Bibliography
- Fattore L, Fadda P, Spano MS, et al. Neurobiological mechanisms of cannabinoid addiction. Mol Cell Endocrinol 2008;286:S97-S107
- Bisogno T. Endogenous cannabinoids: structure and metabolism. J Neuroendocrinol 2008;20:1-9
- Mackie K. Cannabinoid receptors: where they are and what they do. J Neuroendocrinol 2008;20:10-14
- Pertwee RG. The pharmacology of canabinoid receptors and their ligands: an overview. Int J Obes 2006;30:S13-8
- Mackie K. Signaling via CNS cannabinoid receptors. Mol Cell Endocrinol 2008;286:S60-5
- Ghasemi M, Sadeghipour H, Dehpour AR. Anandamide improves the impaired nitric oxide-mediated neurogenic relaxation of the corpus cavernosum in diabetic rats: involvement of cannabinoid CB1 and vanilloid VR1 receptors. BJU Int 2007;100:1385-90
- Oz M. Receptor-independent actions of cannabinoids on cell membranes: focus on endocannabinoids. Pharmacol Ther 2006;111:114-44
- Brown AJ. Novel cannabinoid receptors. Br J Pharmacol 2007;152:567-75
- Di Marzo V. Endocannabinoids: synthesis and degradation. Rev Physiol Biochem Pharmacol 2008;160:1-24
- Blankman JL, Simon GM, Cravatt BF. A comprehensive profile of brain enzymes that hydrolyze the endocannabinoid 2-arachidonoylglycerol. Chem Biol 2007;14:1347-56
- Fowler CJ. The contribution of cyclooxygenase-2 to endocannabinoid metabolism and action. Br J Pharmacol 2007;152:594-601
- Marnett LJ. Decoding endocannabinoid signaling. Nat Chem Biol 2008;5:8-9
- Long JZ, Li W, Booker L, et al. Selective blockade of 2-arachidonoylglyerol hydrolysis produces cannabinoid behavioral effects. Nat Chem Biol 2008;5:37-44
- Vemuri KV, Janero DR, Makryannis A. Pharmacotherapeutic targeting of the endocannabinoid signaling system: Drugs for obesity and the metabolic syndrome. Physiol Behav 2008;93:671-86
- Di Marzo V, Petrosino S. Endocannabinoids and the regulation of their levels in health and disease. Curr Opin Lipidol 2007;18:129-40
- Janero DR, Makriyannis A. Targeted modulators of the endogenous cannabinoid system: future medications to treat addiction disorders and obesity. Curr Psychiatry Rep 2007;9:365-73
- Vandevoorde S. Overview of the chemical families of fatty acid amide hydrolase and monoacylglycerol lipase inhibitors. Curr Top Med Chem 2008;8:247-67
- Pavlopoulos S, Thakur GA, Nikas SP, et al. Cannabinoid receptors as therapeutic targets. Curr Pharm Des 2006;12:1751-69
- Pei Y, Mercier RW, Anday JK, et al. Ligand-binding architecture of human CB2 cannabinoid receptor: evidence for receptor subtype-specific binding motif and modeling GPCR activation. Chem Biol 2008;15:1207-19
- Ibrahim MM, Deng H, Zvonok A, et al. Activation of CB2 cannabinoid receptors by AM1241 inhibits experimental neuropathic pain inhibition by receptors not present in the CNS. Proc Natl Acad Sci USA 2003;100:10529-33
- Ross RA. Tuning the endocannabinoid system: allosteric modulators of the CB1 receptor. Br J Pharmacol 2007;152:565-66
- Scheen AJ. CB1 receptor blockade and its impact on cardiometabolic risk factors: overview of the RIO program with rimonabant. J Neuroendocrinol 2008;20(Suppl 1):139-46
- Cohen DA. Neurophysiological pathways to obesity: below awareness and beyond individual control. Diabetes 2008;57:1768-73
- Wisse BE, Kim F, Schwartz MW. An integrative view of obesity. Science 2007;318:928-9
- James WP. The epidemiology of obesity: the size of the problem. J Intern Med 2008;263:336-52
- Jolliffe D. Extent of overweight among US children and adolescents from 1971 to 2000. Int J Obes Relat Metab Disord 2004;28:4-9
