The 5-HT2C receptor agonist, lorcaserin, and the 5-HT6 receptor antagonist, SB-742457, promote satiety; A microstructural analysis of feeding behaviour

Psychopharmacology

Volumn 233, Issue 3, 2016, Pages 417-424

  Higgs, Suzanne ^a   Cooper, Alison J ^a   Barnes, Nicholas M ^a  

^a UNIVERSITY OF BIRMINGHAM   (United Kingdom)

Author keywords

5 HT2C receptor; 5 HT6 receptor; Feeding behaviour; Lorcaserin; Microstructural analysis; Obesity

Indexed keywords

3 PHENYLSULFONYL 8 (1 PIPERAZINYL)QUINOLINE; LORCASERIN; 3-BENZENESULFONYL-8-PIPERAZIN-1-YLQUINOLINE; BENZAZEPINE DERIVATIVE; GLUCOSE; QUINOLINE DERIVATIVE; SEROTONIN 2 AGONIST; SEROTONIN 2C RECEPTOR; SEROTONIN 6 RECEPTOR; SEROTONIN ANTAGONIST; SEROTONIN RECEPTOR; SULFONE;

ADULT; ANIMAL EXPERIMENT; ANORECTIC ACTIVITY; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG ACTIVITY; DRUG MEGADOSE; FEEDING BEHAVIOR; GLUCOSE INTAKE; LICKING; MALE; NONHUMAN; PRIORITY JOURNAL; RAT; SATIETY; STRUCTURE ANALYSIS; ANIMAL; DRUG EFFECTS; INSTRUMENTAL CONDITIONING; PSYCHOPHYSIOLOGY;

ANIMALS; BENZAZEPINES; CONDITIONING, OPERANT; DOSE-RESPONSE RELATIONSHIP, DRUG; FEEDING BEHAVIOR; GLUCOSE; MALE; QUINOLINES; RATS; RECEPTOR, SEROTONIN, 5-HT2C; RECEPTORS, SEROTONIN; SATIETY RESPONSE; SEROTONIN 5-HT2 RECEPTOR AGONISTS; SEROTONIN ANTAGONISTS; SULFONES;

EID: 84954505976     PISSN: 00333158     EISSN: 14322072     Source Type: Journal    
DOI: 10.1007/s00213-015-4112-x     Document Type: Article

References (65)

