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Serotonin 5-HT3 and 5-HT4 Ligands: An Update of Medicinal Chemistry Research in the Last Few Years

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The biogenic amine serotonin (5-hydroxytryptamine, 5-HT) is one of the most studied neurotransmitters in the central nervous system. It acts through the activation of at least fourteen 5-HT receptor subtypes. Over the last two decades, high attention was devoted to the 5-HT3 and 5-HT4 receptors due to their colocalization in the gastrointestinal tract and because their ligands are useful in the treatment of intestinal serotonergic system dysfunctions. The focus of this review is to discuss the literature concerning recent advances on 5-HT3R and 5-HT4R ligands and their structure-activity relationships from a medicinal chemistry perspective. During the last few years, new and significant progresses have been made in the field of novel potent and selective ligands, mixed ligands, agonists, partial agonists, and antagonists, and a number of patents have been filed. Furthermore several ligands targeting the 5-HT3R and 5-HT4R have been proposed for novel therapeutic indications such as the treatment of various psychiatric disorders.

Keywords: 5-HT3R; 5-HT3R ligands; 5-HT4R; 5-HT4R ligands; G protein-coupled receptors; Serotonin; ligand-gated ion channels; serotonin receptor subtypes

Document Type: Research Article


Affiliations: Dipartimento di Scienze Farmaceutiche, Facolta di Farmacia, Universita di Catania, Viale A. Doria 6, 95125 Catania, Italy.

Publication date: February 1, 2010

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

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