The development of tolerance to drugs that suppress food intake

Pharmacology and Therapeutics

Volumn 117, Issue 1, 2008, Pages 105-122

  Fernstrom, John D ^a   Choi, SuJean ^a  

^a UNIVERSITY OF PITTSBURGH SCHOOL OF MEDICINE   (United States)

Author keywords

Appetite suppressants; Food intake; Human; Obesity; Rodents; Tolerance

Indexed keywords

(3 CHLOROPHENYL)PIPERAZINE; AMPHETAMINE; ANOREXIGENIC AGENT; CHOLECYSTOKININ OCTAPEPTIDE; FENFLURAMINE; FLUOXETINE; LEPTIN; MELANOTAN 2; N ACETYL ALPHA INTERMEDIN[4-10]CYCLO[4 NORLEUCINE 5 ASPARTIC ACID 7 [3 (2 NAPHTHYL)ALANINE] 10 LYSINAMIDE]; NEUROTRANSMITTER RECEPTOR; PHENTERMINE; PLACEBO; RIMONABANT; SIBUTRAMINE; UNCLASSIFIED DRUG;

BODY WEIGHT; CLINICAL TRIAL; DOWN REGULATION; DRUG EFFICACY; DRUG MECHANISM; DRUG MEGADOSE; DRUG TOLERANCE; DRUG USE; DRUG WITHDRAWAL; FOOD INTAKE; HUMAN; HUNGER; LATERAL HYPOTHALAMUS; LONG TERM CARE; LOW DRUG DOSE; NEUROTRANSMISSION; NONHUMAN; OBESITY; PRIORITY JOURNAL; REVIEW; SINGLE DRUG DOSE; WEIGHT CHANGE; WEIGHT GAIN; WEIGHT REDUCTION;

ANIMALS; APPETITE DEPRESSANTS; BODY WEIGHT; CYCLOBUTANES; DRUG TOLERANCE; EATING; FENFLURAMINE; HUMANS; LEPTIN; OBESITY; RATS; TIME FACTORS; WEIGHT LOSS;

EID: 36649019357     PISSN: 01637258     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.pharmthera.2007.09.001     Document Type: Review

References (153)

1. 2C receptor protein in human and rat brain using specific antisera. Neuropharmacology 34 (1995) 1635-1645
2. Antelman S.M., Rowland N., and Kocan D. Anorectics: lack of cross tolerance among serotonergic drugs and sensitization of amphetamine's effect. In: Garattini S., and Samanin R. (Eds). Anorectic agents: mechanisms of action and tolerance (1981), Raven Press, New York 45-62
3. Antin J., Gibbs J., Holt J., Young R.C., and Smith G.P. Cholecystokinin elicits the complete behavioral sequence of satiety in rats. J Comp Physiol Psychol 89 (1975) 784-790
4. Arnold J.C., Hunt G.E., McGregor I.S., Arnold J.C., Hunt G.E., and McGregor I.S. Effects of the cannabinoid receptor agonist CP 55,940 and the cannabinoid receptor antagonist SR 141716 on intracranial self-stimulation in Lewis rats. Life Sci 70 (2001) 97-108
5. Banks W.A., Kastin A.J., Huang W., Jaspan J.B., and Maness L.M. Leptin enters the brain by a saturable system independent of insulin. Peptides 17 (1996) 305-311
6. 3 substituted phenethylamines. In: Costa E., and Garattini S. (Eds). Amphetamines and Related Compounds (1970), Raven Press, New York 21-61
7. Berridge K.C. Food reward: brain substrates of wanting and liking. Neurosci Biobehav Rev 20 (1996) 1-25
8. Berridge K.C., and Robinson T.E. Parsing reward. Trends Neurosci 26 (2003) 507-513
9. Berthoud H.R. Multiple neural systems controlling food intake and body weight. Neurosci Biobehav Rev 26 (2002) 393-428
10. Berthoud H.R. Mind versus metabolism in the control of food intake and energy balance. Physiol Behav 81 (2004) 781-793
11. Berthoud H.R. Neural control of appetite: cross-talk between homeostatic and non-homeostatic systems. Appetite 43 (2004) 315-317
12. Biel J.H. Structure-activity relationships of amphetamine and derivatives. In: Costa E., and Garattini S. (Eds). Amphetamines and Related Compounds (1970), Raven Press, New York 3-19
13. Blundell J.E. Serotonin and appetite. Neuropharmacology 23 (1984) 1537-1551
14. Blundell J.E. Serotonin manipulations and the structure of feeding behaviour. Appetite 7 Suppl (1986) 39-56
15. Blundell J.E. What foods do people habitually eat? A dilemma for nutrition, an enigma for psychology. Am J Clin Nutr 71 (2000) 3-5
16. Blundell J.E., and Halford J.C. Serotonin and appetite regulation: implications for the pharmacological treatment of obesity. CNS Drugs 9 (1998) 473-495
