A rigidified AAZTA‐like ligand as efficient chelator for 68 Ga radiopharmaceuticals Article Swipe
Adrienn Vágner
,
Calogero D’Alessandria
,
G Gambino
,
Markus Schwaiger
,
Silvio Aime
,
Alessandro Maiocchi
,
Imre Tóth
,
Zsolt Baranyai
,
Lorenzo Tei
·
YOU?
·
· 2016
· Open Access
·
· DOI: https://doi.org/10.1002/slct.201500051
YOU?
·
· 2016
· Open Access
·
· DOI: https://doi.org/10.1002/slct.201500051
The new cyclohexane‐fused CyAAZTA ligand was synthesized to increase the structural rigidity of the heptadentate chelator AAZTA with the aim of improving the overall stability of its Ga III complex. The stability constant of Ga(CyAAZTA) − , determined both by pH‐potentiometry (log K GaL =21.39) and by 71 Ga NMR (log K GaL =21.92), was found similar to that of GaAAZTA (log K GaL =22.18). The kinetic inertness of Ga(CyAAZTA) − was investigated by following its transmetallation and ligand exchange reactions with Cu 2+ and human serum transferrin, respectively. The formation of a hydroxido‐complex near pH 7 decreases the half‐life ( t 1/2 ) of the dissociation reactions for Ga(CyAAZTA) − compared to Ga(AAZTA) − (8.5 h vs 21 h, pH 7.4). However, at pH < 7 the t 1/2 of Ga(CyAAZTA) − is much longer (234 h at pH 6). Finally, CyAAZTA was successfully radiolabelled with 68 Ga in acetate buffer at pH 3.8, in 15 minutes at room temperature at [CyAAZTA]=10 μM, with a labelling yield higher than 80 %. A 1 μM solution of CyAAZTA was successfully labelled (L.Y.: 97.4 %) in 5 minutes at 90 °C. Stability tests in human serum and in the presence of 50 mM DTPA showed no significant decomposition of 68 GaCyAAZTA over 90 minutes.
Related Topics
Concepts
Chemistry
Ligand (biochemistry)
Chelation
Transferrin
Dissociation (chemistry)
Cyclohexane
Decomposition
Yield (engineering)
Transmetalation
Nuclear chemistry
Medicinal chemistry
Radiochemistry
Inorganic chemistry
Physical chemistry
Catalysis
Receptor
Organic chemistry
Materials science
Biochemistry
Metallurgy
Metadata
- Type
- article
- Language
- en
- Landing Page
- https://doi.org/10.1002/slct.201500051
- OA Status
- green
- Cited By
- 24
- References
- 45
- Related Works
- 10
- OpenAlex ID
- https://openalex.org/W2556557646
All OpenAlex metadata
Raw OpenAlex JSON
- OpenAlex ID
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https://openalex.org/W2556557646Canonical identifier for this work in OpenAlex
- DOI
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https://doi.org/10.1002/slct.201500051Digital Object Identifier
- Title
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A rigidified AAZTA‐like ligand as efficient chelator for 68 Ga radiopharmaceuticalsWork title
- Type
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articleOpenAlex work type
- Language
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enPrimary language
- Publication year
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2016Year of publication
- Publication date
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2016-02-01Full publication date if available
- Authors
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Adrienn Vágner, Calogero D’Alessandria, G Gambino, Markus Schwaiger, Silvio Aime, Alessandro Maiocchi, Imre Tóth, Zsolt Baranyai, Lorenzo TeiList of authors in order
- Landing page
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https://doi.org/10.1002/slct.201500051Publisher landing page
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YesWhether a free full text is available
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greenOpen access status per OpenAlex
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https://hdl.handle.net/2437/234761Direct OA link when available
- Concepts
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Chemistry, Ligand (biochemistry), Chelation, Transferrin, Dissociation (chemistry), Cyclohexane, Decomposition, Yield (engineering), Transmetalation, Nuclear chemistry, Medicinal chemistry, Radiochemistry, Inorganic chemistry, Physical chemistry, Catalysis, Receptor, Organic chemistry, Materials science, Biochemistry, MetallurgyTop concepts (fields/topics) attached by OpenAlex
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24Total citation count in OpenAlex
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2025: 4, 2024: 5, 2023: 2, 2022: 2, 2021: 2Per-year citation counts (last 5 years)
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45Number of works referenced by this work
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10Other works algorithmically related by OpenAlex
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