Comparison of iodine-123 labelled 2 beta-carbomethoxy-3 beta-(4-iodophenyl)tropane and 2 beta-carbomethoxy-3 beta-(4-iodophenyl)-N-(3-fluoropropyl)nortropane for imaging of the dopamine transporter in the living human brain

Eur J Nucl Med. 1995 Apr;22(4):356-60. doi: 10.1007/BF00941854.

Abstract

Several cocaine congeners are of potential for imaging the dopamine transporter (DAT). Previous studies have shown that iodine-123 labelled 2 beta-carbomethoxy-3 beta-(4-iodophenyl)tropane ([123I] beta-CIT) is a promising radiotracer for imaging the serotonin (5-HT) and dopamine (DA) transporters in the living human brain with single-photon emission tomography (SPET). [123I] beta-CIT was found to be not very practical for 1-day DAT imaging protocols since peak DAT uptake occurs later than 8 h. Here we report a pilot comparison of [123I] beta-CIT and 2 beta-carbomethoxy-3 beta-(4-iodophenyl)-N-(3-fluoropropyl)nortropane ([123I] beta-CIT-FP), using SPET imaging in four healthy male subjects. Peak uptake of [123I] beta-CIT-FP into the basal ganglia occurred earlier (3-4 h after injection of tracer) than that of [123I] beta-CIT (> 8 h). However, the specific DAT binding of [123I] beta-CIT-FP in the basal ganglia was somewhat less (0.813 +/- 0.047) than that of [123I] beta-CIT (0.922 +/- 0.004). Imaging quality is excellent with both tracers and they are potentially of value for brain imaging in various neuropsychiatric disorders.

Publication types

  • Comparative Study

MeSH terms

  • Brain / diagnostic imaging*
  • Brain Chemistry
  • Carrier Proteins / analysis*
  • Cocaine / analogs & derivatives*
  • Dopamine / analysis*
  • Dopamine Plasma Membrane Transport Proteins
  • Humans
  • Iodine Radioisotopes*
  • Male
  • Membrane Glycoproteins*
  • Membrane Transport Proteins*
  • Middle Aged
  • Nerve Tissue Proteins*
  • Pilot Projects
  • Radionuclide Imaging
  • Time Factors
  • Tissue Distribution
  • Tropanes*

Substances

  • Carrier Proteins
  • Dopamine Plasma Membrane Transport Proteins
  • Iodine Radioisotopes
  • Membrane Glycoproteins
  • Membrane Transport Proteins
  • Nerve Tissue Proteins
  • SLC6A3 protein, human
  • Tropanes
  • 2-carbomethoxy-8-(3-fluoropropyl)-3-(4-iodophenyl)tropane
  • 2beta-carbomethoxy-3beta-(4-iodophenyl)tropane
  • Cocaine
  • Dopamine