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@ARTICLE{Blenau:829982,
author = {Blenau, Wolfgang and Daniel, Stöppler and Balfanz, Sabine
and Thamm, Markus and Baumann, A.},
title = {{D}m5-{HT}$_{2{B}}$: {P}harmacological {C}haracterization
of the {F}ifth {S}erotonin {R}eceptor {S}ubtype of
{D}rosophila melanogaster},
journal = {Frontiers in systems neuroscience},
volume = {11},
issn = {1662-5137},
address = {Lausanne},
publisher = {Frontiers Research Foundation},
reportid = {FZJ-2017-03584},
pages = {28},
year = {2017},
abstract = {Serotonin (5-hydroxytryptamine, 5-HT) is an important
regulator of physiological and behavioral processes in both
protostomes (e.g., insects) and deuterostomes (e.g.,
mammals). In insects, serotonin has been found to modulate
the heart rate and to control secretory processes,
development, circadian rhythms, aggressive behavior, as well
as to contribute to learning and memory. Serotonin exerts
its activity by binding to and activating specific membrane
receptors. The clear majority of these receptors belong to
the superfamily of G-protein-coupled receptors. In
Drosophila melanogaster, a total of five genes have been
identified coding for 5-HT receptors. From this family of
proteins, four have been pharmacologically examined in
greater detail, so far. While Dm5-HT1A, Dm5-HT1B, and
Dm5-HT7 couple to cAMP signaling cascades, the Dm5-HT2A
receptor leads to Ca2+ signaling in an
inositol-1,4,5-trisphosphate-dependent manner. Based on
sequence similarity to homologous genes in other insects, a
fifth D. melanogaster gene was uncovered coding for a
Dm5-HT2B receptor. Knowledge about this receptor’s
pharmacological properties is very limited. This is quite
surprising because Dm5-HT2B has been attributed to distinct
physiological functions based on genetic interference with
its gene expression. Mutations were described reducing the
response of the larval heart to 5-HT, and specific knockdown
of Dm5-HT2B mRNA in hemocytes resulted in a higher
susceptibility of the flies to bacterial infection. To gain
deeper understanding of Dm5-HT2B’s pharmacology, we
evaluated the receptor’s response to a series of
established 5-HT receptor agonists and antagonists in a
functional cell-based assay. Metoclopramide and mianserin
were identified as two potent antagonists that may allow
pharmacological interference with Dm5-HT2B signaling in
vitro and in vivo.},
cin = {ICS-4},
ddc = {610},
cid = {I:(DE-Juel1)ICS-4-20110106},
pnm = {552 - Engineering Cell Function (POF3-552)},
pid = {G:(DE-HGF)POF3-552},
typ = {PUB:(DE-HGF)16},
UT = {WOS:000401656800002},
pubmed = {pmid:28553207},
doi = {10.3389/fnsys.2017.00028},
url = {https://juser.fz-juelich.de/record/829982},
}