Radioiodination and biological evaluation of Cimetidine as a new highly selective radiotracer for peptic ulcer disorder detection

Mahmoud H. Sanad; Safaa B. Challan; Fawzy A. Marzook; Sayed M. Abd-Elhaliem; Ebtisam A. Marzook

doi:10.1515/ract-2020-0046

Article

Radioiodination and biological evaluation of Cimetidine as a new highly selective radiotracer for peptic ulcer disorder detection

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Published/Copyright: November 6, 2020

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From the journal Radiochimica Acta Volume 109 Issue 2

Abstract

One of the most famous techniques for stomach ulcer imaging is the nuclear imaging technique. We aim to focus on the synthesis of ¹²⁵I-cimetidine (¹²⁵I-cim) as an agent for peptic ulcer imaging. Cimetidine was labeled with Iodine-125 using a different oxidizing agent (Ch-T, NBS). All factors affecting the labeling yield were optimized. The radiochemical yield of ¹²⁵I-cim was 98 ± 0.22% at optimum conditions. In vitro stability, in vivo biodistribution of ¹²⁵I-cimetidine was studied in three groups: control group, pretreated group, and ulcer bearing group. In vivo biodistribution studies of ¹²⁵I-cim revealed high uptake in the stomach ulcer, reaching about 75.4 ± 1.2% ID/g at 15 min post-injection, than pretreated groups compared to the control. The results showed the suitability of using ¹²⁵I-cimetidine for stomach ulcer imaging.

Keywords: chloramine-T(Ch-T); 125I-cimetidine; iodine-125; in vivo biodistribution; N-bromosuccinimide (NBS); stomach ulcer imaging

Corresponding authors: Mahmoud H. Sanad and Safaa B. Challan, Labeled Compounds Department, Radioisotopes Production and Radioactive Sources Division, Hot Laboratories Center, Egyptian Atomic Energy Authority, P.O. Box 13759, Cairo, Egypt, E-mail: drsanad74@gmail.com (M. H. Sanad), safaabekheet@yahoo.com (S. B. Challan)

Author contribution: All the authors have accepted responsibility for the entire content of this submitted manuscript and approved submission.
Research funding: None declared.
Conflict of interest statement: All authors declare that they have no conflict of interest.

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Received: 2020-04-30

Accepted: 2020-10-01

Published Online: 2020-11-06

Published in Print: 2021-02-23

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https://doi.org/10.1515/ract-2020-0046

Keywords for this article

chloramine-T(Ch-T); 125I-cimetidine; iodine-125; in vivo biodistribution; N-bromosuccinimide (NBS); stomach ulcer imaging