[11C]PR04.MZ, a promising DAT ligand for low concentration imaging: synthesis, efficient 11C-0-methylation and initial small animal PET studies
PR04.MZ was designed as a highly selective dopamine transporter inhibitor, derived from natural cocaine. Its binding profile indicates that [{sup 11}C]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 [{sup 11}C]MeI mediated synthesis of [{sup 11}C]PR04.MZ from an O-desmethyl precursor trifluoroacetic acid salt with Rb{sub 2}CO{sub 3} in DMF in up to 95 {+-} 5% labelling yield. A preliminary {mu}PET-experiment demonstrates the reversible, highly specific binding of [{sup 11}C]PR04.MZ in the brain of a male Sprague-Dawley rat.
- Research Organization:
- Brookhaven National Lab. (BNL), Upton, NY (United States)
- Sponsoring Organization:
- USDOE SC OFFICE OF SCIENCE (SC)
- DOE Contract Number:
- DE-AC02-98CH10886
- OSTI ID:
- 1040191
- Report Number(s):
- BNL-90579-2009-JA; R&D Project: MO085; KP1503010; TRN: US1202345
- Journal Information:
- Bioorganic and Medicinal Chemistry Letters, Vol. 19, Issue 15; ISSN 0960-894X
- Country of Publication:
- United States
- Language:
- English
Similar Records
Fluroine-18 labeled 28-carbomethoxy-3{beta}-(4-chlorophenyl)-8-[-3-fluoropropyl] nortropane(FPT): Synthesis and tissue distribution of a potential, radioligand for mapping cocaine receptor sites by PET
Comparison of [11C]cocaine binding at tracer and pharmacological doses of baboon brain: A PET study