Design of Tc-labeled zinc-chelating imaging probe for SPECT imaging of the pancreas.

Bioorg Med Chem Lett

Department of Pharmaceutical Sciences, College of Pharmacy, 1110 North Stonewall Avenue, University of Oklahoma Health Sciences Center, and Oklahoma City, Oklahoma 73117, USA. Electronic address:

Published: November 2021


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Article Abstract

Early and sensitive diagnosis of pancreatic diseases is a contemporary clinical challenge. Zinc level in pancreatic tissue and its secretion in pancreatic juice has long been considered a surrogate marker of pancreatic function. The objective of this study was to design a Zn-chelating imaging probe (ZCIP) which could be labeled with Tc radionuclide for imaging of pancreas using single photon emission tomography (SPECT). We synthesized ZCIP as a bifunctional chelate consisting of diethylene triamine pentaacetic acid for Tc-chelation at one end and bispicolylethylamine for Zn-complexation at the other end. ZCIP was labeled with Tc by standard Sn-based reduction method. The Tc-labeled ZCIP was studied in normal mice (0.3 mCi) for SPECT imaging. We found that ZCIP consistently labeled with Tc radionuclide with over 95% efficiency. Addition of ZCIP altered the spectrum of standard dithizone-Zn complex, indicating its ability to chelate Zn. SPECT data demonstrated the ability of Tc-ZCIP to image pancreas with high sensitivity in a non-invasive manner; liver and spleen were the other major organs of Tc-ZCIP uptake. Based on these results, we conclude that Tc-ZCIP presents as a novel radiotracer for pancreas imaging for diagnosis of diseases such as pancreatitis.

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http://dx.doi.org/10.1016/j.bmcl.2021.128385DOI Listing

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