- Ogden CL, Carroll MD, Curtin LR, et al. Prevalence of overweight and obesity in the United States, 1999-2004. JAMA 2006;295:1549-55
- World Health Organization. Obesity and overweight. 2006. Available from: http://www.who.int/mediacentre/factsheets/fs311/en/index.html
- International Obesity TaskForce. IOTF prevalence data. 2008. Available from: http://www.iotf.org/database/
- Corica F, Corsonello A, Apalone G, et al. Metabolic syndrome, psychological status and quality of life in obesity: the QUOVADIS study. Int J Obesity 2008;32:185-91
- Perrini S, Leonardini A, Laviola L, et al. Biological specificity of visceral adipose tissue and therapeutic intervention. Arch Physiol Biochem 2008;114:277-86
- Fernandez ML. The metabolic syndrome. Nutr Rev 2007;65:S30-4
- Ritchie SA, Connell JM. The link between abdominal obesity, metabolic syndrome and cardiovascular disease. Nutr Metab Cardiovasc Dis 2007;17:319-26
- Ford ES, Giles WH, Mokdad AH. Increasing prevalence of the metabolic syndrome among US adults. Diabetes Care 2004;27:2444-9
- Wang Y, Beydoun MA. The obesity epidemic in the United States: gender, age, socioeconomic, racial/ethnic, and geographic characteristics. A systematic review and meta-regression analysis. Epidemiol Rev 2007;29:6-28
- Sullivan PW, Ghushchyan V, Wyatt HR, et al. The medical cost of cardiometabolic risk factor clusters in the United States. Obesity 2007;15:3150-58
- Jones LR, Wilson CI, Wadden TA. Lifestyle modification in the treatment of obesity: an educational challenge and opportunity. Clin Pharmacol Ther 2007;81:776-79
- Ong KL, Cheung BM, Man YB, et al. Prevalence, awareness, treatment, and control of hypertension among United States adults 1999-2004. Hypertension 2007;49:69-75
- Hoerger TJ, Ahmann AJ. The impact of diabetes and associated cardiometabolic risk factors on members: strategies for optimizing outcomes. J Manag Care Pharm 2008;14:S2-14
- Bult MJ, van Dalen T, Muller AF .Surgical treatment of obesity. Eur J Endocrinol 2008;158:135-45
- Abell TL, Minocha A. Gastrointestinal complications of bariatric surgery: diagnosis and therapy. Am J Med Sci 2006;331:214-18
- Genco A, Cipriano M, Bacci V, et al. BioEnterics intragastric balloon (BIB): a short-term, double-blind, randomised, controlled, crossover study on weight reduction in morbidly obese patients. Int J Obes 2006;30:129-33
- Fernandes M, Atallah AN, Soares BG, et al. Intragastric balloon for obesity. Cochrane Database Syst Rev 2007. Published online 24 January 2007, doi:10.1002/14651858.CD004931.pub2
- Colman E. Anorectics on trial: a half century of federal regulation of prescription appetite suppressants. Ann Int Med 2005;143:380-85
- Hofbauer KG, Nicholson JR, Boss O. The obesity epidemic: current and future pharmacological treatments. Annu Rev Pharmacol Toxicol 2007;47:565-92
- Padwal RS, Majumdar SR. Drug treatments for obesity: orlistat, sibutramine, and rimonabant. Lancet 2007;369:71-77
- Drew BS, Dixon AF, Dixon JB. Obesity management: update on orlistat. Vasc Health Risk Manag 2007;3:817-21
- Bray GA. Are non-prescription medications needed for weight control? Obesity 2008;16:509-14
- Sharma B, Henderson DC. Sibutramine: current status as an anti-obesity drug and its future perspectives. Expert Opin Pharmacother 2008;9:2161-73
- Fillippatos TD, Derdemezis CS, Gazi IF, et al. Orlistat-associated adverse effects and drug interactions: a critical review. Drug Saf 2008;31:53-65
- Florentin M, Liberopoulos EN, Elisaff MS. Sibutramine-associated adverse effects: a practical guide for its safe use. Obes Rev 2008;9:378-87
