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| Hauptseite > Publikationsdatenbank > Synthesis and first evaluation of [18F]fluorocyano- and [18F]fluoronitro-quinoxalinedione as putative AMPA receptor antagonists |
| Hauptseite > Publikationsdatenbank > Synthesis and first evaluation of [18F]fluorocyano- and [18F]fluoronitro-quinoxalinedione as putative AMPA receptor antagonists |
| Journal Article | FZJ-2014-04146 |
; ; ;
2015
Bentham Sc. Publ.
Bussum [u.a.]
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Please use a persistent id in citations: doi:10.2174/1573406410666140428151318
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
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