[11C]PR04.MZ, a Promising DAT Ligand for Low Concentration Imaging: Synthesis, Efficient 11C-O-Methylation and Initial Small Animal PET Studies
Access StatusFull text of the requested work is not available in DASH at this time ("restricted access"). For more information on restricted deposits, see our FAQ.
Riss, Patrick J.
Fowler, Joanna S.
MetadataShow full item record
CitationRiss, Patrick J., Jacob M. Hooker, David Alexoff, Sung-Won Kim, Joanna S. Fowler, and Frank Rösch. 2009. “[11C]PR04.MZ, a Promising DAT Ligand for Low Concentration Imaging: Synthesis, Efficient 11C-O-Methylation and Initial Small Animal PET Studies.” Bioorganic & Medicinal Chemistry Letters 19 (15) (August): 4343–4345. doi:10.1016/j.bmcl.2009.05.090.
AbstractPR04.MZ was designed as a highly selective dopamine transporter inhibitor, derived from natural cocaine. Its binding profile indicates that [11C]PR04.MZ may be suited as a PET radioligand for the non-invasive exploration of striatal and extrastriatal DAT populations. As a key feature, its structural design facilitates both, labelling with fluorine-18 at its terminally fluorinated butynyl moiety and carbon-11 at its methyl ester function. The present report concerns the efficient [11C]MeI mediated synthesis of [11C]PR04.MZ from an O-desmethyl precursor trifluoroacetic acid salt with Rb2CO3 in DMF in up to 95 ± 5% labelling yield. A preliminary μPET-experiment demonstrates the reversible, highly specific binding of [11C]PR04.MZ in the brain of a male Sprague–Dawley rat.
Citable link to this pagehttp://nrs.harvard.edu/urn-3:HUL.InstRepos:33471158
- HMS Scholarly Articles