- Nelson DL, Gehlert DR. Central nervous system biogenic amine targets for control of appetite and energy expenditure. Endocrine 2006;29:49-60
- Ryan DH. Use of sibutramine and other nonadrenergic and serotonergic drugs in the management of obesity. Endocrine 2000;13:193-99
- Greenway FL, Caruso MK. Safety of obesity drugs. Expert Opin Drug Saf 2005;4:1083-95
- Raebel MA, Malone DC, Conner DA, et al. Health services use and health care costs of obese and nonobese individuals. Arch Intern Med 2004;164:2135-40
- Runge CF. Economic consequences of the obese. Diabetes 2007;56:2668-72
- Shen C, Sambamoorthi U, Rust G. Co-occurring mental illness and health care utilization and expenditures in adults with obesity and chronic physical illness. Dis Manag 2008;11:153-60
- Sullivan PW, Ghushchyan V, Wyatt HR, et al. Productivity costs associated with cardiometabolic risk factor clusters in the United States. Value Health 2007;10:443-50
- Padwal RS. Trends in obesity and overweight-related office visits and drug prescriptions in Canada, 1998 to 2004. Obes Res 2005;13:1905-8
- Srishanmuganathan J, Patel H, Car J, et al. National trends in the use and costs of anti-obesity medications in England 1998-2005. J Public Health 2007;29:199-202
- Datamonitor. Commercial and pipeline perspectives: obesity. Datamonitor Report dhmc2236. 2006. Available from: http://www.datamonitor.com/Products/Free/report?DHMC2236/020DMHC2236.html
- Driscoll P. Obesity management products segment sales growth. MedMarket Diligence, LLC report #S825. 2007. Available from: http://mediligence.com/blog/category/obesity
- Cowen and Company. Therapeutic Categories Outlook. New York: Cowen & Co.; 2008
- Rumsfeld JS, Nallamothu BK. The hope and fear of rimonabant. JAMA 2008;99:1601-2
- Sanofi-Aventis. Sanofi-Aventis is complying with the EMEA's recommendation to temporarily suspend the marketing authorization of Acomplia® in obese and overweight patients. 2008. Available from: www.sanofi-aventis.com
- Sanofi-Aventis. Sanofi-Aventis to discontinue all clinical trials with rimonabant. 2008. Available from: www.sanofi-aventis.com
- Fulmer T. Not cutting the fat. BioCentury 2008;16:A9-10
- Merck. Merck discontinues development of investigational medicine taranabant for obesity. 2008. Available from: http://www.merck.com/newsroom/press_releases/research_and_development/2008_1002.html
- Pfizer. Pfizer discontinues development program for its phase 3 obesity compound (CP-945-598). 2008. Available from: http://mediaroom.pfizer.com/news/Pfizer/20081105006339/en
- Jones D. End of the line for cannabinoid receptor 1 as an anti-obesity target? Nature Rev Drug Discov 2008;7:961-2
- Stern JS, Kazaks A, Downey M. Future and implications of reimbursement for obesity treatment. J Am Diet Assoc 2005;105:S104-9
- Bellocchio L, Cervino C, Pasquali R, et al. The endocannabinoid system and energy metabolism. J Neuroendocrinol 2008;20:850-7
- Matias I, Cristino L, Di Marzo V. Endocannabinoids: some like it fat (and sweet too). J Neuroendocrinol 2008;20(Suppl 1):100-9
- Di Marzo V. The endocannabinoid system in obesity and type 2 diabetes. Diabetologia 2008;51:1356-67
- Engeli S. Dysregulation of the endocannabinoid system in obesity. J Neuroendocrinol 2008;20(Suppl 1):110-5
- Kunos G, Osei-Hyiaman D, Liu J, et al. Endocannabinoids and the control of energy homeostasis. J Biol Chem 2008;283:33021-5
- Wang J, Ueda N. Role of the endocannabinoid system in metabolic control. Curr Opin Nephrol Hypertens 2008;17:1-0
- Jesudason D, Wittert G. Endocannabinoid system in food intake and metabolic regulation. Curr Opin Lipidol 2008;19:344-48
