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Literature DB >> 19589055

The serotonin 5-HT6 receptor: a viable drug target for treating cognitive deficits in Alzheimer's disease.

Werner J Geldenhuys¹, Cornelis J Van der Schyf.

Abstract

The serotonin 6 receptor is attracting attention as an etiological contributor in cognition deficits in diseases such as Alzheimer's disease, anxiety/depression and schizophrenia. In this review, we discuss the role of this recently discovered G protein-coupled receptor in cognition and memory, particularly in Alzheimer's disease. A surge in publications that describe the development of ligands for this receptor have recently come to light, underscoring the emerging interest in this receptor as a drug target. We also explore the current status of structure-activity relationship studies that have focused on the design of novel antagonists for the serotonin 6 receptor.

Entities: Chemical Disease Gene

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Year: 2009 PMID： 19589055 DOI： 10.1586/ern.09.51

Source DB: PubMed Journal: Expert Rev Neurother ISSN： 1473-7175 Impact factor: 4.618

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Cited

15 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

2. Chemocentric informatics approach to drug discovery: identification and experimental validation of selective estrogen receptor modulators as ligands of 5-hydroxytryptamine-6 receptors and as potential cognition enhancers.

Authors: Rima Hajjo; Vincent Setola; Bryan L Roth; Alexander Tropsha
Journal: J Med Chem Date: 2012-06-11 Impact factor: 7.446

3. ADN-1184 a monoaminergic ligand with 5-HT(6/7) receptor antagonist activity: pharmacological profile and potential therapeutic utility.

Authors: M Kołaczkowski; P Mierzejewski; P Bieńkowski; A Wesołowska; A Newman-Tancredi
Journal: Br J Pharmacol Date: 2014-02 Impact factor: 8.739

4. Central nervous system effects of the interaction between risperidone (single dose) and the 5-HT6 antagonist SB742457 (repeated doses) in healthy men.

Authors: Marieke Liem-Moolenaar; Mandana Rad; Stefano Zamuner; Adam F Cohen; Francesca Lemme; Kari L Franson; Joop M A van Gerven; Emilio Merlo Pich
Journal: Br J Clin Pharmacol Date: 2011-06 Impact factor: 4.335

5. Novel and Potent 5-Piperazinyl Methyl-N 1-aryl Sulfonyl Indole Derivatives as 5-HT6 Receptor Ligands.

Authors: Ramakrishna V S Nirogi; Prabhakar Kothmirkar; Ramasastri Kambhampati; Jagadish Babu Konda; Sobhanadri Arepalli; Narasimhareddy G Pamuleti; Amol D Deshpande; Trinathreddy Bandyala; Anil K Shinde; P K Dubey
Journal: ACS Med Chem Lett Date: 2010-06-24 Impact factor: 4.345

10. Reactive oxygen species are required for 5-HT-induced transactivation of neuronal platelet-derived growth factor and TrkB receptors, but not for ERK1/2 activation.

Authors: Jeff S Kruk; Maryam S Vasefi; John J Heikkila; Michael A Beazely
Journal: PLoS One Date: 2013-09-27 Impact factor: 3.240

The serotonin 5-HT6 receptor: a viable drug target for treating cognitive deficits in Alzheimer's disease.

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

2. Chemocentric informatics approach to drug discovery: identification and experimental validation of selective estrogen receptor modulators as ligands of 5-hydroxytryptamine-6 receptors and as potential cognition enhancers.

3. ADN-1184 a monoaminergic ligand with 5-HT(6/7) receptor antagonist activity: pharmacological profile and potential therapeutic utility.

4. Central nervous system effects of the interaction between risperidone (single dose) and the 5-HT6 antagonist SB742457 (repeated doses) in healthy men.

5. Novel and Potent 5-Piperazinyl Methyl-N 1-aryl Sulfonyl Indole Derivatives as 5-HT6 Receptor Ligands.

6. In vivo brain microdialysis: advances in neuropsychopharmacology and drug discovery.

Review 7. Role of serotonin in Alzheimer's disease: a new therapeutic target?

Review 8. The role of G protein-coupled receptors in the pathology of Alzheimer's disease.

Review 9. The role of serotonin in memory: interactions with neurotransmitters and downstream signaling.

10. Reactive oxygen species are required for 5-HT-induced transactivation of neuronal platelet-derived growth factor and TrkB receptors, but not for ERK1/2 activation.