Literature DB >> 21330209

Targeting 5-HT receptors for the treatment of obesity.

Bruce J Sargent1, Alan J Henderson.   

Abstract

Serotonin is known to have anorectic properties through centrally acting mechanisms. Three serotonin receptors have been implicated in mediating these effects: 5-HT(1B), 5-HT(2C) and 5-HT(6). Hypophagic effects are elicited through agonism of the former two receptors, whereas antagonism of the 5-HT(6) receptor appears to have an anorectic effect. All three targets have been validated through extensive studies including knockout mice and selective ligand assessment. 5-HT(1B) receptor agonists have limited utility due to mechanism-based side effects, whereas 5-HT(2C) receptor agonists suffer from challenges associated with selectivity over the closely related 5-HT(2A) and 5-HT(2B) receptors. 5-HT(6) receptor antagonists appear to offer great promise, although the mechanisms through which they reduce food intake and body weight are not fully understood.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21330209     DOI: 10.1016/j.coph.2011.01.005

Source DB:  PubMed          Journal:  Curr Opin Pharmacol        ISSN: 1471-4892            Impact factor:   5.547


  11 in total

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Authors:  Jianjun Cheng; Patrick M Giguère; Oluseye K Onajole; Wei Lv; Arsen Gaisin; Hendra Gunosewoyo; Claire M Schmerberg; Vladimir M Pogorelov; Ramona M Rodriguiz; Giulio Vistoli; William C Wetsel; Bryan L Roth; Alan P Kozikowski
Journal:  J Med Chem       Date:  2015-02-10       Impact factor: 7.446

3.  The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.

Authors:  Stephen P H Alexander; Helen E Benson; Elena Faccenda; Adam J Pawson; Joanna L Sharman; Michael Spedding; John A Peters; Anthony J Harmar
Journal:  Br J Pharmacol       Date:  2013-12       Impact factor: 8.739

4.  Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT2C Receptor Agonists.

Authors:  Guy Rouquet; Dianna E Moore; Malcolm Spain; Daniel M Allwood; Claudio Battilocchio; David C Blakemore; Paul V Fish; Stephen Jenkinson; Alan S Jessiman; Steven V Ley; Gordon McMurray; R Ian Storer
Journal:  ACS Med Chem Lett       Date:  2015-01-20       Impact factor: 4.345

5.  Metabolic and Cardiovascular Benefits and Risks of EMD386088-A 5-HT6 Receptor Partial Agonist and Dopamine Transporter Inhibitor.

Authors:  Magdalena Kotańska; Joanna Śniecikowska; Magdalena Jastrzębska-Więsek; Marcin Kołaczkowski; Karolina Pytka
Journal:  Front Neurosci       Date:  2017-02-08       Impact factor: 4.677

6.  Comparison of brain serotonin transporter using [I-123]-ADAM between obese and non-obese young adults without an eating disorder.

Authors:  Chih-Hsing Wu; Chin-Sung Chang; Yen Kuang Yang; Lie-Hang Shen; Wei-Jen Yao
Journal:  PLoS One       Date:  2017-02-09       Impact factor: 3.240

7.  Idalopirdine, a selective 5-HT6 receptor antagonist, reduces food intake and body weight in a model of excessive eating.

Authors:  Magdalena Kotańska; Klaudia Lustyk; Adam Bucki; Monika Marcinkowska; Joanna Śniecikowska; Marcin Kołaczkowski
Journal:  Metab Brain Dis       Date:  2018-01-03       Impact factor: 3.584

8.  Identification of Optically Active Pyrimidine Derivatives as Selective 5-HT2C Modulators.

Authors:  Juhyeon Kim; Hanbyeol Jo; Hyunseung Lee; Hyunah Choo; Hak Joong Kim; Ae Nim Pae; Yong Seo Cho; Sun-Joon Min
Journal:  Molecules       Date:  2017-08-26       Impact factor: 4.411

9.  Idalopirdine - a small molecule antagonist of 5-HT6 with therapeutic potential against obesity.

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Journal:  Metab Brain Dis       Date:  2015-09-29       Impact factor: 3.584

Review 10.  Can We Selectively Reduce Appetite for Energy-Dense Foods? An Overview of Pharmacological Strategies for Modification of Food Preference Behavior.

Authors:  Ewa Bojanowska; Joanna Ciosek
Journal:  Curr Neuropharmacol       Date:  2016       Impact factor: 7.363

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