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• W2613699566 abstract "Presently available PET ligands for the NMDAr ion channel generally suffer from fast metabolism. The purpose of this study was to develop a metabolically more stable ligand for the NMDAr ion channel, taking [11C]GMOM ([11C]1) as the lead compound. [11C]1, its fluoralkyl analogue [18F]PK209 ([18F]2) and the newly synthesized fluorovinyloxy analogue [11C]7b were evaluated ex vivo in male Wistar rats for metabolic stability. In addition, [11C]7b was subjected to a biodistribution study and its affinity (Ki) and lipophilicity (logD7.4) values were determined. The addition of a vinyl chain in the fluoromethoxy moiety did not negatively alter the affinity of [11C]7b for the NMDAr, while lipophilicity was increased. Biodistribution studies showed higher uptake of [11C]7b in forebrain regions compared with cerebellum. Pre-treatment with MK-801 decreased the overall brain uptake significantly, but not in a region-specific manner. 45 min after injection 78, 90 and 87% of activity in the brain was due to parent compound for [11C]1, [18F]2 and [11C]7b, respectively. In plasma, 26–31% of activity was due to parent compound. Complete substitution of the alpha-carbon increased lipophilicity to more favorable values. Substitution of one or more hydrogens of the alpha-carbon atom in the methoxy moiety improved metabolic stability. In plasma, more parent compound was found for [18F]2 and [11C]7b then for [11C]1, although differences were not significant. At 45 min, significantly more parent [18F]2 and [11C]7b was measured in the brain compared with [11C]1." @default.
• W2613699566 created "2017-05-19" @default.
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• W2613699566 date "2017-08-01" @default.
• W2613699566 modified "2023-09-26" @default.
• W2613699566 title "Synthesis, radiolabeling and preclinical evaluation of a [ 11 C]GMOM derivative as PET radiotracer for the ion channel of the N-methyl-D-aspartate receptor" @default.
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• W2613699566 doi "https://doi.org/10.1016/j.nucmedbio.2017.05.003" @default.
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