期刊
NEUROPHARMACOLOGY
卷 55, 期 6, 页码 969-976出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.neuropharm.2008.06.014
关键词
5-HT2c receptor; Constitutive activity; RNA editing; Dopamine; Microdialysis
资金
- National Institutes of Health [GM58652]
- National Alliance for Research on Schizophrenia and Depression
- National Institute on Drug Abuse [DA022506, DA 06511, DA020087]
- Institut National de la Sante e de la Recherche Medicale (INSERM)-Bordeaux 2 University
The serotonin(2C) receptor (5-HT2CR) 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-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. (C) 2008 Elsevier Ltd. All rights reserved.
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