Synthesis and biological evaluation of a technetium-99m(I)-tricarbonyl-labelled phenyltropane derivative

Bioorg Med Chem Lett. 2006 Jan 15;16(2):382-6. doi: 10.1016/j.bmcl.2005.09.071. Epub 2005 Nov 3.

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.

MeSH terms

  • Animals
  • Brain / drug effects
  • Brain / metabolism
  • Drug Evaluation, Preclinical
  • In Vitro Techniques
  • Isotope Labeling
  • Mice
  • Molecular Conformation
  • Organotechnetium Compounds / chemistry*
  • Structure-Activity Relationship
  • Tissue Distribution
  • Tropanes / chemical synthesis*
  • Tropanes / chemistry
  • Tropanes / pharmacokinetics*

Substances

  • Organotechnetium Compounds
  • Tropanes