title: Synthesis and biological evaluation of a technetium-99m(I)-tricarbonyl-labelled phenyltropane derivative.
abstract: A new tropane derivative was synthesized by combining a tridentate ligand, N-(2-picolylamine)-N-acetic acid (2-PAA), and a phenyltropane derivative. It was labelled with a [(99m)Tc(CO)(3)](+) moiety, resulting in the formation of two stable and neutral lipophilic isomers. Their identity was confirmed using radio-LC-MS. In normal mice, no brain uptake was observed for any of the isomers and in vitro autoradiography using mouse brain sections showed no specific uptake in the striatal area.
authors.affiliation: Laboratory of Radiopharmaceutical Chemistry, University Hospital Gasthuisberg, Herestraat 49, B-3000 Leuven, Belgium.
authors.forename: Davy M
authors.initials: DM
authors.lastname: Kieffer
authors.forename: Bernard J
authors.initials: BJ
authors.lastname: Cleynhens
authors.forename: Hubert P
authors.initials: HP
authors.lastname: Vanbilloen
authors.forename: Dirk
authors.initials: D
authors.lastname: Rattat
authors.forename: Christelle Y
authors.initials: CY
authors.lastname: Terwinghe
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; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D004353:Drug Evaluation, Preclinical; D066298:In Vitro Techniques; D007553:Isotope Labeling; D051379:Mice; D008968:Molecular Conformation; D015609:Organotechnetium Compounds / Q000737:chemistry*; D013329:Structure-Activity Relationship; D014018:Tissue Distribution; D014326:Tropanes / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics*
chemical_list: D015609:Organotechnetium Compounds; D014326:Tropanes