Brain serotonin transporter occupancy by oral sibutramine dosed to steady state: A PET study using 11C-DASB in healthy humans

Neuropsychopharmacology

Volumn 35, Issue 3, 2010, Pages 741-751

  Talbot, Peter S ^a   Bradley, Stefan ^b   Clarke, Cyril P ^b   Babalola, Kola O ^a   Philipp, Andrew W ^b   Brown, Gavin ^a   McMahon, Adam W ^a   Matthews, Julian C ^a  

^a UNIVERSITY OF MANCHESTER   (United Kingdom)

^b ICON Development Solutions   (United States)

Author keywords

11C DASB; Appetite suppression; High Resolution Research Tomograph (HRRT); Positron emission tomography (PET); Serotonin transporter (SERT); Sibutramine

Indexed keywords

CARBON 11; CARBON 11 DASB; DI DESMETHYLSIBUTRAMINE; DRUG METABOLITE; MONO DESMETHYLSIBUTRAMINE; PLACEBO; SEROTONIN TRANSPORTER; SIBUTRAMINE; UNCLASSIFIED DRUG;

ADULT; ANOREXIA; ARTICLE; BRAIN REGION; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DOSE RESPONSE; DOUBLE BLIND PROCEDURE; DRUG BINDING; DRUG BLOOD LEVEL; DRUG METABOLISM; HUMAN; HUMAN EXPERIMENT; MALE; NORMAL HUMAN; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; STEADY STATE;

ADMINISTRATION, ORAL; ADULT; BENZYLAMINES; BRAIN; CARBON RADIOISOTOPES; COHORT STUDIES; CROSS-OVER STUDIES; CYCLOBUTANES; DOUBLE-BLIND METHOD; HUMANS; MALE; MIDDLE AGED; POSITRON-EMISSION TOMOGRAPHY; SEROTONIN PLASMA MEMBRANE TRANSPORT PROTEINS;

EID: 75749140852     PISSN: 0893133X     EISSN: None     Source Type: Journal    
DOI: 10.1038/npp.2009.182     Document Type: Article

References (57)

