Synthesis and Evaluation of <sup>125</sup>I-IMPY: Application in Neuroblastoma Tracing and Treatment

Background: Radiolabeled compounds can serve as diagnostic or therapeutic agents depending on the characteristics of the isotopes used. IMPY (6-iodo-2-(4′-dimethylamino)-phenyl-imidazo[1,2-a]pyridine) is a lipophilic derivative of thioflavin-T, designed to function as a tracer when labeled with radi...

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Main Authors: Tsung-Ming Wang, Shih-Chang Chuang, Kuo-Chen Hung, Chang-Ching Yu, Tzu-Chuan Ho, Kuo-Pin Chuang, Cheng-Hui Yuan, Ming-Hui Yang, Yu-Chang Tyan
Format: Article
Language:English
Published: MDPI AG 2025-06-01
Series:Life
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Online Access:https://www.mdpi.com/2075-1729/15/6/930
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Summary:Background: Radiolabeled compounds can serve as diagnostic or therapeutic agents depending on the characteristics of the isotopes used. IMPY (6-iodo-2-(4′-dimethylamino)-phenyl-imidazo[1,2-a]pyridine) is a lipophilic derivative of thioflavin-T, designed to function as a tracer when labeled with radioactive iodine. While it has been primarily studied for imaging applications, its potential therapeutic effects when labeled with iodine-125 (<sup>125</sup>I) remain to be explored. Methods: In this study, IMPY was synthesized and labeled with <sup>125</sup>I for therapeutic purposes. Three different labeling methods were employed: isotope exchange reaction, redox reaction, and the Iodogen technique. The radiochemical yield of each method was determined to identify the most effective approach. Additionally, the effects of <sup>125</sup>I-IMPY on neuroblastoma cells were evaluated by assessing its toxicity and cellular uptake. Results: The radiochemical yields for the isotope exchange reaction, redox reaction, and Iodogen technique were found to be 0.96%, 10.74%, and 96.52%, respectively. The Iodogen technique exhibited the highest yield, exceeding 90% even after 48 h, making it the most efficient method. Furthermore, the impact of <sup>125</sup>I-IMPY on neuroblastoma cells was analyzed, revealing significant cellular uptake and potential therapeutic effects. Conclusions: This study demonstrated that the Iodogen technique is the most effective method for labeling IMPY with <sup>125</sup>I. The high labeling efficiency and observed cellular effects suggest that <sup>125</sup>I-IMPY could be considered not only as a tracer but also as a potential therapeutic agent for neuroblastoma. Further studies are needed to explore its full therapeutic potential and mechanism of action.
ISSN:2075-1729