, 124: 619-22.
43. 1 receptor antagonist N-(piperidinyl)-5-(4- chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716). J Med Chem 2002, 45: 2708-19.
44. 1 receptor antagonists. Chem Pharm Bull 2002, 50: 1109-13.
45. Kanyonyo, M., Govaerts, S.J., Hermans, E., Poupaert, J.H., Lambert, D.M. 3-Alkyl-(5,5′-diphenyl)imidazolidinediones as new cannabinoid receptor ligands. Bioorg Med Chem Lett 1999, 9: 2233-6.
46. 1 cannabinoid receptor ligands and potential antagonists: Synthesis, lipophilicity, affinity, and molecular modeling. J Med Chem 2002, 45: 1748-56.
47. 1 receptor. Mol Pharmacol 2002, 62: 1274-87.
48. 1 receptor antagonist properties in vitro and in vivo. 34th Annu Meet Soc Neurosci (Oct 23-27, San Diego) 2004, Abst 1009.4.
49. 1 cannabinoid receptor: Biochemical and pharmacological characterization. J Pharmacol Exp Ther 2004, 310: 905-14.