17. Blundell J.E., and McArthur R.A. Behavioural flux and feeding: continuous monitoring of food intake and food selection, and the video-recording of appetitive and satiety sequences for the analysis of drug action. In: Garattini S., and Samanin R. (Eds). Anorectic Agents: Mechanisms of Action (1981), Raven Press, New York 19-43
18. Bray G.A., Ryan D.H., Gordon D., Heidingsfelder S., Cerise F., and Wilson K. A double-blind randomized placebo-controlled trial of sibutramine. Obes Res 4 (1996) 263-270
19. Broberger C. Brain regulation of food intake and appetite: molecules and networks. J Intern Med 258 (2005) 301-327
20. Brown M., Bing C., King P., Pickavance L., Heal D., and Wilding J. Sibutramine reduces feeding, body fat and improves insulin resistance in dietary-obese male Wistar rats independently of hypothalamic neuropeptide Y. Br J Pharmacol 132 (2001) 1898-1904
21. Bruinvels A.T., Landwehrmeyer B., Gustafson E.L., Durkin M.M., Mengod G., Branchek T.A., et al. Localization of 5HT1B, 5HT1Dα, 5HT1E and 5HT1F receptor messenger RNA in rodent and primate brain. Neuropharmacology 33 (1994) 367-386
22. Buckett W.R., Thomas P.C., and Luscombe G.P. The pharmacology of sibutramine hydrochloride (BTS 54 524), a new antidepressant which induces rapid noradrenergic down-regulation. Prog Neuropsychopharmacol Biol Psychiatry 12 (1988) 575-584
23. Cabeza de Vaca S., Kim G.Y., and Carr K.D. The melanocortin receptor agonist MTII augments the rewarding effect of amphetamine in ad-libitum-fed and food-restricted rats. Psychopharmacology (Berlin) 161 (2002) 77-85
24. Cabeza de Vaca S., Hao J., Afroz T., Krahne L.L., and Carr K.D. Feeding, body weight, and sensitivity to non-ingestive reward stimuli during and after 12-day continuous central infusions of melanocortin receptor ligands. Peptides 26 (2005) 2314-2321
25. Calogero A.E., Bernardini R., Margioris A.N., Bagdy G., Gallucci W.T., Munson P.J., et al. Effects of serotonergic agonists and antagonists on corticotropin-releasing hormone secretion by explanted rat hypothalami. Peptides 10 (1989) 189-200
26. Carlton J., and Rowland N. Effects of initial body weight on anorexia and tolerance to fenfluramine in rats. Pharmacol Biochem Behav 23 (1985) 551-554
27. Carlton J., and Rowland N.E. Long term actions of d-fenfluramine in two rat models of obesity: I. Sustained reductions in body weight and adiposity without depletion of brain serotonin. Int J Obes 13 (1989) 825-847
28. Carlton P.L., and Wolgin D.L. Contingent tolerance to the anorexigenic effects of amphetamine. Physiol Behav 7 (1971) 221-223
29. Choi S., Jonak E.M., Simpson L., Patil V., and Fernstrom J.D. Intermittent, chronic fenfluramine administration to rats repeatedly suppresses food intake despite substantial brain serotonin reductions. Brain Res 928 (2002) 30-39
30. Choi S., Blake V., Cole S., and Fernstrom J.D. Effects of chronic fenfluramine administration on hypothalamic neuropeptide mRNA expression. Brain Res 1087 (2006) 83-86
31. Clark J.T., Kalra P.S., Crowley W.R., and Kalra S.P. Neuropeptide Y and human pancreatic polypeptide stimulate feeding behavior in rats. Endocrinology 115 (1984) 427-429
32. Clifton P.G. Meal patterning in rodents: psychopharmacological and neuroanatomical studies. Neurosci Biobehav Rev 24 (2000) 213-222
33. Clifton P.G., Barnfield A.M., and Philcox L. A behavioural profile of fluoxetine-induced anorexia. Psychopharmacology (Berlin) 97 (1989) 89-95
34. Cone R.D. Anatomy and regulation of the central melanocortin system. Nat Neurosci 8 (2005) 571-578
