Calle EE, Thun MJ, Petrelli JM, Rodriguez C, Heath CW. Body-mass index and mortality in a prospective cohort of U.S. adults. N Engl J Med. 1999;341:1097–105. http://www.nejm.org/doi/abs/10.1056/NEJM199910073411501.

Article  PubMed  CAS  Google Scholar 

Prospective Studies Collaboration. Body-mass index and cause-specific mortality in 900 000 adults: collaborative analyses of 57 prospective studies. Lancet. 2009;373:1083–96. https://linkinghub.elsevier.com/retrieve/pii/S0140673609603184.

Article  PubMed Central  Google Scholar 

Lauby-Secretan B, Scoccianti C, Loomis D, Grosse Y, Bianchini F, Straif K. Body fatness and cancer—viewpoint of the IARC Working Group. N Engl J Med. 2016;375:794–8. http://www.nejm.org/doi/10.1056/NEJMsr1606602.

Article  PubMed  PubMed Central  Google Scholar 

Anstey KJ, Cherbuin N, Budge M, Young J. Body mass index in midlife and late-life as a risk factor for dementia: a meta-analysis of prospective studies. Obes Rev. 2011;12:e426–37.

Article  PubMed  CAS  Google Scholar 

Yumuk V, Tsigos C, Fried M, Schindler K, Busetto L, Micic D, et al. European guidelines for obesity management in adults. Obes Facts. 2015;8:402–24. https://www.karger.com/Article/FullText/442721.

Article  PubMed  PubMed Central  Google Scholar 

Galen KA, Horst KW, Serlie MJ. Serotonin, food intake, and obesity. Obes Rev. 2021;22. https://onlinelibrary.wiley.com/doi/10.1111/obr.13210.

Halford J, Harrold J, Lawton C, Blundell J. Serotonin (5-HT) drugs: effects on appetite expression and use for the treatment of obesity. CDT. 2005;6:201–13. http://www.eurekaselect.com/openurl/content.php?genre=article&issn=1389-4501&volume=6&issue=2&spage=201.

Article  CAS  Google Scholar 

European Medicines Agency. Questions and answers: withdrawal marketing authorisation application Belviq (lorcaserin). 30 May 2013. https://www.ema.europa.eu/en/documents/medicine-qa/questions-answers-withdrawal-marketing-authorisation-application-belviq_en.pdf. Accessed 7 Nov 2020

Sharretts J, Galescu O, Gomatam S, Andraca-Carrera E, Hampp C, Yanoff L. Cancer risk associated with Lorcaserin—the FDA’s review of the CAMELLIA-TIMI 61 trial. N Engl J Med. 2020;383:1000–2. http://www.nejm.org/doi/10.1056/NEJMp2003873.

Article  PubMed  CAS  Google Scholar 

Marazziti D, Baroni S, Pirone A, Giannaccini G, Betti L, Schmid L, et al. Distribution of serotonin receptor of type 6 (5-HT6) in human brain post-mortem. A pharmacology, autoradiography and immunohistochemistry study. Neurochem Res. 2012;37:920–7.

Article  PubMed  CAS  Google Scholar 

Heal D, Gosden J, Smith S. The 5-HT6 receptor as a target for developing novel antiobesity drugs. Int Rev Neurobiol. 2011:73–109. https://linkinghub.elsevier.com/retrieve/pii/B9780123859020000048.

Woolley ML, Bentley JC, Sleight AJ, Marsden CA, Fone KCF. A role for 5-ht6 receptors in retention of spatial learning in the Morris water maze. Neuropharmacology. 2001;41:210–9. https://linkinghub.elsevier.com/retrieve/pii/S0028390801000569.

Article  PubMed  CAS  Google Scholar 

Svartengren J, Öhman B, Edling N, Svensson M, Fhölenhag K, Axelsson-Lendin P, et al. The serotonin 5-HT6 receptor antagonist BVT.5182 reduces body weight of high fat diet-induced mice. Int J Obes. 2003b;27:1–94.

Google Scholar 

Perez-García G, Meneses A. Oral administration of the 5-HT6 receptor antagonists SB-357134 and SB-399885 improves memory formation in an autoshaping learning task. Pharm Biochem Behav. 2005;81:673–82.

Article  Google Scholar 

Dudek M, Marcinkowska M, Bucki A, Olczyk A, Kołaczkowski M. Idalopirdine—a small molecule antagonist of 5-HT6 with therapeutic potential against obesity. Metab Brain Dis. 2015;30:1487–94. http://link.springer.com/10.1007/s11011-015-9736-3.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Lubelska A, Latacz G, Jastrzębska-Więsek M, Kotańska M, Kurczab R, Partyka A, et al. Are the hydantoin-1,3,5-triazine 5-HT6R ligands a hope to a find new procognitive and anti-obesity drug? Considerations based on primary in vivo assays and ADME-Tox profile in vitro. Molecules 2019;24:4472. https://www.mdpi.com/1420-3049/24/24/4472.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Frassetto A, Zhang J, Lao JZ, White A, Metzger JM, Fong TM, et al. Reduced sensitivity to diet-induced obesity in mice carrying a mutant 5-HT6 receptor. Brain Res. 2008;1236:140–4. https://linkinghub.elsevier.com/retrieve/pii/S0006899308019872.

