Radiosynthesis and in vivo evaluation of a 18F-labelled styryl-benzoxazole derivative for β-amyloid targeting

Detalhes bibliográficos
Autor(a) principal: Morais, G. Ribeiro
Data de Publicação: 2013
Outros Autores: Gano, L., Kniess, T., Bergmann, R., Abrunhosa, A., Santos, I., Paulo, A.
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: http://hdl.handle.net/10316/27724
https://doi.org/10.1016/j.apradiso.2013.07.003
Resumo: The formation of β-amyloid deposits is considered a histopathological feature of Alzheimer′s disease (AD). In vivo molecular imaging by means of amyloid-avid radiotracers will allow for an early and conclusive diagnostic of AD. Herein, we describe the radiosynthesis of the radiofluorinated styryl benzoxazole derivative [18F]-[2-[N-methyl-N-(2′-fluoroethyl)-4′-aminostyryl]benzoxazole] ([18F]-1) and its pre-clinical evaluation, including metabolic and biodistribution studies in male Wistar rats. The in vivo biological evaluation of [18F]-1 showed that this new radiotracer has a moderate brain uptake with a slow brain washout and a poor in vivo stability.
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spelling Radiosynthesis and in vivo evaluation of a 18F-labelled styryl-benzoxazole derivative for β-amyloid targetingAlzheimer′s Diseaseβ-Amyloid aggregationMolecular imagingFluorine-18The formation of β-amyloid deposits is considered a histopathological feature of Alzheimer′s disease (AD). In vivo molecular imaging by means of amyloid-avid radiotracers will allow for an early and conclusive diagnostic of AD. Herein, we describe the radiosynthesis of the radiofluorinated styryl benzoxazole derivative [18F]-[2-[N-methyl-N-(2′-fluoroethyl)-4′-aminostyryl]benzoxazole] ([18F]-1) and its pre-clinical evaluation, including metabolic and biodistribution studies in male Wistar rats. The in vivo biological evaluation of [18F]-1 showed that this new radiotracer has a moderate brain uptake with a slow brain washout and a poor in vivo stability.Elsevier2013-12info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://hdl.handle.net/10316/27724http://hdl.handle.net/10316/27724https://doi.org/10.1016/j.apradiso.2013.07.003engMORAIS, G. Ribeiro [et. al] - Radiosynthesis and in vivo evaluation of a 18F-labelled styryl-benzoxazole derivative for β-amyloid targeting. "Applied Radiation and Isotopes". ISSN 0969-8043. Vol. 82 (2013) p. 100-1040969-8043http://www.sciencedirect.com/science/article/pii/S0969804313002923Morais, G. RibeiroGano, L.Kniess, T.Bergmann, R.Abrunhosa, A.Santos, I.Paulo, A.info:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2020-05-29T09:42:29Zoai:estudogeral.uc.pt:10316/27724Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T20:53:40.176573Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse
dc.title.none.fl_str_mv Radiosynthesis and in vivo evaluation of a 18F-labelled styryl-benzoxazole derivative for β-amyloid targeting
title Radiosynthesis and in vivo evaluation of a 18F-labelled styryl-benzoxazole derivative for β-amyloid targeting
spellingShingle Radiosynthesis and in vivo evaluation of a 18F-labelled styryl-benzoxazole derivative for β-amyloid targeting
Morais, G. Ribeiro
Alzheimer′s Disease
β-Amyloid aggregation
Molecular imaging
Fluorine-18
title_short Radiosynthesis and in vivo evaluation of a 18F-labelled styryl-benzoxazole derivative for β-amyloid targeting
title_full Radiosynthesis and in vivo evaluation of a 18F-labelled styryl-benzoxazole derivative for β-amyloid targeting
title_fullStr Radiosynthesis and in vivo evaluation of a 18F-labelled styryl-benzoxazole derivative for β-amyloid targeting
title_full_unstemmed Radiosynthesis and in vivo evaluation of a 18F-labelled styryl-benzoxazole derivative for β-amyloid targeting
title_sort Radiosynthesis and in vivo evaluation of a 18F-labelled styryl-benzoxazole derivative for β-amyloid targeting
author Morais, G. Ribeiro
author_facet Morais, G. Ribeiro
Gano, L.
Kniess, T.
Bergmann, R.
Abrunhosa, A.
Santos, I.
Paulo, A.
author_role author
author2 Gano, L.
Kniess, T.
Bergmann, R.
Abrunhosa, A.
Santos, I.
Paulo, A.
author2_role author
author
author
author
author
author
dc.contributor.author.fl_str_mv Morais, G. Ribeiro
Gano, L.
Kniess, T.
Bergmann, R.
Abrunhosa, A.
Santos, I.
Paulo, A.
dc.subject.por.fl_str_mv Alzheimer′s Disease
β-Amyloid aggregation
Molecular imaging
Fluorine-18
topic Alzheimer′s Disease
β-Amyloid aggregation
Molecular imaging
Fluorine-18
description The formation of β-amyloid deposits is considered a histopathological feature of Alzheimer′s disease (AD). In vivo molecular imaging by means of amyloid-avid radiotracers will allow for an early and conclusive diagnostic of AD. Herein, we describe the radiosynthesis of the radiofluorinated styryl benzoxazole derivative [18F]-[2-[N-methyl-N-(2′-fluoroethyl)-4′-aminostyryl]benzoxazole] ([18F]-1) and its pre-clinical evaluation, including metabolic and biodistribution studies in male Wistar rats. The in vivo biological evaluation of [18F]-1 showed that this new radiotracer has a moderate brain uptake with a slow brain washout and a poor in vivo stability.
publishDate 2013
dc.date.none.fl_str_mv 2013-12
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://hdl.handle.net/10316/27724
http://hdl.handle.net/10316/27724
https://doi.org/10.1016/j.apradiso.2013.07.003
url http://hdl.handle.net/10316/27724
https://doi.org/10.1016/j.apradiso.2013.07.003
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv MORAIS, G. Ribeiro [et. al] - Radiosynthesis and in vivo evaluation of a 18F-labelled styryl-benzoxazole derivative for β-amyloid targeting. "Applied Radiation and Isotopes". ISSN 0969-8043. Vol. 82 (2013) p. 100-104
0969-8043
http://www.sciencedirect.com/science/article/pii/S0969804313002923
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.publisher.none.fl_str_mv Elsevier
publisher.none.fl_str_mv Elsevier
dc.source.none.fl_str_mv reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
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repository.name.fl_str_mv Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
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