35. Curzon G., Gibson E.L., and Oluyomi A.O. Appetite suppression by commonly used drugs depends on 5HT receptors but not on 5HT availability. Trends Pharmacol Sci 18 (1997) 21-25
36. De Vry J., and Schreiber R. Effects of selected serotonin 5HT(1) and 5HT(2) receptor agonists on feeding behavior: possible mechanisms of action. Neurosci Biobehav Rev 24 (2000) 341-353
37. Deroche-Gamonet V., LeMoal M., Piazza P.V., and Soubrie P. SR141716, a CB1 receptor antagonist, decreases the sensitivity to the reinforcing effects of electrical brain stimulation in rats. Psychopharmacology (Berlin) 157 (2001) 254-259
38. Dryden S., Frankish H.M., Wang Q., Pickavance L., and Williams G. The serotonergic agent fluoxetine reduces neuropeptide Y levels and neuropeptide Y secretion in the hypothalamus of lean and obese rats. Neuroscience 72 (1996) 557-566
39. Dryden S., Wang Q., Frankish H.M., and Williams G. Differential effects of the 5HT 1B/2C receptor agonist mCPP and the 5HT1A agonist flesinoxan on hypothalamic neuropeptide Y in the rat: evidence that NPY may mediate serotonin's effects on food intake. Peptides 17 (1996) 943-949
40. Dube M.G., Sahu A., Phelps C.P., Kalra P.S., and Kalra S.P. Effect of d-fenfluramine on neuropeptide Y concentration and release in the paraventricular nucleus of food-deprived rats. Brain Res Bull 29 (1992) 865-869
41. Eiden S., Simon E., and Schmidt I. Dose-related steady states of fat loss in long-term leptin-treated ob/ob mice: leptin resistance or desensitization versus counterregulatory signaling. J Comp Physiol B 175 (2005) 487-497
42. Evans S.A., Parsons A.D., and Overton J.M. Homeostatic responses to caloric restriction: influence of background metabolic rate. J Appl Physiol 99 (2005) 1336-1342
43. Fan W., Boston B.A., Kesterson R.A., Hruby V.J., and Cone R.D. Role of melanocortinergic neurons in feeding and the agouti obesity syndrome. Nature 385 (1997) 165-168
44. Fernstrom J.D., Courcoulas A.P., Houck P.R., and Fernstrom M.H. Chronic changes in blood pressure in extremely obese patients who have undergone bariatric surgery. Arch Surg 141 (2006) 276-283
45. Finlayson G., King N., and Blundell J.E. Liking vs. wanting food: importance for human appetite control and weight regulation. Neurosci Biobehav Rev 31 (2007) 987-1002
46. Fone K.C., Austin R.H., Topham I.A., Kennett G.A., and Punhani T. Effect of chronic m-CPP on locomotion, hypophagia, plasma corticosterone and 5HT2C receptor levels in the rat. Br J Pharmacol 123 (1998) 1707-1715
47. Fulton S., Woodside B., and Shizgal P. Modulation of brain reward circuitry by leptin. Science 287 (2000) 125-128
48. Garattini S., Bizzi A., Codegoni A.M., Caccia S., and Mennini T. Progress report on the anorexia induced by drugs believed to mimic some of the effects of serotonin on the central nervous system. Am J Clin Nutr 55 (1992) 160S-166S
49. Goris A.H., Westerterp-Plantenga M.S., and Westerterp K.R. Undereating and underrecording of habitual food intake in obese men: selective underreporting of fat intake. Am J Clin Nutr 71 (2000) 130-134
50. Grignaschi G., Fanelli E., Scagnol I., and Samanin R. Studies on the role of serotonin receptor subtypes in the effect of sibutramine in various feeding paradigms in rats. Br J Pharmacol 127 (1999) 1190-1194
51. Guy J., Pelletier G., and Bosler O. Serotonin innervation of neuropeptide Y-containing neurons in the rat arcuate nucleus. Neurosci Lett 85 (1988) 9-13
52. Guy Grand B.J.P. A new approach to the treatment of obesity: a discussion. Ann N Y Acad Sci 499 (1987) 313-317
53. Guy Grand B., Apfelbaum M., Crepaldi G., Gries A., Lefebvre P., and Turner P. International trial of long-term dexfenfluramine in obesity. Lancet 2 (1989) 1142-1145
