期刊
CHEMICAL COMMUNICATIONS
卷 52, 期 77, 页码 11599-11602出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c6cc05936h
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资金
- Agence Nationale de la Recherche (ANR) [ANR-12-BS07-0008-01]
- INSA Rouen
- Rouen-Normandie University
- Centre National de la Recherche Scientifique (CNRS)
- Region Haute-Normandie (CRUNCh network)
- Labex SynOrg [ANR-11-LABX-0029]
- Agence Nationale de la Recherche (ANR) [ANR-12-BS07-0008] Funding Source: Agence Nationale de la Recherche (ANR)
Two near infra-red (NIR) fluorescent probes HupNIR1 and HupNIR2 based on the huprine scaffold and cyanine 5.0 dye have been synthesised and evaluated in situ for the detection of acetylcholin-esterases in different tissues. As anticipated by the initial properties of huprine, both probes displayed a high affinity and selectivity for AChE toward BChE, with IC50 values in the nanomolar range and without any non-specific binding in the tissues. HupNIR2 appears the best probe for AChE with a great selectivity and sensitivity for AChE even in the brain region displaying a low AChE concentration as striatum. Moreover, the binding of HupNIR2 is affected when AChE is inhibited with toxic molecules such as organ ophosphates. This work provides a new tool to visualize active AChE in biological applications.
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