Amino acid based gallium-68 chelators capable of radiolabeling at neutral pH

Kód výsledku v 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>

Výsledek na webu

<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>

Jazyk výsledku

angličtina

Název v původním jazyce

Amino acid based gallium-68 chelators capable of radiolabeling at neutral pH

Popis výsledku v původním jazyce

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.

Název v anglickém jazyce

Amino acid based gallium-68 chelators capable of radiolabeling at neutral pH

Popis výsledku anglicky

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.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

10402 - Inorganic and nuclear chemistry

Projekt

—

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2017

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

46

Číslo periodika v rámci svazku

48

Stát vydavatele periodika

GB - Spojené království Velké Británie a Severního Irska

Počet stran výsledku

10

Strana od-do

16973-16982

Kód UT WoS článku

000417846200029

EID výsledku v databázi Scopus

2-s2.0-85038237529