Literature DB >> 20166958

5-HT6 receptor antagonists as potential therapeutics for cognitive impairment.

Gérard Rossé1, Hervé Schaffhauser.   

Abstract

Cognitive impairment (CI) has been recognized as a core feature of Alzheimer's disease (AD) and schizophrenia. The 5-HT(6) receptor is an attractive target for the development of cognitive enhancers due to its unique localization and pharmacology. 5-HT(6) receptor antagonists have been shown to modulate multiple neurotransmitter systems and therefore enhance cognition in preclinical studies. This premise translated into the clinical efficacy of the 5-HT(6) receptor antagonist SB-742457 in mild-to-moderate AD patients. Advances in the understanding of the structure-activity-relationship, the design of novel 5-HT(6) receptor ligands and their potential application for the treatment of CI are reviewed.

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Year:  2010        PMID： 20166958     DOI： 10.2174/156802610790411036

Source DB:  PubMed          Journal:  Curr Top Med Chem        ISSN： 1568-0266            Impact factor:   3.295


  10 in total

1.  Distribution of serotonin receptor of type 6 (5-HT₆) in human brain post-mortem. A pharmacology, autoradiography and immunohistochemistry study.

Authors:  Donatella Marazziti; Stefano Baroni; Andrea Pirone; Gino Giannaccini; Laura Betti; Lara Schmid; Elena Vatteroni; Lionella Palego; Franco Borsini; Fabio Bordi; Ilaria Piano; Claudia Gargini; Maura Castagna; Mario Catena-Dell'osso; Antonio Lucacchini
Journal:  Neurochem Res       Date:  2012-01-26       Impact factor: 3.996

Review 2.  Neurotransmitter receptors and cognitive dysfunction in Alzheimer's disease and Parkinson's disease.

Authors:  Yunqi Xu; Junqiang Yan; Peng Zhou; Jiejie Li; Huimin Gao; Ying Xia; Qing Wang
Journal:  Prog Neurobiol       Date:  2012-02-25       Impact factor: 11.685

3.  Benzenesulfonyl and Benzenesulfonamide as Modulators of the 5-HT6 Receptor: Patent Highlight.

Authors:  Gerard Rosse
Journal:  ACS Med Chem Lett       Date:  2012-10-26       Impact factor: 4.345

4.  5-HT6 Receptor Agonist and Antagonist Against β-Amyloid-Peptide-Induced Neurotoxicity in PC-12 Cells.

Authors:  Anand M Bokare; A K Praveenkumar; Mandar Bhonde; Yogendra Nayak; Ravindra Pal; Rajan Goel
Journal:  Neurochem Res       Date:  2017-03-07       Impact factor: 3.996

Review 5.  Serotonin 5-HT6 Receptor Antagonists in Alzheimer's Disease: Therapeutic Rationale and Current Development Status.

Authors:  Hilda Ferrero; Maite Solas; Paul T Francis; Maria J Ramirez
Journal:  CNS Drugs       Date:  2017-01       Impact factor: 5.749

6.  Ro 04-6790-induced cognitive enhancement: no effect in trace conditioning and novel object recognition procedures in adult male Wistar rats.

Authors:  K E Thur; A J D Nelson; H J Cassaday
Journal:  Pharmacol Biochem Behav       Date:  2014-10-24       Impact factor: 3.533

Review 7.  AVN-101: A Multi-Target Drug Candidate for the Treatment of CNS Disorders.

Authors:  Alexandre V Ivachtchenko; Yan Lavrovsky; Ilya Okun
Journal:  J Alzheimers Dis       Date:  2016-05-25       Impact factor: 4.472

8.  Two randomized controlled trials of SB742457 in mild-to-moderate Alzheimer's disease.

Authors:  Gareth Maher-Edwards; Carolyn Watson; John Ascher; Carly Barnett; Diane Boswell; John Davies; Manuel Fernandez; Alexander Kurz; Orazio Zanetti; Beth Safirstein; Juan Paul Schronen; Marina Zvartau-Hind; Michael Gold
Journal:  Alzheimers Dement (N Y)       Date:  2015-05-07

9.  Engaging sulfinate salts via Ni/photoredox dual catalysis enables facile Csp2 -SO2R coupling.

Authors:  María Jesús Cabrera-Afonso; Zhi-Peng Lu; Christopher B Kelly; Simon B Lang; Ryan Dykstra; Osvaldo Gutierrez; Gary A Molander
Journal:  Chem Sci       Date:  2018-02-22       Impact factor: 9.825

Review 10.  G Protein-Coupled Receptors (GPCRs) in Alzheimer's Disease: A Focus on BACE1 Related GPCRs.

Authors:  Juan Zhao; Yulin Deng; Zhaotan Jiang; Hong Qing
Journal:  Front Aging Neurosci       Date:  2016-03-24       Impact factor: 5.750
  10 in total

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