NODAPA-OH and NODAPA-(NCS)n: synthesis, 68Ga-radiolabelling and in vitro characterisation of novel versatile bifunctional chelators for molecular imaging

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5364-7. doi: 10.1016/j.bmcl.2008.09.054. Epub 2008 Sep 18.

Abstract

This report concerns synthesis, (68)Ga-radiolabelling and stability data of 1,4,7-triazacyclononane-1,4-diacetic acid-7-p-isothio-cyanatophenyl-acetic acid (NODAPA-NCS), 1,4,7-triazacyclononane-1-acetic acid-4,7-di-p-isothiocyanatophenyl-acetic acid (NODAPA-(NCS)(2)) and 1,4,7-triazacyclononane-1,4-diacetic acid-7-p-hydroxyphenyl-acetic acid (NODAPA-OH), versatile bifunctional chelators with potential for molecular imaging. Protein binding and exemplified conjugation are also reported.

MeSH terms

  • Chelating Agents / chemical synthesis
  • Chelating Agents / chemistry
  • Chelating Agents / pharmacology*
  • Chemistry, Pharmaceutical / methods*
  • Drug Design
  • Gallium Radioisotopes / chemistry*
  • Heterocyclic Compounds / chemistry
  • Heterocyclic Compounds, 1-Ring / chemical synthesis*
  • Hydrogen-Ion Concentration
  • In Vitro Techniques
  • Isotope Labeling / methods
  • Models, Chemical
  • Phenylacetates / chemistry
  • Positron-Emission Tomography / instrumentation*
  • Positron-Emission Tomography / methods
  • Radioisotopes / chemistry*

Substances

  • 1,4,7-triazacyclononane-1,4-diacetic acid-7-p-hydroxyphenylacetic acid
  • 1,4,7-triazacyclononane-1,4-diacetic acid-7-p-isothiocyanatophenylacetic acid
  • 1,4,7-triazacyclononane-1-acetic acid-4,7-di-p-isothiocyanatophenylacetic acid
  • Chelating Agents
  • Gallium Radioisotopes
  • Heterocyclic Compounds
  • Heterocyclic Compounds, 1-Ring
  • Phenylacetates
  • Radioisotopes
  • 1,4,7-triazacyclononane-N,N',N''-triacetic acid