54. Hakansson M.L., Brown H., Ghilardi N., Skoda R.C., and Meister B. Leptin receptor immunoreactivity in chemically defined target neurons of the hypothalamus. J Neurosci 18 (1998) 559-572
55. Halaas J.L., Boozer C., Blair-West J., Fidahusein N., Denton D.A., and Friedman J.M. Physiological response to long-term peripheral and central leptin infusion in lean and obese mice. Proc Natl Acad Sci U S A 94 (1997) 8878-8883
56. Harvey J.A., and McMaster S.E. Fenfluramine: evidence for a neurotoxic action on midbrain and a long-term depletion of serotonin. Psychopharm Commun 1 (1975) 217-228
57. Harvey J.A., and McMaster S.E. Fenfluramine: cumulative neurotoxicity after chronic treatment with low dosages in the rat. Commun Psychopharmacol 1 (1977) 3-17
58. Heal D.J., Butler S.A., Hurst E.M., and Buckett W.R. Antidepressant treatments, including sibutramine hydrochloride and electroconvulsive shock, decrease beta 1-but not beta 2-adrenoceptors in rat cortex. J Neurochem 53 (1989) 1019-1025
59. Heal D.J., Aspley S., Prow M.R., Jackson H.C., Martin K.F., and Cheetham S.C. Sibutramine: a novel anti-obesity drug. A review of the pharmacological evidence to differentiate it from d-amphetamine and d-fenfluramine. Int J Obes 22 Suppl 1 (1998) S18-S28
60. Heal D.J., Cheetham S.C., Prow M.R., Martin K.F., and Buckett W.R. A comparison of the effects on central 5HT function of sibutramine hydrochloride and other weight-modifying agents. Br J Pharmacol 125 (1998) 301-308
61. 2-adrenoceptor function in the brain: rapid down-regulation by sibutramine hydrochloride. Psychopharmacology (Berlin) 103 (1991) 251-257
62. Heisler L.K., Cowley M.A., Tecott L.H., Fan W., Low M.J., Smart J.L., et al. Activation of central melanocortin pathways by fenfluramine. Science 297 (2002) 609-611
63. Heisler L.K., Jobst E.E., Sutton G.M., Zhou L., Borok E., Thornton-Jones Z., et al. Serotonin reciprocally regulates melanocortin neurons to modulate food intake. Neuron 51 (2006) 239-249
64. Hewitt K.N., Lee M.D., Dourish C.T., and Clifton P.G. Serotonin 2C receptor agonists and the behavioural satiety sequence in mice. Pharmacol Biochem Behav 71 (2002) 691-700
65. 1C receptor mRNA in adult rat brain. FEBS Lett 247 (1989) 453-462
66. Hoyer D., Hannon J.P., and Martin G.R. Molecular, pharmacological and functional diversity of 5HT receptors. Pharmacol Biochem Behav 71 (2002) 533-554
67. Jackson H.C., Bearham M.C., Hutchins L.J., Mazurkiewicz S.E., Needham A.M., and Heal D.J. Investigation of the mechanisms underlying the hypophagic effects of the 5HT and noradrenaline reuptake inhibitor, sibutramine, in the rat. Br J Pharmacol 121 (1997) 1613-1618
68. Jackson H.C., Needham A.M., Hutchins L.J., Mazurkiewicz S.E., and Heal D.J. Comparison of the effects of sibutramine and other monoamine reuptake inhibitors on food intake in the rat. Br J Pharmacol 121 (1997) 1758-1762
69. James W.P., Astrup A., Finer N., Hilsted J., Kopelman P., Rossner S., et al. Effect of sibutramine on weight maintenance after weight loss: a randomised trial. Lancet 356 (2000) 2119-2125
70. Javed A., Kamradt M.C., Van de Kar L.D., and Gray T.S. d-Fenfluramine induces serotonin-mediated Fos expression in corticotropin-releasing factor and oxytocin neurons of the hypothalamus, and serotonin-independent Fos expression in enkephalin and neurotensin neurons of the amygdala. Neuroscience 90 (1999) 851-858
71. Jonsson L., Skarphedinsson J.O., Skuladottir G.V., Watanobe H., and Schioth H.B. Food conversion is transiently affected during 4-week chronic administration of melanocortin agonist and antagonist in rats. J Endocrinol 173 (2002) 517-523
