Riss, Patrick J.Hooker, JacobAlexoff, DavidKim, Sung-WonFowler, Joanna S.Rösch, Frank2017-07-202009Riss, 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.2009.05.090.0960-894Xhttp://nrs.harvard.edu/urn-3:HUL.InstRepos:33471158PR04.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.en-USdopamine transporterMicroPETcarbon-11test-blockO-methylationJournal Article10.1016/j.bmcl.2009.05.090