M. A. Motaleb, I. T. Ibrahim, H. A. Shweeta, S. M. Abd El-Halem
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引用次数: 0
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.
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.