1. Asin KE, Davis JD, Bednarz L (1992) Differential effects of serotonergic and cathecholaminergic drugs on ingestive behaviour. Psychopharmacology 109:415-421
2. Balcioglu A, Wurtman RJ (2000) Sibutramine, a serotonin uptake inhibitor, increases dopamine concentrations in rat striatal and hypothalamic extracellular fluid. Neuropharmacology 39:2352-2359
3. 2C receptors in pro-opiomelanocortin neurons regulate energy and glucose homeostasis. J Clin Invest 123:5061-5070
4. Berthoud HR (2011) Metabolic and hedonic drives in the neural control of appetite: who is the boss? Curr Opin Neurobiol 21:888-896
5. Blundell JE (1977) Is there a role for serotonin (5-hydroxytryptamine) in feeding? Int J Obes 1:15-42
6. Breslin PAS, Davis JD, Rosenak R (1996) Saccharin increases the effectiveness of glucose in stimulating ingestion in rats but has little effect on negative feedback. Physiol Behav 60:411-416
7. Burke LK, Doslikova B, D'Agostino G, Garfield AS, Farooq G, Burdakov D, Low MJ, Rubinstein M, Evans ML, Bilups B, Heisler LK (2014) 5-HT obesity medication via POMC-activation in maintained during ageing. Endocrinology 155:3732-3738
8. Cabanac M (1971) Physiological role of pleasure. Science 173:1103-1107
9. Chan EW, He Y, Chui CS, Wong AY, Lau WC, Wong IC (2013) Efficacy and safety of lorcaserin in obese adults: a meta-analysis of 1-year randomised controlled trials (RCTs) and narrative review on short-term RCTs. Obes Rev 14:383-392
10. 2C receptor agonist, and d-fenfluramine on feeding patterns in the rat. Psychopharmacology 152:256-267
11. Cooper SJ, Higgs S (2005) Benzodiazepine effects on licking responses for sodium chloride solutions in water-deprived male rats. Physiol Behav 85:252-258
12. Danaei G, Ding EL, Mozaffarian D, Taylor B, Rehm J, Murray CJL, Ezzati M (2009) The preventable causes of death in the United States: comparative risk assessment for dietary, lifestyle, and metabolic risk factors. Plos Med 6, e1000058
13. Davis JD, Levine MW (1977) A model for the control of ingestion. Psychol Rev 84:379-412
14. Davis JD, Smith GP (1992) Analysis of the microstructure of the rhythmic tongue movements of rats ingesting maltose and sucrose solutions. Behav Neurosci 106:217-228
15. Davis JD, Smith GP, Singh B, McCann DL (2001) The impact of sucrose-derived unconditioned and conditioned negative feedback on the microstructure of ingestive behaviour. Physiol Behav 72:393-402
16. 6 antagonist GSK-742457 on PCP-induced deficits in reversal learning in the two-lever operant task in male Sprague Dawley rats. Behav Brain Res 244:15-28
17. Di Matteo V, Cacchio M, Di Giulio C, Esposito E (2002) Role of serotonin 2C receptors in the control of brain dopaminergic function. Pharmacol Biochem Behav 71:727-734
18. 2C receptor agonists. Drug Discov Today: Ther Strategies 3:577-583
19. Fidler MC, Sanchez M, Raether B, Weissman NJ, Smith SR, Shanahan WR, Anderson CM (2011) A one-year randomised trial of lorcaserin for weight loss in obese and overweight adults: the BLOSSOM trial. J Clin Endocrinol Metab 96:3067-3077
20. 6 receptor modulation by E-6837 induces hypophagia and sustained weight loss in diet-induced obese rats. Br J Pharmacol 148:973-983
21. 2B receptors in the cardiopathy associated with fenfluramine. Mol Pharmacol 57:75-81
22. 2C receptor ligands on motor activity and feeding behaviour in 5-HT2C receptor knockout mice. Neuropharmacology 57:259-267
23. 6 receptor antagonist, reduces food intake and body weight. Proceedings of the Serotonin Club Sixth IUPHAR Satellite Meeting on Serotonin, Hokkaido, Japan. 2006
24. 6 receptor antagonist-induced hypophagia. Behav Bran Res 266:201-206
25. Garfield AS, Li C, Madara JC, Shah BP, Webber E, Steger JS, Campbell JN, Gavrilova O, Lee CE, Olson DP, Elmquist JK, Tannous BA, Krashes MJ, Lowell BB (2015) A neural basis for melanocortin-4 receptor-regulated appetite. Nat Neurosci 18:863-871
26. Halford JC, Boyland EJ, Lawton CL, Blundell JE, Harrold JA (2011) Serotonergic anti-obesity agents: past experience and future prospects. Drugs 71:2247-2255
27. 6 receptor ligands: progress in the development of a novel pharmacological approach to the treatment of obesity and related metabolic disorders. Pharmacol Ther 117:207-231
28. Heisler LK, Cowley MA, Tecott LH, Fan W, Low MJ, Smart JL, Rubinstein M, Tatro JB, Marcus JN, Holstege H, Lee CE, Cone RD, Elmquist JK (2002) Activation of central melanocortin pathways by fenfluramine. Science 297:609-611
29. Heisler LK, Jobst EE, Sutton GM, Zhou L, Borok E, Thornton-Jones Z, Liu HY, Zigman JM, Balhasar N, Kishi T, Lee CE, Aschkenasi CJ, Zhang CY, Yu J, Boss O, Mountjoy KG, Clifton PG, Lowell BB, Friedman JM, Horvath T, Butler AA, Elmquist JK, Cowley MA (2006) Serotonin reciprocally regulates melanocortin neurons to modulate food intake. Neuron 51:239-249
30. Higgins GA, Silenieks LB, Roßmann A, Rizos Z, Noble K, Soko AD, Fletcher PJ (2012) The 5-HT2C receptor agonist lorcaserin reduces nicotine self-administration, discrimination, and reinstatement: relationship to feeding behavior and impulse control. Neuropsychopharmacology 37(5):1177-1191
31. 2C receptor agonist lorcaserin on efficacy and safety measures in a rat model of diet-induced obesity. Pharmacol Res Perspect 3, e00084
32. Higgs S, Cooper SJ (1996) Effects of the benzodiazepine receptor inverse agonist. Ro 15-4513 on the ingestion of sucrose and sodium saccharin solutions: a microstructural analysis of licking behavior. Behav Neurosci 110:559-566
