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PMID: 18602407 Published · ppublish English Journal Article Research Support, N.I.H., Extramural Research Support, Non-U.S. Gov't Review

Fine-tuning serotonin2c receptor function in the brain: molecular and functional implications.

Neuropharmacology ·Vol. 55 ·No. 6 ·2008-11-00 ·Pages 969-76

Berg KA, Clarke WP, Cunningham KA, Spampinato U

Abstract

The serotonin(2C) receptor (5-HT(2C)R) is a member of the serotonin(2) family of 7-transmembrane-spanning (7-TMS) receptors, which possesses unique molecular and pharmacological properties such as constitutive activity and RNA editing. The 5-HT(2C)R is widely expressed within the central nervous system, where is thought to play a major role in the regulation of neuronal network excitability. In keeping with its ability to modulate dopamine (DA) neuron function in the brain, the 5-HT(2C)R is currently considered as a major target for improved treatments of neuropsychiatric disorders related to DA neuron dysfunction, such as depression, schizophrenia, Parkinson's disease or drug addiction. The aim of this review is to provide an update of the functional status of the central 5-HT(2C)R, covering molecular, cellular, anatomical, biochemical and behavioral aspects to highlight its distinctive regulatory properties, the emerging functional significance of constitutive activity and RNA editing in vivo, and the therapeutic potential of inverse agonism.

MeSH Terms
Animals Brain/cytology,physiology Dopamine/metabolism Humans Neurons/physiology RNA Editing Receptor, Serotonin, 5-HT2C/genetics,metabolism Serotonin/metabolism
Chemicals
Receptor, Serotonin, 5-HT2C Serotonin Dopamine
Authors & Affiliations
4 authors, click to expand affiliations / ORCID
Berg Kelly A
Department of Pharmacology, University of Texas Health Science Center, San Antonio, TX 78229-3900, USA.
Clarke William P
Cunningham Kathryn A
Spampinato Umberto
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Article Info
Journal
Neuropharmacology
Abbr.
Neuropharmacology
ISSN
0028-3908
DOI
10.1016/j.neuropharm.2008.06.014
Published
2008-11-00
Epub
2008-00-17
Pages
969-76
Language
English
Region
England
NLM ID
0236217
PMCID
PMC3124806
Subset
IM
Grants
NIDA NIH HHS · K05 DA020087-01 · United States
NIDA NIH HHS · K05 DA020087-04 · United States
NIDA NIH HHS · R01 DA006511-15 · United States
NIDA NIH HHS · K05 DA020087-05 · United States
NIDA NIH HHS · R01 DA006511-10 · United States
NIGMS NIH HHS · GM58652 · United States
NIDA NIH HHS · R01 DA006511 · United States
NIDA NIH HHS · R01 DA006511-13 · United States
NIDA NIH HHS · DA022506 · United States
NIDA NIH HHS · R01 DA006511-12 · United States
NIDA NIH HHS · DA 06511 · United States
NIDA NIH HHS · K05 DA020087-03 · United States
NIDA NIH HHS · DA020087 · United States
NIDA NIH HHS · R01 DA006511-10S1 · United States
NIDA NIH HHS · K05 DA020087-02 · United States
NIDA NIH HHS · R01 DA006511-14A1 · United States
NIDA NIH HHS · R01 DA006511-11 · United States
NIDA NIH HHS · R01 DA006511-11S1 · United States
NIDA NIH HHS · K05 DA020087 · United States
NIGMS NIH HHS · R01 GM058652 · United States
External Links
PubMed source DOI: 10.1016/j.neuropharm.2008.06.014 PMC Full Text View journal details
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