1. Arterburn DE, Crane PK, Veenstra DL (2004). The efficacy and safety of sibutramine for weight loss: a systematic review. Arch Intern Med 164: 994-1003.
2. Babalola KO, Cootes TF, Twining CJ, Petrovic V, Taylor CJ (2008). 3D brain segmentation using active appearance models and local regressors. Proceedings of the 11th International Conference on Medical Image Computing and Computer Assisted Intervention (MICCAI), Lecture Notes in Computer Science 5241: 401-408.
3. Bae SK, Cao S, Seo K-A, Kim H, Kim M-J, Shon J-H et al (2008). Cytochrome P450 2B6 catalyzes the formation of pharmacologically active sibutramine (N-{1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutyl}-N,N-dimethylamine) metabolites in human liver microsomes. Drug Metab Dispos 36: 1679-1688.
4. Baxter K (ed). (2007). Stockley's Drug Interactions, 8th Revised edn. Pharmaceutical Press: London, UK.
5. BNF (2009). Joint Formulary Committee. British National Formulary, 57th edn. British Medical Association and Royal Pharmaceutical Society of Great Britain: London.
6. Buckett WR, Thomas PC, Luscombe GP (1988). The pharmacology of sibutramine hydrochloride (BTS 54524), a new antidepressant which induces rapid noradrenergic down-regulation. Prog Neuropsychopharmacol Biol Psychiatry 12: 575-584.
7. Byars LG, Sibomana M, Burbar Z, Jones J, Panin V, Barker WC; et al (2005). Variance reduction on randoms from coincidence histograms for the HRRT. IEEE Nuclear Science Symposium Conference Record 5: 2622-2626.
8. Cheetham SC, Viggers JA, Slater NA, Heal DJ, Buckett WR (1993). [3H]paroxetine binding in rat frontal cortex strongly correlates with [3H]5-HT uptake: effect of administration of various antidepressant treatments. Neuropharmacology 32: 737-743.
9. de Jong HWAM, van Velden FHP, Kloet RW, Buijs FL, Boellaard R, Lammertsma AA (2007). Performance evaluation of the ECAT HRRT: an LSO-LYSO double layer high resolution, high sensitivity scanner. Phys Med Biol 52: 1505-1526.
10. Frankle WG, Huang Y, Hwang D-R, Talbot PS, Slifstein M, Van Heertum R et al (2004). Comparative evaluation of serotonin transporter radioligands 11C-DASB and 11C-McN 5652 in healthy humans. J Nucl Med 45: 682-694.
11. Frankle WG, Slifstein M, Gunn RN, Huang Y, Hwang D-R, Darr EA et al (2006). Estimation of serotonin transporter parameters with 11C-DASB in healthy humans: reproducibility and comparison of methods. J Nucl Med 47: 815-826.
12. Garratt CJ, Hind ID, Haddock RE (1995). Single/repeat dose kinetics of sibutramine metabolites in obese subjects. J Clin Pharmacol 35: 928 (abstract).
13. Glick SD, Haskew RE, Maisonneuve IM, Carlson JN, Jerussi TP (2000). Enantioselective behavioral effects of sibutramine metabolites. Eur J Pharmacol 397: 93-102.
14. Grignaschi G, Fanelli E, Scagnol I, Samanin R (1999). Studies on the role of serotonin receptor subtypes in the effect of sibutramine in various feeding paradigms in rats. Br J Pharmacol 127: 1190-1194.
15. Grudell ABM, Sweetser S, Camilleri M, Eckert DJ, Vazquez-Roque MI, Carlson PJ et al (2008). A controlled pharmacogenetic trial of sibutramine on weight loss and body composition in obese or overweight adults. Gastroenterology 135: 1142-1154.
16. Hainer V, Kabrnova K, Aldhoon B, Kunesova M, Wagenknecht M (2006). Serotonin and norepinephrine reuptake inhibition and eating behavior. Ann NY Acad Sci 1083: 252-269.
17. Hakala KS, Link M, Szotakova B, Skalova L, Kostiainen R, Ketola RA (2009). Characterization of metabolites of sibutramine in primary cultures of rat hepatocytes by liquid chroma-tography-ion trap mass spectrometry. Anal Bioanal Chem 393: 1327-1336.
18. Halford JCG, Harrold JA, Boyland EJ, Lawton CL, Blundell JE (2007). Serotonergic drugs: effects on appetite expression and use for the treatment of obesity. Drugs 67: 27-55.
19. Heal DJ, Cheetham SC, Prow MR, Martin KF, Buckett WR (1998). A comparison of the effects on central 5-HT function of sibutramine hydrochloride and other weight-modifying agents. Br J Pharmacol 125: 301-308.
