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000154935 0247_ $$2doi$$a10.2174/1573406410666140428151318
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000154935 0247_ $$2ISSN$$a1875-6638
000154935 037__ $$aFZJ-2014-04146
000154935 041__ $$aEnglish
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000154935 1001_ $$0Extern$$aOlma, Sebastian$$b0$$eCorresponding author
000154935 245__ $$aSynthesis and first evaluation of [18F]fluorocyano- and [18F]fluoronitro-quinoxalinedione as putative AMPA receptor antagonists
000154935 260__ $$aBussum [u.a.]$$bBentham Sc. Publ.$$c2015
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000154935 520__ $$aAbstract:Derivatives of quinoxalinedione (QX) were chosen as chemical lead for the development of new radioligands of the AMPA receptor, since there are several examples of QX-derivatives with high affinity. The radiosyntheses of the new compounds 6-[18F]fluoro-7-nitro-QX ([18F]FNQX) and 7-[18F]fluoro-6-cyano-QX ([18F]FCQX) with radiochemical yields of 8 ± 2 and 3 ± 2 %, respectively, as well as the evaluation of their binding properties to the AMPA-receptor were performed. A comparison of the Ki-values of the new QX-derivatives FCQX and FNQX with mono-substituted cyanoand nitro-QX shows negligibly small differences of affinity (within the range of 1.4 to 5 µM), but exhibits a tenfold lower affinity than derivatives with two electron withdrawing groups like the 7-cyano-6-nitro-compound CNQX and the 6,7- dinitro compound DNQX. Thus, with respect to the low affinity and a high non-specific binding with in vitro and ex vivo autoradiographic studies, the new compounds do not lend themselves for in vivo imaging.- See more at: http://www.eurekaselect.com/121871/article#sthash.JGpS3IVS.dpuf
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000154935 7001_ $$0P:(DE-Juel1)131818$$aErmert, Johannes$$b1
000154935 7001_ $$0P:(DE-HGF)0$$aSihver, Wiebke$$b2
000154935 7001_ $$0P:(DE-Juel1)131816$$aCoenen, Heinrich Hubert$$b3
000154935 773__ $$0PERI:(DE-600)2220268-7$$a10.2174/1573406410666140428151318$$gVol. 11, no. 1, p. 13 - 20$$n1$$p13 - 20$$tMedicinal chemistry$$v11$$x1573-4064$$y2015
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