72. Kageyama K., Tozawa F., Horiba N., Watanobe H., and Suda T. Serotonin stimulates corticotropin-releasing factor gene expression in the hypothalamic paraventricular nucleus of conscious rats. Neurosci Lett 243 (1998) 17-20
73. Kawai K., Sugimoto K., Nakashima K., Miura H., and Ninomiya Y. Leptin as a modulator of sweet taste sensitivities in mice. Proc Natl Acad Sci U S A 97 (2000) 11044-11049
74. Keesey R.E., and Hirvonen M.D. Body weight set points: determination and adjustment. J Nutr 127 (1997) 1875S-1883S
75. Keesey R.E., and Powley T.L. The regulation of body weight. Annu Rev Psychol 37 (1986) 109-133
76. Kelley A.E., Baldo B.A., Pratt W.E., and Will M.J. Corticostriatal-hypothalamic circuitry and food motivation: integration of energy, action and reward. Physiol Behav 86 (2005) 773-795
77. Kiss J., Leranth C., and Halasz B. Serotoninergic endings on VIP-neurons in the suprachiasmatic nucleus and on ACTH-neurons in the arcuate nucleus of the rat hypothalamus. A combination of high resolution autoradiography and electron microscopic immunocytochemistry. Neurosci Lett 44 (1984) 119-124
78. Krahn D.D., Gosnell B.A., Levine A.S., and Morley J.E. Behavioral effects of corticotropin-releasing factor: localization and characterization of central effects. Brain Res 443 (1988) 63-69
79. Kuo D.Y., Hsu C.T., and Cheng J.T. Role of hypothalamic neuropeptide Y (NPY) in the change of feeding behavior induced by repeated treatment of amphetamine. Life Sci 70 (2001) 243-251
80. Laflamme N., Bovetto S., Richard D., and Rivest S. Effect of dexfenfluramine on the transcriptional activation of CRF and its type 1 receptor within the paraventricular nucleus of the rat hypothalamus. Br J Pharmacol 117 (1996) 1021-1034
81. Lee M.D., Aloyo V.J., Fluharty S.J., and Simansky K.J. Infusion of the serotonin1B (5HT1B) agonist CP-93,129 into the parabrachial nucleus potently and selectively reduces food intake in rats. Psychopharmacology (Berlin) 136 (1998) 304-307
82. 1B receptor knockout mice. Psychopharmacology (Berlin) 176 (2004) 39-49
83. Leibowitz S.F., Weiss G.F., and Shor Posner G. Hypothalamic serotonin: pharmacological, biochemical, and behavioral analyses of its feeding-suppressive action. Clin Neuropharmacol 11 Suppl 1 (1988) S51-S71
84. Levin B.E., and Dunn-Meynell A.A. Sibutramine alters the central mechanisms regulating the defended body weight in diet-induced obese rats. Am J Physiol 279 (2000) R2222-R2228
85. Levine A.S., and Morley J.E. Neuropeptide Y: a potent inducer of consummatory behavior in rats. Peptides 5 (1984) 1025-1029
86. Levitsky D.A., Strupp B.J., and Lupoli J. Tolerance to anorectic drugs: pharmacological or artifactual. Pharmacol Biochem Behav 14 (1981) 661-667
87. Li B.H., and Rowland N.E. Dexfenfluramine induces fos-like immunoreactivity in discrete brain regions in rats. Brain Res Bull 31 (1993) 43-48
88. Li B.H., and Rowland N.E. Effect of chronic dexfenfluramine on Fos in rat brain. Brain Res 728 (1996) 188-192
89. Li B.H., Spector A.C., and Rowland N.E. Reversal of dexfenfluramine-induced anorexia and c-Fos/c-Jun expression by lesion in the lateral parabrachial nucleus. Brain Res 640 (1994) 255-267
90. Liposits Z., Phelix C., and Paull W.K. Synaptic interaction of serotonergic axons and corticotropin releasing factor (CRF) synthesizing neurons in the hypothalamic paraventricular nucleus of the rat. A light and electron microscopic immunocytochemical study. Histochemistry 86 (1987) 541-549
91. Lucas J.J., Yamamoto A., Scearce-Levie K., Saudou F., and Hen R. Absence of fenfluramine-induced anorexia and reduced c-fos induction in the hypothalamus and central amygdaloid complex of serotonin 1b receptor knock-out mice. J Neurosci 18 (1998) 5537-5544
