680591-44-0Relevant academic research and scientific papers
Radiosynthesis and evaluation of [11C]EMPA as a potential PET tracer for orexin 2 receptors
Wang, Changning,Moseley, Christian K.,Carlin, Stephen M.,Wilson, Colin M.,Neelamegam, Ramesh,Hooker, Jacob M.
, p. 3389 - 3392 (2013/06/27)
EMPA is a selective antagonist of orexin 2 (OX2) receptors. Previous literature with [3H]-EMPA suggest that it may be used as an imaging agent for OX2 receptors; however, brain penetration is known to be modest. To evaluate the potential of EMPA as a PET radiotracer in non-human primate (as a step to imaging in man), we radiolabeled EMPA with carbon-11. Radiosynthesis of [11C]N-ethyl-2-(N-(6-methoxypyridin-3- yl)-2-methylphenylsulfonamido)-N-(pyridin-3-ylmethyl)acetamide ([ 11C]EMPA), and evaluation as a potential PET tracer for OX 2 receptors is described. Synthesis of an appropriate non-radioactive O-desmethyl precursor was achieved from EMPA with sodium iodide and chlorotrimethylsilane. Selective O-methylation using [11C]CH 3I in the presence of cesium carbonate in DMSO at room temp afforded [11C]EMPA in 1.5-2.5% yield (non-decay corrected relative to trapped [11C]CH3I at EOS) with ≥95% chemical and radiochemical purities. The total synthesis time was 34-36 min from EOB. Studies in rodent suggested that uptake in tissue was dominated by nonspecific binding. However, [11C]EMPA also showed poor uptake in both rats and baboon as measured with PET imaging.
SULFONYLAMINO-ACETIC ACID DERIVATIVES
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Page 71, (2010/02/06)
The invention relates to novel sulfonylamino-acetic acid derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of such compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.
