Technetium-99m labelled integrated tropane-BAT as a potential dopamine transporter tracer

Bioorg Med Chem. 2005 Feb 15;13(4):1053-8. doi: 10.1016/j.bmc.2004.11.036.

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.

MeSH terms

  • Animals
  • Chromatography, Liquid
  • Dopamine Plasma Membrane Transport Proteins
  • Magnetic Resonance Spectroscopy
  • Membrane Glycoproteins / chemistry*
  • Membrane Transport Proteins / chemistry*
  • Nerve Tissue Proteins / chemistry*
  • Organotechnetium Compounds / chemistry*
  • Radiometry
  • Rats
  • Spectrometry, Mass, Electrospray Ionization
  • Tropanes / chemistry*

Substances

  • Dopamine Plasma Membrane Transport Proteins
  • Membrane Glycoproteins
  • Membrane Transport Proteins
  • Nerve Tissue Proteins
  • Organotechnetium Compounds
  • Tropanes