Strategies for designing novel positron emission tomography (PET) radiotracers to cross the blood-brain barrier.
J Labelled Comp Radiopharm
; 66(9): 205-221, 2023 07.
Article
em En
| MEDLINE
| ID: mdl-36815704
ABSTRACT
Positron emission tomography (PET) is a powerful tool for imaging biological processes in the central nervous system (CNS). Designing PET radiotracers capable of crossing the blood-brain barrier (BBB) remains a major challenge. In addition to being brain-penetrant, a quantifiable CNS PET radiotracer must have high target affinity and selectivity, appropriate pharmacokinetics, minimal non-specific binding, negligible radiometabolites in the brain, and generally must be amenable to labeling with carbon-11 (11 C) or fluorine-18 (18 F). This review aims to give an overview of some of the critical physicochemical and biochemical contributors specific for CNS PET radiotracer design and how they can differ from pharmaceutical drug development, including in vitro assays, in silico predictions, and in vivo studies, with examples for how such methods can be implemented to optimize brain uptake of radiotracers based on experiences from our neuroimaging program.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Barreira Hematoencefálica
/
Tomografia por Emissão de Pósitrons
Idioma:
En
Revista:
J Labelled Comp Radiopharm
Ano de publicação:
2023
Tipo de documento:
Article
País de afiliação:
Canadá