Therapeutic Potential of 5-HT2C Receptor Ligands

Serotonin 2C receptors are G protein-coupled receptors expressed by GABAergic, glutamatergic, and dopaminergic neurons. Anatomically, they are present in various brain regions, including cortical areas, hippocampus, ventral midbrain, striatum, nucleus accumbens, hypothalamus, and amygdala. A large b...

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Main Authors: Nanna H. Jensen, Thomas I. Cremers, Florence Sotty
Format: Article
Language:English
Published: Wiley 2010-01-01
Series:The Scientific World Journal
Online Access:http://dx.doi.org/10.1100/tsw.2010.180
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author Nanna H. Jensen
Thomas I. Cremers
Florence Sotty
author_facet Nanna H. Jensen
Thomas I. Cremers
Florence Sotty
author_sort Nanna H. Jensen
collection DOAJ
description Serotonin 2C receptors are G protein-coupled receptors expressed by GABAergic, glutamatergic, and dopaminergic neurons. Anatomically, they are present in various brain regions, including cortical areas, hippocampus, ventral midbrain, striatum, nucleus accumbens, hypothalamus, and amygdala. A large body of evidence supports a critical role of serotonin 2C receptors in mediating the interaction between serotonergic and dopaminergic systems, which is at the basis of their proposed involvement in the regulation of mood, affective behavior, and memory. In addition, their expression in specific neuronal populations in the hypothalamus would be critical for their role in the regulation of feeding behavior. Modulation of these receptors has therefore been proposed to be of interest in the search for novel pharmacological strategies for the treatment of various pathological conditions, including schizophrenia and mood disorders, as well as obesity. More precisely, blockade of serotonin 2C receptors has been suggested to provide antidepressant and anxiolytic benefit, while stimulation of these receptors may offer therapeutic benefit for the treatment of psychotic symptoms in schizophrenia and obesity. In addition, modulation of serotonin 2C receptors may offer cognitive-enhancing potential, albeit still a matter of debate. In the present review, the most compelling evidence from the literature is presented and tentative hypotheses with respect to existing controversies are outlined.
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spelling doaj-art-833df36f32df493abb1a6c063be273c42025-02-03T06:06:58ZengWileyThe Scientific World Journal1537-744X2010-01-01101870188510.1100/tsw.2010.180Therapeutic Potential of 5-HT2C Receptor LigandsNanna H. Jensen0Thomas I. Cremers1Florence Sotty2Department of Neurophysiology, H. Lundbeck A/S, Copenhagen-Valby, DenmarkBrains On-Line LLC, South San Francisco, CA, USADepartment of Neurophysiology, H. Lundbeck A/S, Copenhagen-Valby, DenmarkSerotonin 2C receptors are G protein-coupled receptors expressed by GABAergic, glutamatergic, and dopaminergic neurons. Anatomically, they are present in various brain regions, including cortical areas, hippocampus, ventral midbrain, striatum, nucleus accumbens, hypothalamus, and amygdala. A large body of evidence supports a critical role of serotonin 2C receptors in mediating the interaction between serotonergic and dopaminergic systems, which is at the basis of their proposed involvement in the regulation of mood, affective behavior, and memory. In addition, their expression in specific neuronal populations in the hypothalamus would be critical for their role in the regulation of feeding behavior. Modulation of these receptors has therefore been proposed to be of interest in the search for novel pharmacological strategies for the treatment of various pathological conditions, including schizophrenia and mood disorders, as well as obesity. More precisely, blockade of serotonin 2C receptors has been suggested to provide antidepressant and anxiolytic benefit, while stimulation of these receptors may offer therapeutic benefit for the treatment of psychotic symptoms in schizophrenia and obesity. In addition, modulation of serotonin 2C receptors may offer cognitive-enhancing potential, albeit still a matter of debate. In the present review, the most compelling evidence from the literature is presented and tentative hypotheses with respect to existing controversies are outlined.http://dx.doi.org/10.1100/tsw.2010.180
spellingShingle Nanna H. Jensen
Thomas I. Cremers
Florence Sotty
Therapeutic Potential of 5-HT2C Receptor Ligands
The Scientific World Journal
title Therapeutic Potential of 5-HT2C Receptor Ligands
title_full Therapeutic Potential of 5-HT2C Receptor Ligands
title_fullStr Therapeutic Potential of 5-HT2C Receptor Ligands
title_full_unstemmed Therapeutic Potential of 5-HT2C Receptor Ligands
title_short Therapeutic Potential of 5-HT2C Receptor Ligands
title_sort therapeutic potential of 5 ht2c receptor ligands
url http://dx.doi.org/10.1100/tsw.2010.180
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