%0 Journal Article
%A Olma, Sebastian
%A Ermert, Johannes
%A Sihver, Wiebke
%A Coenen, Heinrich Hubert
%T Synthesis and first evaluation of [18F]fluorocyano- and [18F]fluoronitro-quinoxalinedione as putative AMPA receptor antagonists
%J Medicinal chemistry
%V 11
%N 1
%@ 1573-4064
%C Bussum [u.a.]
%I Bentham Sc. Publ.
%M FZJ-2014-04146
%P 13 - 20
%D 2015
%X 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
%F PUB:(DE-HGF)16
%9 Journal Article
%R 10.2174/1573406410666140428151318
%U https://juser.fz-juelich.de/record/154935