Amino acid based gallium-68 chelators capable of radiolabeling at neutral pH
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11310%2F17%3A10366436" target="_blank" >RIV/00216208:11310/17:10366436 - isvavai.cz</a>
Result on the web
<a href="http://dx.doi.org/10.1039/c7dt03398b" target="_blank" >http://dx.doi.org/10.1039/c7dt03398b</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1039/c7dt03398b" target="_blank" >10.1039/c7dt03398b</a>
Alternative languages
Result language
angličtina
Original language name
Amino acid based gallium-68 chelators capable of radiolabeling at neutral pH
Original language description
Gallium-68 (Ga-68) has been the subject of increasing interest for its potential in the production of radio-tracers for diagnosis of diseases. In this work we report the complexation of Ga-68 by the amino acid based tripodal chelate H(3)Dpaa, 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 mu M H3Dpaa achieved a radiochemical yield of 95% at pH 7.4 in 5 minutes at 37 degrees C. The bifunctional derivatives H(4)Dpaa.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 K-GaDpaa = 18.53, log K-GaDpaa.dab = 22.08, log K-GaDpaa.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 Ga-68 under physiological conditions.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10402 - Inorganic and nuclear chemistry
Result continuities
Project
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Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2017
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Dalton Transactions
ISSN
1477-9226
e-ISSN
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Volume of the periodical
46
Issue of the periodical within the volume
48
Country of publishing house
GB - UNITED KINGDOM
Number of pages
10
Pages from-to
16973-16982
UT code for WoS article
000417846200029
EID of the result in the Scopus database
2-s2.0-85038237529