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锝-99m三羰基标记的广谱喹诺酮作为感染性疾病的特异性显像剂

Technetium-99m Tricarbonyl Labeled a Broad-spectrum Quinolone as a Specific Imaging Agent in Infection Diseases.

作者信息

Khoramrouz Seyed Javad, Erfani Mostafa, Athari Allaf Mitra

机构信息

Science and Research branch, Islamic Azad University, P.O. Box: 14515-775, Tehran, Iran.

Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), P.O.Box: 14395-836, Tehran, Iran.

出版信息

Iran J Pharm Res. 2017 Spring;16(2):611-618.

Abstract

Nuclear medicine imaging has been used to localize infection sites, and efforts have been continued to develop modified infection specific radiopharmaceuticals. In this study gemifloxacin as a broad-spectrum quinolone has been labeled with [Tc (CO) (HO)] core in order to evaluate its feasibility as an infection imaging agent for use. The stability of radioconjugate was checked in human serum at 37 °C and biodistribution was studied in mice. Labeling yield of > 95% was obtained corresponding to a specific activity of 0.14 GBq/μmol. The radioconjugate showed good stability in human serum. Our main achievement was the high accumulation in the infected muscle in mice (T/NT = 2.93 ± 0.3 at 1 h post injection), which may diagnostically be beneficial for differentiate sites of infection from sites of inflammation.

摘要

核医学成像已被用于定位感染部位,并且一直在持续努力开发改良的感染特异性放射性药物。在本研究中,广谱喹诺酮类药物吉米沙星已用[Tc(CO)(HO)]核心进行标记,以评估其作为感染显像剂使用的可行性。在37℃的人血清中检查了放射性缀合物的稳定性,并在小鼠中研究了生物分布。标记产率>95%,对应比活为0.14GBq/μmol。放射性缀合物在人血清中显示出良好的稳定性。我们的主要成果是在小鼠感染肌肉中的高蓄积(注射后1小时T/NT = 2.93±0.3),这在诊断上可能有利于区分感染部位和炎症部位。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5ad5/5603869/7987682bb0fa/ijpr-16-611-g001.jpg

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