Radiosynthesis of 99MTc-Montelukast as a Novel Potential Radiopharmaceutical Model for Lung Scanning

IF 0.8 4区 医学 Q4 CHEMISTRY, MEDICINAL
M. A. Motaleb, I. T. Ibrahim, H. A. Shweeta, S. M. Abd El-Halem
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Abstract

Montelukast, a leukotriene receptor antagonist with a high affinity and selectivity for the cysteinyl leukotriene receptor type-1, was radiolabeled with 99mTc using a direct tagging procedure. The processing parameters—amounts of both montelukast and reducing agent, pH of the reaction mixture, reaction temperature, time of reaction, and in vitro stability of the 99mTc-montelukast complex—were thoroughly investigated. The 99mTc-montelukast complex had a percent radiolabeling yield of 92 ± 0.23 and an in vitro stability of 6 hours. According to biological distribution studies, the maximum uptake of 99mTc-montelukast complex for the lungs was 35.89 ± 1.03 % injected activity/gm tissue at 15 minutes following injection and remained high in the lungs for another hour (15.88 ± 0.39%), whereas the washout of mice organs appeared to primarily occur via the urinary tract. Because the 99mTc-montelukast complex is not a blood product, it is safer. To summarize, the 99mTc-montelukast complex is a new radiopharmaceutical that might be utilized for perfusion imaging of the lungs that is both safer and more useful.

Abstract Image

将 99MTc-Montelukast 放射性合成作为肺部扫描的新型潜在放射性药物模型
孟鲁司特是一种白三烯受体拮抗剂,对半胱氨酰白三烯受体 1 型具有高亲和力和选择性,采用直接标记法对其进行 99mTc 放射性标记。对处理参数--孟鲁司特和还原剂的用量、反应混合物的 pH 值、反应温度、反应时间以及 99mTc- 孟鲁司特复合物的体外稳定性--进行了深入研究。99m锝-孟鲁司特复合物的放射性标记率为 92 ± 0.23%,体外稳定性为 6 小时。根据生物分布研究,注射后 15 分钟,肺部对 99mTc-montelukast 复合物的最大摄取量为 35.89 ± 1.03 %(注射活性/克组织),并在肺部保持了一小时的高摄取量(15.88 ± 0.39%),而小鼠器官的洗脱似乎主要通过尿路进行。由于 99mTc-montelukast 复合物不是血液制品,因此更安全。总之,99m锝-孟鲁司特复合物是一种可用于肺灌注成像的新型放射性药物,它既安全又有用。
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来源期刊
Pharmaceutical Chemistry Journal
Pharmaceutical Chemistry Journal CHEMISTRY, MEDICINAL-PHARMACOLOGY & PHARMACY
CiteScore
1.30
自引率
22.20%
发文量
226
审稿时长
3-8 weeks
期刊介绍: Pharmaceutical Chemistry Journal is a monthly publication devoted to scientific and technical research on the creation of new drugs and the improvement of manufacturing technology of drugs and intermediates. International contributors cover the entire spectrum of new drug research, including: methods of synthesis; results of pharmacological, toxicological, and biochemical studies; investigation of structure - activity relationships in prediction of new compounds; methods and technical facilities used; and problems associated with the development of ecologically safe and economically feasible methods of industrial production. In addition, analytical reviews of the international literature in the field provide coverage of the most recent developments around the world. Pharmaceutical Chemistry Journal is a translation of the Russian journal Khimiko-Farmatsevticheskii Zhurnal. The Russian Volume Year is published in English from April. All articles are peer-reviewed.
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