Article  PubMed  CAS  Google Scholar 

Tecott LH, Brennan TJ. Serotonin 5-HT6 receptor knockout mouse. US Patent 6060642. 2000. http://www.freepatentsonline.com/6060642.html.

Kotańska M, Lustyk K, Bucki A, Marcinkowska M, Śniecikowska J, Kołaczkowski M. Idalopirdine, a selective 5-HT6 receptor antagonist, reduces food intake and body weight in a model of excessive eating. Metab Brain Dis. 2018;33:733–40.

Article  PubMed  PubMed Central  Google Scholar 

Kurczab R, Ali W, Łażewska D, Kotańska M, Jastrzębska-Więsek M, Satała G, et al. Computer-aided studies for novel arylhydantoin 1,3,5-triazine derivatives as 5-HT6 serotonin receptor ligands with antidepressive-like, anxiolytic and antiobesity action in vivo. Molecules 2018;23:2529. http://www.mdpi.com/1420-3049/23/10/2529.

Article  PubMed  PubMed Central  Google Scholar 

Becker G, Colomb J, Sgambato-Faure V, Tremblay L, Billard T, Zimmer L. Preclinical evaluation of [18F]2FNQ1P as the first fluorinated serotonin 5-HT6 radioligand for PET imaging. Eur J Nucl Med Mol Imaging. 2015;42:495–502. http://link.springer.com/10.1007/s00259-014-2936-y.

Article  PubMed  CAS  Google Scholar 

Colomb J, Becker G, Fieux S, Zimmer L, Billard T. Syntheses, radiolabelings, and in vitro evaluations of fluorinated PET radioligands of 5-HT6 serotoninergic receptors. J Med Chem. 2014;57:3884–90. http://pubs.acs.org/doi/10.1021/jm500372e.

Article  PubMed  CAS  Google Scholar 

Courault P, Bouvard S, Bouillot C, Bolbos R, Iecker T, Billard T, et al. Influence of obesity on brain 5-HT6 receptor expression: an in-vivo study with the PET radiotracer [18F]2FNQ1P. 2021. https://zenodo.org/record/4700238.

Guerville M, Leroy A, Sinquin A, Laugerette F, Michalski MC, Boudry G. Western-diet consumption induces alteration of barrier function mechanisms in the ileum that correlates with metabolic endotoxemia in rats. Am J Physiol Endocrinol Metab. 2017;313:E107–20. https://www.physiology.org/doi/10.1152/ajpendo.00372.2016.

Article  PubMed  Google Scholar 

Kaya M, Ahishali B. Assessment of permeability in barrier type of endothelium in brain using tracers: Evans Blue, sodium fluorescein, and horseradish peroxidase. In: Turksen K, editor. Permeability barrier (Methods in molecular biology, Vol. 763). Totowa, NJ: Humana Press; 2011. pp. 369–82. http://link.springer.com/10.1007/978-1-61779-191-8_25.

Barrière DA, Magalhães R, Novais A, Marques P, Selingue E, Geffroy F, et al. The SIGMA rat brain templates and atlases for multimodal MRI data analysis and visualization. Nat Commun. 2019;10:5699.

Article  PubMed  PubMed Central  Google Scholar 

Marques C, Meireles M, Norberto S, Leite J, Freitas J, Pestana D, et al. High-fat diet-induced obesity rat model: a comparison between Wistar and Sprague-Dawley Rat. Adipocyte. 2016;5:11–21. http://www.tandfonline.com/doi/full/10.1080/21623945.2015.1061723.

Article  PubMed  CAS  Google Scholar 

Roberts JC, Reavill C, East SZ, Harrison PJ, Patel S, Routledge C, et al. The distribution of 5-HT6 receptors in rat brain: an autoradiographic binding study using the radiolabelled 5-HT6 receptor antagonist [125I]SB-258585. Brain Res. 2002;934:49–57. https://linkinghub.elsevier.com/retrieve/pii/S0006899302023600.

Article  PubMed  CAS  Google Scholar 

Woolley M, Marsden C, Fone K. 5-ht6 receptors. CDTCNSND. 2004;3:59–79. http://www.eurekaselect.com/openurl/content.php?genre=article&issn=1568-007X&volume=3&issue=1&spage=59.

Article  CAS  Google Scholar 

Broberger C. Brain regulation of food intake and appetite: molecules and networks. J Intern Med. 2005;258:301–27. https://onlinelibrary.wiley.com/doi/10.1111/j.1365-2796.2005.01553.x.

Article  PubMed  CAS  Google Scholar 

Woods S, Clarke N, Layfield R, Fone K. 5-HT6 receptor agonists and antagonists enhance learning and memory in a conditioned emotion response paradigm by modulation of cholinergic and glutamatergic mechanisms: 5-HT6 receptor effects on associative learning. Br J Pharmacol. 2012;167:436–49. https://onlinelibrary.wiley.com/doi/10.1111/j.1476-5381.2012.02022.x.

Article  PubMed  PubMed Central  CAS  Google Scholar 

Liśkiewicz, Liśkiewicz AD, Marczak D, Przybyła M, Grabowska K, Student S, et al. Obesity-associated deterioration of the hippocampus is partially restored after weight loss. Brain Behav Immun. 2021;96:212–26. https://linkinghub.elsevier.com/retrieve/pii/S0889159121002312.

Article  PubMed  Google Scholar