AI Article Synopsis
- The enzyme butyrylcholinesterase (BChE) plays a key role in detoxifying harmful substances in the blood and is linked to various health issues such as neurodegenerative disorders, type 2 diabetes, obesity, and cardiovascular diseases.
- Researchers developed carbamate-based inhibitors that can be labeled with fluorine-18 and carbon-11 isotopes to create PET radiotracers for visualizing BChE distribution in the body.
- Through experiments on mouse brain slices, the study demonstrated that these radiolabeled inhibitors can selectively and permanently attach to BChE, potentially offering a new method to investigate BChE's role in related diseases with high imaging resolution.
Article Abstract
The enzyme butyrylcholinesterase (BChE) is known to be involved in the detoxification of xenobiotics in blood plasma and is associated with the progress of neurodegenerative disorders, diabetes type 2, obesity, and diseases of the cardiovascular system. In the present study, we developed carbamate-based inhibitors serving as positron emission tomography (PET) radiotracers with (18) F and (11) C as radioisotopes to visualize BChE distribution. These inhibitors are radiolabeled at the carbamate site and transfer this moiety onto BChE, which thus results in covalent and permanent radiolabeling of the enzyme. There are no comparable radiotracers for cholinesterases described to date. By ex vivo autoradiography experiments on mice brain slices and kinetic investigations, selective and covalent transfer of the radiolabeled carbamate moiety onto BChE was proven. These tracers might provide high resolution of BChE distribution in vivo to enable investigations into the pathophysiological mechanisms of diseases associated with alterations in BChE occurrence.
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| http://dx.doi.org/10.1002/cmdc.201600223 | DOI Listing |
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