Design of a multivalent bifunctional chelator for diagnostic 64Cu PET imaging in Alzheimer's disease.
Proc Natl Acad Sci U S A
; 117(49): 30928-30933, 2020 12 08.
Article
em En
| MEDLINE
| ID: mdl-33234563
Herein, we report a 64Cu positron emission tomography (PET) imaging agent that shows appreciable in vivo brain uptake and exhibits high specific affinity for beta-amyloid (Aß) aggregates, leading to the successful PET imaging of amyloid plaques in the brains of 5xFAD mice versus those of wild-type mice. The employed approach uses a bifunctional chelator with two Aß-interacting fragments that dramatically improves the Aß-binding affinity and lipophilicity for favorable blood-brain barrier penetration, while the use of optimized-length spacers between the Cu-chelating group and the Aß-interacting fragments further improves the in vivo Aß-binding specificity and brain uptake of the corresponding 64Cu PET imaging agent.
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Base de dados:
MEDLINE
Assunto principal:
Radioisótopos de Cobre
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Quelantes
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Tomografia por Emissão de Pósitrons
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Doença de Alzheimer
Tipo de estudo:
Diagnostic_studies
Limite:
Animals
Idioma:
En
Ano de publicação:
2020
Tipo de documento:
Article