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Tc-99m-alafosfalin: an antibiotic peptide infection imaging agent

机译:TC-99M-ALAFOSFALIN:抗生素肽感染显像剂

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The radiolabeled antibiotic peptide Tc-99m-alafosfalin was assessed as an infection imaging agent in a rat model by comparison with Tc-99m-DTPA and Tc-99m-leukocytes. Tc-99m-alafosfalin was prepared via an instant cold kit and Tc-99m-leukocytes were prepared using Tc-99m-stannous fluoride colloid in an ex vivo labeling procedure of whole blood. In separate experiments, the three radiotracers were administered to rats infected with staphylococcus aureus. Quantitative biodistribution studies were performed as well as scintigraphic images and histopathology. Tc-99m-alafosfalin is a stable product, obtained in high radiochemical purity (>95%). This agent was mainly renally excreted, with low liver, spleen and bone uptake, and resulted in a mean ratio of infectedon-infected thighs of 4.3/1.0 at 4 hr post radiotracer injection. Tc-99m-DTPA gave a corresponding ratio of 1.9/1.0 and Tc-99m-leukocytes gave 20.0/1.0 at the same time point. An in vitro assay found the level of Tc-99m-alafosfalin binding to staphylococcus aureas higher than Tc-99m-DTPA (10% versus 1% respectively). Tc-99m-alafosfalin accumulates at sites of infection in a rat model better than the perfusion molecule Tc-99m-DTPA, yet less than Tc-99m-leukocytes. The distribution characteristics of this Tc-99m-antibiotic peptide would be an advantage in imaging abdominal and soft tissue infection. (C) 2003 Elsevier Science Inc. All rights reserved. [References: 32]
机译:通过与Tc-99m-DTPA和Tc-99m-白细胞进行比较,将放射性标记的抗生素肽Tc-99m-alafosfalin在大鼠模型中评估为感染显像剂。通过即时冷试剂盒制备Tc-99m-alafosfalin,并在全血的体外标记过程中,使用Tc-99m-氟化锡胶体制备Tc-99m-白细胞。在单独的实验中,将三种放射性示踪剂施用于感染了金黄色葡萄球菌的大鼠。进行了定量生物分布研究以及闪烁显像和组织病理学。 Tc-99m-alafosfalin是稳定的产物,以高放射化学纯度(> 95%)获得。该药物主要通过肾脏排泄,肝脏,脾脏和骨骼的摄取较低,在注射放射性示踪剂后4小时,受感染/未受感染的大腿平均比率为4.3 / 1.0。在同一时间点,Tc-99m-DTPA的对应比率为1.9 / 1.0,Tc-99m-白细胞的比率为20.0 / 1.0。体外试验发现,Tc-99m-alafosfalin与金黄色葡萄球菌的结合水平高于Tc-99m-DTPA(分别为10%和1%)。 Tc-99m-alafosfalin在大鼠模型中的感染部位积累的能力优于灌注分子Tc-99m-DTPA,但少于Tc-99m-白细胞。这种Tc-99m抗生素肽的分布特征在腹部和软组织感染成像中将是一个优势。 (C)2003 Elsevier Science Inc.保留所有权利。 [参考:32]

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