radium-223

• 分子结构分类: 无机化合物 - 混合金属/非金属化合物 - 各种混合金属/非金属
• 英文名称: radium-223
• 英文别名: 223-radium；radium；(223)Ra；radium dihydride
• 化学式: Ra
• 分子量: 223.0
• InChiKey: DQXWBJUMYKQGMA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.54
• 重原子数：
  1.0
• 可旋转键数：
  0.0
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  0.0
• 氢给体数：
  0.0
• 氢受体数：
  0.0

反应信息

• 作为反应物：
  描述：

  radium-223 、 macropa 在 碳酸氢钠 作用下， 反应 1.0h， 生成 (223Ra)macropa
  参考文献：
  名称：

  [EN] COMPOSITIONS AND METHODS FOR RADIOTHERAPY USING CHELATED RADIOTHERAPEUTIC AGENTS AND NON-TARGET TISSUE BLOCKADE
  [FR] COMPOSITIONS ET MÉTHODES DE RADIOTHÉRAPIE UTILISANT DES AGENTS RADIO-THÉRAPEUTIQUES CHÉLATÉS ET LEUR BLOCAGE AU NIVEAU DES TISSUS NON CIBLÉS

  摘要：

  Among the various aspects of the present disclosure is the provision of compositions of isotope-ligand complexes, methods of use thereof, and methods of chelating isotopes. The present disclosure also provides for methods for modulating ion channel transportation of radiopharmaceuticals. For example, the inhibition of radiopharmaceutical transport comprises administering an ion channel transport modulating or inhibiting agent (e.g., a calcium channel inhibitor) in an amount effective to inhibit gastrointestinal uptake.

  公开号：

  WO2020180756A1
• 作为产物：
  描述：

  以 硝酸 为溶剂， 生成 radium-223
  参考文献：
  名称：

  ²¹²Pb@C₆₀ and Its Water-Soluble Derivatives:  Synthesis, Stability, and Suitability for Radioimmunotherapy

  摘要：

  Fullerenes could potentially play a valuable role in radioimmunotherapy by more stably encapsulating radionuclides, especially where conventional chelation chemistry is inadequate due to the physical and/or chemical properties of the radionuclide. One of the therapeutically useful radionuclides that requires improved containment in vivo is Pb-212 (tau(1/2) = 10.6 h), the beta-emitting parent to alpha-emitting Bi-212 (tau(1/2) = 60.6 min). Myelotoxicity resulting from the accumulation of Pb-212 in the bone marrow has limited the use of this radionuclide despite its favorable decay characteristics. In this work, Pb-212@C-60 and its malonic ester derivatives were prepared for the first time by allowing the Pb-212 to recoil into C-60 following alpha-decay from its parent, 0.15-s Po-216, generated in situ from the decay of Ra-224 (tau(1/2) = 15 days). Repeated washing of the organic phase containing the Pb-212@C-60 malonic esters with challenge solutions containing cold Pb2+ ions demonstrated that some of the Pb-212 could not be exchanged and was apparently inside of the fullerenes. Malonic esters of endohedral alpha-emitting Bi-213 (tau(1/2) = 45 min) fullerenes were prepared by an analogous procedure. Following acidification of the esters, a preliminary biodistribution study in mice was performed with the untargeted water-soluble radiofullerenes. It was found that Pb-212 did not accumulate in bone after being administered as an endohedral fullerene, in contrast to results with polyhydroxylated radiofullerenes and conventional polyaminocarboxylate chelators for Pb-212. The results indicate that Pb-212 is held more tightly in the fullerene than in other methods and suggest that fullerenes may have an important role in the targeted delivery of Pb-212.

  DOI：

  10.1021/ja068639b

文献信息

• Selective ²²⁶Ra²⁺ Ionophores Provided by Self-Assembly of Guanosine and Isoguanosine Derivatives
  作者：Fijs W. B. van Leeuwen、Willem Verboom、Xiaodong Shi、Jeffery T. Davis、David N. Reinhoudt

  DOI：10.1021/ja0455650

  日期：2004.12.1

  226Ra2+ extraction even at a 0.35 x 10(6) fold excess of Na+, K+, Rb+, Cs+, Mg2+, or Ca2+ (10(-2) M) to 226Ra2+ (2.9 x 10(-8) M) and at a 100-fold salt to ionophore excess. In the case of the G 1-picrate assembly, more competition was observed from Sr2+ and Ba2+, as extraction of 226Ra2+ ceased at an M2+/226Ra2+ ratio of 10(6) and 10(4), respectively. With the isoG 2 assembly, 226Ra2+ extraction also occurred

  自组装鸟苷 (G 1) 基十六聚体和异鸟苷 (isoG 2) 基十聚体即使在存在过量碱（Na+、K+、Rb+ 和 Cs+）和碱土（Mg2+、Ca2+）的情况下也是出色的 226Ra2+ 选择性离子载体、Sr2+ 和 Ba2+) 阳离子，pH 范围为 3-11。G 1 需要额外的苦味酸阴离子以提供中性组装，而 isoG 2 组装提取 226Ra2+ 阳离子而无需任何此类添加剂。G 1-苦味酸盐和 isoG 2 组件均显示 226Ra2+ 提取，即使 Na+、K+、Rb+、Cs+、Mg2+ 或 Ca2+ (10(-2) M) 至 226Ra2+ (2.9 x 10 (-8) M) 和离子载体过量的 100 倍盐。在 G 1-苦味酸盐组件的情况下，从 Sr2+ 和 Ba2+ 观察到更多的竞争，因为 226Ra2+ 的提取在 M2+/226Ra2+ 比率分别为 10(6) 和 10(4) 时停止。使用
• Towards the stable chelation of radium for biomedical applications with an 18-membered macrocyclic ligand
  作者：Diane S. Abou、Nikki A. Thiele、Nicholas T. Gutsche、Alexandria Villmer、Hanwen Zhang、Joshua J. Woods、Kwamena E. Baidoo、Freddy E. Escorcia、Justin J. Wilson、Daniel L. J. Thorek

  DOI：10.1039/d0sc06867e

  日期：——

  The therapeutic alpha-emitter ²²³Ra can be stably complexed in vivo, creating opportunities for the development of targeted radiopharmaceutical agents with this radionuclide.

  治疗用阿尔法发射体 223Ra 可以在体内稳定复合，这为开发使用这种放射性核素的靶向放射性药物制剂创造了机会。
• Gmelin Handbuch der Anorganischen Chemie, Gmelin Handbook: Ba: SVol., 49, page 256 - 258
  作者：

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• Nikitin, B. A., 1937, vol. 3, p. 228 - 228
  作者：Nikitin, B. A.

  DOI：——

  日期：——
• Gmelin Handbuch der Anorganischen Chemie, Gmelin Handbook: Ba: SVol., 50, page 258 - 260
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