The potential use of selective 5-HT_2C agonists in treating obesity

Bibliography

• FLEGAL KM, CARROLL MD, OGDEN CL, JOHNSON CL: Prevalence and trends in obesity among US adults, 1999-2000. J. Am. Med. Assoc. (2002) 288(14):1723-1727.
   PubMed Web of Science ®Google Scholar
• NATIONAL TASK FORCE ON THE PREVENTION AND TREATMENT OF OBESITY: Overweight, obesity, and health risk. Arch. Intern. Med. (2000) 160:898-904.
   PubMed Web of Science ®Google Scholar
• MOKDAD AH, MARKS JS, STROUP DF, GERBERDING JL: Actual causes of death in the United States, 2000. J. Am. Med. Assoc. (2004) 291(10):1238-1245.
   PubMed Web of Science ®Google Scholar
• YUSEF S, HAWKEN S, OUNPUU S et al.: Obesity and the risk of myocardial infarction in 27000 participants from 52 countries: a case-control study. Lancet (2005) 366:1640-1649.
   Google Scholar
• KLEIN S: Outcome success in obesity. Obes. Res. (2001) 9:354S-358S.
   PubMedGoogle Scholar
• COLMAN E: Anorectics on trial: a half century of federal regulation of prescription appetite suppressants. Ann. Intern. Med. (2005) 143:380-385.
   PubMed Web of Science ®Google Scholar
• LE DOUAREC JC, SCHMITT H: Comparison pharmacologique de sept medicaments anorexiques. Therapie (1964) 19:831-841.
   PubMedGoogle Scholar
• DUHAULT J, VERDAVAINNE C: Modification du taux de serotonine cerebrale chez le rat par les trifluoromethyl-phenyl-2-ethyl- aminopropane (fenfluramine 768 S). Arch. Int. Pharmacodyn. Ther. (1967) 170:276-286.
   PubMedGoogle Scholar
• HALFORD JCG, HARROLD JA, LAWTON CL, BLUNDELL JE: Serotonin (5-HT) drugs: effects on appetite expression and use for the treatment of obesity. Curr. Drug Targets (2005) 6:201-213.
   PubMed Web of Science ®Google Scholar
• CLIFTON PG: Meal patterning in rodents: psychopharmacological and neuroanatomical studies. Neurosci. Biobehav. Rev. (2000) 24:213-222.
   PubMed Web of Science ®Google Scholar
• FOTLIN RW, HANEY M, COMER SD, FISCHMAN MW: Effect of fenfluramine on food intake, mood, and performance of humans living in a residential laboratory. Physiol. Behav. (1996) 59(2):295-305.
   PubMed Web of Science ®Google Scholar
• HOYER D, HANNON JP, MARTIN GR: Molecular, pharmacological and functional diversity of 5-HT receptors. Pharmacol. Biochem. Behav. (2002) 71:533-554.
   PubMedGoogle Scholar
• MILLER KJ: Serotonin 5-HT2C receptor agonists: Potential for the treatment of obesity. Mol. Int. (2005) 5(5):282-291.
   PubMed Web of Science ®Google Scholar
• VICKERS SP, DOURISH CT, KENNETT GA: Evidence that hypophagia induced by d-fenfluramine and d-norfenfluramine in the rat is mediated by 5-HT2C receptors. Neuropharmacology (2001) 41(2):200-209.
   PubMed Web of Science ®Google Scholar
• MARTIN JR, BOS M, JENCK F et al.: 5-HT2C receptor agonists: Pharmacological characteristics and therapeutic potential. J. Pharmacol. Exp. Ther. (1998) 286:913-924.
   PubMed Web of Science ®Google Scholar
• BICKERDIKE MJ: 5-HT2C receptor agonists as potential drugs for the treatment of obesity. Curr. Top. Med. Chem. (2003) 3:885-897.
   PubMed Web of Science ®Google Scholar
• VICKERS SP, CLIFTON PG, DOURISH CT, TECOTT LH: Reduced satiating effect of d-fenfluramine in serotonin 5-HT2C receptor mutant mice. Psychopharmacology (1999) 143(3):309-314.
   PubMed Web of Science ®Google Scholar
• TECOTT LH, SUN LM, AKANA SF et al.: Eating disorder and epilepsy in mice lacking 5-HT2C serotonin receptors. Nature (1995) 374:542-546.
   PubMed Web of Science ®Google Scholar
• CONNOLLY HM, CRARY JL, McGOON MD et al.: Valvular heart disease associated with fenfluramine–phentermine. N. Engl. J. Med. (1997) 337(9):581-588.
   PubMed Web of Science ®Google Scholar
• FITZGERALD LW, BURN TC, BROWN BS et al.: Possible role of valvular serotonin 5-HT(2B) receptors in the cardiopathy associated with fenfluramine. Mol. Pharm. (2000) 57(1):75-81.
