Fluorescent 2-styrylpyridazin-3(2H)-one derivatives as probes targeting amyloid-beta plaques in Alzheimer's disease.
Bioorg Med Chem Lett
; 22(12): 4106-10, 2012 Jun 15.
Article
en En
| MEDLINE
| ID: mdl-22578456
Amyloid plaques, which are primarily composed of aggregated amyloid-beta (Aß) peptide, are the neuropathological hallmarks of Alzheimer's disease (AD). Fluorescent markers containing 2-styrylpyridazin-3(2H)-ones were developed to detect intracellular aggregated Aß peptides. Nine compounds exhibited a greater than 10-fold increase of in emission spectra before and after mixing with Aß aggregates compared with before mixing. Among these compounds, compound 9n exhibited the highest affinity for Aß aggregates (K(d)=1.84 µM) and selectively stained both aggregated intracellular Aß and Aß plaques in the transgenic AD model mice (APP/PS1). These preliminary results indicate that 2-styrylpyridazin-3(2H)-one derivatives are promising alternative fluorescence imaging agent for the study of AD.
Texto completo:
1
Base de datos:
MEDLINE
Asunto principal:
Piridazinas
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Péptidos beta-Amiloides
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Placa Amiloide
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Enfermedad de Alzheimer
/
Colorantes Fluorescentes
Tipo de estudio:
Diagnostic_studies
/
Prognostic_studies
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2012
Tipo del documento:
Article