dc.contributor.author | Riss, Patrick J. | |
dc.contributor.author | Hooker, Jacob M | |
dc.contributor.author | Alexoff, David | |
dc.contributor.author | Kim, Sung-Won | |
dc.contributor.author | Fowler, Joanna S. | |
dc.contributor.author | Rösch, Frank | |
dc.date.accessioned | 2017-07-20T21:34:50Z | |
dc.date.issued | 2009 | |
dc.identifier.citation | Riss, 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. | en_US |
dc.identifier.issn | 0960-894X | en_US |
dc.identifier.uri | http://nrs.harvard.edu/urn-3:HUL.InstRepos:33471158 | |
dc.description.abstract | PR04.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_US |
dc.description.sponsorship | Chemistry and Chemical Biology | en_US |
dc.language.iso | en_US | en_US |
dc.publisher | Elsevier BV | en_US |
dc.relation.isversionof | doi:10.1016/j.bmcl.2009.05.090 | en_US |
dash.license | META_ONLY | |
dc.subject | dopamine transporter | en_US |
dc.subject | MicroPET | en_US |
dc.subject | carbon-11 | en_US |
dc.subject | test-block | en_US |
dc.subject | O-methylation | en_US |
dc.title | [11C]PR04.MZ, a Promising DAT Ligand for Low Concentration Imaging: Synthesis, Efficient 11C-O-Methylation and Initial Small Animal PET Studies | en_US |
dc.type | Journal Article | en_US |
dc.description.version | Version of Record | en_US |
dc.relation.journal | Bioorganic & Medicinal Chemistry Letters | en_US |
dash.depositing.author | Hooker, Jacob M | |
dash.embargo.until | 10000-01-01 | |
dc.identifier.doi | 10.1016/j.bmcl.2009.05.090 | * |
dash.contributor.affiliated | Hooker, Jacob | |