33. Higgs S, Cooper SJ (1997) Midazolam induced rapid changes in licking behaviour: evidence for involvement of endogenous opioid peptides. Psychopharmacology 131:278-286
34. Higgs S, Cooper SJ (1998) Effects of benzodiazepine receptor ligands on the ingestion of sucrose, intralipid, and maltodextrin: an investigation using a microstructural analysis of licking behavior in a brief contact test. Behav Neurosci 112:447-457
35. Higgs S, Cooper SJ (2000) The effect of the dopamine D2 receptor antagonist raclopride on the pattern of licking microstructure induced by midazolam in the rat. Eur J Pharmacol 409(1):73-80
36. Higgs S, Williams CM, Kirkham TC (2003) Cannabinoid influences on palatability: microstructural analysis of sucrose drinking after Δ9-THC, anandamide, 2-AG and SR141716. Psychopharmacology 165:370-377
37. 2C receptor antagonist. Psychopharmacology 214:941-947
38. Hillebrand JJG, de Wied D, Adan RAH (2002) Neuropeptides, food intake and body weight regulation: a hypothalamic focus. Peptides 23:2283-2306
39. 2A receptor mechanisms. Psychopharmacology 208:23-36
40. Jackson HC, Bearham MC, Hutchins LJ, Mazurkiewicz SE, Needham AM, Heal DJ (1997) Investigation of the mechanisms underlying the hypophagic effects of the 5-HT and noradrenaline reuptake inhibitor, sibutramine, in the rat. Br J Pharmacol 121:1613-1618
41. Lam DD, Przydzial MJ, Ridley SH, Yeo GS, Rochford JJ, O'Rahilly S, Heisler LK (2008) Serotonin 5-HT2C receptor agonist promotes hypophagia via downstream activation of melanocortin 4 receptors. Endocrinology 149:1323-1328
42. Launay JM, Herve P, Peoc'h K, Tournois C, Callebert J, Nebigil CG, Etienne N, Drouet L, Humbert M, Simonneau G, Maroteaux L (2002) Function of the serotonin 5-hydroxytryptmine2B receptor in pulmonary hypertension. Nat Med 8:1129-1135
43. Maher-Edwards G, Dixon R, Hunter J, Gold M, Hopton G, Jacobs G, Hunter J, Williams P (2011) SB-742457 and donepezil in Alzheimer disease: a randomised, placebo-controlled study. Int J Geriatr Psychiatry 26:536-544
44. 2C receptor agonist, reduces body weight by decreasing energy intake without influencing energy expenditure. J Clin Endocrinol Metab 96:837-845
45. McNeely W, Goa KL (1998) Sibutramine: a review of its contribution to the management of obesity. Drugs 56:1093-1124
46. Meltzer HY, Roth BL (2013) Lorcaserin and pimavanserin: emerging selectivity of serotonin receptor subtype-targeted drugs. J Clin Invest 123:4986-4991
47. Michino M, Beuming T, Donthamsetti P, Newman AH, Javitch JA, Shi L (2015) What can crystal structures of aminergic receptors tell us about designing subtype-selective ligands? Pharmacol Rev 67:198-213
48. Nichols DE (2004) Hallucingens. Pharmacol Ther 101:131-181
49. O'Neil PM, Smith SR, Weissman NJ, Fidler MC, Sanchez M, Zhang J, Raether B, Anderson CM, Shanahan WR (2012) Randomized placebo-controlled clinical trial of lorcaserin for weight loss in type 2 diabetes mellitus: the BLOOM-DM study. Obesity 20:1426-1436
50. Ogden CL, Carroll MD, Kit BK, Flegal KM (2014) Prevalence of childhood and adult obesity in the United States, 2011-2012. JAMA 311:806-814
51. 2B receptors in the cardiac valvulopathy associated with fenfluramine and other serotonergic medications. Circulation 102:2836-2841
52. 2C receptor agonist for the treatment of obesity. J Med Chem 51:305-313
53. Smith SR, Weissman NJ, Anderson CM, Sanchez M, Chuang E, Stubbe S, Bays H, Shanahan WR (2010) Multicenter. Placebo-controlled trial of lorcaserin for weight management. N Eng J Med 363:245-256
54. Stellar E, Hill JH (1952) The rat's rate of drinking as a function of water deprivation. J Comp Physiol Psychol 5:96-102
55. Tallett AJ, Blundell JE, Rodgers RJ (2009) Sibutramine-induced anorexia: potent, dose-dependent and behaiourally-selective profile in male rats. Behav Brain Res 198:359-365
56. Thomas JM, Dourish CT, Tomlinson JW, Hassan-Smith Z, Higgs S (2014) Effects of the 5-HT2C receptor agonist meta-chlorophenylpiperazine on appetite, food intake and emotional processing in healthy volunteers. Psychopharmacology 231(12):2449-2459
57. 2C agonist: in vitro and in vivo pharmacological characterization. J Pharmacol Exp Ther 325:577-587
58. Vickers SP, Dourish CT (2004) Serotonin receptor ligands and the treatment of obesity. Curr Opin Investig Drugs 5:377-388
59. 2C receptor mutant mice. Psychopharmacology 143:309-314
60. Weintraub M, Hasday JD, Mushlin AI, Lockwood DH (1984) A double-blind clinical trial in weight control: use of fenfluramine and phentermine alone and in combination. Arch Intern Med 144:1143-1148
61. Weissman NJ, Sanchez M, Koch GG, Smith SR, Shanahan WR, Anderson CM (2013) Echocardiographic assessment of cardiac valular regurgitation with lorcaserin from analysis of 3 phase 3 clinical trials. Circ Cardiovasc Imaging 6:560-567
62. 6) receptors in vivo. Eur J Pharmacol 676:6-11
63. Woolley ML, Bentley JC, Sleight AJ, Marsden CA, Fone KC (2001) A role for 5-ht6 receptors in retention of spatial learning in the Morris water maze. Neuropharmacology 41:210-219
64. 2CRs expressed by pro-opiomelanocortin neurons regulate energy homeostasis. Neuron 60:582-589
65. Xu Y, Jones JE, Lauzon DA, Anderson JG, Balthasar N, Heisler LK, Zinn AR, Lowell BB, Elmquist JK (2010) A serotonin and melanocortin circuit mediates D-defenfluramine anorexia. J Neurosci 30:14630-14634