1224933-72-5Relevant academic research and scientific papers
Radiosynthesis of [5-[11C]methanesulfonyl-2-((S)-2,2,2- trifluoro-1-methyl-ethoxy)-phenyl]-[5-(tetrahydro-pyran-4-yl)-1, 3-dihydro-isoindol-2-yl]-methanone ([11C]RO5013853), a novel PET tracer for the glycine transporter type i (GlyT1)
Pinard, Emmanuel,Burner, Serge,Cueni, Philipp,Hartung, Thomas,Norcross, Roger D.,Schmid, Philipp,Waldmeier, Pius,Zielinski, Guy,Ravert, Hayden T.,Holt, Daniel P.,Dannals, Robert F.
experimental part, p. 702 - 707 (2012/07/28)
The glycine transporter type 1 (GlyT1) has emerged as a key novel target for the treatment of schizophrenia. We have recently discovered and developed [11C]RO5013853 as a novel positron emission tomography tracer for GlyT1 for which a reliable five-step synthetic route was established. The incorporation of the radioisotope was achieved in the final step through methylation of a sodium sulfinate precursor, itself easily accessible upon reduction of the corresponding sulfonyl-chloride analog. [11C] RO5013853 was prepared with high specific activity (>49 GBq/μmol) and high radiochemical purity (100%). A validation study of [11C]RO5013853 in animal imaging studies is in progress. Copyright
RADIOLABELLED INHIBITORS OF THE GLYCINE 1 TRANSPORTER
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, (2010/05/13)
The present invention relates to novel radiolabelled inhibitors of formula I for the Glycine 1 transporter (GlyT1), useful for the labelling and diagnostic imaging of the glycine 1 transporter functionality. wherein R1 is isopropoxy or 2,2,2-trifluoro-1-methyl-ethoxy; and R2 is a radiolabelled group CH3, wherein the radionuclide is 3H or 11C. The radiolabelled compounds of formula I may be used as PET (Positron Emission Tomography) radiotracer for the labelling and diagnostic molecular imaging of the glycine 1 transporter functionality.
