Jump to main content
Jump to site search

Issue 48, 2017
Previous Article Next Article

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., 2017,46, 16973-16982
  • Open access: Creative Commons BY-NC license
  •   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, 46, 16973
    DOI: 10.1039/C7DT03398B

    This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence. Material from this article can be used in other publications provided that the correct acknowledgement is given with the reproduced material and it is not used for commercial purposes.

    Reproduced material should be attributed as follows:

    • For reproduction of material from NJC:
      [Original citation] - Published by The Royal Society of Chemistry (RSC) on behalf of the Centre National de la Recherche Scientifique (CNRS) and the RSC.
    • For reproduction of material from PCCP:
      [Original citation] - Published by the PCCP Owner Societies.
    • For reproduction of material from PPS:
      [Original citation] - Published by The Royal Society of Chemistry (RSC) on behalf of the European Society for Photobiology, the European Photochemistry Association, and RSC.
    • For reproduction of material from all other RSC journals:
      [Original citation] - Published by The Royal Society of Chemistry.

    Information about reproducing material from RSC articles with different licences is available on our Permission Requests page.

Search articles by author

Spotlight

Advertisements