The central 5-HT3 receptor
in CNS disorders

by
Bloom FE, Morales M
The Scripps Research Institute,
Department of Neuropharmacology,
La Jolla, CA 92037, USA.
fbloom@scripps.edu
Neurochem Res 1998 May; 23(5):653-9


ABSTRACT

Among the characterized 5-HT receptors of the central nervous system, the type 3 receptor subtype (5-HT3R) is the only one known to be a ligand-gated ion channel. Its early pharmacological characterization and mapping by radioligand binding autoradiography suggested that this receptor may, among other actions, regulate dopamine release in the nigro-striatal pathway and reduce alcohol consumption in experimental animals while antagonists of this receptor have been reported to treat anxiety disorders. Following the cloning of this receptor in 1991, direct cellular localization was made possible by in situ hybridization and immunohistochemical analysis. Here we summarize our recent efforts showing that 5-HT3R-expressing neurons are mainly GABA containing cells in the rat neocortex, olfactory cortex, hippocampus, and amygdala which also often contain cholecystokinin (CCK) immunoreactivity. These results provide a means to unify some of the initial pharmacological observations.
GABA
SSRIs
5-HT2
5-HT3
5-HT1a
5-HT1b
5-HT2a
Serotonin
Ondansetron
Cholecystokinin
5-HT2b/5-HT2b
Serotonergic drugs
5-HT3a receptors and anxiety


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