Synthesis and First Evaluation of [18F]Fluorocyano- and [18F]Fluoronitroquinoxalinedione as Putative AMPA Receptor Antagonists

ISSN: 1875-6638 (Online)
ISSN: 1573-4064 (Print)


Volume 10, 8 Issues, 2014


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Medicinal Chemistry

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Editor-in-Chief:
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Kings College
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Synthesis and First Evaluation of [18F]Fluorocyano- and [18F]Fluoronitroquinoxalinedione as Putative AMPA Receptor Antagonists

Author(s): Sebastian Olma, Johannes Ermert, Wiebke Sihver and Heinz H. Coenen

Affiliation: Institut für Neurowissenschaften und Medizin, INM-5: Nuklearchemie, Forschungszentrum Jülich GmbH, 52425 Jülich, Germany

Abstract

Derivatives of quinoxalinedione (QX) were chosen as chemical lead for the development of new radioligands for 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 6-[18F]fluoro-7-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 cyano- and 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

Keywords: AMPA receptor, fluorine-18, glutamate receptor, positron emission tomography, quinoxalinedione, radiofluorination

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Article Details

Volume: 10
First Page: 1
Last Page: 8
Page Count: 8
DOI: 10.2174/1573406410666140428151318
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