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Radiolabeling of DOTA-like conjugated peptides with generator-produced (68)Ga and using NaCl-based cationic elution method
Gallium-68 ((68)Ga) is a generator-produced radionuclide with a short half-life (t(½) = 68 min) that is particularly well suited for molecular imaging by positron emission tomography (PET). Methods have been developed to synthesize (68)Ga-labeled imaging agents possessing certain drawbacks, such as...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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2016
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5506837/ https://www.ncbi.nlm.nih.gov/pubmed/27172166 http://dx.doi.org/10.1038/nprot.2016.060 |
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author | Mueller, Dirk Breeman, Wouter A P Klette, Ingo Gottschaldt, Michael Odparlik, Andreas Baehre, Manfred Tworowska, Izabela Schultz, Michael K |
author_facet | Mueller, Dirk Breeman, Wouter A P Klette, Ingo Gottschaldt, Michael Odparlik, Andreas Baehre, Manfred Tworowska, Izabela Schultz, Michael K |
author_sort | Mueller, Dirk |
collection | PubMed |
description | Gallium-68 ((68)Ga) is a generator-produced radionuclide with a short half-life (t(½) = 68 min) that is particularly well suited for molecular imaging by positron emission tomography (PET). Methods have been developed to synthesize (68)Ga-labeled imaging agents possessing certain drawbacks, such as longer synthesis time because of a required final purification step, the use of organic solvents or concentrated hydrochloric acid (HCl). In our manuscript, we provide a detailed protocol for the use of an advantageous sodium chloride (NaCl)-based method for radiolabeling of chelator-modified peptides for molecular imaging. By working in a lead-shielded hot-cell system, (68)Ga(3+) of the generator eluate is trapped on a cation exchanger cartridge (100 mg, ∼8 mm long and 5 mm diameter) and then eluted with acidified 5 M NaCl solution directly into a sodium acetate-buffered solution containing a DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) or DOTA-like chelator-modified peptide. The main advantages of this procedure are the high efficiency and the absence of organic solvents. It can be applied to a variety of peptides, which are stable in 1 M NaCl solution at a pH value of 3–4 during reaction. After labeling, neutralization, sterile filtration and quality control (instant thin-layer chromatography (iTLC), HPLC and pH), the radiopharmaceutical can be directly administered to patients, without determination of organic solvents, which reduces the overall synthesis-to-release time. This procedure has been adapted easily to automated synthesis modules, which leads to a rapid preparation of (68)Ga radiopharmaceuticals (12–16 min). |
format | Online Article Text |
id | pubmed-5506837 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2016 |
record_format | MEDLINE/PubMed |
spelling | pubmed-55068372017-07-12 Radiolabeling of DOTA-like conjugated peptides with generator-produced (68)Ga and using NaCl-based cationic elution method Mueller, Dirk Breeman, Wouter A P Klette, Ingo Gottschaldt, Michael Odparlik, Andreas Baehre, Manfred Tworowska, Izabela Schultz, Michael K Nat Protoc Article Gallium-68 ((68)Ga) is a generator-produced radionuclide with a short half-life (t(½) = 68 min) that is particularly well suited for molecular imaging by positron emission tomography (PET). Methods have been developed to synthesize (68)Ga-labeled imaging agents possessing certain drawbacks, such as longer synthesis time because of a required final purification step, the use of organic solvents or concentrated hydrochloric acid (HCl). In our manuscript, we provide a detailed protocol for the use of an advantageous sodium chloride (NaCl)-based method for radiolabeling of chelator-modified peptides for molecular imaging. By working in a lead-shielded hot-cell system, (68)Ga(3+) of the generator eluate is trapped on a cation exchanger cartridge (100 mg, ∼8 mm long and 5 mm diameter) and then eluted with acidified 5 M NaCl solution directly into a sodium acetate-buffered solution containing a DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) or DOTA-like chelator-modified peptide. The main advantages of this procedure are the high efficiency and the absence of organic solvents. It can be applied to a variety of peptides, which are stable in 1 M NaCl solution at a pH value of 3–4 during reaction. After labeling, neutralization, sterile filtration and quality control (instant thin-layer chromatography (iTLC), HPLC and pH), the radiopharmaceutical can be directly administered to patients, without determination of organic solvents, which reduces the overall synthesis-to-release time. This procedure has been adapted easily to automated synthesis modules, which leads to a rapid preparation of (68)Ga radiopharmaceuticals (12–16 min). 2016-05-12 2016-06 /pmc/articles/PMC5506837/ /pubmed/27172166 http://dx.doi.org/10.1038/nprot.2016.060 Text en http://creativecommons.org/licenses/by/2.0/ Reprints and permissions information is available online at http://www.nature.com/reprints/index.html. |
spellingShingle | Article Mueller, Dirk Breeman, Wouter A P Klette, Ingo Gottschaldt, Michael Odparlik, Andreas Baehre, Manfred Tworowska, Izabela Schultz, Michael K Radiolabeling of DOTA-like conjugated peptides with generator-produced (68)Ga and using NaCl-based cationic elution method |
title | Radiolabeling of DOTA-like conjugated peptides with generator-produced (68)Ga and using NaCl-based cationic elution method |
title_full | Radiolabeling of DOTA-like conjugated peptides with generator-produced (68)Ga and using NaCl-based cationic elution method |
title_fullStr | Radiolabeling of DOTA-like conjugated peptides with generator-produced (68)Ga and using NaCl-based cationic elution method |
title_full_unstemmed | Radiolabeling of DOTA-like conjugated peptides with generator-produced (68)Ga and using NaCl-based cationic elution method |
title_short | Radiolabeling of DOTA-like conjugated peptides with generator-produced (68)Ga and using NaCl-based cationic elution method |
title_sort | radiolabeling of dota-like conjugated peptides with generator-produced (68)ga and using nacl-based cationic elution method |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5506837/ https://www.ncbi.nlm.nih.gov/pubmed/27172166 http://dx.doi.org/10.1038/nprot.2016.060 |
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