About: Comparison of different phosphorus-containing ligands complexing Ga-68 for PET-imaging of bone metabolism     Goto   Sponge   NotDistinct   Permalink

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Description
  • Tc-99m-phosphonate structures are well established tracers for bone tumour imaging. Our objective was to investigate different Ga-68-labelled phosphonate ligands concerning labelling kinetics, binding to hydroxyapatite and bone imaging using mu-PET. Seven macrocyclic phosphorus-containing ligands and EDTMP were labelled in nanomolar scale with n.c.a. Ga-68 in Na-HEPES buffer at pH similar to 4. Except for DOTP, all ligands were labelled with } 92% yield. Binding of the Ga-68-ligand complexes on hydroxyapatite was analysed to evaluate the effect of the number of the phosphorus acid groups on adsorption parameters. Adsorption of Ga-68-EDTMP and Ga-68-DOTP was } 83%. For the Ga-68-NOTA-phosphonates an increasing binding with increasing number of phosphonate groups was observed but was still lower than Ga-68-DOTP and Ga-68-EDTMP. mu-PET studies in vivo were performed with Ga-68-EDTMP and Ga-68-DOTP with Wistar rats. While Ga-68-EDTMP-PET showed uptake on bone structures, an excess amount of the ligand (} 1.5 mg EDTMP/kg body weight) had to be used, otherwise the Ga-68(3+) a is released from the complex and forms gallium hydroxide or it is transchelated to Ga-68-transferrin. As a result, the main focus of further phosphonate structures has to be on complex formation in high radiochemical yields with macrocyclic ligands with phosphonate groups that are not required for complexing Ga-68.
  • Tc-99m-phosphonate structures are well established tracers for bone tumour imaging. Our objective was to investigate different Ga-68-labelled phosphonate ligands concerning labelling kinetics, binding to hydroxyapatite and bone imaging using mu-PET. Seven macrocyclic phosphorus-containing ligands and EDTMP were labelled in nanomolar scale with n.c.a. Ga-68 in Na-HEPES buffer at pH similar to 4. Except for DOTP, all ligands were labelled with } 92% yield. Binding of the Ga-68-ligand complexes on hydroxyapatite was analysed to evaluate the effect of the number of the phosphorus acid groups on adsorption parameters. Adsorption of Ga-68-EDTMP and Ga-68-DOTP was } 83%. For the Ga-68-NOTA-phosphonates an increasing binding with increasing number of phosphonate groups was observed but was still lower than Ga-68-DOTP and Ga-68-EDTMP. mu-PET studies in vivo were performed with Ga-68-EDTMP and Ga-68-DOTP with Wistar rats. While Ga-68-EDTMP-PET showed uptake on bone structures, an excess amount of the ligand (} 1.5 mg EDTMP/kg body weight) had to be used, otherwise the Ga-68(3+) a is released from the complex and forms gallium hydroxide or it is transchelated to Ga-68-transferrin. As a result, the main focus of further phosphonate structures has to be on complex formation in high radiochemical yields with macrocyclic ligands with phosphonate groups that are not required for complexing Ga-68. (en)
Title
  • Comparison of different phosphorus-containing ligands complexing Ga-68 for PET-imaging of bone metabolism
  • Comparison of different phosphorus-containing ligands complexing Ga-68 for PET-imaging of bone metabolism (en)
skos:prefLabel
  • Comparison of different phosphorus-containing ligands complexing Ga-68 for PET-imaging of bone metabolism
  • Comparison of different phosphorus-containing ligands complexing Ga-68 for PET-imaging of bone metabolism (en)
skos:notation
  • RIV/00216208:11310/11:10089979!RIV12-MSM-11310___
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • Z(MSM0021620857)
http://linked.open...iv/cisloPeriodika
  • 1
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
http://linked.open.../riv/druhVysledku
http://linked.open...iv/duvernostUdaju
http://linked.open...titaPredkladatele
http://linked.open...dnocenehoVysledku
  • 191104
http://linked.open...ai/riv/idVysledku
  • RIV/00216208:11310/11:10089979
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • protonation; hydroxyapatite; pre-vivo; pain palliation; potential agent; nuclear magnetic-resonance (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • DE - Spolková republika Německo
http://linked.open...ontrolniKodProRIV
  • [1B6860BA882B]
http://linked.open...i/riv/nazevZdroje
  • Radiochimica Acta
http://linked.open...in/vavai/riv/obor
http://linked.open...ichTvurcuVysledku
http://linked.open...cetTvurcuVysledku
http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 99
http://linked.open...iv/tvurceVysledku
  • Fellner, M.
  • Geraldes, Carlos F. G. C.
  • Kovacs, Z.
  • Loktionova, N. S.
  • Lukeš, Ivan
  • Riss, P.
  • Rösch, Frank
  • Thews, O.
  • Zhernosekov, K. P.
http://linked.open...ain/vavai/riv/wos
  • 000286917000007
http://linked.open...n/vavai/riv/zamer
issn
  • 0033-8230
number of pages
http://bibframe.org/vocab/doi
  • 10.1524/ract.2011.1791
http://localhost/t...ganizacniJednotka
  • 11310
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