Scandium(III) complexes of monophosphorus acid DOTA analogues: a thermodynamic and radiolabelling study with Sc-44 from cyclotron and from a Ti-44/Sc-44 generator
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11310%2F16%3A10323193" target="_blank" >RIV/00216208:11310/16:10323193 - isvavai.cz</a>
Result on the web
<a href="http://dx.doi.org/10.1039/c5dt04084a" target="_blank" >http://dx.doi.org/10.1039/c5dt04084a</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1039/c5dt04084a" target="_blank" >10.1039/c5dt04084a</a>
Alternative languages
Result language
angličtina
Original language name
Scandium(III) complexes of monophosphorus acid DOTA analogues: a thermodynamic and radiolabelling study with Sc-44 from cyclotron and from a Ti-44/Sc-44 generator
Original language description
The complexation ability of DOTA analogs bearing one methylenephosphonic (DO3AP) or methylene-phosphinic (DO3AP(PrA) and DO3A(PA3n)) acid pendant arm toward scandium was evaluated. Stability constants of their scandium(iii) complexes were determined by potentiometry combined with Sc-45 NMR spectroscopy. The stability constants of the monophosphinate analogues are somewhat lower than that of the Sc-DOTA complex. The phosphorus acid moiety interacts with trivalent scandium even in very acidic solutions forming out-of-cage complexes; the strong affinity of the phosphonate group to Sc(iii) precludes stability constant determination of the Sc-DO3AP complex. These results were compared with those obtained by the free-ion selective radiotracer extraction (FISRE) method which is suitable for trace concentrations. FISRE underestimated the stability constants but their relative order was preserved. Nonetheless, as this method is experimentally simple, it is suitable for a quick relative comparison of stability constant values under trace concentrations. Radiolabelling of the ligands with Sc-44 was performed using the radioisotope from two sources, a Ti-44/Sc-44 generator and 44(m)Sc/Sc-44 from a cyclotron. The best radio labelling conditions for the ligands were pH = 4, 70 degrees C and 20 min which were, however, not superior to those of the parent DOTA. Nonetheless, in vitro behaviour of the Sc(iii) complexes in the presence of hydroxyapatite and rat serum showed sufficient stability of "Sc complexes of these ligands for in vivo applications. PET images and ex vivo biodistribution of the Sc-44-DO3AP complex performed on healthy Wistar male rats showed no specific bone uptake and rapid clearance through urine.
Czech name
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Czech description
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Classification
Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
CA - Inorganic chemistry
OECD FORD branch
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Result continuities
Project
<a href="/en/project/GA13-08336S" target="_blank" >GA13-08336S: Hybrid materials based on macrocyclic ligands for medical applications</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)
Others
Publication year
2016
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
45
Issue of the periodical within the volume
4
Country of publishing house
GB - UNITED KINGDOM
Number of pages
12
Pages from-to
1398-1409
UT code for WoS article
000369088000018
EID of the result in the Scopus database
2-s2.0-84955588106