- Perkins JM, Davis SN. Endocannabinoid system overactivity and the metabolic syndrome: Prospects for treatment. Curr Diab Rep 2008;8:12-19
- Nogueiras R, Rohner-Jeanrenaud F, Woods SC, et al. The endocannabinoid system and the control of glucose homeostasis. J Neuroendocrinol 2008;20(Suppl 1):147-51
- Di Marzo V, Goparaju SK, Wang L, et al. Leptin-regulated endocannabinoids are involved in maintaining food intake. Nature 2001;410:822-5
- 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;115:1298-305
- D'Eton TM, Pierce KA, Roix JJ, et al. The role of adipocyte insulin resistance in the pathogenesis of obesity-related elevations in endocannabinoids. Diabetes 2008;57:1262-8
- Wilner LS, Arnold RM. Cannabinoids in the treatment of symptoms in cancer and AIDS. J Palliat Med 2006;9:802-04
- Matias I, Gonthier MP, 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;91:3171-80
- Pagotto U, Marsicano G, Cota D, et al. The emerging role of the endocannabinoid system in endocrine regulation and energy balance. Endocr Rev 2006;27:73-100
- Duffy D, Rader D. Endocannabinoid antagonism: Blocking the excess in the treatment of high-risk abdominal obesity. Trends Cardiovasc Med 2007;17:35-43
- Blüher M, Engeli S, Klöting N, et al. Dysregulation of the peripheral and adipose tissue endocannabinoid system in human abdominal obesity. Diabetes 2006;55:3053-60
- Côté M, Matias I, Lemieux I, et al. Circulating endocannabinoid levels, abdominal adiposity and related cardiometabolic risk factors in obese men. Int J Obes 2007;31:692-9
- Matias I, Petrosoino S, Racioppi A, et al. Dysregulation of peripheral endocannabinoid levels in hyperglycemia and obesity: effect of high fat diets. Mol Cell Endocrinol 2008;286(Suppl 1):S66-78
- Starowicz KM, Cristino L, Matias I, et al. Endocannabinoid dysregulation in the pancreas and adipose tissue of mice fed with a high-fat diet. Obesity 2008;16:553-65
- 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(2):213-7
- Benzinou M, Chevre JC, Ward KJ, et al. Endocannabinoid receptor 1 gene variations increase risk for obesity and modulate body mass index in European populations. Hum Mol Genet 2008;17:1916-21
- Wright SM, Dikkers C, Aronne LJ. Rimonabant: new data and emerging experience. Curr Atheroscler Rep 2008;10:71-8
- Nogueiras R, Veyrat-Durebex C, Suchanek PM, et al. Peripheral, but not central, CB1 antagonism provides food intake independent metabolic benefits in diet-induced obese rats. Diabetes 2008;57:2977-91
- 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;118:3160-9
- Greasley PJ, Clapham JC. Inverse agonism or neutral antagonism at G-protein coupled receptors: a medicinal chemistry challenge worth pursuing? Eur J Pharmacol 2006;553:1-9
- Bond RA, Ijzerman AP. Recent developments in constitutive receptor activity and inverse agonist, and their potential for GPCR drug discovery. Trends Pharmacol Sci 2006;27:92-96
- Canals M, Milligan G. Constitutive activity of the cannabinoid CB1 receptor regulates the function of co-expressed mu opioid receptors. J Biol Chem 2008;283:11424-34
- Leterrier C, Lainé J, Darmon M, et al. Constutitive activation drives compartment-selective endocytosis and axonal targeting of type 1 cannabinoid receptors. J Neurosci 2006;26:3141-53
- Neuman-Tancredi A, Audinot V, Moreira C, et al. Inverse agonism and constitutive activity as functional correlates of serotonin h5-HT1B receptor/G-protein stoichiometry. Mol Pharmacol 2000;58:1042-49
- Wurch T, Pauwels PJ. Analytical pharmacology of G protein-coupled receptors by stoichiometric expression of the receptor and Go protein subunits. J Pharmacol Toxicol Meth 2001;45:3-16
