Sheikholislam Zahra, Soleimani Zohreh, Moghimi Abolghasem, Shahhosseini Soraya
Pharmaceutical Chemistry Department, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran, P O Box: 14155-6153.
Department of Chemistry, University of Imam Hossein.
Iran J Pharm Res. 2013 Fall;12(4):729-33.
Radioiodinated meta-iodobenzylguanidine (MIBG) is one of the important radiopharmaceuticals in Nuclear Medicine. [(123/131)I] MIBG is used for imaging of Adrenal medulla, studying heart sympathetic nerves, treatment of pheochromacytoma and neuroblastoma. For clinical application, radioiodinated MIBG is prepared through isotopic exchange method, which includes replacement of radioactive iodine in a nucleophilic substitution reaction with cold iodine ((127)I). The unlabelled MIBG hemisulfate is synthesized by the procedure described by Wieland et al. (1980). The availability of a more practical and cost-effective procedure for MIBG preparation encouraged us to study the MIBG synthesis methods. In this study the preparation of MIBG through different methods were evaluated and a new method, which is one step, simple and cost-effective is introduced. The method has ability to be scaled up for production of unlabelled MIBG.
放射性碘化间碘苄胍(MIBG)是核医学中重要的放射性药物之一。[(123/131)I]MIBG用于肾上腺髓质成像、研究心脏交感神经、治疗嗜铬细胞瘤和神经母细胞瘤。对于临床应用,放射性碘化MIBG通过同位素交换法制备,该方法包括在亲核取代反应中用冷碘((127)I)取代放射性碘。未标记的MIBG半硫酸盐通过Wieland等人(1980年)描述的方法合成。一种更实用且成本效益更高的MIBG制备方法的出现促使我们研究MIBG的合成方法。在本研究中,评估了通过不同方法制备MIBG的情况,并介绍了一种一步法、简单且经济高效的新方法。该方法有能力扩大规模以生产未标记的MIBG。