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Role of the 5-HT7 receptor in the central nervous system: from current status to future perspectives

Anne Matthys UGent, Guy Haegeman UGent, Kathleen Van Craenenbroeck UGent and Peter Vanhoenacker (2011) MOLECULAR NEUROBIOLOGY. 43(3). p.228-253
abstract
Pharmacological and genetic tools targeting the 5-hydroxytryptamine (5-HT)7 receptor in preclinical animal models have implicated this receptor in diverse (patho)physiological processes of the central nervous system (CNS). Some data obtained with 5-HT7 receptor knockout mice, selective antagonists, and, to a lesser extent, agonists, however, are quite contradictory. In this review, we not only discuss in detail the role of the 5-HT7 receptor in the CNS but also propose some hypothetical models, which could explain the observed inconsistencies. These models are based on two novel concepts within the field of G protein-coupled receptors (GPCR), namely biphasic signaling and G protein-independent signaling, which both have been shown to be mediated by GPCR dimerization. This led us to suggest that the 5-HT7 receptor could reside in different dimeric contexts and initiate different signaling pathways, depending on the neuronal circuitry and/or brain region. In conclusion, we highlight GPCR dimerization and G protein-independent signaling as two promising future directions in 5-HT7 receptor research, which ultimately might lead to the development of more efficient dimer- and/or pathway-specific therapeutics.
Please use this url to cite or link to this publication:
author
organization
year
type
journalArticle (original)
publication status
published
subject
keyword
RAT DENTATE GYRUS, SEROTONIN RECEPTOR, SUPRACHIASMATIC NUCLEUS, ANTAGONIST SB-269970, REM-SLEEP, 5-HT7 receptor, IN-VIVO, Circadian rhythm, REM sleep, Thermoregulation, Depression, Substance abuse, Schizophrenia, Anxiety, Pain, MIDDLE MENINGEAL ARTERY, Memory, NOVELTY-SEEKING BEHAVIOR, OBSESSIVE-COMPULSIVE DISORDER, DORSAL RAPHE NUCLEUS
journal title
MOLECULAR NEUROBIOLOGY
Mol. Neurobiol.
volume
43
issue
3
pages
228 - 253
Web of Science type
Article
Web of Science id
000290229300008
JCR category
NEUROSCIENCES
JCR impact factor
5.735 (2011)
JCR rank
32/242 (2011)
JCR quartile
1 (2011)
ISSN
0893-7648
DOI
10.1007/s12035-011-8175-3
language
English
UGent publication?
yes
classification
A1
copyright statement
I have transferred the copyright for this publication to the publisher
id
1234403
handle
http://hdl.handle.net/1854/LU-1234403
date created
2011-05-24 16:06:44
date last changed
2012-01-16 15:21:37
@article{1234403,
  abstract     = {Pharmacological and genetic tools targeting the 5-hydroxytryptamine (5-HT)7 receptor in preclinical animal models have implicated this receptor in diverse (patho)physiological processes of the central nervous system (CNS). Some data obtained with 5-HT7 receptor knockout mice, selective antagonists, and, to a lesser extent, agonists, however, are quite contradictory. In this review, we not only discuss in detail the role of the 5-HT7 receptor in the CNS but also propose some hypothetical models, which could explain the observed inconsistencies. These models are based on two novel concepts within the field of G protein-coupled receptors (GPCR), namely biphasic signaling and G protein-independent signaling, which both have been shown to be mediated by GPCR dimerization. This led us to suggest that the 5-HT7 receptor could reside in different dimeric contexts and initiate different signaling pathways, depending on the neuronal circuitry and/or brain region. In conclusion, we highlight GPCR dimerization and G protein-independent signaling as two promising future directions in 5-HT7 receptor research, which ultimately might lead to the development of more efficient dimer- and/or pathway-specific therapeutics.},
  author       = {Matthys, Anne and Haegeman, Guy and Van Craenenbroeck, Kathleen and Vanhoenacker, Peter},
  issn         = {0893-7648},
  journal      = {MOLECULAR NEUROBIOLOGY},
  keyword      = {RAT DENTATE GYRUS,SEROTONIN RECEPTOR,SUPRACHIASMATIC NUCLEUS,ANTAGONIST SB-269970,REM-SLEEP,5-HT7 receptor,IN-VIVO,Circadian rhythm,REM sleep,Thermoregulation,Depression,Substance abuse,Schizophrenia,Anxiety,Pain,MIDDLE MENINGEAL ARTERY,Memory,NOVELTY-SEEKING BEHAVIOR,OBSESSIVE-COMPULSIVE DISORDER,DORSAL RAPHE NUCLEUS},
  language     = {eng},
  number       = {3},
  pages        = {228--253},
  title        = {Role of the 5-HT7 receptor in the central nervous system: from current status to future perspectives},
  url          = {http://dx.doi.org/10.1007/s12035-011-8175-3},
  volume       = {43},
  year         = {2011},
}

Chicago
Matthys, Anne, Guy Haegeman, Kathleen Van Craenenbroeck, and Peter Vanhoenacker. 2011. “Role of the 5-HT7 Receptor in the Central Nervous System: From Current Status to Future Perspectives.” Molecular Neurobiology 43 (3): 228–253.
APA
Matthys, A., Haegeman, G., Van Craenenbroeck, K., & Vanhoenacker, P. (2011). Role of the 5-HT7 receptor in the central nervous system: from current status to future perspectives. MOLECULAR NEUROBIOLOGY, 43(3), 228–253.
Vancouver
1.
Matthys A, Haegeman G, Van Craenenbroeck K, Vanhoenacker P. Role of the 5-HT7 receptor in the central nervous system: from current status to future perspectives. MOLECULAR NEUROBIOLOGY. 2011;43(3):228–53.
MLA
Matthys, Anne, Guy Haegeman, Kathleen Van Craenenbroeck, et al. “Role of the 5-HT7 Receptor in the Central Nervous System: From Current Status to Future Perspectives.” MOLECULAR NEUROBIOLOGY 43.3 (2011): 228–253. Print.