- Yao BB, Mukherjee S, Fan Y, et al. In vitro pharmacological characterization of AM1241: a protean agonist at the cannabinoid CB2 receptor? Br J Pharmacol 2006;149:145-54
- Henness S, Robinson DM, Lyseng-Williamson KA. Rimonabant. Drugs 2006;66:2109-19
- Bifulco M, Grimaldi C, Gazzerro P, et al. Rimonabant: just an antiobesity drug? Current evidence on its pleiotropic effects. Mol Pharmacol 2007;71:1445-56
- Xie S, Furjanic MA, Ferrara JJ, et al. The endocannabinoid system and rimonabant: a new drug with a novel mechanism of action involving cannabinoid CB1 receptor antagonism – or inverse agonism – as potential obesity treatment and other therapeutic use. J Clin Pharm Ther 2007;32:209-31
- Landsman RS, Burkey TH, Consroe P, et al. SR141716A is an inverse agonist at the human cannabinoid CB1 receptor. Eur J Pharmacol 1997;334:R1-2
- Ward SJ, Dykstra LA. The role of CB1 receptors in sweet versus fat reinforcement: effect of CB1 receptor deletion, CB1 receptor antagonism (SR141716A) and CB1 receptor agonism (CP-55940). Behav Pharmacol 2005;16:381-88
- Bergman J, Delatte MS, Paronis CA, et al. Some effects of CB1 antagonists with inverse agonist and neutral biochemical properties. Physiol Behav 2008;93:666-70
- Kintscher U. The cardiometabolic drug rimonabant: after 2 years of RIO-Europe and Stradivarius. Eur Heart J 2008;29:1709-10
- Patel PN, Pathak R. Rimonabant: a novel selective cannabinoid-1 receptor antagonist for treatment of obesity. Am J Health Syst Pharm 2007;64:481-89
- Despres JP, Golay A, Sjostrom L. Effects of rimonabant on metabolic risk factors in overweight patients with dyslipidemia. N Engl J Med 2005;353:2121-34
- Van Gaal LF, Rissanen AM, Scheen AJ, et al. 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;365:1389-97
- Pi-Sunyer FX, Aronne LJ, Heshmati HM, et al. 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;295:761-75
- Scheen AJ, Finer N, Hollander P, et al. Efficacy and tolerability of rimonabant in overweight or obese patients with type 2 diabetes: a randomised controlled study. Lancet 2006;368:1660-72
- Christensen R, Kristensen PK, Bartels EM, et al. Efficacy and safety of the weight-loss drug rimonabant: a meta-analysis of randomised trials. Lancet 2007;370:1706-13
- Scheen AJ, Van Gaal LF. Cardiometabolic effects of rimonabant in obese/overweight subjects with dyslipidaemia or type 2 diabetes. Rev Med Liege 2007;62:81-5
- Van Gaal L, Pi-Sunyer X, Despres JP, et al. 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:S229-40
- Van Gaal LF, Scheen AJ, Rissanen AM, et al. Long-term effect of CB1 blockade with rimonabant on cardiometabolic risk factors: two year results from the RIO-Europe study. Eur Heart J 2008;29:1761-71
- Ruilope LM, Despres JP, Scheen A, et al. Effect of rimonabant on blood pressure in overweight/obese patients with/without co-morbidities: analysis of pooled RIO study results. J Hypertens 2008;26:357-67
- Rosenstock J, Hollander P, Chevalier S, et al. The SERENADE trial: effects of monotherapy with rimonabant, the first selective CB1 receptor antagonist, on glycemic control, body weight and lipid profile in drug-naive type 2 diabetes. Diabetes Care 2008;31:2169-76
- Despres JP, Ross R, Boka G, et al. Rimonabant reduces both intra-abdominal adiposity and liver fat and improves cardiometabolic risk factors: the ADAGIO-LIPIDS trial. The 77th European Atherosclerosis Society Congress, Istanbul, Turkey, April 26 – 29 2008
- 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;299:1547-60