20. Hill AJ, Rogers PJ, Blundell JE (1995). Techniques for the experimental measurement of human eating behaviour and food intake: a practical guide. Int J Obes Relat Metab Disord 19: 361-375.
21. Hind ID, Mangham JE, Ghani SP, Haddock RE, Garratt CJ, Jones RW (1999). Sibutramine pharmacokinetics in young and elderly healthy subjects. Eur J Clin Pharmacol 54: 847-849.
22. Huang Y, Narendran R, Bae S-A, Erritzoe D, Guo N, Zhu Z et al (2004). A PET imaging agent with fast kinetics: synthesis and in vivo evaluation of the serotonin transporter ligand [11C]2-[2-dimethylaminomethylphenylthio)]-5- fluorophenylamine ([11C] AFA). Nucl Med Biol 31: 727-738.
23. Innis RB, Cunningham VJ, Delforge J, Fujita M, Gjedde A, Gunn RN et al (2007). Consensus nomenclature for in vivo imaging of reversibly binding radioligands. J Cereb Blood Flow Metab 27: 1533-1539.
24. Jackson HC, Bearham MC, Hutchins LJ, Mazurkiewicz SE, Needham AM, Heal DJ (1997a). Investigation of the mechanisms underlying the hypophagic effects of the 5-HT and noradrena-line reuptake inhibitor, sibutramine, in the rat. Br J Pharmacol 121: 1613-1618.
25. Jackson HC, Needham AM, Hutchins LJ, Mazurkiewicz SE, Heal DJ (1997b). Comparison of the effects of sibutramine and other monoamine reuptake inhibitors on food intake in the rat. Br J Pharmacol 121: 1758-1762.
26. Kelly F, Jones SP, Lee JK (1995). Sibutramine: weight loss in depressed patients. Int J Obes Relat Metab Disord 19: p397.
27. King DJ, Devaney N (1988). Clinical pharmacology of sibutramine hydrochloride (BTS 54524), a new antidepressant, in healthy volunteers. Br J Clin Pharmacol 26: 607-611.
28. Kissileff HR, Klingsberg G, Van Itallie TB (1980). Universal eating monitor for continuous recording of solid or liquid consumption in man. Am J Physiol 238: R14-R22.
29. Larsen P, Ulin J, Dahlstrom K, Jensen M (1997). Synthesis of [11C]iodomethane by iodination of [11C]methane. Appl Radiat Isot 48: 153.
30. Li Z, Maglione M, Tu W, Mojica W, Arterburn D, Shugarman LR et al (2005). Meta-analysis: pharmacologic treatment of obesity. Ann Intern Med 142: 532-546.
31. Link M, Hakala KS, Wsol V, Kostiainen R, Ketola RA (2006). Metabolite profile of sibutramine in human urine: a liquid chromatography-electrospray ionization mass spectrometric study. J Mass Spectrom 41: 1171-1178.
32. Liu YL, Heal DJ, Stock MJ (2002). Mechanism of the thermogenic effect of Metabolite 2 (BTS 54505), a major pharmacologically active metabolite of the novel anti-obesity drug, sibutramine. Int J Obes Relat Metab Disord 26: 1245-1253.
33. Liu YL, Kashani SMZ, Heal DJ, Stock MJ (1996). Effect of sibutramine on tissue glucose utilisation in the rat. Br J Pharmacol 117: 324P.
34. Logan J, Fowler JS, Volkow ND, Wang GJ, Ding YS, Alexoff DL (1996). Distribution volume ratios without blood sampling from graphical analysis of PET data. J Cereb Blood Flow Metab 16: 834-840.
35. Luscombe GP, Hopcroft RH, Thomas PC, Buckett WR (1989). The contribution of metabolites to the rapid and potent down-regulation of rat cortical beta-adrenoceptors by the putative antidepressant sibutramine hydrochloride. Neuropharmacology 28: 129-134.
36. Luscombe GP, Slater NA, Lyons MB, Wynne RD, Scheinbaum ML, Buckett WR (1990). Effect on radiolabelled-monoamine uptake in vitro of plasma taken from healthy volunteers administered the antidepressant sibutramine HCl. Psychopharmacology (Berl) 100: 345-349.
37. McNeely W, Goa KL (1998). Sibutramine. A review of its contribution to the management of obesity. Drugs 56: 1093-1124. (Pubitemid 29010230)
38. Meyer JH (2007). Imaging the serotonin transporter during major depressive disorder and antidepressant treatment. J Psychiatry Neurosci 32: 86-102.
