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Development of a freeze-dried kit formulation for the preparation of 99mTc-NTP 15-5, a radiotracer for scintigraphic imaging of proteoglycans.

Development of a freeze-dried kit formulation for the preparation of 99mTc-NTP 15-5, a radiotracer for scintigraphic imaging of proteoglycans.

Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine (2015-03-31)

Aurélien Vidal, Vincent Gaumet, Marie-Josèphe Galmier, Sophie Besse, Fernand Leal, Françoise Gachon, Gilles Viot, Jacques Métin, Jean-Michel Chezal, Elisabeth Miot-Noirault, Philippe Auzeloux

摘要

The cartilage-targeting strategy is based on the strong affinity of quaternary ammonium (QA) functions for cartilage proteoglycans. We use a bifunctional agent containing QA moiety and a polyazamacrocycle structure able to complex technetium-99m. (99m)Tc-NTP 15-5 was selected for its high stability and its high affinity for proteoglycans in vivo. Labeling conditions of NTP 15-5 were optimized, and a lyophilized kit was developed for radiolabeling of (99m)Tc-NTP 15-5 (radiochemical yields 94.6±1.8%). (99m)Tc-NTP 15-5 was stable and resulted in favorable biological evaluations.

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