Serotonin2c receptor constitutive activity: in vivo direct and indirect evidence and functional significance.

Sylvia Navailles, Mélanie Lagière, Martin Guthrie, Philippe Deurwaerdère
CNSAMC. 2013-10-01; 13(2): 98-107
DOI: 10.2174/1871524911313020002

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Serotonin2c (5-HT2c) receptors are widely expressed in the central nervous system
where they play a pivotal role in the regulation of neuronal network
excitability. Along with this fundamental physiological function, 5-HT2c
receptors are thought to be implicated in the pathophysiology of several
neuropsychiatric disorders and have become a major pharmacological target for the
development of improved treatments of these disorders. In the past decade, many
studies have focused on the constitutive activity of 5-HT2c receptors and the
therapeutic potential of drugs acting as inverse agonists. Although the
constitutive activity of the 5-HT2c receptor has been clearly described in vitro,
the transposition of this concept to living animals is often difficult to
ascertain. Nevertheless, cumulating evidence has demonstrated the functional
relevance of such property in regulating physiological systems in vivo both at
the level of the central and peripheral nervous systems. The present review
provides an update of the growing number of studies that show, by means of
pharmacological tools, the participation of the constitutive activity of 5-HT2c
receptors in the control of various biochemical and behavioural functions in vivo
and emphasizes the functional organization of this constitutive control together
with the phasic and tonic (involving the spontaneous release of 5-HT) modalities
of the 5-HT2c receptor in the brain.


Auteurs Bordeaux Neurocampus