- Muccioli GG. Blocking the cannabinoid recpetors: drug candidates andtherapeutic promises. Chem Biodivers 2007;4:1805-27
- Jagerovic N, Fernandez-Fernandez C, Goya P. CB1 cannabinoid antagonists: structure-activity relationships and potential therapeutic applications. Curr Top Med Chem 2008;8:205-30
- Fremming BA, Boyd ST. Taranabant, a novel cannabinoid type 1 receptor inverse agonist. Curr Opin Investig Drugs 2008;9:1116-29
- Hagmann WK. The discovery of taranabant, a selective cannabinoid-1 receptor inverse agonist for the treatment of obesity. Arch Pharm Chem Life Sci 2008;341:405-11
- Addy C, Li S, Agrawal N, et al. Safety, tolerability, pharmacokinetics, and pharmacodynamic properties of taranabant, a novel selective cannabinoid-1 receptor inverse agonist, for the treatment of obesity: results from a double-blind, placebo-controlled, single oral dose study in healthy volunteers. J Clin Pharmacol 2008;48:418-27
- Addy C, Rothenberg P, Li S, et al. Multiple-dose pharmacokinetics, pharmacodynamics, and safety of taranabant, a novel selective cannabinoid-1 receptor inverse agonist, in healthy male volunteers. J Clin Pharmacol 2008;48:734-44
- 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
- A multicenter study to evaluate the efficacy and safety of four doses of SR147778 in obese patients. 2004. Available from: http://wwwclinicaltrials.gov/ct2/show/NCT00239174
- Multiple-dose study to evaluate the efficacy, safety and pharmacokinetics of BMS-646256 in obese subjects. 2006. Available from: http://wwwclinicaltrials.gov/ct/show/NCT0038609
- Srivastava BK, Soni R, Joharapurkar A, et al. Bioisosteric replacement of dihydropyrazole of 4s-(-)-3-(4-chlorophenyl)-n-methyl-n′-[(4-chlorophenyl)-sulfonyl]-4-phenyl-4,5-di hydro-1h-pyrazole-1-caboxamidine (SLV-319) a potent CB1 receptor antagonist by imidazole and oxazole. Bioorg Med Chem Lett 2008;18:963-68
- BMS-646256 in obese and overweight type 2 diabetics. 2007. Available from: http://wwwclinicaltrials.gov/ct/show/NCT00541567
- Herling AW, Gossel M, Haschke G, et al. CB1 receptor antagonist AVE1625 affects primarily metabolic parameters independently of reduced food intake in Wistar rats. Am J Physiol Endocrinol Metab 2007;293:E826-E32
- Dose-ranging study evaluating AVE1625 in abdominally obese patients with atherogenic dyslipidemia. 2006. Available from: http://wwwclinicaltrials.gov/ct/show/NCT00345410
- Activity of AVE1625 in mild to moderate Alzheimer's patients. 2006. Available from: http://wwwclinicaltrials.gov/ct/show/NCT00380302
- Efficacy and safety of AVE1625 as co-treatment with antipsychotic therapy in schizophrenia (CONNECT). 2007. Available from: http://wwwclinicaltrials.gov/ct/show/NCT00439634
- A study of 6-month duration to evaluate the weight loss effect of various doses of CP-945,598 in obese subjects. 2005. Available from: http://wwwclinicaltrials.gov/ct/show/NCT00134199
- A long-term study to examine the effects of CP-945,598 on weight loss and safety. 2006. Available from: http://wwwclinicaltrials.gov/ct/show/NCT00375401
- A 1-year study on the effects of CP-945,598 for the treatment of obesity in overweight type 2 diabetic patients. 2006. Available from: http://wwwclinicaltrials.gov/ct/show/NCT00391196
- Effect of 2-year administration of CP-945,598 on weight loss efficacy and safety. 2007. Available from: http://wwwclinicaltrials.gov/ct/show/NCT00396448
- A 14-month study on the effects of CP-945,598 for the prevention of weight regain in obese patients. 2008. Available from: http://wwwclinicaltrials.gov/ct/show/NCT00483171
