用于制备99mTc-NTP 15-5（一种用于蛋白聚糖闪烁成像的放射性示踪剂）的冻干试剂盒配方的研发。
Development of a freeze-dried kit formulation for the preparation of 99mTc-NTP 15-5, a radiotracer for scintigraphic imaging of proteoglycans.
作者信息
Vidal Aurélien, Gaumet Vincent, Galmier Marie-Josèphe, Besse Sophie, Leal Fernand, Gachon Françoise, Viot Gilles, Métin Jacques, Chezal Jean-Michel, Miot-Noirault Elisabeth, Auzeloux Philippe
机构信息
Inserm, UMR 990, F-63005 , France; Clermont Université, Université d'Auvergne, Imagerie moléculaire et thérapie vectorisée, BP 10448, F-63000 Clermont-Ferrand, France.
Inserm, UMR 990, F-63005 , France; Clermont Université, Université d'Auvergne, Imagerie moléculaire et thérapie vectorisée, BP 10448, F-63000 Clermont-Ferrand, France.
出版信息
Appl Radiat Isot. 2015 Jul;101:1-9. doi: 10.1016/j.apradiso.2015.03.010. Epub 2015 Mar 11.
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.
软骨靶向策略基于季铵（QA）官能团与软骨蛋白聚糖的强亲和力。我们使用一种含有QA部分和能够络合锝-99m的聚氮杂大环结构的双功能试剂。选择（99m）Tc-NTP 15-5是因为其在体内具有高稳定性和对蛋白聚糖的高亲和力。优化了NTP 15-5的标记条件，并开发了一种冻干试剂盒用于（99m）Tc-NTP 15-5的放射性标记（放射化学产率为94.6±1.8%）。（99m）Tc-NTP 15-5稳定，并产生了良好的生物学评价结果。
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