   PubMed Web of Science ®Google Scholar
• ROTHMAN RB, BAUMANN MH, SAVAGE JE et al.: Evidence for possible involvement of 5-HT(2B) receptors in the cardiac valvulopathy associated with fenfluramine and other serotonergic medications. Circulation (2000) 102(23):2836-2841.
   PubMed Web of Science ®Google Scholar
• SETOLA V, ROTH BL: Screening the receptorome reveals molecular targets responsible for drug-induced side effects: focus on ‘fen-phen.’ Expert Opin. Drug Metab. Toxicol. (2005) 1(3):377-387.
   PubMedGoogle Scholar
• GUSTAFSSON BI, TOMMERAS K, NORDRUM I et al.: Long-term serotonin administration induces heart valve disease in rats. Circulation (2005) 111:1517-1522.
   Google Scholar
• FISHMAN AP: Aminorex to fen/phen. An epidemic foretold. Circulation (1999) 99:156-161.
   Google Scholar
• ABENHAIM L, MORIDE Y, BRENOT F et al.: Appetite-suppressant drugs and the risk of pulmonary hypertension. N. Engl. J. Med. (1996) 335(9):609-616.
   PubMed Web of Science ®Google Scholar
• RICH S, RUBIN L, WALKER AM et al.: Anorexigens and pulmonary hypertension in the United States: results from the surveillance of North American pulmonary hypertension. Chest (2000) 117:870-874.
   PubMed Web of Science ®Google Scholar
• MacLEAN MR, HERVE P, EDDAHIBI S, ADNOT S: 5-Hydroxytryptamine and the pulmonary circulation: receptors, transporters and relevance to pulmonary arterial hypertension. Br. J. Pharmacol. (2000) 131:161-168.
   PubMed Web of Science ®Google Scholar
• LUANAY JM, HERVE P, PEOC’H K et al.: Function of the serotonin 5-hydroxytryptamine 2B receptor in pulmonary hypertension. Nat. Med. (2002) 8(10):1129-1135.
   PubMed Web of Science ®Google Scholar
• MARCOS E, FADEL E, SANCHEZ O et al.: Serotonin-induced smooth muscle hyperplasia in various forms of human pulmonary hypertension. Circ. Res. (2004) 94:1263-1270.
   PubMed Web of Science ®Google Scholar
• NICHOLS DE: Hallucinogens. Pharmacol. Behav. (2004) 101:131-181.
   Google Scholar
• FONE KC, JOHNSON JV, BENNETT GW, MARSDEN CA: Involvement of 5-HT2 receptors in the behaviours produced by intrathecal administration of selected 5-HT agonists and the TRH analogue (CG 3509) to rats. Br. J. Pharmacol. (1989) 96:599-608.
   PubMed Web of Science ®Google Scholar
• BISHOP MJ, NILSSON BM: New 5-HT2C receptor agonists. Expert Opin. Ther. Patents (2003) 13(11):1691-1705.
   Web of Science ®Google Scholar
• JENCK F, BOS M, WICHMANN J, STADLER H, MARTIN JR, MOREAU JL: The role of 5-HT2C receptors in affective disorders. Expert Opin. Invest. Drugs (1998) 7(10):1587-1599.
   PubMedGoogle Scholar
• BENTLEY JM, ADAMS DR, BEBBINGTON D et al.: Indoline derivatives as 5-HT2C receptor agonists. Bioorg. Med. Chem. Lett. (2004) 14:2367-2370.
   PubMed Web of Science ®Google Scholar
• RICHTER HG, ADAMS DR, BENARDEAU A et al.: Synthesis and biological evaluation of novel pyrido[3′,2′:4,5]pyrrolo[1,2-A]pyrazines as potent and selective 5-HT2C receptor agonists. Abstracts of Papers, 230th ACS National Meeting, Washington, DC, USA (28 August – 1 September 2005).
   Google Scholar
• ADAMS D, BENARDEAU A, BICKERDIKE MJ et al.: 5-HT2C receptor agonists for the treatment of obesity. Biological and chemical adventures. Chimia (2004) 58(9):613-620.
   Web of Science ®Google Scholar
• PETERS R, WALDMEIER P, JONCOUR A: Efficient synthesis of a 5-HT2C receptor agonist precursor. Org. Proc. Res. Dev. (2005) 9(4):508-512.
   Web of Science ®Google Scholar
• ROSENZWEIG-LIPSON S, COUPET J, DUNLOP J, McGONIGLE P: Antiobesity-like effects of the selective 5-HT2C agonist Way-161503. FASEB J. (2000) 14:A1321.
