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Pharmaceuticals 2019, 12(1), 25; https://doi.org/10.3390/ph12010025

Comparative Study of Two Oxidizing Agents, Chloramine T and Iodo-Gen®, for the Radiolabeling of β-CIT with Iodine-131: Relevance for Parkinson’s Disease

1
Department of Physiological Sciences, School of Medical Sciences, Santa Casa de Sao Paulo, Rua Cesario Mota Junior 61, Sao Paulo 01221-020, Brazil
2
Hospital Israelita Albert Einstein, Avenida Albert Einstein 627/701, Sao Paulo 05652-900, Brazil
*
Author to whom correspondence should be addressed.
Received: 30 November 2018 / Revised: 18 January 2019 / Accepted: 31 January 2019 / Published: 5 February 2019
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Abstract

Parkinson’s disease (PD) is a neurodegenerative disease characterized by the loss of dopaminergic neurons in the substantia nigra pars compacta, leading to alteration of the integrity of dopaminergic transporters (DATs). In recent years, some radiopharmaceuticals have been used in the clinic to evaluate the integrity of DATs. These include tropane derivatives such as radiolabeled β-CIT and FP-CIT with iodine-123 (123I), and TRODAT-1 with metastable technetium-99 (99mTc). Radiolabeling of β-CIT with radioactive iodine is based on electrophilic radioiodination using oxidizing agents, such as Chloramine T or Iodo-Gen®. For the first time, the present work performed a comparative study of the radiolabeling of β-CIT with iodine-131 (131I), using either Chloramine T or Iodo-Gen® as oxidizing agents, in order to improve the radiolabeling process of β-CIT and to choose the most advantageous oxidizing agent to be used in nuclear medicine. Both radiolabeling methods were similar and resulted in high radiochemical yield (> 95%), with suitable 131I-β-CIT stability up to 72 h. Although Chloramine T is a strong oxidizing agent, it was as effective as Iodo-Gen® for β-CIT radiolabeling with 131I, with the advantage of briefer reaction time and solubility in aqueous medium. View Full-Text
Keywords: Chloramine T; electrophilic radioiodination; iodine-131; Iodo-Gen®; oxidizing agent; β-CIT. Chloramine T; electrophilic radioiodination; iodine-131; Iodo-Gen®; oxidizing agent; β-CIT.
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R. Durante, A.C.; V. Sobral, D.; C. Miranda, A.C.; V. de Almeida, É.; L. Fuscaldi, L.; R. F. F. de Barboza, M.; Malavolta, L. Comparative Study of Two Oxidizing Agents, Chloramine T and Iodo-Gen®, for the Radiolabeling of β-CIT with Iodine-131: Relevance for Parkinson’s Disease. Pharmaceuticals 2019, 12, 25.

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