Cell-Permeable Esterase-Activated Ca(II)-Sensitive MRI Contrast Agent.
Bioconjug Chem
; 27(2): 465-73, 2016 Feb 17.
Article
em En
| MEDLINE
| ID: mdl-26689452
ABSTRACT
Calcium [Ca(II)] is a fundamental transducer of electrical activity in the central nervous system (CNS). Influx of Ca(II) into the cytosol is responsible for action potential initiation and propagation, and initiates interneuronal communication via release of neurotransmitters and activation of gene expression. Despite the importance of Ca(II) in physiology, it remains a challenge to visualize Ca(II) flux in the central nervous system (CNS) in vivo. To address these challenges, we have developed a new generation, Ca(II)-activated MRI contrast agent that utilizes ethyl esters to increase cell labeling and prevent extracellular divalent Ca(II) binding. Following labeling, the ethyl esters can be cleaved, thus allowing the agent to bind Ca(II), increasing relaxivity and resulting in enhanced positive MR image contrast. The ability of this probe to discriminate between extra- and intracellular Ca(II) may allow for spatiotemporal in vivo imaging of Ca(II) flux during seizures or ischemia where large Ca(II) fluxes (1-10 µM) can result in cell death.
Texto completo:
1
Bases de dados:
MEDLINE
Assunto principal:
Imageamento por Ressonância Magnética
/
Cálcio
/
Meios de Contraste
/
Esterases
Tipo de estudo:
Diagnostic_studies
Limite:
Animals
Idioma:
En
Revista:
Bioconjug Chem
Assunto da revista:
BIOQUIMICA
Ano de publicação:
2016
Tipo de documento:
Article
País de afiliação:
Estados Unidos