Central Serotonin2C Receptor: From Physiology to Pathology

Giuseppe Di      Giovanni; Vincenzo Di      Matteo; Massimo      Pierucci; Arcangelo      Benigno; Ennio      Esposito

doi:10.2174/156802606778522113

Abstract

Since the 1950s, when serotonin (5-HT) was discovered in the mammalian central nervous system (CNS), an enormous amount of experimental evidence has revealed the pivotal role of this biogenic amine in a number of cognitive and behavioural functions. Although 5-HT is synthesized by a small group of neurons within the raphe nuclei of the brain stem, almost all parts of the CNS receive serotonergic projections. Furthermore, the importance of 5-HT modulation and the fine-tuning of its action is underlined by the large number of 5-HT binding sites found in the CNS. Hitherto, up to 15 different 5-HT receptors subtypes have been identified. This review was undertaken to summarize the work that has explored the pathophysiological role of one of these receptors, the 5-HT2C receptor, that has been emerged as a prominent central serotonin receptor subtype. The physiology, pharmacology and anatomical distribution of the 5-HT2C receptors in the CNS will be firstly reviewed. Finally, their potential involvement in the pathophysiology of depression, schizophrenia, Parkinson ’ s disease and drug abuse will be also discussed.

Keywords: Serotonergic receptors, Depression, Schizophrenia, Drug of abuse, selective 5-HT2C drugs

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