- Esteve. EP-01944293. Described in: Curr Opin Drug Discov Devel 2008;11:591-8
- Safety and efficacy of low doses of V24343 in obese subjects. 2008. Available from: http://clinicaltrials.gov/ct2/show/NCT00734201
- Hainer V, Toplak H, Mitrakou A. Treatment modalities of obesity: what fits whom? Diabetes Care 2008;31:S269-77
- Rimonabant regulatory update in the United States. Sanofi-Aventis, 2007. Available from: http://en.sanofi-aventis.com/Images/070629_rimonabant_US_en_tem24-17003.pdf
- Sanofi-Aventis received from the FDA an approvable letter for rimonabant for weight management and a nonapprovable letter for smoking cessation. 2006. Available from: http://www.sanofi-aventis.us/live/us/medias/7B804B87-CB40-4690-AD95-7880055B20A9.pdf
- European Medicines Agency recommends Acomplia must not be used in patients on antidepressants or with major depression. EMEA, 2007. Available from: http://wwwemeaeuropaeuhumandocs/PDFs/EPAR/acomplia/32982607enpdf 2007
- Soyka M, Koller G, Schmidt P, et al. Cannabinoid receptor 1 blocker rimonabant (SR 141716) for treatment of alcohol dependence. Results from a placebo-controlled, double-blind trial. J Clin Psychopharmacol 2008;28:317-24
- Le Foll B, Forget B, Aubin HJ, et al. Blocking cannabinoid CB1 receptors for the treatment of nicotine dependence: insights from pre-clinical and clinical studies. Addict Biol 2008;13:239-52
- Doggrell SA. Is rimonabant efficacious and safe in the treatment of obesity? Expert Opin Pharmacother 2008;9:2727-31
- Gantz I, Erondu N, Suryawanshi S, et al. A two-year study to assess the efficacy, safety, and tolerability of taranabat in obese patients: 52 week results. American College of Cardiology Annual Scientific Session, Chicago, Illinois, USA, 29 March – 1 April 2008
- Akbas F, Gasteyger C, Sjodin A, et al. A critical review of the cannabinoid receptor as a drug target for obesity management. Obes Revs 2009;10:58-67
- Di Marzo V. Targeting the endocannabinoid system: to enhance or reduce? Nat Rev Drug Discov 2008;7:438-55
- Lafenêtre P, Chaouloff F, Marsicano G. The endocannabinoid system in the processing of anxiety and fear and how CB1 receptors may modulate fear extinction. Pharmacol Res 2007;56:367-81
- Atherosclerosis underlying development assessed by intima-media thickness in patients on rimonabant (Auditor) 2005. Available from: http://wwwclinicaltrials.gov/ct/show/NCT00228176
- STRADIVARIUS (strategy to reduce atherosclerosis development involving administration of rimonabant – the intravascular ultrasound study). 2005. Available from: http://wwwclinicaltrials.gov/ct/show/NCT00124332
- Study evaluating rimonabant efficacy in drug-naïve diabetic patients (SERENADE). 2005. Available from: http://wwwclinicaltrials.gov/ct/show/NCT00257257
- An international study of rimonabant in dyslipidemia with atherogenic risk in abdominally obese patients (ADAGIO-lipids). 2005. Available from: http://wwwclinicaltrials.gov/ct/show/NCT00239967
- Comprehensive rimonabant evaluation study of cardiovascular endpoints and outcomes (CRESCENDO). 2005. Available from: http://wwwclinicaltrials.gov/ct/show/NCT00263042
- Study evaluating rimonabant efficacy in insulin-treated diabetic patients (ARPEGGIO). 2006. Available from: http://wwwclinicaltrials.gov/ct/show/NCT00288236
- Visceral fat reduction assessed by CT-scan on rimonabant (VICTORIA). 2006. Available from: http://wwwclinicaltrials.gov/ct/show/NCT00299325
- Rimonabant in prediabetic subjects to delay onset of type 2 diabetes (RAPSODI). 2006. Available from: http://wwwclinicaltrials.gov/ct/show/NCT00325650
