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

Kód výsledku v 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>

Výsledek na webu

<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>

Jazyk výsledku

angličtina

Název v původním jazyce

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

Popis výsledku v původním jazyce

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.

Název v anglickém jazyce

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

Popis výsledku anglicky

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.

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

CA - Anorganická chemie

OECD FORD obor

—

Projekt

<a href="/cs/project/GA13-08336S" target="_blank" >GA13-08336S: Hybridní materiály založené na makrocyklických ligandech pro využití v medicíně</a><br>

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Rok uplatnění

2016

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Dalton Transactions

ISSN

1477-9226

e-ISSN

—

Svazek periodika

45

Číslo periodika v rámci svazku

4

Stát vydavatele periodika

GB - Spojené království Velké Británie a Severního Irska

Počet stran výsledku

12

Strana od-do

1398-1409

Kód UT WoS článku

000369088000018

EID výsledku v databázi Scopus

2-s2.0-84955588106