The Influence of the Combination of Carboxylate and Phosphinate Pendant Arms in 1,4,7-Triazacyclononane-Based Chelators on Their 68Ga Labelling Properties

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11310%2F15%3A10319182" target="_blank" >RIV/00216208:11310/15:10319182 - isvavai.cz</a>

Výsledek na webu

<a href="http://dx.doi.org/10.3390/molecules200713112" target="_blank" >http://dx.doi.org/10.3390/molecules200713112</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.3390/molecules200713112" target="_blank" >10.3390/molecules200713112</a>

Jazyk výsledku

angličtina

Název v původním jazyce

The Influence of the Combination of Carboxylate and Phosphinate Pendant Arms in 1,4,7-Triazacyclononane-Based Chelators on Their 68Ga Labelling Properties

Popis výsledku v původním jazyce

In order to compare the coordination properties of 1,4,7-triazacyclononane (tacn) derivatives bearing varying numbers of phosphinic/ carboxylic acid pendant groups towards Ga-68, 1,4,7-triazacyclononane-7-acetic-1,4-bis(methylenephosphinic) acid (NOPA) and 1,4,7triazacyclononane-4,7-diacetic-1-[methylene(2-carboxyethyl) phosphinic] acid (NO2AP) were synthesized using Mannich reactions with trivalent or pentavalent forms of H-phosphinic acids as phosphorus components. Stepwise protonation constants logK(1-3) 12.06, 3.90 and 1.95, and stability constants with Ga-III and Cu-II, logK(GaL) 24.01 and logK(CuL) 16.66, were potentiometrically determined for NOPA. Both ligands were labelled with Ga-68 and compared with NOTA (tacn-N, N', N ''-triacetic acid) andNOPO, a TRAP-type [tacn-N, N', N ''-tris( methylenephosphinic acid)] chelator. At pH 3, NOPO and NOPA showed higher labelling efficiency (binding with lower ligand excess) at both room temperature and 95 degrees C, compared to NO2AP and

Název v anglickém jazyce

The Influence of the Combination of Carboxylate and Phosphinate Pendant Arms in 1,4,7-Triazacyclononane-Based Chelators on Their 68Ga Labelling Properties

Popis výsledku anglicky

In order to compare the coordination properties of 1,4,7-triazacyclononane (tacn) derivatives bearing varying numbers of phosphinic/ carboxylic acid pendant groups towards Ga-68, 1,4,7-triazacyclononane-7-acetic-1,4-bis(methylenephosphinic) acid (NOPA) and 1,4,7triazacyclononane-4,7-diacetic-1-[methylene(2-carboxyethyl) phosphinic] acid (NO2AP) were synthesized using Mannich reactions with trivalent or pentavalent forms of H-phosphinic acids as phosphorus components. Stepwise protonation constants logK(1-3) 12.06, 3.90 and 1.95, and stability constants with Ga-III and Cu-II, logK(GaL) 24.01 and logK(CuL) 16.66, were potentiometrically determined for NOPA. Both ligands were labelled with Ga-68 and compared with NOTA (tacn-N, N', N ''-triacetic acid) andNOPO, a TRAP-type [tacn-N, N', N ''-tris( methylenephosphinic acid)] chelator. At pH 3, NOPO and NOPA showed higher labelling efficiency (binding with lower ligand excess) at both room temperature and 95 degrees C, compared to NO2AP and

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

S - Specificky vyzkum na vysokych skolach<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2015

Kód důvěrnosti údajů

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

Název periodika

Molecules

ISSN

1420-3049

e-ISSN

—

Svazek periodika

20

Číslo periodika v rámci svazku

7

Stát vydavatele periodika

CH - Švýcarská konfederace

Počet stran výsledku

15

Strana od-do

13112-13126

Kód UT WoS článku

000368695400089

EID výsledku v databázi Scopus

2-s2.0-84938375640