Abstract
Over the past 15 years, there have been various attempts to rationally develop selective ligands for serotonin 5-HT2C receptor subtypes. To this end, the studies performed by researchers at GlaxoSmithKline have led to the identification of several potent and selective 5-HT2C receptor antagonists characterized by indole- or indoline-containing structure. The large body of data on antagonists has allowed a detailed description of a pharmacophore model for 5-HT2C receptor antagonists as well as the description of the topography of the antagonist binding site of the receptor. On the other hand, studies from different laboratories have led to the identification of functionally selective 5-HT2C receptor agonists. This was a difficult task because the 5-HT2C receptor structure is closely related to that of the 5-HT2A and 5-HT2B receptor subtypes. The most frequently used frameworks for agonists were arylpiperazines and their isosters, indoles, and benzazepines. This chapter describes in detail the structure–activity relationships of the 5-HT2C selective agents.
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Leopoldo, M., Lacivita, E., De Giorgio, P., Berardi, F., Perrone, R. (2011). The Medicinal Chemistry of 5-HT2C Receptor Ligands. In: Di Giovanni, G., Esposito, E., Di Matteo, V. (eds) 5-HT2C Receptors in the Pathophysiology of CNS Disease. The Receptors, vol 22. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-60761-941-3_3
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DOI: https://doi.org/10.1007/978-1-60761-941-3_3
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