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@ARTICLE{Willmann:892695,
author = {Willmann, Michael and Hegger, Julian and Neumaier, Bernd
and Ermert, Johannes},
title = {{R}adiosynthesis and {B}iological {E}valuation of
[18{F}]{R}91150, a {S}elective 5-{HT}2{A} {R}eceptor
{A}ntagonist for {PET}-{I}maging},
journal = {ACS medicinal chemistry letters},
volume = {12},
number = {5},
issn = {1948-5875},
address = {Washington, DC},
publisher = {ACS},
reportid = {FZJ-2021-02273},
pages = {738 - 744},
year = {2021},
abstract = {Serotonergic 5-HT2A receptors in cortical and forebrain
regions are an important substrate for the neuromodulatory
actions of serotonin in the brain. They have been implicated
in the etiology of many neuropsychiatric disorders and serve
as a target for antipsychotic, antidepressant, and
anxiolytic drugs. Positron emission tomography imaging using
suitable radioligands can be applied for in vivo
quantification of receptor densities and receptor occupancy
for therapy evaluation. Recently, the radiosynthesis of the
selective 5-HT2AR antagonist [18F]R91150 was reported.
However, the six-step radiosynthesis is cumbersome and
time-consuming with low radiochemical yields (RCYs) of
$<5\%.$ In this work, [18F]R91150 was prepared using
late-stage Cu-mediated radiofluorination to simplify its
synthesis. The detailed protocol enabled us to obtain RCYs
of 14 ± $1\%,$ and the total synthesis time was reduced to
60 min. In addition, autoradiographic studies with
[18F]R91150 in rat brain slices revealed the typical uptake
pattern of 5-HT2A receptor ligands.},
cin = {INM-5},
ddc = {610},
cid = {I:(DE-Juel1)INM-5-20090406},
pnm = {525 - Decoding Brain Organization and Dysfunction
(POF4-525)},
pid = {G:(DE-HGF)POF4-525},
typ = {PUB:(DE-HGF)16},
pubmed = {34055220},
UT = {WOS:000651790900010},
doi = {10.1021/acsmedchemlett.0c00658},
url = {https://juser.fz-juelich.de/record/892695},
}