   Google Scholar
• WELMAKER GS, NELSON JA, SABALSKI JE et al.: Synthesis and 5-hydroxytryptamine (5HT) activity of 2,3,4,4a-tetrahydro-1H-pyrazino[1,2-a] quinoxalin-5-(6H)ones and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinoxalines. Bioorg. Med. Chem. Lett. (2000) 10:1991-1994.
   PubMed Web of Science ®Google Scholar
• DUNLOP J, SABB AL, MAZANDARANI H et al.: WAY-163909 [(7bR,10aR)-1,2,3,4,8,9,10,10a-octahydro-7bH-cyclopenta-[b][1,4]diazepino[6,7,1hi] indole, a novel 5-hydroxytryptamine 2C receptor-selective agonist with anorectic activity. J. Pharmaco. Exp. Ther. (2005) 313(2):862-869.
   PubMed Web of Science ®Google Scholar
• ROBICHAUD AJ, CHEN W, McCLUNG C et al.: Synthesis and biological evaluation of novel, selective 5-HT2C receptor agonists for the treatment of obesity. Abstracts of Papers, 221st ACS National Meeting, San Diego, USA (1 – 5 April 2001).
   Google Scholar
• CHEN Y: Selective 5-HT2C receptor agonists provide anti-obesity drugs. Metabolic Diseases Drug Discovery World Summit, San Diego, USA (29 July 2003).
   Google Scholar
• HESTER JB, TANG AH, KEASLING HH, VELDCAMP W: Azepineindoles. I. Hexahydroazepino[4,5-b]indoles. J. Med. Chem. (1968) 11:101-106.
   PubMed Web of Science ®Google Scholar
• GALLANT DM, BISHOP MP, BISHOP G, O’MEALLIE L: U-22,394A: A controlled evaluation in chronic schizophrenic patients. Curr. Ther. Res. (1967) 9:579-581.
   PubMed Web of Science ®Google Scholar
• McCALL RB, FRANKLIN SR, HYSLOP DK et al.: PNU-22394, a 5-HT2C receptor agonist, reduces feeding in rodents and produces weight loss in humans. Abstracts of Papers, 31st Soc. Neurosci. Meeting, San Diego, USA (2001) 27:309.2.
   Google Scholar
• WALSH AE, SMITH KA, OLDMAN AD: m-Chlorophenylpiperazine decreases food intake in a test meal. Psychopharmacology (1994) 116:120-122.
   PubMed Web of Science ®Google Scholar
• COWEN PJ, SARGENT PA, WILLIAMS C, GOODALL EM, OLIKOV AB: Hypophagic, endocrine and subjective responses to m-chlorophenylpiperazine in healthy men and women. Hum. Psychopharmacol. (1995) 10:385-391.
   Web of Science ®Google Scholar
• SARGENT PA, SHARPLEY AL, WILLIAMS C, GOODALL EM, COWEN PJ: 5-HT2C receptor activation decreases appetite and body weight in obese subjects. Psychopharmacology (1997) 133:309-312.
   PubMed Web of Science ®Google Scholar
• VAN GAAL LF, RISSANEN AM, SCHEEN AJ ZIEGLER O, ROSSNER 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.
   PubMed Web of Science ®Google Scholar
• HADDOCK CK, POSTON WSC, DILL PL FOREYT JP, ERICSSON M: Pharmacotherapy for obesity: a quantitative analysis of four decades of published randomized clinical trials. Int. J. Obes. (2002) 26:262-273.
   PubMed Web of Science ®Google Scholar
• THOMSON HEALTHCARE: Product information: adipex-P. In: Physicians’ Desk Reference. Medical Economics Company, Montvale, USA (2002):1406-1407.
   Google Scholar
• DESPRES JP, GOLAY A, SJOSTROM L: Effects of Rimonabant on metabolic risk factors in overweight patients with dyslipidemia. N. Engl. J. Med. (2005) 353(20):2121-2134.
   PubMed Web of Science ®Google Scholar
• JANDACEK RJ: APD356 Arena. Curr. Opin. Invest. Drugs (2005) 6(10):1051-1056.
   PubMedGoogle Scholar
• SMITH BM, SMITH JM, TSAI JH et al.: Discovery and SAR of new benzazepines as potent and selective 5-HT2C receptor agonists for the treatment of obesity. Bioorg. Med. Chem. Lett. (2005) 15:1467-1470.
   PubMed Web of Science ®Google Scholar
• SMITH BM: 5-HT2C receptor agonists for the treatment of obesity. Abstracts of Papers, 229th ACS National Meeting, San Diego, USA (13 – 17 March 2005).
   Google Scholar
• BLANCK HM, KHAN LK, SERDULA MK: Prescription weight loss pill use among Americans: patterns of pill use and lessons learned from the fen–phen market withdrawal. Preventive Med. (2004) 39:1243-1248.
   PubMed Web of Science ®Google Scholar