Discovery of Environment-Sensitive Fluorescent Agonists for α1-Adrenergic Receptors.
Anal Chem
; 91(19): 12173-12180, 2019 10 01.
Article
en En
| MEDLINE
| ID: mdl-31321979
ABSTRACT
A series of novel fluorescent agonists were well developed herein with turn-on switch for α1-adrenergic receptors (α1-ARs) by conjugating the environment-sensitive fluorophore 4-chloro-7-nitrobenzoxadiazole with phenylephrine. Overall, these probes exhibited efficient binding and apparent fluorescence intensity changes (up to 10-fold) upon binding with α1-ARs. Moreover, these probes have been successfully applied for selectively imaging α1-ARs in the living cells. The dynamic process of α1-ARs internalization was traced successfully with these newly designed fluorescent agonists. Fluorescence polarization assay demonstrated specific interactions between these probes and α1-ARs. With these new probes, a bioluminescence resonance energy transfer binding assay has been well established and applied to the high-throughput screening of unlabeled α1-ARs agonist and antagonist. It is expected that these environment-sensitive fluorescent turn-on agonists may provide useful new tools in studying pharmacology and physiology of α1-ARs during drug discovery.
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Receptores Adrenérgicos alfa 1
/
Ensayos Analíticos de Alto Rendimiento
/
Agonistas de Receptores Adrenérgicos alfa 1
Tipo de estudio:
Diagnostic_studies
Límite:
Humans
Idioma:
En
Revista:
Anal Chem
Año:
2019
Tipo del documento:
Article
País de afiliación:
China