Jump to main content
Jump to site search


Amino acid based gallium-68 chelators capable of radiolabeling at neutral pH

Author affiliations

Abstract

Gallium-68 (68Ga) has been the subject of increasing interest for its potential in the production of radiotracers for diagnosis of diseases. In this work we report the complexation of 68Ga by the amino acid based tripodal chelate H3Dpaa, and two bifunctional derivatives, H3Dpaa.dab and H4Dpaa.ga, under a range of conditions with particular emphasis on the rapid complexation of 68Ga at pH 7.4. 100 μM H3Dpaa achieved a radiochemical yield of 95% at pH 7.4 in 5 minutes at 37 °C. The bifunctional derivatives H4Dpaa.ga and H3Dpaa.dab achieved 94% and 84% radiochemical yields, respectively, under the same conditions. The resulting Ga(III) complexes show thermodynamic stabilities of log KGaDpaa = 18.53, log KGaDpaa.dab = 22.08, log KGaDpaa.ga = 18.36. Unfortunately, the resulting radiolabelled species do not present sufficient serum stability for in vivo application. Herein we show a flexible synthesis for bifunctional chelators based on amino acids that rapidly complex 68Ga under physiological conditions.

Graphical abstract: Amino acid based gallium-68 chelators capable of radiolabeling at neutral pH

Back to tab navigation

Supplementary files

Publication details

The article was received on 12 Sep 2017, accepted on 16 Nov 2017 and first published on 17 Nov 2017


Article type: Paper
DOI: 10.1039/C7DT03398B
Citation: Dalton Trans., 2017, Advance Article
  •   Request permissions

    Amino acid based gallium-68 chelators capable of radiolabeling at neutral pH

    T. W. Price, J. Gallo, V. Kubíček, Z. Böhmová, T. J. Prior, J. Greenman, P. Hermann and G. J. Stasiuk, Dalton Trans., 2017, Advance Article , DOI: 10.1039/C7DT03398B

Search articles by author

Spotlight

Advertisements