Ga(III) chelates of amphiphilic DOTA-based ligands : synthetic route and in vitro and in vivo studies
| Main Author: | |
|---|---|
| Publication Date: | 2011 |
| Other Authors: | , , |
| Format: | Article |
| Language: | eng |
| Source: | Repositórios Científicos de Acesso Aberto de Portugal (RCAAP) |
| Download full: | https://hdl.handle.net/1822/14267 |
Summary: | In this work we report a synthetic strategy of amphiphilic DOTA-based chelators bearing a variable size α-alkyl chain at one of the pendant acetate arms (from six to fourteen carbon atoms), compatible with their covalent coupling to amine-bearing biomolecules. The amphiphilic behavior of the micelles-forming Ga(III) chelates (critical micelle concentration), their stability in blood serum and their lipophilicity (logP) were investigated. Biodistribution studies with the 67Ga-labeled chelates were performed in Wistar rats showing a predominant liver uptake with almost no traces of the radiochelates in the body after 24 hours. |
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Ga(III) chelates of amphiphilic DOTA-based ligands : synthetic route and in vitro and in vivo studiesDOTAGalliumAmphiphilicMicellesRadiopharmacyPETScience & TechnologyIn this work we report a synthetic strategy of amphiphilic DOTA-based chelators bearing a variable size α-alkyl chain at one of the pendant acetate arms (from six to fourteen carbon atoms), compatible with their covalent coupling to amine-bearing biomolecules. The amphiphilic behavior of the micelles-forming Ga(III) chelates (critical micelle concentration), their stability in blood serum and their lipophilicity (logP) were investigated. Biodistribution studies with the 67Ga-labeled chelates were performed in Wistar rats showing a predominant liver uptake with almost no traces of the radiochelates in the body after 24 hours.Fundação para a Ciência e a Tecnologia (FCT)ElsevierUniversidade do MinhoFontes, André Filipe Gomes SoaresPrata, M. Isabel M.Geraldes, Carlos F. G. C.André, João P.20112011-01-01T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttps://hdl.handle.net/1822/14267eng0969-805110.1016/j.nucmedbio.2010.10.00321492785http://www.elsevier.com/wps/find/journaldescription.cws_home/525482/descriptioninfo:eu-repo/semantics/openAccessreponame:Repositórios Científicos de Acesso Aberto de Portugal (RCAAP)instname:FCCN, serviços digitais da FCT – Fundação para a Ciência e a Tecnologiainstacron:RCAAP2025-04-12T04:23:27Zoai:repositorium.sdum.uminho.pt:1822/14267Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireinfo@rcaap.ptopendoar:https://opendoar.ac.uk/repository/71602025-05-28T15:06:28.667687Repositórios Científicos de Acesso Aberto de Portugal (RCAAP) - FCCN, serviços digitais da FCT – Fundação para a Ciência e a Tecnologiafalse |
| dc.title.none.fl_str_mv |
Ga(III) chelates of amphiphilic DOTA-based ligands : synthetic route and in vitro and in vivo studies |
| title |
Ga(III) chelates of amphiphilic DOTA-based ligands : synthetic route and in vitro and in vivo studies |
| spellingShingle |
Ga(III) chelates of amphiphilic DOTA-based ligands : synthetic route and in vitro and in vivo studies Fontes, André Filipe Gomes Soares DOTA Gallium Amphiphilic Micelles Radiopharmacy PET Science & Technology |
| title_short |
Ga(III) chelates of amphiphilic DOTA-based ligands : synthetic route and in vitro and in vivo studies |
| title_full |
Ga(III) chelates of amphiphilic DOTA-based ligands : synthetic route and in vitro and in vivo studies |
| title_fullStr |
Ga(III) chelates of amphiphilic DOTA-based ligands : synthetic route and in vitro and in vivo studies |
| title_full_unstemmed |
Ga(III) chelates of amphiphilic DOTA-based ligands : synthetic route and in vitro and in vivo studies |
| title_sort |
Ga(III) chelates of amphiphilic DOTA-based ligands : synthetic route and in vitro and in vivo studies |
| author |
Fontes, André Filipe Gomes Soares |
| author_facet |
Fontes, André Filipe Gomes Soares Prata, M. Isabel M. Geraldes, Carlos F. G. C. André, João P. |
| author_role |
author |
| author2 |
Prata, M. Isabel M. Geraldes, Carlos F. G. C. André, João P. |
| author2_role |
author author author |
| dc.contributor.none.fl_str_mv |
Universidade do Minho |
| dc.contributor.author.fl_str_mv |
Fontes, André Filipe Gomes Soares Prata, M. Isabel M. Geraldes, Carlos F. G. C. André, João P. |
| dc.subject.por.fl_str_mv |
DOTA Gallium Amphiphilic Micelles Radiopharmacy PET Science & Technology |
| topic |
DOTA Gallium Amphiphilic Micelles Radiopharmacy PET Science & Technology |
| description |
In this work we report a synthetic strategy of amphiphilic DOTA-based chelators bearing a variable size α-alkyl chain at one of the pendant acetate arms (from six to fourteen carbon atoms), compatible with their covalent coupling to amine-bearing biomolecules. The amphiphilic behavior of the micelles-forming Ga(III) chelates (critical micelle concentration), their stability in blood serum and their lipophilicity (logP) were investigated. Biodistribution studies with the 67Ga-labeled chelates were performed in Wistar rats showing a predominant liver uptake with almost no traces of the radiochelates in the body after 24 hours. |
| publishDate |
2011 |
| dc.date.none.fl_str_mv |
2011 2011-01-01T00:00:00Z |
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info:eu-repo/semantics/publishedVersion |
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info:eu-repo/semantics/article |
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article |
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publishedVersion |
| dc.identifier.uri.fl_str_mv |
https://hdl.handle.net/1822/14267 |
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https://hdl.handle.net/1822/14267 |
| dc.language.iso.fl_str_mv |
eng |
| language |
eng |
| dc.relation.none.fl_str_mv |
0969-8051 10.1016/j.nucmedbio.2010.10.003 21492785 http://www.elsevier.com/wps/find/journaldescription.cws_home/525482/description |
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openAccess |
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application/pdf |
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Elsevier |
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Elsevier |
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