Abstract
Cognitive impairment (CI) has been recognized as a core feature of Alzheimers disease (AD) and schizophrenia. The 5-HT6 receptor is an attractive target for the development of cognitive enhancers due to its unique localization and pharmacology. 5-HT6 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- HT6 receptor antagonist SB-742457 in mild-to-moderate AD patients. Advances in the understanding of the structureactivity- relationship, the design of novel 5-HT6 receptor ligands and their potential application for the treatment of CI are reviewed.
Keywords: Serotonin, G-Protein coupled receptor, medicinal chemistry, chemical biology, drug design, Alzheimer's disease, schizophrenia, neurological disorders
Current Topics in Medicinal Chemistry
Title: 5-HT6 Receptor Antagonists as Potential Therapeutics for Cognitive Impairment
Volume: 10 Issue: 2
Author(s): Gerard Rosse and Herve Schaffhauser
Affiliation:
Keywords: Serotonin, G-Protein coupled receptor, medicinal chemistry, chemical biology, drug design, Alzheimer's disease, schizophrenia, neurological disorders
Abstract: Cognitive impairment (CI) has been recognized as a core feature of Alzheimers disease (AD) and schizophrenia. The 5-HT6 receptor is an attractive target for the development of cognitive enhancers due to its unique localization and pharmacology. 5-HT6 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- HT6 receptor antagonist SB-742457 in mild-to-moderate AD patients. Advances in the understanding of the structureactivity- relationship, the design of novel 5-HT6 receptor ligands and their potential application for the treatment of CI are reviewed.
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Cite this article as:
Rosse Gerard and Schaffhauser Herve, 5-HT6 Receptor Antagonists as Potential Therapeutics for Cognitive Impairment, Current Topics in Medicinal Chemistry 2010; 10 (2) . https://dx.doi.org/10.2174/156802610790411036
DOI https://dx.doi.org/10.2174/156802610790411036 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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