title: Technetium-99m labelled integrated tropane-BAT as a potential dopamine transporter tracer.
abstract: To reduce the molecular weight of 99mTc-labelled tropanes with the aim to enhance the passage over the blood-brain barrier, a so-called integrated tropane-BAT construct was developed. For this purpose a mercaptoethyl substituent was attached to the amine nitrogen atom of a nortropane precursor and the methyl carboxylate in 2beta-position was converted to a 2-mercaptoethylaminomethylene substituent. This integrated tropane-BAT construct could be labelled efficiently (85-90%) with technetium-99m. Results of LC-MS analysis of the tracer agent support the assumed structure. Biodistribution studies in normal rats (n=3) showed a slightly higher brain uptake for the new tracer agents as compared to 99mTc-TRODAT-1. These results indicate that further biological evaluation of the integrated 99mTc-tropane-BAT is warranted.
authors.affiliation: Laboratory of Radiopharmaceutical Chemistry, University Hospital Gasthuisberg, Herestraat 49, B-3000 Leuven, Belgium.
authors.forename: Bernard J
authors.initials: BJ
authors.lastname: Cleynhens
authors.forename: Tjibbe J
authors.initials: TJ
authors.lastname: de Groot
authors.forename: Hubert P
authors.initials: HP
authors.lastname: Vanbilloen
authors.forename: Davy
authors.initials: D
authors.lastname: Kieffer
authors.forename: Luc
authors.initials: L
authors.lastname: Mortelmans
authors.forename: Guy M
authors.initials: GM
authors.lastname: Bormans
authors.forename: Alfons M
authors.initials: AM
authors.lastname: Verbruggen
mesh_terms: D000818:Animals; D002853:Chromatography, Liquid; D050483:Dopamine Plasma Membrane Transport Proteins; D009682:Magnetic Resonance Spectroscopy; D008562:Membrane Glycoproteins / Q000737:chemistry*; D026901:Membrane Transport Proteins / Q000737:chemistry*; D009419:Nerve Tissue Proteins / Q000737:chemistry*; D015609:Organotechnetium Compounds / Q000737:chemistry*; D011874:Radiometry; D051381:Rats; D021241:Spectrometry, Mass, Electrospray Ionization; D014326:Tropanes / Q000737:chemistry*
chemical_list: D050483:Dopamine Plasma Membrane Transport Proteins; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; D009419:Nerve Tissue Proteins; D015609:Organotechnetium Compounds; D014326:Tropanes