m-[131I]iodobezylguanidine hemisulfate

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: m-[131I]iodobezylguanidine hemisulfate
• 英文别名: (m-[131I]Iodobenzyl)guanidine sulfate (2:1)；2-[(3-(131I)iodanylphenyl)methyl]guanidine;sulfuric acid
• 化学式: C₈H₁₀IN₃*0H₂O₄S
• 分子量: 328.227
• InChiKey: NMHJRGCKGFRFAQ-ZKFIMABGSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.41
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  147
• 氢给体数：
  4
• 氢受体数：
  5

ADMET

毒理性

• 在妊娠和哺乳期间的影响

◉ 母乳喂养期间使用总结：本记录中的信息是指将碘苯扎胺 I 123（I 123 邻碘苄基胍；I 123 MIBG）用作诊断剂。根据 I 123 的物理半衰期，制造商建议母亲至少泵奶并丢弃 6 天的奶，尽管根据有效半衰期，停止 3.5 天可能更一致。然而，美国核能管理委员会的一个小组委员会建议，在剂量高达 11 mCi 的情况下，无需停止哺乳。如果停止哺乳，并且母亲在检查前已经表达并保存了乳汁，她可以在哺乳中断期间给婴儿喂食。母亲在哺乳中断期间泵出的奶可以丢弃，或者冷藏储存，并在经过大约 5.5 天或 10 个物理半衰期后给婴儿食用。 担心乳汁中放射性水平的母亲可以要求在医院核医学科进行检测。当放射性水平达到安全水平时，她可以恢复哺乳。已经发表了一种测量乳汁放射性并确定母亲可以安全恢复哺乳的时间的方法。 ◉ 对哺乳婴儿的影响：截至修订日期，未找到相关已发表信息。 ◉ 对泌乳和母乳的影响：截至修订日期，未找到相关已发表信息。

◉ Summary of Use during Lactation:Information in this record refers to the use of iobenguane I 123 (I 123 meta-iodobenzylguanidine; I 123 MIBG) as a diagnostic agent. The manufacturer recommends that mothers should pump and discard milk for at least 6 days based on the physical half-life of I 123, although discontinuation for 3.5 days would be more consistent with the effective half-life. However, a US Nuclear Regulatory Commission subcommittee has recommended that nursing need not be discontinued with doses up to 11 mCi. If breastfeeding is discontinued and the mother has expressed and saved milk prior to the examination, she can feed it to the infant during the period of nursing interruption. The milk that is pumped by the mother during the time of breastfeeding interruption can either be discarded or stored refrigerated and given to the infant after 10 physical half-lives, or about 5.5 days, have elapsed. Mothers concerned about the level of radioactivity in their milk could ask to have it tested at a nuclear medicine facility at their hospital. When the radioactivity is at a safe level, she may resume breastfeeding. A method for measuring milk radioactivity and determining the time when a mother can safely resume breastfeeding has been published. ◉ Effects in Breastfed Infants:Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk:Relevant published information was not found as of the revision date.

来源:Drugs and Lactation Database (LactMed)

反应信息

• 作为产物：
  描述：

  m-iodobenzyl guanidine sulfate 在 ammonium sulfate 、 copper(ll) sulfate pentahydrate 、 sodium iodide 作用下， 以 溶剂黄146 为溶剂， 反应 0.5h， 生成 m-[131I]iodobezylguanidine hemisulfate
  参考文献：
  名称：

  Establishment of a fast and high yield method for routine production of [¹³¹I]MIBG and investigation of its radiochemical stability for diagnosis and treatment uses

  摘要：

  In this work, exchange radioiodination of metaiodobenzylguanidine (MIBG) was carried out at optimum conditions that facilitates the production of [131I]MIBG both quickly and efficiently. The radiochemical purity and yield of the labeled product are typically as high as 99% and 90% for diagnostic dose and 95% and 80% for therapeutic dose, respectively. Stability studies show that labeled material at the room temperature met the demand of the clinical application. This labeling procedure will be used in the routine production process of [131I]MIBG for diagnosis and treatment uses.

  DOI：

  10.1002/jlcr.3099

文献信息

• Establishment of a fast and high yield method for routine production of [¹³¹I]MIBG and investigation of its radiochemical stability for diagnosis and treatment uses
  作者：M. R. Davarpanah、S. Attar Nosrati、H. A. Khoshhosn、M. Fazlali、M. Kazemi Boudani

  DOI：10.1002/jlcr.3099

  日期：2013.11

  In this work, exchange radioiodination of metaiodobenzylguanidine (MIBG) was carried out at optimum conditions that facilitates the production of [131I]MIBG both quickly and efficiently. The radiochemical purity and yield of the labeled product are typically as high as 99% and 90% for diagnostic dose and 95% and 80% for therapeutic dose, respectively. Stability studies show that labeled material at the room temperature met the demand of the clinical application. This labeling procedure will be used in the routine production process of [131I]MIBG for diagnosis and treatment uses.