Chapter 23: Serotonin 5-HT4 Receptors as Pharmacological Targets for the Treatment of Alzheimer's Disease Check Access
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Published:07 May 2010
I. Berque-Bestel and F. Lezoualc'h, in Emerging Drugs and Targets for Alzheimer's Disease: Volume 2: Neuronal Plasticity, Neuronal Protection and Other Miscellaneous Strategies, ed. A. Martinez and A. Martinez, The Royal Society of Chemistry, 2010, vol. 2, ch. 23, pp. 169-190.
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The serotonin 5-HT4 receptor (5-HT4R) is a member of the seven transmembrane-spanning G-protein-coupled receptor (GPCR) family. Since its discovery in mouse colliculi neurons, the 5-HT4R has received a considerable attention for its physiological effect in the central nervous system (CNS). Thanks to the availability of selective 5-HT4 ligands and the cloning of 5-HT4 receptor C-terminal splice variants, many studies have shown the involvement of the 5-HT4R in cognitive processes making this GPCR as a possible therapeutic target for symptomatic treatment of memory disorders such as Alzheimer's disease (AD). After an introduction to the chemistry of 5-HT4R ligands, and the molecular identification and pharmacological characterization of recombinant 5-HT4R, here we discuss on the potential use of 5-HT4R agonists as therapeutical agents influencing the cholinergic system and the amyloid precursor protein processing for the treatment of AD.