4.6 Article

Acetamidobenzoxazolone conjugated DOTA system for assessing 18 kDa translocator protein during pulmonary inflammation

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JOURNAL OF MOLECULAR STRUCTURE
卷 1271, 期 -, 页码 -

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ELSEVIER
DOI: 10.1016/j.molstruc.2022.134006

关键词

TSPO; MRI; Gd; SPECT; DOTA; Tc-99m( )

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In this study, a new molecule DOTA-MBP was designed and its binding affinity towards translocator protein (TSPO) was evaluated through in-silico studies. The stability of DOTA-MBP as a magnetic resonance contrast agent was assessed. In vivo studies using a mouse model showed that DOTA-MBP could locate lung inflammation and monitor the severity of the disease through radioactivity imaging techniques.
Translocator protein (TSPO) is well known inflammatory target. We have designed a new molecule DOTA-MBP. In-silico studies have been performed to evaluate the binding affinity potential of MBP towards the TSPO. The stability of DOTA-MBP was assessed for Gd (III) for possible application as chelating vehicle or other MR contrast agent. For in vivo studies LPS induced lung inflammation model was develop in mice and after 24 h of LPS administration biodistribution and Tc-99m-DOTA-MBP imaging have been performed to monitor the uptake and distribution of radioactivity in different peripheral organs with time. In conclusion we can say that DOTA-MBP as potential candidate to locate the lung inflammation as well as monitor the severity of disease through SPECT or MRI. (C) 2022 Elsevier B.V. All rights reserved.

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