TY - JOUR
T1 - Fine-tuning serotonin2c receptor function in the brain
T2 - Molecular and functional implications
AU - Berg, Kelly A.
AU - Clarke, William P.
AU - Cunningham, Kathryn A.
AU - Spampinato, Umberto
N1 - Funding Information:
The authors wish to acknowledge support from the National Institutes of Health (USPHS grant GM58652), the National Alliance for Research on Schizophrenia and Depression, the National Institute on Drug Abuse DA022506, DA 06511 and DA020087, and the Institut National de la Santé e de la Recherche Médicale (INSERM)–Bordeaux 2 University. We thank Marcy J. Bubar, Ph.D., for many thoughtful discussions about the 5-HT 2C R structure and function over the last 10 years.
PY - 2008/11
Y1 - 2008/11
N2 - 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.
AB - 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.
KW - 5-HT receptor
KW - Constitutive activity
KW - Dopamine
KW - Microdialysis
KW - RNA editing
UR - http://www.scopus.com/inward/record.url?scp=53449089516&partnerID=8YFLogxK
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U2 - 10.1016/j.neuropharm.2008.06.014
DO - 10.1016/j.neuropharm.2008.06.014
M3 - Article
C2 - 18602407
AN - SCOPUS:53449089516
VL - 55
SP - 969
EP - 976
JO - Neuropharmacology
JF - Neuropharmacology
SN - 0028-3908
IS - 6
ER -