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

Gallium-68 ( Ga) 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 Ga by the amino acid based tripodal chelate H Dpaa, and two bifunctional derivatives, H Dpaa.dab and H Dpaa.ga, under...

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Published in:Dalton transactions : an international journal of inorganic chemistry 2017, Vol.46 (48), p.16973-16982
Main Authors: Price, Thomas W, Gallo, Juan, Kubíček, Vojtěch, Böhmová, Zuzana, Prior, Timothy J, Greenman, John, Hermann, Petr, Stasiuk, Graeme J
Format: Article
Language:English
Subjects:
Amino acids
Chelates
Complexation
Derivatives
Gallium
Radiochemistry
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Summary:Gallium-68 ( Ga) 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 Ga by the amino acid based tripodal chelate H Dpaa, and two bifunctional derivatives, H Dpaa.dab and H Dpaa.ga, under a range of conditions with particular emphasis on the rapid complexation of Ga at pH 7.4. 100 μM H Dpaa achieved a radiochemical yield of 95% at pH 7.4 in 5 minutes at 37 °C. The bifunctional derivatives H Dpaa.ga and H Dpaa.dab achieved 94% and 84% radiochemical yields, respectively, under the same conditions. The resulting Ga(iii) complexes show thermodynamic stabilities of log K = 18.53, log K = 22.08, log K = 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 Ga under physiological conditions.
ISSN:1477-9226
1477-9234
DOI:10.1039/c7dt03398b