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Neuropharmacology. 2008 Nov;55(6):969-76. doi: 10.1016/j.neuropharm.2008.06.014. Epub 2008 Jun 17.

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

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  • 1Department of Pharmacology, University of Texas Health Science Center, San Antonio, TX 78229-3900, USA.


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.

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