84773-29-5Relevant articles and documents
COMPOUNDS FOR USE IN IMAGING, DIAGNOSING AND/OR TREATMENT OF DISEASES OF THE CENTRAL NERVOUS SYSTEM
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Page/Page column 38, (2012/05/05)
This invention relates to novel compounds suitable as precursors for the preparation of certain 18F labelled positron emission tomography (PET) tracers. Furthermore, the invention relates to the preparation of such precursor molecules and to th
Synthesis of three novel fluorine-18 labeled analogues of l -deprenyl for Positron Emission Tomography (PET) studies of Monoamine Oxidase B (MAO-B)
Nag, Sangram,Lehmann, Lutz,Heinrich, Tobias,Thiele, Andrea,Kettschau, Georg,Nakao, Ryuji,Gulyás, Balázs,Halldin, Christer
supporting information; experimental part, p. 7023 - 7029 (2011/12/15)
The aim in this project was to synthesize and to study fluorine-18 labeled analogues of l-deprenyl which bind selectively to the enzyme monoamine oxidase B (MAO-B). Three fluorinated l-deprenyl analogues have been generated in multistep organic syntheses. The most promising fluorine-18 compound N-[(2S)-1-[18F]fluoro-3-phenylpropan-2-yl]-N-methylprop-2-yn-1-amine (4c) was synthesized by a one-step fluorine-18 nucleophilic substitution reaction. Autoradiography on human brain tissue sections demonstrated specific binding for compound 4c to brain regions known to have a high content of MAO-B. In addition, the corresponding nonradioactive fluorine-19 compound (13) inhibited recombinant human MAO-B with an IC50 of 170.5 ±29 nM but did not inhibit recombinant human MAO-A (IC50 > 2000 nM), demonstrating its specificity. Biodistribution of 4c in mice showed high initial brain uptake leveling at 5.2 ±0.04%ID/g after 2 min post injection. In conclusion, compound 4c is a specific inhibitor of MAO-B with high initial brain uptake in mice and is, therefore, a candidate for further investigation in PET.
COMPOUNDS FOR USE IN IMAGING, DIAGNOSING, AND/OR TREATMENT OF DISEASES OF THE CENTRAL NERVOUS SYSTEM OR OF TUMORS
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Page/Page column 72, (2009/05/28)
This invention relates to novel compounds suitable for labelling or already labelled by 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds