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@ARTICLE{Olma:154935,
author = {Olma, Sebastian and Ermert, Johannes and Sihver, Wiebke and
Coenen, Heinrich Hubert},
title = {{S}ynthesis and first evaluation of [18{F}]fluorocyano- and
[18{F}]fluoronitro-quinoxalinedione as putative {AMPA}
receptor antagonists},
journal = {Medicinal chemistry},
volume = {11},
number = {1},
issn = {1573-4064},
address = {Bussum [u.a.]},
publisher = {Bentham Sc. Publ.},
reportid = {FZJ-2014-04146},
pages = {13 - 20},
year = {2015},
abstract = {Abstract:Derivatives of quinoxalinedione (QX) were chosen
as chemical lead for the development of new radioligands of
the AMPA receptor, since there are several examples of
QX-derivatives with high affinity. The radiosyntheses of the
new compounds 6-[18F]fluoro-7-nitro-QX ([18F]FNQX) and
7-[18F]fluoro-6-cyano-QX ([18F]FCQX) with radiochemical
yields of 8 ± 2 and 3 ± 2 $\%,$ respectively, as well as
the evaluation of their binding properties to the
AMPA-receptor were performed. A comparison of the Ki-values
of the new QX-derivatives FCQX and FNQX with
mono-substituted cyanoand nitro-QX shows negligibly small
differences of affinity (within the range of 1.4 to 5 µM),
but exhibits a tenfold lower affinity than derivatives with
two electron withdrawing groups like the
7-cyano-6-nitro-compound CNQX and the 6,7- dinitro compound
DNQX. Thus, with respect to the low affinity and a high
non-specific binding with in vitro and ex vivo
autoradiographic studies, the new compounds do not lend
themselves for in vivo imaging.- See more at:
http://www.eurekaselect.com/121871/article#sthash.JGpS3IVS.dpuf},
cin = {INM-5},
ddc = {610},
cid = {I:(DE-Juel1)INM-5-20090406},
pnm = {573 - Neuroimaging (POF3-573) / 573 - Neuroimaging
(POF3-573)},
pid = {G:(DE-HGF)POF3-573 / G:(DE-HGF)POF3-573},
typ = {PUB:(DE-HGF)16},
doi = {10.2174/1573406410666140428151318},
url = {https://juser.fz-juelich.de/record/154935},
}