92. Luscombe G.P., Hopcroft R.H., Thomas P.C., and Buckett W.R. The contribution of metabolites to the rapid and potent down-regulation of rat cortical β-adrenoceptors by the putative antidepressant sibutramine hydrochloride. Neuropharmacology 28 (1989) 129-134
93. 1B) receptors in the normal rat hypothalamus. Neurosci Lett 328 (2002) 155-159
94. 1A autoreceptor response and its evaluation as a model to selectively identify antidepressants. Br J Pharmacol 107 (1992) 15-21
95. Martin R.L., Perez E., He Y.J., Dawson Jr. R., and Millard W.J. Leptin resistance is associated with hypothalamic leptin receptor mRNA and protein downregulation. Metabolism 49 (2000) 1479-1484
96. McCann U.D., Yuan J., Hatzidimitriou G., and Ricaurte G. Selective serotonin reuptake inhibitors dissociate fenfluramine's anorectic and neurotoxic effects: importance of dose, species and drug. J Pharmacol Exp Ther 281 (1997) 1487-1498
97. McClelland R.C., and Hoebel B.G. d-Fenfluramine and self-stimulation: loss of inhibitory effect in underweight rats. Brain Res Bull 27 (1991) 341-345
98. McClelland R.C., Sarfaty T., Hernandez L., and Hoebel B.G. The appetite suppressant, d-fenfluramine, decreases self-stimulation at a feeding site in the lateral hypothalamus. Pharmacol Biochem Behav 32 (1989) 411-414
99. Meister B., and Hakansson M.L. Circumventricular organs: gateways to the brainleptin receptors in hypothalamus and circumventricular organs. Clin Exp Pharmacol Physiol 28 (2001) 610-617
100. 2C receptor agonsits: potential for the treatment of obesity. Mol Interv 5 (2005) 282-291
101. Mokdad A.H., Serdula M.K., Dietz W.H., Bowman B.A., Marks J.S., and Koplan J.P. The spread of the obesity epidemic in the United States, 1991-1998. JAMA 282 (1999) 1519-1522
102. Molineaux S.M., Jessell T.M., Axel R., and Julius D. 5HT1c receptor is a prominent serotonin receptor subtype in the central nervous system. Proc Natl Acad Sci U S A 86 (1989) 6793-6797
103. Must A., Spadano J., Coakley E.H., Field A.E., Colditz G., and Dietz W.H. The disease burden associated with overweight and obesity. JAMA 282 (1999) 1523-1529
104. Neter J.E., Stam B.E., Kok F.J., Grobbee D.E., and Geleijnse J.M. Influence of weight reduction on blood pressure: a meta-analysis of randomized controlled trials. Hypertension 42 (2003) 878-884
105. NHLBI Obesity Education Initiative Expert Panel on the Identification, Evaluation and Treatment of Overweight and Obesity in Adults. Clinical guidelines on the identification, evaluation, and treatment of overweight and obesity in adults - the evidence report. Obes Res 6 (1998) 51S-209S
106. Ollmann M.M., Wilson B.D., Yang Y.K., Kerns J.A., Chen Y., Gantz I., et al. Antagonism of central melanocortin receptors in vitro and in vivo by agouti-related protein. Science 278 (1997) 135-138
107. Pal R., and Sahu A. Leptin signaling in the hypothalamus during chronic central leptin infusion. Endocrinology 144 (2003) 3789-3798
108. Pi-Sunyer F.X., Aronne L.J., Heshmati H.M., Devin J., and 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 295 (2006) 761-775
109. Poulos C.X. Homeostatic regulation and Pavlovian conditioning in tolerance to amphetamine-induced anorexia. J Comp Physiol Psychol 95 (1981) 735-746
110. Rogers P.J., and Blundell J.E. Effect of anorexic drugs on food intake and the micro-structure of eating in human subjects. Psychopharmacology (Berlin) 66 (1979) 159-165
111. Rogers P., McKibbin P.E., and Williams G. Acute fenfluramine administration reduces neuropeptide Y concentrations in specific hypothalamic regions of the rat: possible implications for the anorectic effect of fenfluramine. Peptides 12 (1991) 251-255
