Synthesis and biological evaluation of a technetium-99m(I)-tricarbonyl-labelled phenyltropane derivative.
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.
Kieffer
Davy M
DM
Laboratory of Radiopharmaceutical Chemistry, University Hospital Gasthuisberg, Herestraat 49, B-3000 Leuven, Belgium.
Cleynhens
Bernard J
BJ
Vanbilloen
Hubert P
HP
Rattat
Dirk
D
Terwinghe
Christelle Y
CY
Mortelmans
Luc
L
Bormans
Guy M
GM
Verbruggen
Alfons M
AM
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*
D015609:Organotechnetium Compounds; D014326:Tropanes