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| Hauptseite > Publikationsdatenbank > Synthesis and first evaluation of [18F]fluorocyano- and [18F]fluoronitro-quinoxalinedione as putative AMPA receptor antagonists > print |
| Hauptseite > Publikationsdatenbank > Synthesis and first evaluation of [18F]fluorocyano- and [18F]fluoronitro-quinoxalinedione as putative AMPA receptor antagonists > print |
| 001 | 154935 | ||
| 005 | 20220930130031.0 | ||
| 024 | 7 | _ | |a 10.2174/1573406410666140428151318 |2 doi |
| 024 | 7 | _ | |a 1573-4064 |2 ISSN |
| 024 | 7 | _ | |a 1875-6638 |2 ISSN |
| 037 | _ | _ | |a FZJ-2014-04146 |
| 041 | _ | _ | |a English |
| 082 | _ | _ | |a 610 |
| 100 | 1 | _ | |a Olma, Sebastian |0 Extern |b 0 |e Corresponding author |
| 245 | _ | _ | |a Synthesis and first evaluation of [18F]fluorocyano- and [18F]fluoronitro-quinoxalinedione as putative AMPA receptor antagonists |
| 260 | _ | _ | |a Bussum [u.a.] |c 2015 |b Bentham Sc. Publ. |
| 336 | 7 | _ | |a Journal Article |b journal |m journal |0 PUB:(DE-HGF)16 |s 1437642657_19510 |2 PUB:(DE-HGF) |
| 336 | 7 | _ | |a Output Types/Journal article |2 DataCite |
| 336 | 7 | _ | |a Journal Article |0 0 |2 EndNote |
| 336 | 7 | _ | |a ARTICLE |2 BibTeX |
| 336 | 7 | _ | |a JOURNAL_ARTICLE |2 ORCID |
| 336 | 7 | _ | |a article |2 DRIVER |
| 520 | _ | _ | |a 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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| 588 | _ | _ | |a Dataset connected to CrossRef |
| 700 | 1 | _ | |a Ermert, Johannes |0 P:(DE-Juel1)131818 |b 1 |
| 700 | 1 | _ | |a Sihver, Wiebke |0 P:(DE-HGF)0 |b 2 |
| 700 | 1 | _ | |a Coenen, Heinrich Hubert |0 P:(DE-Juel1)131816 |b 3 |
| 773 | _ | _ | |a 10.2174/1573406410666140428151318 |g Vol. 11, no. 1, p. 13 - 20 |0 PERI:(DE-600)2220268-7 |n 1 |p 13 - 20 |t Medicinal chemistry |v 11 |y 2015 |x 1573-4064 |
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| 914 | 1 | _ | |y 2015 |
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