39. Meyer JH, Wilson AA, Sagrati S, Hussey D, Carella A, Potter WZ et al (2004). Serotonin transporter occupancy of five selective serotonin reuptake inhibitors at different doses: an [11C]DASB positron emission tomography study. Am J Psychiatry 161: 826-835.
40. Michel C, Schmand M, Liu X, Sibomana M, Vollmar S, Knoss C et al (2000). Reconstruction strategies for the HRRT. IEEE Nuclear Science Symposium Conference Record 2: 15/207-215/ 212.
41. Miller JM, Kinnally EL, Ogden RT, Oquendo MA, Mann JJ, Parsey RV (2009). Reported childhood abuse is associated with low serotonin transporter binding in vivo in major depressive disorder. Synapse 63: 565-573.
42. Miller JM, Oquendo MA, Ogden RT, Mann JJ, Parsey RV (2008). Serotonin transporter binding as a possible predictor of one-year remission in major depressive disorder. J Psychiatr Res 42: 1137-1144. doi:10.1002/ 14651858.CD004094.pub2
43. Padwal RS, Rucker D, Li SK, Curioni C, Lau DCW (2003). Long-term pharmacotherapy for obesity and overweight. Cochrane Database Syst Rev, Issue 4. Art. No.: CD004094. doi:10.1002/ 14651858.CD004094.pub2.
44. Perrio MJ, Wilton LV, Shakir SAW (2007). The safety profiles of orlistat and sibutramine: results of prescription-event monitoring studies in England. Obesity 15: 2712-2722.
45. Praschak-Rieder N, Kennedy J, Wilson AA, Hussey D, Boovariwala A, Willeit M et al (2007). Novel 5-HTTLPR allele associates with higher serotonin transporter binding in putamen: a [(11)C] DASB positron emission tomography study. Biol Psychiatry 62: 327-331.
46. Praschak-Rieder N, Willeit M, Wilson AA, Houle S, Meyer JH (2008). Seasonal variation in human brain serotonin transporter binding. Arch Gen Psychiatry 65: 1072-1078.
47. Reimold M, Smolka MN, Schumann G, Zimmer A, Wrase J, Mann K et al (2007). Midbrain serotonin transporter binding potential measured with [11C]DASB is affected by serotonin transporter genotype. J Neural Transm 114: 635-639.
48. Sibomana M, Byars L, Panin V, Lenox M, Kehren F, Rist J et al (2004). Simultaneous measurement of transmission and emission contamination using a collimated 137Cs point source for the HRRT. IEEE Nuclear Science Symposium Conference Record 4: 2647-2651.
49. Stunkard A, Messick S (1985). The Three-factor eating questionnaire to measure dietary restraint, disinhibition and hunger. J Psychosom Res 29: 71-83.
50. Talbot PS, Frankle WG, Hwang D-R, Huang Y, Suckow RF, Slifstein M et al (2005). Effects of reduced endogenous 5-HT on the in vivo binding of the serotonin transporter radioligand 11C-DASB in healthy humans. Synapse 55: 164-175.
51. Talbot PS, Laruelle M (2002). The role of in vivo molecular imaging with PET and SPECT in the elucidation of psychiatric drug action and new drug development. Eur Neuropsychopharmacol 12: 503-511.
52. Thomas GH, Babbs AJ, Chatfield RE, Krulle TM, Widdowson PS, Provost D et al (2009). 5-HT(1A) activation counteracts cardiovascular but not hypophagic effects of sibutramine in rats. Obesity 17: 467-473.
53. van Velden FHP, Kloet RW, van Berckel BNM, Lammertsma AA, Boellaard R (2009). Accuracy of 3-dimensional reconstruction algorithms for the high-resolution research tomograph. J Nucl Med 50: 72-80.
54. Vazquez Roque MI, Camilleri M, Clark MM, Tepoel DA, Jensen MD, Graszer KM et al (2007). Alteration of gastric functions and candidate genes associated with weight reduction in response to sibutramine. Clin Gastroenterol Hepatol 5: 829-837.
55. Watson CC (2000). New, faster, image-based scatter correction for 3D PET. Nuclear Science, IEEE Transactions 47(Part 2): 1587-1594.
56. Weintraub M, Rubio A, Golik A, Byrne L, Scheinbaum ML (1991). Sibutramine in weight control: a dose-ranging, efficacy study. Clin Pharmacol Ther 50: 330-337.
57. Wilson AA, Ginovart N, Schmidt M, Meyer JH, Threlkeld PG, Houle S (2000). Novel radiotracers for imaging the serotonin transporter by positron emission tomography: synthesis, radio-synthesis, and in vitro and ex vivo evaluation of (11)C-labeled 2-(phenylthio)araalkylamines. J Med Chem 43: 3103-3110.