- Pacher P, Mukhopadhyay P, Mohanraj R, et al. Modulation of the endocannabinoid system in cardiovascular disease. Therapeutic potential and limitations. Hypertension 2008;52:601-7
- Viveros MP, Roderiguez de Fonseca F, Bermudez-Silva FJ, et al. Critical role of the endocannabinoid system in the regulation of food intake and energy metabolism, with phylogenic, developmental, and pathophysiological implications. Endocr Metab Immune Disord Drug Targets 2008;8:220-30
- Rimonabant to reduce alcohol consumption. 2003. Available from: http://wwwclinicaltrials.gov/ct/show/NCT00075205
- Kunos G, Osei-Hyiaman D, Bátkai S, et al. 2008. Should peripheral CB1 cannabinoid receptors be selectively targeted for therapeutic gain? Trends Pharmacol Sci 2009;30:1-7
- Pavón FJ, Serrano A, Pérez-Valero V, et al. Central versus peripheral antagonism of cannabinoid CB1 receptor in obesity: effects of LH-21, a peripherally acting neutral cannabinoid receptor antagonist, in Zucker rats. J Neuroendocrinol 2008; 20 (Suppl 1):116-23
- Chen RZ, Frassetto A, Lao JZ, et al. Pharmacological evaluation of LH-21, a newly discovered molecule that binds to cannabinoid CB1 receptor. Eur J Pharmacol 2008;584:338-42
- Sink KS, McLaughlin PJ, Wood JA, et al. The novel cannabinoid CB1 receptor neutral antagonist AM4113 suppresses food intake and food-reinforced behavior but does not induce signs of nausea in rats. Neuropsychopharmacology 2008;33:946-55
- Gardner A, Mallet PE. Suppression of feeding, drinking, and locomotion by a putative cannabinoid receptor ‘silent antagonist’. Eur J Pharmacol 2006;530:103-6
- Järbe TU, Lemay BJ, Olszewska T, et al. Intrinsic effects of AM4113, a putative neutral CB1 receptor selective antagonist, on open-field behaviors in rats. Pharmacol Biochem Behav 2008;91:84-90
- Salamone JD, McLaughlin PJ, Sink K, et al. Cannabinoid CB1 receptor inverse agonists and neutral antagonists: effects on food intake, food-reinforced behavior and food aversions. Physiol Behav 2007;91:383-8
- Chambers AP, Vemuri VK, Peng Y, et al. A neutral CB1 receptor antagonist reduces weight gain in rat. Am J Physiol Regul Integr Comp Physiol 2007;293:R2185-R93
- McLaughlin PJ, Winston K, Swezey L, et al. The cannabinoid CB1 antagonists SR141716a and AM251 suppress food intake and food-reinforced behavior in a variety of tasks in rats. Behav Pharmacol 2003;14:583-8
- Parker LA, Mechoulam R, Schlievert C, et al. Effects of cannabinoids on lithium-induced conditioned rejection reactions in a rat model of nausea. Psychopharmacology 2003;166:156-62
- McLaughlin PJ, Winston KM, Limebeer CL, et al. The cannabinoid CB1 antagonist AM251 produces food avoidance and behaviors associated with nausea but does not impair feeding efficiency in rats. Psychopharmacology 2005;180:286-93
- Parker LA, Limebeer CL. Conditioned gaping in rats: a selective measure of nausea. Auton Neurosci 2006;129:36-41
- Sink KS,Vemuri VK, Wood J, et al. Oral bioavailability of the novel cannabinoid CB1 antagonist AM6527: effects on food-reinforced behavior and comparisons with AM4113. Pharmacol Biochem Behav 2009;91:303-6
- Cheng Y, Hitchcock SA. Targeting endocannabinoid agonists for inflammatory and neuropathic pain. Expert Opin Invest Drugs 2007;16:951-65
- Ashton JC, Glass M. The cannabinoid CB2 receptor as a target for inflammation-dependent neurodegeneration. Curr Neuropharmacol 2007;5:73-80
- Food and Drug Administration. FDA expands warning to consumers about tainted weight loss pills. January 8, 2009. Available at: <http://www.fda.gov/bbs/topics/NEWS/2008/NEW01933.html>.