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Master Thesis

Radiomarquage, caractérisation et biodistribution de la complexation du 99mTc par deux chélates déjà synthétisés comme sidérophores : O-trenox tris (8-hydroxy-quinoléine) et O-trensox tris (8-hydroxy-5-sulfonate-quinoléine)

Abstract : Technetium-99m is the most widely use radioisotope for diagnosis in nuclear medicine. Siderophors such as trenox and trensox are iron chelating agents. Due to the 8-hydroxyquinoline groups of these two siderophors, they could chelate technetium in similar way as iron. Without heating and without pH change, using 50 µg of pyrophosphate as a reducing agent and 150 nmol of chelate and a fresh pertechnetate eluate, we can obtain very easily and quickly the 99mTc-trenox complex with radiochemical purity >98% and the 99mTc-trensox complex with purity >95%. Both complexes are stable in vitro as well as after injection in mice. The first complex is lipophilic and neutral while the second is hydrophilic and negatively charged. The biodistribution study in mice shows a 99mTc-trenox candidate for hepatobiliary imaging with a high accumulation in both tissues due to its lipophilicity. The addition of sulfonate groups to trensox makes it more hydrophilic, hence its predominantly renal biodistribution. These encouraging preliminary results allow us to continue to consider O-trensox and O-trenox/99mTc complexes as serious candidates for SPECT imaging. This study will have to be completed by an evaluation of the complexation of these siderophors with 188Re, an emitting isotope β- having coordination chemistry very close to that of technetium-99m thus allowing an alternative theranostic use to the classical pair (68Ga/177Lu).
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Master Thesis
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https://dumas.ccsd.cnrs.fr/dumas-03021885
Contributor : Jean-Hugues Morneau <>
Submitted on : Tuesday, November 24, 2020 - 3:14:00 PM
Last modification on : Monday, December 7, 2020 - 10:05:22 AM
Long-term archiving on: : Thursday, February 25, 2021 - 8:21:53 PM

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  • HAL Id : dumas-03021885, version 1

Citation

Alexandre Biguet Petit Jean. Radiomarquage, caractérisation et biodistribution de la complexation du 99mTc par deux chélates déjà synthétisés comme sidérophores : O-trenox tris (8-hydroxy-quinoléine) et O-trensox tris (8-hydroxy-5-sulfonate-quinoléine). Sciences pharmaceutiques. 2020. ⟨dumas-03021885⟩

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