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

Kelly A. Berg, William P. Clarke, Kathryn Cunningham, Umberto Spampinato

Research output: Contribution to journalArticle

74 Citations (Scopus)

Abstract

The serotonin2C receptor (5-HT2CR) is a member of the serotonin2 family of 7-transmembrane-spanning (7-TMS) receptors, which possesses unique molecular and pharmacological properties such as constitutive activity and RNA editing. The 5-HT2CR 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-HT2CR 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-HT2CR, 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.

Original languageEnglish (US)
Pages (from-to)969-976
Number of pages8
JournalNeuropharmacology
Volume55
Issue number6
DOIs
StatePublished - Nov 2008

Fingerprint

RNA Editing
Dopaminergic Neurons
Aptitude
Brain
Substance-Related Disorders
Parkinson Disease
Schizophrenia
Central Nervous System
Pharmacology
Depression
Therapeutics

Keywords

  • 5-HT receptor
  • Constitutive activity
  • Dopamine
  • Microdialysis
  • RNA editing

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this

Fine-tuning serotonin2c receptor function in the brain : Molecular and functional implications. / Berg, Kelly A.; Clarke, William P.; Cunningham, Kathryn; Spampinato, Umberto.

In: Neuropharmacology, Vol. 55, No. 6, 11.2008, p. 969-976.

Research output: Contribution to journalArticle

Berg, Kelly A. ; Clarke, William P. ; Cunningham, Kathryn ; Spampinato, Umberto. / Fine-tuning serotonin2c receptor function in the brain : Molecular and functional implications. In: Neuropharmacology. 2008 ; Vol. 55, No. 6. pp. 969-976.
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