112. Rowland N.E. Long-term administration of dexfenfluramine to genetically obese (ob/ob) and lean mice: body weight and brain serotonin changes. Pharmacol Biochem Behav 49 (1994) 287-294
113. Rowland N.E. Tolerance to the anorectic effect of dexfenfluramine in rats: role of serotonin, cholecystokinin, and neuropeptide Y. Physiol Behav 55 (1994) 201-207
114. Rowland N., and Carlton J. Different behavioral mechanisms underlie tolerance to the anorectic effects of fenfluramine and quipazine. Psychopharmacology (Berlin) 81 (1983) 155-157
115. Rowland N.E., and Carlton J. Neurobiology of an anorectic drug: fenfluramine. Prog Neurobiol 27 (1986) 13-62
116. Rowland N., Carlton J., Bartness T., and Smith G. Effect of chronic administration of fenfluramine and quipazine on body weight gain after ovariectomy and on brain serotonin receptor binding. Behav Neurosci 97 (1983) 502-505
117. Rowland N.E., Robertson K., Lo J., and Rema E. Cross tolerance between anorectic action and induction of Fos-ir with dexfenfluramine and 5HT1B/2C agonists in rats. Psychopharmacologia 156 (2001) 108-114
118. Rowland N.E., Robertson K., and Green D.J. Effect of repeated administration of dexfenfluramine on feeding and brain Fos in mice. Physiol Behav 78 (2003) 295-301
119. Rowley H.L., Butler S.A., Prow M.R., Dykes S.G., Aspley S., Kilpatrick I.C., et al. Comparison of the effects of sibutramine and other weight-modifying drugs on extracellular dopamine in the nucleus accumbens of freely moving rats. Synapse 38 (2000) 167-176
120. Sahu A. Resistance to the satiety action of leptin following chronic central leptin infusion is associated with the development of leptin resistance in neuropeptide Y neurones. J Neuroendocrinol 14 (2002) 796-804
121. Sahu A., and Metlakunta A.S. Hypothalamic phosphatidylinositol 3-kinase-phosphodiesterase 3B-cyclic AMP pathway of leptin signalling is impaired following chronic central leptin infusion. J Neuroendocrinol 17 (2005) 720-726
122. 3H-serotonin and serotenergic sensitivity in rats. Eur J Pharmacol 61 (1980) 203-206
123. Schoeller D.A. Limitations in the assessment of dietary energy intake by self-report. Metabolism 44 (1995) 18-22
124. Schwartz M.W., Seeley R.J., Campfield L.A., Burn P., and Baskin D.G. Identification of targets of leptin action in rat hypothalamus. J Clin Invest 98 (1996) 1101-1106
125. Schwartz M.W., Woods S.C., Porte D., Seeley R.J., and Baskin D.G. Central nervous system control of food intake. Nature 404 (2000) 661-671
126. Seeley R.J., Burklow M.L., Wilmer K.A., Matthews C.C., Reizes O., McOsker C.C., et al. The effect of the melanocortin agonist, MT-II, on the defended level of body adiposity. Endocrinology 146 (2005) 3732-3738
127. Shigemura N., Ohta R., Kusakabe Y., Miura H., Hino A., Koyano K., et al. Leptin modulates behavioral responses to sweet substances by influencing peripheral taste structures. Endocrinology 145 (2004) 839-847
128. Shoulson I., and Chase T.N. Fenfluramine in man: hypophagia associated with diminished serotonin turnover. Clin Pharmacol Ther 17 (1975) 616-621
129. Silverstone T. Appetite suppressants: a review. Drugs 43 (1992) 820-836
130. Silverstone T., Wells B., and Trenchard E. Differential dose-response effects of dexamphetamine sulphate on hunger, arousal and mood in human volunteers. Psychopharmacology (Berlin) 79 (1983) 242-245
131. Simansky K.J., and Nicklous D.M. Parabrachial infusion of d-fenfluramine reduces food intake. Blockade by the 5HT(1B) antagonist SB-216641. Pharmacol Biochem Behav 71 (2002) 681-690
132. Sjöström L., Lindroos A.K., Peltonen M., Torgerson J., Bouchard C., Carlsson B., et al. Lifestyle, diabetes, and cardiovascular risk factors 10 years after bariatric surgery. N Engl J Med 351 (2004) 2683-2693
