Literature DB >> 26507582

We Need 2C but Not 2B: Developing Serotonin 2C (5-HT2C) Receptor Agonists for the Treatment of CNS Disorders.

Jianjun Cheng1, Alan P Kozikowski2.   

Abstract

The serotonin 2C (5-HT2C ) receptor has been identified as a potential drug target for the treatment of a variety of central nervous system (CNS) disorders, such as obesity, substance abuse, and schizophrenia. In this Viewpoint article, recent progress in developing selective 5-HT2C agonists for use in treating these disorders is summarized, including the work of our group. Challenges in this field and the possible future directions are described. Homology modeling as a method to predict the binding modes of 5-HT2C ligands to the receptor is also discussed. Compared to known ligands, the improved pharmacological profiles of the 2-phenylcyclopropylmethylamine-based 5-HT2C agonists make them preferred candidates for further studies.
© 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Entities:  

Keywords:  drug discovery; medicinal chemistry; receptors; schizophrenia; serotonin

Mesh：

Substances：

Year:  2015        PMID： 26507582      PMCID： PMC4832415          DOI： 10.1002/cmdc.201500437

Source DB:  PubMed          Journal:  ChemMedChem        ISSN： 1860-7179            Impact factor:   3.466


  43 in total

1.  HTS and rational drug design to generate a class of 5-HT(2C)-selective ligands for possible use in schizophrenia.

Authors:  Alan P Kozikowski; Sung Jin Cho; Niels H Jensen; John A Allen; Andreas M Svennebring; Bryan L Roth
Journal:  ChemMedChem       Date:  2010-08-02       Impact factor: 3.466

Review 2.  Pharmacological and genetic interventions in serotonin (5-HT)(2C) receptors to alter drug abuse and dependence processes.

Authors:  Małgorzata Filip; Umberto Spampinato; Andrew C McCreary; Edmund Przegaliński
Journal:  Brain Res       Date:  2012-03-23       Impact factor: 3.252

Review 3.  5-HT2C receptor modulators: a patent survey.

Authors:  Junwon Lee; Myung Eun Jung; Jinhwa Lee
Journal:  Expert Opin Ther Pat       Date:  2010-09-17       Impact factor: 6.674

4.  Rational Drug Design Leading to the Identification of a Potent 5-HT(2C) Agonist Lacking 5-HT(2B) Activity.

Authors:  Gang Chen; Sung Jin Cho; Xi-Ping Huang; Niels H Jensen; Andreas Svennebring; Maria F Sassano; Bryan L Roth; Alan P Kozikowski
Journal:  ACS Med Chem Lett       Date:  2011-10-10       Impact factor: 4.345

5.  The Serotonin 2C Receptor Agonist Lorcaserin Attenuates Intracranial Self-Stimulation and Blocks the Reward-Enhancing Effects of Nicotine.

Authors:  Fiona D Zeeb; Guy A Higgins; Paul J Fletcher
Journal:  ACS Chem Neurosci       Date:  2015-03-17       Impact factor: 4.418

Review 6.  A proposed new nomenclature for 5-HT receptors.

Authors:  P P Humphrey; P Hartig; D Hoyer
Journal:  Trends Pharmacol Sci       Date:  1993-06       Impact factor: 14.819

Review 7.  From obesity to substance abuse: therapeutic opportunities for 5-HT2C receptor agonists.

Authors:  Guy A Higgins; Edward M Sellers; Paul J Fletcher
Journal:  Trends Pharmacol Sci       Date:  2013-09-13       Impact factor: 14.819

8.  Parallel functional activity profiling reveals valvulopathogens are potent 5-hydroxytryptamine(2B) receptor agonists: implications for drug safety assessment.

Authors:  Xi-Ping Huang; Vincent Setola; Prem N Yadav; John A Allen; Sarah C Rogan; Bonnie J Hanson; Chetana Revankar; Matt Robers; Chris Doucette; Bryan L Roth
Journal:  Mol Pharmacol       Date:  2009-07-01       Impact factor: 4.436

9.  5-HT2C receptor activation decreases appetite and body weight in obese subjects.

Authors:  P A Sargent; A L Sharpley; C Williams; E M Goodall; P J Cowen
Journal:  Psychopharmacology (Berl)       Date:  1997-10       Impact factor: 4.530

10.  Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT₂C) receptor agonists with exquisite functional selectivity over 5-HT₂A and 5-HT₂B receptors.

Authors:  R Ian Storer; Paul E Brennan; Alan D Brown; Peter J Bungay; Kelly M Conlon; Matthew S Corbett; Robert P DePianta; Paul V Fish; Alexander Heifetz; Danny K H Ho; Alan S Jessiman; Gordon McMurray; Cesar Augusto F de Oliveira; Lee R Roberts; James A Root; Veerabahu Shanmugasundaram; Michael J Shapiro; Melanie Skerten; Dominique Westbrook; Simon Wheeler; Gavin A Whitlock; John Wright
Journal:  J Med Chem       Date:  2014-06-17       Impact factor: 7.446
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  4 in total

1.  Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT2C) receptor agonist without 5-HT2B agonism.

Authors:  Guiping Zhang; John D McCorvy; Sida Shen; Jianjun Cheng; Bryan L Roth; Alan P Kozikowski
Journal:  Eur J Med Chem       Date:  2019-08-14       Impact factor: 6.514

Review 2.  The serotonergic system and cognitive function.

Authors:  Dubravka Švob Štrac; Nela Pivac; Dorotea Mück-Šeler
Journal:  Transl Neurosci       Date:  2016-05-09       Impact factor: 1.757

Review 3.  Serotonin receptors in epilepsy: Novel treatment targets?

Authors:  Jo Sourbron; Lieven Lagae
Journal:  Epilepsia Open       Date:  2022-02-02

Review 4.  Use of Zebrafish Models to Boost Research in Rare Genetic Diseases.

Authors:  Lucie Crouzier; Elodie M Richard; Jo Sourbron; Lieven Lagae; Tangui Maurice; Benjamin Delprat
Journal:  Int J Mol Sci       Date:  2021-12-12       Impact factor: 5.923
  4 in total

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