133. Stallone D.D., and Stunkard A.J. Long-term use of appetite suppressant medication: rationale and recommendations. Drug Dev Res 26 (1992) 1-20
134. Stanley B.G., and Leibowitz S.F. Neuropeptide Y: stimulation of feeding and drinking by injection into the paraventricular nucleus. Life Sci 35 (1984) 2635-2642
135. Strack A.M., Shu J., Camacho R., Gorski J.N., Murphy B., MacIntyre D.E., et al. Regulation of body weight and carcass composition by sibutramine in rats. Obes Res 10 (2002) 173-181
136. Stunkard A.J. Anorectic agents lower a body weight set point. Life Sci 30 (1982) 2043-2055
137. Sugrue M.F. Neuropharmacology of drugs affecting food intake. Pharmacol Ther 32 (1987) 145-182
138. Swanson L.W., Sawchenko P.E., Rivier J., and Vale W.W. Organization of ovine corticotropin-releasing factor immunoreactive cells and fibers in the rat brain: an immunohistochemical study. Neuroendocrinology 36 (1983) 165-186
139. Trifunovic R., and Reilly S. Medial parabrachial nucleus neurons modulate d-fenfluramine-induced anorexia through 5HT2C receptors. Brain Res 1067 (2006) 170-176
140. Vickers S.P., and Dourish C.T. Serotonin receptor ligands and the treatment of obesity. Curr Opin Investig Drugs 5 (2004) 377-388
141. Vickers S.P., Clifton P.G., Dourish C.T., and Tecott L.H. Reduced satiating effect of d-fenfluramine in serotonin 5HT(2C) receptor mutant mice. Psychopharmacology (Berlin) 143 (1999) 309-314
142. Vickers S.P., Benwell K.R., Porter R.H., Bickerdike M.J., Kennett G.A., and Dourish C.T. Comparative effects of continuous infusion of mCPP, Ro 60-0175 and d-fenfluramine on food intake, water intake, body weight and locomotor activity in rats. Br J Pharmacol 130 (2000) 1305-1314
143. Vickers S.P., Dourish C.T., and Kennett G.A. Evidence that hypophagia induced by d-fenfluramine and d-norfenfluramine in the rat is mediated by 5HT2C receptors. Neuropharmacology 41 (2001) 200-209
144. Vickers S.P., Easton N., Webster L.J., Wyatt A., Bickerdike M.J., Dourish C.T., et al. Oral administration of the 5HT2C receptor agonist, mCPP, reduces body weight gain in rats over 28 days as a result of maintained hypophagia. Psychopharmacology (Berlin) 167 (2003) 274-280
145. Vickers S.P., Webster L.J., Wyatt A., Dourish C.T., and Kennett G.A. 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 (Berlin) 167 (2003) 103-111
146. Weintraub M. Long-term weight control: The National Heart, Lung, and Blood Institute funded multimodal intervention study. Clin Pharmacol Ther 51 (1992) 581-646
147. Weintraub M., Hasday J.D., Mushlin A.I., and Lockwood D.H. A double-blind clinical trial in weight control. Use of fenfluramine and phentermine alone and in combination. Arch Intern Med 144 (1984) 1143-1148
148. Wellman P.J., Jones S.L., and Miller D.K. Effects of preexposure to dexfenfluramine, phentermine, dexfenfluramine-phentermine, or fluoxetine on sibutramine-induced hypophagia in the adult rat. Pharmacol Biochem Behav 75 (2003) 103-114
149. Wirth A., and Krause J. Long-term weight loss with sibutramine: a randomized controlled trial. JAMA 286 (2001) 1331-1339
150. Wise R.A. Forebrain substrates of reward and motivation. J Comp Neurol 493 (2005) 115-121
151. Wolgin D.L. Contingent tolerance to amphetamine hypophagia: new insights into the role of environmental context in the expression of stereotypy. Neurosci Biobehav Rev 24 (2000) 279-294
152. Wolgin D.L. Effects of chronic amphetamine on the appetitive and consummatory phases of feeding. Appetite 38 (2002) 221-223
153. Woods S.C., Seeley R.J., Porte D., and Schwartz M.W. Signals that regulate food intake and energy homeostasis. Science 280 (1998) 1378-1383